Entries |
Document | Title | Date |
20100240597 | METHODS OF DELIVERY OF MOLECULES TO CELLS USING A RICIN SUBUNIT AND COMPOSITIONS RELATING TO SAME - A method of preparing molecules of interest for delivery to eukaryotic cells is shown, wherein a ricin B chain subunit not having a ribosome inactivating subunit and retaining lectin activity is modified by modifying the first cysteine residue to be absent or substituted with an amino acid other than cysteine, or removing a protease sensitive site at the N-terminal of the subunit, or adding an endoplasmic reticulum retrieval signal, and operatively associating the subunit with a molecule of interest. Methods of operatively associating the subunit and molecule of interest include chemical conjugation at primary amines, conjugation with N-glycans of the subunit, a disulfide bond, and assembly of immunoglobulin domains. The invention provides for operatively associating multiple molecules of interest with a ricin B chain subunit, and delivery into targeted cells, cell components, and combination of cells. | 09-23-2010 |
20100249044 | BIOGEL - A biogel, and kits, agents, and methods for formation of the biogel are described. The biogel can be used for a variety of applications, including haemostasis, wound sealing, tissue engineering or localised drug delivery. | 09-30-2010 |
20100261660 | Novel co-stimulatory molecules - The invention provides polynucleotides and polypeptides encoded therefrom having advantageous properties, including an ability of the polypeptides to preferentially bind a CD28 or CTLA-4 receptor at a level greater or less than the ability of human B7-1 to bind CD28 or CTLA-4, or to induce or inhibit altered level of T cell proliferation response greater compared to that generated by human B7-1. The polypeptides and polynucleotides of the invention are useful in therapeutic and prophylactic treatment methods, gene therapy applications, and vaccines. | 10-14-2010 |
20100267648 | Methods and materials relating to stem cell growth factor-like polypeptides and polynucleotides - The invention provides novel polynucleotides and polypeptides encoded by such polynucleotides and mutants or variants thereof that correspond to a novel human secreted stem cell growth factor-like polypeptides. Other aspects of the invention include vectors containing processes for producing novel human secreted stem cell growth factor-like polypeptides, and antibodies specific for such polypeptides. | 10-21-2010 |
20100267649 | VASCULAR ADHESION MOLECULES AND MODULATION OF THEIR FUNCTION - The invention relates to new polypeptides in isolated form belonging to a subfamily of the human immunoglobulin superfamily, which polypeptide shows at least 70% sequence homology with the amino acid sequence of the murine Confluency Regulated Adhesion Molecules 1 or 2 (CRAM-1 or CRAM-2) as depicted in FIG. | 10-21-2010 |
20100279953 | Non-protein stabilized clostridial toxin pharmaceutical compositions - A Clostridial toxin pharmaceutical composition comprising a Clostridial toxin, such as a botulinum toxin, wherein the Clostridial toxin present in the pharmaceutical composition is stabilized by a non-protein excipient such as a polyvinylpyrrolidone, a disaccharides, a trisaccharide, a polysaccharide, an alcohol, a metal, an amino acid, a surfactant and/or a polyethylene glycol. | 11-04-2010 |
20100286068 | MOLECULAR MARKERS OF PLANT EMBRYOGENESIS - The present invention relates generally to a molecular marker for a plant physiological process and more particularly for plant embryogenesis. The molecular marker is, in one form, a genetic sequence from a monocot plant such as but not limited to oil-palm plants. In another form, the molecular marker is a polypeptide encoded by said genetic sequence. More particularly, the molecular marker of the present invention enables embryogenic tissue to be detected in vitro. The early detection of embryogenic tissue enables non-embryogenic tissue to be discarded. The ability to detect embryogenesis facilitates maximization of embryogenic potential. The present invention further contemplates a molecular marker comprising in one form a sequence of nucleotides encoding an antioxidant or in another form a sequence of amino acids defining a polypeptide having antioxidant activity. The antioxidant according to this aspect of the present invention is particularly useful in tablet or cream form as an anti-aging agent. The molecular markers of the present invention therefore also have uses in the inhibition or retardation of apoptotic processes. Such an effect has benefits in both plant and animal cells. The present invention further contemplates a promoter sequence encoding the molecular marker and its use in generating male sterile plants. | 11-11-2010 |
20100292170 | METHODS FOR DIAGNOSING AND TREATING PELVIC PAIN DISORDERS VIA BETA-CATENIN - Methods for diagnosing a pelvic pain disorder that include analyzing samples for increased levels and/or nuclear accumulation of beta-catenin, which indicates presence of the pelvic pain disorder, particularly interstitial cystitis. Therapeutic treatment of a pelvic pain disorder, particularly interstitial cystitis, includes the administration to a patient of an effective amount of an inhibitor of beta-catenin activity. This can be carried out by direct administration of the therapeutic agent or via gene therapy. | 11-18-2010 |
20100292171 | Competitive Regulation of Hepcidin mRNA by Soluble and Cell-Associated Hemojuvelin - Disclosed herein are hemojuvelin-specific siRNAs that vary hemojuvelin mRNA concentration. Also disclosed herein, GPI-hemojuvelin positively regulated hepcidin mRNA expression, independently of the IL-6 pathway, whereas soluble hemojuvelin (s-hemojuvelin) suppressed hepcidin mRNA expression in primary human hepatocytes in a log-linear dosedependent manner. Disclosed are compositions and methods for modulating diseases of iron metabolism and hepcidin expression or hepcidin levels. | 11-18-2010 |
20100298238 | NONTOXIC SHIGA-LIKE TOXIN MUTANT COMPOSITIONS AND METHODS - Disclosed are nontoxic mutants of Shiga-like toxin (Stx1 or Stx2), nucleic acids encoding them, compositions containing the mutants and methods of using the mutants in connection with hemolytic euremic syndrome (HUS). Also disclosed are methods of treating HUS using L3 protein fragments, the nontoxic Stx1 or Stx2 mutants, or combinations thereof. | 11-25-2010 |
20100305049 | Novel Wheat Allergens - The present invention relates to the field of IgE-mediated allergy, particularly occupational asthma such as bakers asthma. More specifically the invention relates to the identification of a novel wheat allergen and the use thereof in therapy and diagnosis of IgE-mediated allergy. Furthermore the present invention provides the use of known peptides and proteins in therapy and diagnosis. The invention also relates to methods for diagnosis and treatment of IgE-mediated allergy in mammals. | 12-02-2010 |
20100311671 | TRANSDERMAL DELIVERY OF PKC MODULATORY PEPTIDES THROUGH MICROPORATED SKIN - Disclosed herein are methods for transdermal delivery of PKC modulatory peptides. Generally, methods comprise the delivery of an isozyme specific PKC peptide modulator through skin that has been microporated, e.g., with an array of microneedles. Such methods may be used to administer therapeutically effective amounts of an isozyme selective PKC peptide inhibitor or activator. | 12-09-2010 |
20100317598 | Isolated BRCA1 Peptides and Method of Use - The invention provides isolated peptides of a BRCA1 domain, which bind to p53 cognate DNA and stimulate transcription activities and cancer cell apoptosis. Nucleic acids encoding the peptides, and methods of expression thereof, are also provided. The invention provides pharmaceutical compositions, and methods of use thereof, for treating breast and ovarian cancer using the peptides. | 12-16-2010 |
20100317599 | PROCESS FOR THE PRODUCTION OF A PEPTIDE - The present invention describes a polypeptide, comprising at least one repeat domain, further comprising a recombinant peptide of interest. The present invention further describes a process for the production of a recombinant peptide of interest. The invention further describes the use of a repeat protein for the production of a recombinant peptide of interest. | 12-16-2010 |
20100323974 | Inhibitors of PARP Activity and Uses Thereof - The present invention relates to new inhibitors of the nucleic enzyme poly(adenosine 5′-diphospho-ribose) polymerase [“poly(ADP-ribose) polymerase” or “PARP”, which is also sometimes called “PARS” for poly(ADP-ribose) synthetase]. More particularly, the invention relates to the use of PARP inhibitors to prevent and/or treat tissue damage resulting from cell damage or death due to necrosis or apoptosis; neural tissue damage resulting from ischemia and reperfusion injury; neurological disorders and neurodegenerative diseases; to prevent or treat vascular stroke; to treat or prevent cardiovascular disorders; to treat other conditions and/or disorders such as age-related macular degeneration, AIDS and other immune senescence diseases, arthritis, atherosclerosis, cachexia, cancer, degenerative diseases of skeletal muscle involving replicative senescence, diabetes, head trauma, immune senescence, inflammatory bowel disorders (such as colitis and Crohn's disease), muscular dystrophy, osteoarthritis, osteoporosis, chronic and acute pain (such as neuropathic pain), renal failure, retinal ischemia, septic shock (such as endotoxic shock), and skin aging; to extend the lifespan and proliferative capacity of cells; to alter gene expression of senescent cells; or to radiosensitize hypoxic tumor cells. | 12-23-2010 |
20110003755 | Tumor Endothelial Marker 5-alpha Molecules and Uses Thereof - The present invention provides Tumor Endothelial Marker 5α (TEM5α) polypeptides and nucleic acid molecules encoding the same. The invention also provides selective binding agents, vectors, host cells, and methods for producing TEM5α polypeptides. The invention further provides pharmaceutical compositions and methods for the diagnosis, treatment, amelioration, or prevention of diseases, disorders, and conditions associated with TEM5α polypeptides. | 01-06-2011 |
20110009342 | USES OF PDCD5 POLYPEPTIDE FOR TUMOR CHEMOTHERAPY AND ORGAN PROTECTION - The invention relates to the use of PDCD5 polypeptides or polynucleotides that code the PDCD5 polypeptides in preparation of sensitizers of chemotherapeutic agents for cancers. The invention also relates to the use of PDCD5 polypeptides or polynucleotides that code the PDCD5 polypeptides to protect normal or diseased tissues or organs from damage or further damage, and to pharmaceutical combinations including chemotherapeutic agents and PDCD5 polypeptides or polynucleotides that code the PDCD5 polypeptides in an amount effective for sensitization. Preferably, the pharmaceutical agents are selected from antibiotic and anti-metabolic agents or any combination thereof. | 01-13-2011 |
20110034401 | NOVEL PROCESS FOR SOLUBILIZING PROTEIN FROM A PROTEINACEOUS MATERIAL AND COMPOSITIONS THEREOF - The process for solubilizing proteinaceous material of the present invention includes subjecting the proteinaceous material to a sufficient amount of a basic solution to obtain a supernatant that has a basic pH and exposing the supernatant to the basic solution for a sufficient length of time and temperature for hydrolysis to occur. The process also includes cooling the mixture of the supernatant and proteinaceous material and optionally acidifying the mixture. This process may also include recovering the solubilized protein from the supernatant for use in various applications. Also provided herein is a composition of solubilized proteins from eggshell membrane obtained using processes of the present invention. | 02-10-2011 |
20110046073 | SOLUBLE LYMPHOTOXIN-BETA RECEPTOR FUSION PROTEIN AND METHODS FOR INHIBITING LYMPHOTOXIN BETA-RECEPTOR SIGNALING - This invention relates to compositions and methods comprising “lymphotoxin-β-receptor blocking agents”, which block lymphotoxin-β receptor signalling. Lymphotoxin-β receptor blocking agents are useful for treating lymphocyte-mediated immunological diseases, and more particularly, for inhibiting Th1 cell-mediated immune responses. This invention relates to soluble forms of the lymphotoxin-β.receptor extracellular domain that act as lymphotoxin-β receptor blocking agents. This invention also relates to the use of antibodies directed against either the lymphotoxin-β.receptor or its ligand, surface lymphotoxin, that act as lymphotoxin-β receptor blocking agents. A novel screening method for selecting soluble receptors, antibodies and other agents that block LT-β receptor signalling is provided. | 02-24-2011 |
20110046074 | HIGHLY PERMEABLE POLYMERIC MEMBRANES - Provided are substantially flat membranes that include a block or graft co-polymer and a water transport protein, such as Aquaporin-Z, or a synthetic mimic of such proteins. Also provided are methods of removing contaminants from a liquid, by contacting the liquid with a substantially flat membrane that includes a block or graft co-polymer and a water transport protein or synthetic mimic thereof. Also provided are methods of making such membranes. Further provided are compositions that include at least one active ingredient and vesicles surrounding the active ingredient, where the vesicles include a block or graft copolymer and a water transport protein or synthetic mimic surrounding the active ingredient. Also provided are methods that include administering such compositions to patients. | 02-24-2011 |
20110053865 | AMINO ACID SEQUENCES DIRECTED AGAINST HETERODIMERIC CYTOKINES AND/OR THEIR RECEPTORS AND POLYPEPTIDES COMPRISING THE SAME - The present invention relates to amino acid sequences that are directed against (at defined herein) heterodimeric cytokines and/or their receptors, as well as to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consists of one or more such amino acid sequences ( also referred to herein as “amino acid sequences of the invention”, “compounds of the invention”, and “polypeptides of the invention”, respectively). The invention also relates to nucleic acids encoding such amino acid sequences and polypeptides (also referred to herein as “nucleic acids of the invention” or “nucleotides sequences of the invention”); to methods for preparing such amino acid sequences and polypeptides; to hose cells expressing or capable of expressing such amino acid sequences or polypeptides; to compositions, and in particular to pharmaceutical compositions, that complete such amino acid sequences, polypeptides, nucleic acids and/or host cells; and to uses of such amino acid sequences or polypeptides, nucleic acids, host cells and/or compositions, in particular for prophylactic, therapeutic or diagnostic purposes, such as the prophylactic, therapeutic or diagnostic purposes mentioned herein. | 03-03-2011 |
20110053866 | PHARMACEUTICAL COMPOSITIONS - The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder. | 03-03-2011 |
20110059905 | METHODS OF TREATING DISEASE-INDUCED ATAXIA AND NON-ATAXIC IMBALANCE - Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity. | 03-10-2011 |
20110065653 | TAT-UTROPHIN AS A PROTEIN THERAPY FOR DYSTROPHINOPATHIES - Disclosed is a fusion protein including a full-length TAT-utrophin or an anti-dystrophinopathic fragment thereof, a method of treating dystrophinopathies (including Duchenne muscular dystrophy) using the fusion protein, a pharmaceutical composition for treating dystrophinopathies in mammals comprising the fusion protein, and nucleic acid constructs for expressing the fusion protein. | 03-17-2011 |
20110065654 | COMPOSITIONS AND METHODS FOR ALZHEIMER'S DISEASE - The present invention concerns methods and compositions of use for treatment of Alzheimer's Disease (AD). In certain embodiments, the methods concern preparation of phage-display single chain antibody libraries and screening against amyloid-beta (Aβ) protein or peptide. Anti-Aβ antibodies are selected and sequenced. In certain embodiments, synthetic Aβ binding peptides are designed and prepared, using portions of the anti-Aβ antibody sequences. The antibodies and peptides are of use for treatment of AD or for treatment of individuals at risk of developing AD. Compositions comprising anti-Aβ antibodies or Aβ binding peptides are also disclosed. | 03-17-2011 |
20110077210 | HDAC REGULATION ASSAYS, COMPOUNDS AND THERAPEUTIC COMPOSITIONS - This invention relates to the field of assays for compounds that interact with the binding of a PTB-containing protein, i.e. APPL (Adaptor protein containing PH domain, PTB domain and Leucine zipper motif) with histone deacetylase, in particular HDAC1. Compounds identified using said assays are useful in inhibiting HDAC activity and as a medicine, in particular in the manufacture of a medicament to inhibit proliferative conditions, such as cancer and psoriasis. | 03-31-2011 |
20110077211 | METHODS AND COMPOSITIONS FOR TREATING LUMINAL INFLAMMATORY DISEASE - Compositions, articles, and methods for treating and imaging vulnerable plaque and other inflamed regions in a patient rely on delivery of a conversion electron emitting source (CEES) to a body location. The CEES may be delivered by coupling to a substance which preferentially binds to vulnerable plaque or other inflammatory marker. Alternatively, the CEES can be delivered on a catheter, scaffold, or other device. | 03-31-2011 |
20110082093 | Methods and compositions for treating trinucleotide repeat disorders - Disclosed herein are methods and compositions for treating trinucleotide repeat disorders. | 04-07-2011 |
20110082094 | Mammalian Cytokine-Like Polypeptide-10 - A mammalian cytokine-like polypeptide, called Zcyto10, polynucleotides encoding the same, antibodies which specifically bind to the polypeptide, and anti-idiotypic antibodies which bind to the antibodies. Zcyto10 is useful for promoting the healing of wounds and for stimulating the proliferation of platelets. | 04-07-2011 |
20110082095 | NUCLEIC ACIDS AND CORRESPONDING PROTEINS ENTITLED 158P3D2 USEFUL IN TREATMENT AND DETECTION OF CANCER - A novel gene 158P3D2 and its encoded protein, and variants thereof, are described wherein 158P3D2 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, 158P3D2 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 158P3D2 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with 158P3D2 can be used in active or passive immunization. | 04-07-2011 |
20110092448 | Peptide Conjugate for Oral Delivery of Hydrophilic Peptide Analgesics - The present invention provides a method of improving the oral delivery of a parent peptide, comprising the step of linking the parent peptide to an added peptide to form a conjugate which has greater oral bioavailability than the parent molecule alone, the added peptide comprising a balance of hydrophobic and hydrophilic residues as defined herein. Conjugates for use in the method are also provided, as are pharmaceutical compositions comprising the conjugate and methods of treatment using the conjugate or pharmaceutical composition. | 04-21-2011 |
20110092449 | TREATMENT OF FIBROTIC CONDITIONS - Compositions, articles, devices and methods for the treatment of fibrosis and fibrotic diseases, disorders, and conditions in humans and non-human animals. | 04-21-2011 |
20110092450 | METHOD OF ENHANCING THE MOBILIZATION OF HEMATOPOIETIC STEM CELLS USING TAT-HOXB4H - The present invention relates to a new and nonobvious method of producing the C-terminal histidine tagged TAT-HOXB4 fusion protein (TAT-HOXB4H), providing unexpected benefits of increased yield and stability to allow for in vivo administration of this protein, and pharmaceutical composition comprising an effective ingredient, TAT-HOXB4H, having stimulatory activity on the production of hematopoietic cells. More specifically, recombinant TAT-HOXB4H protein enhances engraftment of bone marrow transplants, hematopoietic reconstruction, bone marrow re-population and number of circulating stem cells, particularly after chemotherapy or irradiation. | 04-21-2011 |
20110118194 | Therapeutic Use of LPI, a Staphylococcal Lectin Pathway Inhibitor in Inflammatory Diseases - The invention relates to nucleic acid molecules encoding (poly)peptides having LPI (Lectin Pathway Inhibitor) activity, to recombinant vectors harboring such molecules, and the host cells carrying the vectors. The invention further relates to methods for preparing recombinant (poly)peptides having LPI activity and to the use of such recombinant (poly)peptides having LPI activity for diagnosis, prophylaxis and treatment, such as the treatment of inflammation reactions. In addition the invention provides therapeutic and diagnostic compositions comprising as the active ingredient the (poly)peptide having LPI activity. | 05-19-2011 |
20110124580 | REGULATION OF LUNG TISSUE BY HEDGEHOG-LIKE POLYPEPTIDES, AND FORMULATIONS AND USES RELATED THERETO - The present application relates to a method for modulating the growth state of an lung tissue, or a cell thereof, e.g., by ectopically contacting the tissue, in vitro or in vivo, with a hedgehog therapeutic, a ptc therapeutic, or an FGF-10 therapeutic in an amount effective to alter the rate (promote or inhibit) of proliferation of cells in the lung tissue, e.g., relative to the absence of administration of the hedgehog therapeutic or ptc therapeutic. The subject method can be used, for example, to modulate the growth state of epithelial and/or mesenchymal cells of a lung tissue, such as may be useful as part of a regimen for prevention of a disease state, or in the treatment of an existing disease state or other damage to the lung tissue. | 05-26-2011 |
20110124581 | NUCLEIC AND AMINO ACID SEQUENCES FOR THE CONTROL OF PATHOGEN AGENTS - The present invention reveals a nucleic acid sequence from | 05-26-2011 |
20110130347 | IDENTIFICATION OF NEW SPLICE-VARIANTS OF G-PROTEIN COUPLED RECEPTOR EP3 AND USES THEREOF - The present invention is directed to a polynucleotide sequence of the novel G-Protein Coupled Receptors EP3-11 OR EP3-12. The present invention provides polynucleotide sequences comprising the nucleic acid sequence SEQ ID NO: 20 or SEQ ID NO: 21 or nucleic acid sequences that hybridize to SEQ ID NO: 20 or SEQ ID NO: 21 or its complimentary strand having at least 40% sequence identity. The invention also provides the human EP3-11 or EP3-12 as targets for the identification of compounds useful for the treatment and prevention of cardiovascular diseases, inflammation, reproduction disorders and cancer as a result of relative quantification of the mRNA distribution in different human tissues by expression profiling. The invention also provides assays for the identification of compounds modulating EP3-11 or EP3-12. | 06-02-2011 |
20110144036 | HIP/PAP Polypeptide Composition for Use in Liver Regeneration and for the Prevention of Liver Failure - This invention is based on the experimental finding that HIP/PAP has mitogenic and antiapoptotic effects in vitro on hepatocytes in primary culture. Moreover, HIP/PAP is a mitogenic and anti-apoptotic molecule for hepatocytcs, in vivo, during liver failure and liver regeneration. The present invention is also based on the experimental finding that HIP/PAP administration has no adverse effects in mammals. This invention concerns a pharmaceutical composition for stimulating liver regeneration in vivo including after chronic/acute liver failure, comprising an effective amount of a polypeptide comprising an amino acid sequence having 90% amino acid identity with the polypeptide consisting of the amino acid sequence starting at the amino acid residue (36) and ending at the amino acid residue (175) of sequence SEQ ID No 1, in combination with at least one physiologically acceptable excipient. | 06-16-2011 |
20110152202 | DEVELOPMENT OF C-REACTIVE PROTEIN MUTANT WITH IMPROVED THERAPEUTIC BENEFIT IN IMMUNE THROMBOCYTOPENIA AND LUPUS NEPHRITIS - The present invention relates to the use of a mutant CRP molecule in which tyrosine 175 is replaced by leucine (Y175L CRP) or the leucine 176 is replaced by glutamic acid (L176E CRP) for the treatment of various disease states and conditions associated with SLE, including lupus of the skin (discoid), systemic lupus of the joints, lungs and kidneys, hematological conditions including hemolytic anemia and low lymphocyte counts, lymphadenopathy and CNS effects, including memory loss, seizures and psychosis, among numerous others as otherwise disclosed herein. In another aspect of the invention, the reduction in the likelihood that a patient who is at risk for an outbreak of a disease state or condition associated with SLE will have an outbreak is an additional aspect of the present invention. The present invention relates to the use of mutant Y175L CRP or L176E CRP in the treatment of a number of disease states or conditions that occur secondary to systemic lupus SLE. The present invention also relates to the treatment of immune thrombocytopenic purpura. Pharmaceutical compositions are also disclosed based these mutant CRP molecules. | 06-23-2011 |
20110172168 | ILT-2 (LIR1) VARIANTS WITH INCREASED AFFINITY FOR MHC CLASS I MOLECULES - The present invention provides ILT-2 variants having the property of binding to a given Class IpMHC with a K | 07-14-2011 |
20110172169 | Method of Detection of Nucleic Acids with a Specific Sequence Composition - This invention is a novel method for detecting and localizing specific nucleic acid sequences in a sample with a high degree of sensitivity and specificity. The method and novel compositions used in the method involve the use of Probe Nucleic Acids, the production of nucleic acid binding regions and the use of nucleic acid Target Binding Assemblies to detect and localize specific Target Nucleic Acids. The detection and localization of the Target Nucleic Acid is accomplished even in the presence of nucleic acids which have similar sequences. The method provides for a high degree of amplification of the signal produced by each specific binding event. In particular, methods and compositions are presented for the detection of HIV and HPV nucleic acid in samples. These methods and compositions find use in diagnosis of disease, genetic monitoring, forensics, and analysis of nucleic acid mixtures. Some of the novel compositions used in the detection method are useful in preventing or treating pathogenic conditions. | 07-14-2011 |
20110172170 | INTERFERON-LIKE PROTEIN ZCYTO21 - The present invention relates to polynucleotide and polypeptide molecules for Zcyto21, an interferon-like protein, which is most closely related to interferon-α at the amino acid sequence level. The present invention also includes antibodies to the Zcyto21 polypeptides, and methods of using the polynucleotides and polypeptides. | 07-14-2011 |
20110178029 | Modified Human Apolipoprotein A-1 and Their Uses - Modified human apolipoprotein A-I polypeptides and uses thereof are provided. | 07-21-2011 |
20110178030 | METHODS OF TREATING INFLAMMATORY INTESTINAL DISEASE AND MANAGING SYMPTOMS THEREOF - Methods and products are disclosed for treating an inflammatory intestinal disease in a mammalian subject in need thereof, or preventing or reducing a symptom of inflammatory intestinal disease. These method include administering to the subject a therapeutically effective dose of (i) an isolated AvrA protein or polypeptide fragment thereof or (ii) a nucleic acid molecule encoding the isolated AvrA protein or polypeptide fragment. Preferred inflammatory intestinal diseases include Inflammatory Bowel Disease, Celiac Disease, and gastroenteritis. | 07-21-2011 |
20110183920 | MODIFIED IL-4 MUTEIN RECEPTOR ANTAGONISTS - This invention relates to modified IL-4 mutein receptor antagonists comprising an IL-4 mutein receptor antagonist coupled to polyethylene glycol. Related formulations and dosages and methods of administration thereof for therapeutic purposes are also provided. These modified IL-4 mutein receptor antagonists, compositions and methods provide a treatment option for those individuals afflicted with a respiratory disorder such as asthma by inhibiting IL-4 and IL-13-mediated airway hyperresponsiveness and eosinophilia. More particularly, these antagonists have an increased duration of effect versus unmodified IL-4RA by virtue of a greater plasma half-life. | 07-28-2011 |
20110190223 | HEMCM42 NUCLEIC ACIDS - The present invention relates to novel human secreted proteins and isolated nucleic acids containing the coding regions of the genes encoding such proteins. Also provided are vectors, host cells, antibodies, and recombinant methods for producing human secreted proteins. The invention further relates to diagnostic and therapeutic methods useful for diagnosing and treating disorders related to these novel human secreted proteins. | 08-04-2011 |
20110190224 | Non-Viral Delivery of Compounds to Mitochondria - A conjugate comprises: (a) a mitochondrial membrane-permeant peptide; (b) an active agent or compound of interest such as a detectable group or mitochondrial protein or peptide; and (c) a mitochondrial targeting sequence linking said mitochondrial membrane-permeant peptide and said active mitochondrial protein or peptide. The targeting sequence is one which is cleaved within the mitochondrial matrix, and not cleaved within the cellular cytoplasm, of a target cell into which said compound is delivered. Methods of use of such compounds are also described. | 08-04-2011 |
20110195916 | CYTOKINE PROTEIN FAMILY - The present invention relates to polynucleotide and polypeptide molecules for zcyto20, zcyto21, zcyto22, zycto24, and zcyto25 proteins which are most closely related to interferon-α at the amino acid sequence level. The receptor for this protein family is a class II cytokine receptor. The present invention includes methods of reducing viral infections and increasing monocyte counts. The present invention also includes antibodies to the zcyto20 polypeptides, and methods of producing the polynucleotides and polypeptides. | 08-11-2011 |
20110207677 | Use of Cell-Permeable Peptide Inhibitors of the JNK Signal Transduction Pathway for the Treatment of Chronic or Non-Chronic Inflammatory Digestive Diseases - The present invention refers to the use of protein kinase inhibitors and more specifically to the use of inhibitors of the protein kinase c-Jun amino terminal kinase, JNK inhibitor sequences, chimeric peptides, or of nucleic acids encoding same as well as pharmaceutical compositions containing same, for the treatment of non-chronic or chronic inflammatory digestive diseases, such as colitis, including e.g. Ulcerative colitis, Crohn's disease, diversion colitis, ischemic colitis, infectious colitis, fulminant colitis, chemical colitis, microscopic colitis, lymphocytic colitis, and atypical colitis, etc. | 08-25-2011 |
20110207678 | CD44 POLYPEPTIDES, POLYNUCLEOTIDES ENCODING SAME, ANTIBODIES DIRECTED THEREAGAINST AND METHOD OF USING SAME FOR DIAGNOSING AND TREATING INFLAMMATORY DISEASES - An isolated polypeptide is provided. The isolated polypeptide comprising an antigen recognition domain capable of specifically binding a CD44 polypeptide as set forth in SEQ ID NO: 2 and incapable of binding a CD44 polypeptide selected from the group consisting of: SEQ ID NO: 4 or 6. | 08-25-2011 |
20110245186 | RECOMBINANT E-SELECTIN MADE IN INSECT CELLS - The inventive features include recombinant mammalian E-selectin peptides, nucleic acids encoding said peptides, vectors and cells having these nucleic acids, and methods of making the peptides. Further inventive features include methods of treating diseases and conditions associated with inflammation using recombinant mammalian E-selectin peptides to induce mucosal tolerance to E-selectin. | 10-06-2011 |
20110257104 | METHODS TO IDENTIFY MACROMOLECULE BINDING AND AGGREGATION PRONE REGIONS IN PROTEINS AND USES THEREFOR - The present invention provides methods and computational tools based, at least in part, on computer simulations that identify macromolecule binding regions and aggregation prone regions of a protein. Substitutions may then be made in these aggregation prone regions to engineer proteins with enhanced stability and/or a reduced propensity for aggregation. Similarly, substitutions may then be made in these macromolecule binding regions to engineer proteins with altered binding affinity for the macromolecule. | 10-20-2011 |
20110288034 | Methods of identifying adipocyte specific genes, the genes identified, and their uses - Disclosed is a method of identifying genes that are over-expressed in adipose tissue as compared to pre-adipocyte tissue or other tissues comprising performing differential gene expression analysis between the white adipose tissue (WAT) or stromal vascular tissue (SVT) from any two different mice selected from the group consisting of wild-type, HMGI-C−/−, ob/ob, and HMGI-C−/− ob/ob genotype mice. Based on this method a number of nucleotide sequences are identified whose expression is adipocyte specific. The identified nucleotide sequences and their corresponding polypeptides are then used to prevent adipogenesis, to treat diabetes, and to screen for small-molecules that can modulate or prevent adipogenesis and to treat diabetes. | 11-24-2011 |
20110312900 | BChE ALBUMIN FUSIONS FOR THE TREATMENT OF COCAINE ABUSE - A method of attenuating a biological effect of cocaine exposure in a primate. Such method includes administering to the primate an amount of a BChE-albumin fusion protein comprising the amino acid substitutions A227S, S315G, A356W, and Y360G, wherein the amount of the fusion protein is effective to cause attenuation of the biological effect of cocaine exposure in the primate. | 12-22-2011 |
20110312901 | METHODS OF INHIBITING CELL DEATH OR INFLAMMATION IN A MAMMAL BY ADMINISTERING A BCL PROTEIN - In one aspect the present invention provides methods for inhibiting cell death or inflammation in a mammal, wherein the methods each include the step of administering to a mammal a Bcl protein in an amount sufficient to inhibit cell death or inflammation in the mammal. The invention also provides methods for identifying a Bcl protein that inhibits cell death or inflammation when administered to a mammal. | 12-22-2011 |
20110319344 | FLAGELLIN RELATED POLYPEPTIDES AND USES THEREOF - The use of flagellin and flagellin related polypectides for the protection of mammals from the effects of apoptsis is described. | 12-29-2011 |
20110319345 | Combination Therapy for Treatment of Cancer - The invention relates to compositions and methods for treating diseases. In particular aspects, the invention relates to administering a combination of a disintegrin with a microtubule stabilizing agent useful for treatment of cancer. | 12-29-2011 |
20110319346 | ELECTROSTATIC PROTEIN/GLUCOSINOLATE COMPLEXES - The present invention relates to the field of electrostatic complexes. Embodiments of the present invention relate to food-grade electrostatic complexes containing at least one milk protein and at least one glucosinolate and to the uses of such complexes, e.g., to reduce the perceived bitterness of glucosinolates and/or to form and stabilize emulsions and/or foams. | 12-29-2011 |
20120004185 | POLYPEPTIDE STRUCTURAL MOTIFS ASSOCIATED WITH CELL SIGNALING ACTIVITY - Isolated polypeptides comprising or consisting essentially of specific structural motifs (e.g., three β-sheets and two α-helices) are provided, wherein the polypeptides exhibit at least one cell signaling and/or other non-canonical activity of biological relevance. Also provided are polynucleotides encoding such polypeptides, binding agents that bind such polypeptides, analogs, variants and fragments of such polypeptides, etc., as well as compositions and methods of identifying and using any of the foregoing. | 01-05-2012 |
20120004186 | PLATELET AGGREGATION INHIBITOR COMPOSITION - The invention provides a pharmaceutical composition comprising at least one polypeptide of the following (a) to (d): | 01-05-2012 |
20120015890 | Use of Soluble Forms of CD83 and Nucleic Acids Encoding them for the Treatment or Prevention of Diseases - The present invention provides for the use of soluble forms of CD83 and nucleic acids encoding them for the treatment of diseases caused by the dysfunction or undesired function of a cellular immune response involving dendritic cells, T cells and/or B cells. The invention moreover provides soluble CD83 molecules specifically suited for said purpose, antibodies against said specific soluble CD83 proteins and assay methods and kits comprising said antibodies. | 01-19-2012 |
20120022005 | Synthetic Dragline Spider Silk-Like Proteins - The present application relates to isolated amino acid sequence comprising multiple repeats of a semi-synthetic spider silk protein domain, or any functional homolog, variant, derivative, fragment or mutant thereof. The amino acid sequence of the invention further comprises an N-terminal region and a C-terminal region. The invention further provides a nucleic acid encoding the amino acid sequence of the invention, an expression vector comprising said nucleic acid, a host cell transformed with said expression vector, a recombinant spider silk protein thus produced and a fiber composed of the recombinant spider silk protein. The invention further encompasses a composition comprising as an active ingredient said amino acid sequence or any said recombinant protein or fiber comprising the same. Lastly, the invention relates to an article comprising at least one fiber composed of said recombinant spider silk protein. | 01-26-2012 |
20120040917 | Splice Switching Oligomers for TNF Superfamily Receptors and Their Use in Treatment of Disease - The present invention relates to compositions and methods for preparing splice variants of TNFalpha receptor (TNFR) in vivo or in vitro, and the resulting TNFR protein variants. Such variants may be prepared by controlling the splicing of pre-mRNA molecules and regulating protein expression with splice switching oligonucleotides or splice switching oligomers (SSOs). The preferred SSOs according to the invention target exon 7 or 8 of TNFR1 (TNFRSF1A) or TNFR2 (TNFRSF1A) pre-mRNA, typically resulting in the production of TNFR variants which comprise a deletion in part or the entire exon 7 or 8 respectfully. SSOs targeting exon 7 are found to result in a soluble form of the TNFR, which has therapeutic benefit for treatment of inflammatory diseases. The SSO's are characterized in that they are substantially incapable or incapable of recruiting RNaseH. | 02-16-2012 |
20120071422 | Therapeutic application of isolated naturally-occuring soluble truncated forms of IL-23 receptor - The present invention relates to an isolated naturally-occurring soluble truncated IL-23Rα protein, which is a translated protein resulting from a mRNA splice variant of IL-23Rα. The soluble IL-23Rα proteins (e.g., Δ9 and Δ8,9) represents a novel soluble IL-23Rα protein, which is lacking a transmembrane domain and has a unique eight (8) amino acids (GLKEGSYC) at its C-terminus end (due to frame-shift). ELISA reveals that Δ9 is present in blood and can serve as a diagnostic tool for auto-immune diseases including Crohn's disease. There is also provided a method of recombinant production for this soluble truncated form of IL-23Rα protein. More importantly, the present invention provides an utility application of the Δ9 and Δ8,9 protein in inhibit IL-23R-mediated cell signaling. More particularly, Δ9 and Δ8,9 blocks STAT3 formation as well as Th17 maturation. There is provided a therapeutic application of Δ9 and Δ8,9 in treating a human patient inflicted with Crohn's disease. | 03-22-2012 |
20120077757 | Methods for Affecting Homology-Directed DNA Double Stranded Break Repair - Disclosed herein are methods and composition for alteration of the presence, activity, or concentration of RNF138. Disclosed methods can be utilized to affect DNA double strand break repair. Methods and compositions can be utilized to alter RNF138 so as to prevent interaction between RNF138 and RAD51D. Specifically, methods can prevent RNF138-directed ubiquitylation of RAD51D, which is necessary for DNA double strand break repair. | 03-29-2012 |
20120077758 | INFERTILITY ASSOCIATED DEFB-126 DELETION POLYMORPHISM - The present application provides diagnostic methods for determining the fertility status of a male individual by evaluating his DEFB-126 phenotypic and genotypic status. The present invention relates to a dinucleotide deletion polymorphism in the protein coding sequence of a DEFB-126 nucleic acid. The amino acid sequence of this variant has a significantly altered the carboxyl terminal, carbohydrate-containing domain of DEFB-126 in comparison to a wild-type DEFB-126 polypeptide. This variant results in aberrant protein function and structure, leading to reduced sperm function and fertility. The present invention provides methods for analyzing the genotype of individuals with respect to the gene encoding DEFB-126 in order to determine whether that individual has reduced fertility. Such determination will provide an individual knowledge of whether their genotype is associated with a risk of reduced fertility and to allow that individual to receive appropriate fertility treatment options. The present invention further provides kits that are useful for diagnosing increased risk or probability of infertility based on the presence or absence of the DEFB-126 deletion polymorphism. The application also provides therapeutic methods and compositions for restoring sperm functionality (e.g., to effect conception) in sperm from an individual who expresses insufficient levels of DEFB-126. | 03-29-2012 |
20120083456 | METHODS OF USING IL-31 TO TREAT CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) - Use of IL-31 agonists, including IL-31, are used to treat agonists are used to treat asthma, airway hyper-responsiveness or allergic rhinitis. The method comprise inhibiting, reducing, limiting or minimizing production of proinflammatory cytokines and include administration of the IL-31 agonist during sensitization or challenge resulting in the asthma, airway hyper-responsiveness or allergic rhinitis state. | 04-05-2012 |
20120094935 | METHODS FOR CREATING OR IDENTIFYING COMPOUNDS THAT BIND TUMOR NECROSIS FACTOR ALPHA - Methods for creating therapeutic candidate compounds or of identifying therapeutic candidate compounds for use in treating TNFα-mediated diseases or conditions are described that utilize parameters, including amino acid residues, obtained by analysis of a Yatapoxvirus 2L-TNFα crystal structure. | 04-19-2012 |
20120094936 | MalPEG-Hb Conjugate-Containing Compositions for Delivering Nitric Oxide (NO) to Cells - The present invention relates to compositions for delivering nitric oxide (NO) to cells using heme proteins as carriers. In one embodiment, the present invention relates to the use of MalPEG surface modified hemoglobin to deliver NO to cells. | 04-19-2012 |
20120094937 | MAMMALIAN CELL SURFACE ANTIGENS; RELATED REAGENTS - Purified genes encoding a T cell surface antigen from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this antigen are provided. Methods of using said reagents and diagnostic kits are also provided. | 04-19-2012 |
20120108523 | DISEASE-ASSOCIATED PROTEIN - Disclosed are methods and compositions for early diagnosis, monitoring and treatment of retinal dystrophy, age-related macular degeneration, Bardet-Biedel syndrome, Bassen-kornzweig syndrome, best disease, choroidema, gyrate atrophy, congenital amourosis, refsun syndrome, stargardt disease and Usher syndrome. In particular, the invention relates to a protein, termed “Rdcvf1,” that is differentially transcribed and expressed in subjects suffering from retinal dystrophies and the like, such as retinal dystrophy and age-related macular degeneration compared with nonsufferers, antibodies which recognize this protein, and methods for diagnosing such conditions. | 05-03-2012 |
20120122802 | ANIMAL PROTEIN-FREE PHARMACEUTICAL COMPOSITIONS - Animal protein-free, solid-form Clostridial toxin pharmaceutical compositions comprising a Clostridial toxin active ingredient and at least two excipients. | 05-17-2012 |
20120142611 | REPEAT PROTEIN FROM COLLECTION OF REPEAT PROTEINS COMPRISING REPEAT MODULES - A repeat protein from a collection of repeat proteins, wherein each repeat protein of said collection comprises a repeat domain, which comprises a set of consecutive repeat modules, wherein the repeat modules have the same fold and stack tightly to create a superhelical structure having a joint hydrophobic core, wherein each of the repeat modules is derived from one or more repeat units and wherein the repeat units comprise framework residues, which contribute to the folding topology of the repeat unit or contribute to an interaction with a neighboring repeat unit, and target interaction residues, which contribute to an interaction with a target substance, wherein the repeat proteins of the collection differ from other repeat proteins in the collection in at least one amino acid position of the repeat modules is described as are related pharmaceuticals and nucleic acid molecules. | 06-07-2012 |
20120142612 | CYTOKINE PROTEIN FAMILY - The present invention relates to polynucleotide and polypeptide molecules for zcyto20, zcyto21, zcyto22, zycto24, and zcyto25 proteins which are most closely related to interferon-α at the amino acid sequence level. The receptor for this protein family is a class II cytokine receptor. The present invention includes methods of reducing viral infections and increasing monocyte counts. The present invention also includes antibodies to the zcyto20 polypeptides, and methods of producing the polynucleotides and polypeptides. | 06-07-2012 |
20120149649 | SHORT-CHAIN CATIONIC POLYAMINO ACID AND USE THEREOF - The present invention provides a cationic polyamino acid suitable for a carrier that can form a stable complex with a nucleic acid under a physiological condition and release the nucleic acid in cells suitably. The cationic polyamino acid can associate with a nucleic acid and includes a cationic amino acid residue having a cationic group in a side chain and a hydrophobic amino acid residue having a hydrophobic group in a side chain. The cationic polyamino acid includes 1 to 20 units of the cationic amino acid residue and is represented by the following formula (1). | 06-14-2012 |
20120149650 | Diphtheria Toxin Variant - The present invention relates to methods and compositions of modified variants of diphtheria toxin (DT) that reduce binding to vascular endothelium or vascular endothelial cells, and therefore, reduce the incidence of Vascular Leak Syndrome. One aspect of the present invention relates to a polypeptide toxophore from a modified DT, wherein the mutation is the substitution or deletion at least one amino acid residue at the amino acid residues 6-8, 28-30 or 289-291 of native DT. Another aspect of the present invention relates to a fusion protein which comprises a modified DT and a non-DT fragment. Another aspect of the present invention relates to the use of modified DT for the treatment of cancer. | 06-14-2012 |
20120157393 | BIOPOLYMER, IMPLANT COMPRISING IT AND USES THEREOF - The present invention relates to a biopolymer, bioactive and totally biocompatible, very fluid at ambient temperature, capable of gelling in a sudden manner at 37° C., forming a solid implant, structurally integral and continuous having high mechanical properties. The biopolymer comprises at least a bioactive domain capable of directing in a precise manner the formation of a solid or semisolid implant. Furthermore the invention relates to any of the nucleic acids encoding the amino acid sequence of the biopolymer, implants, pharmaceutically acceptable vehicles, uses thereof, and a method of synthesis thereof. | 06-21-2012 |
20120165274 | THREE-DIMENSIONAL STRUCTURES OF TALL-1 AND ITS COGNATE RECEPTORS AND MODIFIED PROTEINS AND METHODS RELATED THERETO - Disclosed are TALL-1 and TALL-1 receptor protein homologues (agonists and antagonists) designed based on the three-dimensional structure of sTALL-1, eBCMA and eBAFF-R; agonist homologues of APRIL; methods of using wild-type APRIL to inhibit the activity of TALL-1; compositions comprising such homologues, nucleic acid molecules encoding such homologues, and therapeutic methods of using such compounds and compositions. Also disclosed are crystalline complexes of sTALL-1 and sTALL-1 in complex with either BCMA or BAFF-R; models of three-dimensional structures of such crystalline complexes and related structures, methods of drug design using any portion of such structures; methods of design and/or identification of regulatory peptides derived from the such structures; compounds identified by drug design using such structures; and the use of such compounds in therapeutic compositions and methods. | 06-28-2012 |
20120172316 | CLONING, YEAST EXPRESSION, PURIFICATION AND BIOLOGICAL ACTIVITY OF THE EXTENSION REGION OF THE SOYBEAN 7S GLOBULIN ALFA' SUBUNIT INVOLVED IN HEP G2 CELL CHOLESTEROL HOMEOSTASIS - A truncated form of α′ chain (eα′), the soybean 7S globulin, active in controlling the cholesterol and triglyceride homeostasis in in vitro and in vivo models, was cloned and expressed in the yeast | 07-05-2012 |
20120172317 | SILK FIBROIN HYDROGELS AND USES THEREOF - The present specification provides for methods for purifying fibroins, purified fibroins, methods of conjugating biological and synthetic molecules to fibroins, fibroins conjugated to such molecules, methods of making fibroin hydrogels, fibroin hydrogels and fibroin hydrogel formulations useful for a variety of medical uses, including, without limitation uses as bulking agents, tissue space fillers, templates for tissue reconstruction or regeneration, cell culture scaffolds for tissue engineering and for disease models, surface coating to improve medical device function, or drug delivery devices. | 07-05-2012 |
20120178703 | MULTIMERIC POLYPEPTIDES OF HLA-G INCLUDING AT LEAST TWO ALPHA3 DOMAINS AND PHARMACEUTICAL USES THEREOF - Multimeric polypeptides and pharmaceutical uses thereof; multimers comprising alpha3 peptides of an HLA-G antigen and methods of producing such multimers, pharmaceutical compositions comprising the same, as well as their uses for treating various diseases including organ/tissue rejection. | 07-12-2012 |
20120184498 | DERMASEPTIN B2 USED AS AN INHIBITOR OF THE GROWTH OF A TUMOR - The invention relates to the use of peptides corresponding to dermaseptin B2 or fragments thereof for treating proliferative diseases such as cancer or ocular lesions, and to pharmaceutical compositions containing such peptides. | 07-19-2012 |
20120208772 | CYTOKINE ZALPHA11 LIGAND - Antibodies that bind to polypeptides and peptides comprising the sequence of zalpha11 Ligand as shown in SEQ ID NO: 2 are described. The antibodies may bind the full length sequence of 162 amino acid residues or a fragment thereof, including a mature polypeptide of 131 amino acid residues and smaller polypeptide and peptide sequences. The antibodies may include antibodies that are polyclonal, monoclonal, murine, humanized or neutralizing. Methods for producing the antibodies are also described. | 08-16-2012 |
20120208773 | PHARMACEUTICAL COMPOSITIONS WITH TETRABENAZINE - The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder. | 08-16-2012 |
20120232021 | PEPTIDE LINKERS FOR POLYPEPTIDE COMPOSITIONS AND METHODS FOR USING SAME - Disclosed herein are novel peptide linkers and polypeptide compositions comprising the linkers (e.g., chimeric polypeptides) and methods of using the polypeptide compositions. The compositions and methods are particularly useful for targeting/delivering a polypeptide or protein of interest (e.g., a therapeutic polypeptide) to a cell, tissue or organ of interest in order to treat various diseases or disorders (e.g., lysosomal storage disorders). | 09-13-2012 |
20120232022 | BOTULINUM TOXIN TREATMENTS - A method and composition for treating a patient suffering from a disease, disorder or condition and associated pain include the administration to the patient of a therapeutically effective amount of a neurotoxin selected from a group consisting of Botulinum toxin types A, B, C, D, E, F and G. | 09-13-2012 |
20120232023 | WHEY PROTEIN PRODUCT AND A METHOD FOR ITS PREPARATION - The invention relates to a whey protein product having a ratio of whey protein to casein in the range from about 90:10 to about 50:50 and the total protein content of at least 20% on dry matter basis, and a method for its preparation. The product has a favourable amino acid composition and is especially suitable for athletes. | 09-13-2012 |
20120232024 | THERAPEUTIC USES OF SOLUBLE ALPHA-KLOTHO - The present invention relates to therapeutic uses of soluble alpha-Klotho. | 09-13-2012 |
20120238508 | Methods for Promoting Wound Healing and/or Reducing Scar Formation - The present invention provides methods for promoting wound healing and/or reducing scar formation, by administering to an individual in need thereof one or more of the heat shock protein 20-derived polypeptides disclosed herein. | 09-20-2012 |
20120245103 | Silk Proteins - The present invention provides silk proteins, as well as nucleic acids encoding these proteins. The present invention also provides recombinant cells and/or organisms which synthesize silk proteins. Silk proteins of the invention can be used for a variety of purposes such as in the manufacture of personal care products, plastics, textiles, and biomedical products. | 09-27-2012 |
20120270808 | COMPOSITIONS AND METHODS RELATED TO SYNCHRONOUS SELECTION OF HOMING PEPTIDES FOR MULTIPLE TISSUES BY IN VIVO PHAGE DISPLAY - Embodiments of the invention include methods for selecting in parallel (i.e., synchronously or simultaneously) peptides that target a number of organs, in which each peptide targets distinct tissues or organs. Typically, the methods of the invention provide for peptide selection in a Minimal number of subjects and still provides a selectively binding peptide. In certain aspects, methods of identifying peptides that bind to multiple selected tissues or organs of an organism may comprise the steps of administering a phage display library to a first subject; obtaining a sample of two or more selected tissues; obtaining phage displaying peptides that bind to the samples from the first subject; enriching for peptides by administering phage isolated from the samples of the first subject to a second subject; obtaining a sample of two or more selected tissues from the second subject; and identifying the peptides displayed. | 10-25-2012 |
20120270809 | HUMAN TRANSMEMBRANE PROTEINS - The invention provides human transmembrane proteins (HTMPN) and polynucleotides which identify and encode HTMPN. The invention also provides expression vectors, host cells, antibodies, agonists, and antagonists. The invention also provides methods for diagnosing, treating, or preventing disorders associated with expression of HTMPN. | 10-25-2012 |
20120270810 | MODIFICATION OF ENZYMATIC CROSSLINKERS FOR CONTROLLING PROPERTIES OF CROSSLINKED MATRICES - Improved matrix or hydrogel that is formed by enzymatic crosslinking of polymers wherein the crosslinking enzyme molecules have been modified for the purpose of improving the crosslinking density, mechanical properties, or other properties of the matrix, and/or to provide improved control over the rate and/or extent of crosslinking, wherein the enzyme molecules are modified to alter the perceived volume of the enzyme molecules in the crosslinked matrix being formed. Methods of production and of use are also provided. | 10-25-2012 |
20120295854 | Methods of Inducing Tissue Regeneration - Methods are provided for producing cells within a lineage (lineage restricted cells) from post-mitotic differentiated cells of the same lineage ex vivo and in vivo, and for treating a subject in need of tissue regeneration therapy by employing these lineage-restricted cells. In addition, the production of lineage restricted cells from postmitotic tissues derived from patients with diseases allows for a characterization of pathways that have gone awry in these diseases and for screening of drugs that will ameliorate or correct the defects as a means of novel drug discovery. Also provided are kits for performing these methods. | 11-22-2012 |
20130005667 | HETEROLOGOUS EXPRESSION OF NEISSERIAL PROTEINS - Alternative and improved approaches to the heterologous expression of the proteins of Neisseria meningitidis and | 01-03-2013 |
20130005668 | NUCLEIC ACIDS AND CORRESPONDING PROTEINS ENTITLED 158P3D2 USEFUL IN TREATMENT AND DETECTION OF CANCER - A novel gene 158P3D2 and its encoded protein, and variants thereof, are described wherein 158P3D2 exhibits tissue specific expression in normal adult tissue, and is aberrantly expressed in the cancers listed in Table I. Consequently, 158P3D2 provides a diagnostic, prognostic, prophylactic and/or therapeutic target for cancer. The 158P3D2 gene or fragment thereof, or its encoded protein, or variants thereof, or a fragment thereof, can be used to elicit a humoral or cellular immune response; antibodies or T cells reactive with 158P3D2 can be used in active or passive immunization. | 01-03-2013 |
20130012455 | Use of ARC for inhibiting cell death during liver failure - The invention refers to the use of a polynucleotide encoding “apoptosis repressor with caspase recruitment domain” (ARC) or a functional fragment thereof, and/or an ARC polypeptide or a functional fragment thereof for inhibiting cell death of a liver cell, in particular during liver failure. | 01-10-2013 |
20130018003 | COMPOSITIONS AND METHODS FOR TREATING AIDS OR CANCER BY INHIBITING THE SECRETION OF MICROPARTICLES - Novel peptides that inhibit the release of microparticles from cells are disclosed. The peptide contains at least one VGFPV motif at the N-terminal and has a length of 10-100 amino acids. Also disclosed is polynucleotide encoding the peptide, expression vectors carrying the polynucleotide, and methods for treating AIDS and tumors using the novel peptides. | 01-17-2013 |
20130072445 | DEVELOPMENT OF C-REACTIVE PROTEIN MUTANT WITH IMPROVED THERAPEUTIC BENEFIT IN IMMUNE THROMBOCYTOPENIA AND LUPUS NEPHRITIS - The present invention relates to the use of a mutant CRP molecule in which tyrosine 175 is replaced by leucine (Y175L CRP) or the leucine 176 is replaced by glutamic acid (L176E CRP) for the treatment of various disease states and conditions associated with SLE, including lupus of the skin (discoid), systemic lupus of the joints, lungs and kidneys, hematological conditions including hemolytic anemia and low lymphocyte counts, lymphadenopathy and CNS effects, including memory loss, seizures and psychosis, among numerous others as otherwise disclosed herein. In another aspect of the invention, the reduction in the likelihood that a patient who is at risk for an outbreak of a disease state or condition associated with SLE will have an outbreak is an additional aspect of the present invention. The present invention relates to the use of mutant Y175L CRP or L176E CRP in the treatment of a number of disease states or conditions that occur secondary to systemic lupus SLE. The present invention also relates to the treatment of immune thrombocytopenic purpura. Pharmaceutical compositions are also disclosed based these mutant CRP molecules. | 03-21-2013 |
20130085113 | TEAR LIPOCALIN IN MUTEINS BINDING IL-4 R ALPHA - The present invention relates to novel muteins derived from human tear lipocalin, which bind to IL 4 receptor alpha. The sequences of the muteins comprise particular combinations of amino acids. In particular a mutated amino acid residue is present at any one or more of the sequence positions 27, 28, 30, 31, 33, 53, 57, 61, 64, 66, 80, 83, 104-106 and 108 of the linear polypeptide sequence of the mature human tear lipocalin. A mutated amino acid residue is also present at any 2 or more of the sequence positions 26, 32, 34, 55, 56, 58 and 63 of the linear polypeptide sequence of the mature human tear lipocalin. The invention also provides a corresponding nucleic acid molecule encoding such a mutein and a method for producing such a mutein and its encoding nucleic acid molecule. | 04-04-2013 |
20130090294 | NOVEL METHODS OF USE OF HSP70 FOR INCREASED PERFORMANCE OR TREATMENT OF HSP70 RELATED DISORDERS - The present invention relates to novel therapies that utilize exogenous HSP70 for the treatment of disorders or conditions regulated by HSP70 through administration of exogenous HSP70. | 04-11-2013 |
20130109634 | Casein Peptide For Use In The Treatment Of Uterine Infections | 05-02-2013 |
20130116201 | USE OF PEPTIDES AS TRANSPORTERS INTENDED FOR THE INTERNALIZATION OF MOLECULES OF INTEREST INTO TARGET CELLS - The method pertains to a peptide including the amino acid sequence SEQ ID NO: 1, or a peptide including an amino acid sequence having 93%, in particular 95%, particularly 98% sequence identity homology with the sequence SEQ ID NO: 1, in order to obtain a transporter intended for the internalization of a molecule of diagnostic or therapeutic interest into the target cells. | 05-09-2013 |
20130123198 | MODULATION OF SCLERAXIS USING A DOMINANT NEGATIVE SCLERAXIS MUTANT WITH A BASIC DNA-BINDING DOMAIN DELETION - Compositions and kits for modulating expression of scleraxis and/or collagen synthesis in mammalian cells and tissues. The compositions and kits comprise a protein comprising an amino acid sequence that shares at least 75% homology with SEQ ID NO:11. Proteins comprising amino acid sequences that share at least 75% homology with SEQ ID NO: 11 are expressed by mutants of scleraxis gene wherein a nucleotide sequence comprising a basic DNA binding domain has been deleted. Such mutants are exemplified by basic domain deletion ScxΔBD mutants that comprise nucleotide sequences sharing at least 75% homology with SEQ ID NO:8 or SEQ ID NO: 10. Methods for modulating fibrosis in a subject comprising administration of a composition comprising at least one physiologically effective dosage of a protein comprising a polypeptide molecule comprising an amino acid sequence that shares at least 75% homology with SEQ ID NO: 11. | 05-16-2013 |
20130123199 | PROTEIN COMPLEX FOR INTRACELLULAR DELIVERY AND USES THEREOF - A protein complex comprising an in vitro stabilization protein, a membrane translocation sequence domain, a biologically active molecule, and an in vivo stabilization protein, as well as methods for the use and production thereof. | 05-16-2013 |
20130123200 | MAMMALIAN CELL SURFACE ANTIGENS; RELATED REAGENTS - Purified genes encoding a T cell surface antigen from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this antigen are provided. Methods of using said reagents and diagnostic kits are also provided. | 05-16-2013 |
20130172274 | METHODS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS WITH ENHANCED PHARMACOLOGICAL PROPERTIES - Provided herein are methods of enhancing in vivo efficacy of an active agent, comprising: administering to a subject an active agent that is coupled to a bioelastic polymer or elastin-like peptide, wherein the in vivo efficacy of the active agent is enhanced as compared to the same active agent when administered to the subject not coupled to (or not associated with) a bioelastic polymer or ELP. | 07-04-2013 |
20130196931 | MEANS AND METHODS FOR COUNTERACTING PROTEIN AGGREGATION - The invention provides a use of a substance that is capable of enhancing the amount and/or activity of DnaJB8, or a functional part, derivative and/or analogue thereof, for counteracting protein aggregation. | 08-01-2013 |
20130196932 | Frataxin Mutants - Described herein are compositions and methods for treating Friedreich's Ataxia (FRDA). In some aspects, mutant forms of frataxin which are resistant to ubiquitination are provided. In some aspects, pharmaceutical compositions comprising mutant frataxin are provided. In further aspects, methods of using mutant frataxin are provided. | 08-01-2013 |
20130203682 | RANK LIGAND POLYPEPTIDES - Described herein are cell lines and methods for preparing antibodies that bind RANKL, including cell lines that produce blocking antibodies to human RANKL. | 08-08-2013 |
20130210747 | Methods and Therapeutics Comprising Ligand-Targeted ELPs - Disclosed herein are novel methods and compositions for targeting drug delivery systems to specific cells. One aspect relates to a drug delivery system comprising an elastin-like peptide (ELP) component and a ligand selected from the group consisting of mIgA and knob capable of either drug encapsulation or drug attachment. Further aspects relate to drug delivery systems comprising an elastin-like peptide (ELP) component and a ligand; wherein the ligand specifically binds to a receptor selected from the group consisting of CAR and pIgR. Further aspects include the novel transcytosing properties of the elastin-like peptide and the ligand, knob. Also provided are methods and pharmaceutical compositions comprising the disclosed therapeutics. | 08-15-2013 |
20130217637 | MUTANT NGAL PROTEINS AND USES THEREOF - In one aspect the present invention is directed to mutant NGAL proteins that have the ability to bind to siderophores, such as enterochelin, and to chelate and transport iron, and that are excreted in the urine. Such NGAL mutants, and complexes thereof with siderophores, can be used to clear excess iron from the body, for example in the treatment of iron overload. The NGAL mutants of the invention also have antibacterial activity and can be used in the treatment of bacterial infections, such as those of the urinary tract. | 08-22-2013 |
20130231293 | COMPOSITIONS AND METHODS FOR THE THERAPY AND DIAGNOSIS OF INFLAMMATORY BOWEL DISEASE - Compositions and methods for the therapy and diagnosis of Inflammatory Bowel Disease (IBD), including Crohn's Disease and Ulcerative Colitis, are disclosed. Illustrative compositions comprise one or more bacterial polypeptides, immunogenic portions thereof, polynucleotides that encode such polypeptides, antigen presenting cell that expresses such polypeptides, and T cells that are specific for cells expressing such polypeptides. The disclosed compositions are useful, for example, in the diagnosis, prevention and/or treatment of IBD. | 09-05-2013 |
20130244954 | USE OF REG4 AND PHARMACEUTICAL COMPOSITION THEREOF - The invention is in the field of biotechnology. Specifically it describes the application and pharmaceutical composition of Reg4. The invention describes the applications of the protein as following in (a) or (b) in preparing drugs for treating acute pancreatitis: (a) the protein whose amino acid sequence is shown as SEQ ID NO. 1, or bioactive fragments, or analogs; (b) the proteins whose amino acid sequence have at least 70% homology comparing with amino acid sequence described in (a) and have activity for treating acute pancreatitis. The protein described in this invention treats acute pancreatitis effectively and may provide new therapy for treating acute pancreatitis clinically. | 09-19-2013 |
20130244955 | BINDING PROTEINS FOR HEPCIDIN - The present invention relates to novel, specific-binding therapeutic and/or diagnostic proteins directed against Hepcidin, which proteins preferably are muteins of a lipocalin protein. The invention also relates to nucleic acid molecules encoding such proteins and to methods for generation and use of such proteins and nucleic acid molecules. Accordingly, the invention also is directed to pharmaceutical and/or diagnostic compositions comprising such a lipocalin proteins, including uses of these proteins. | 09-19-2013 |
20130296257 | COBALAMIN ACQUISITION PROTEIN AND USE THEREOF - The present invention relates to a cobalamin acquisition protein, compositions containing the cobalamin acquisition protein, and the use of such compositions. | 11-07-2013 |
20130296258 | MUTEINS OF HUMAN LIPOCALIN 2 WITH AFFINITY FOR GLYPICAN-3 (GPC-3) - Described are specific-binding therapeutic and/or diagnostic proteins directed against Glypican-3 (GPC3), which proteins include muteins of a lipocalin protein, such as lipocalin 2 (Lcn2 or NGAL). The invention also relates to nucleic acid molecules encoding such proteins and to methods for generation and use of such proteins and nucleic acid molecules. Accordingly, the invention also is directed to pharmaceutical and/or diagnostic compositions comprising such lipocalin proteins, including uses of these proteins. | 11-07-2013 |
20130296259 | PHARMACEUTICAL COMPOSITIONS CONTAINING BOTULINUM NEUROTOXIN - This invention relates to the use of a composition comprising a polysaccharide and a botulinum toxin for reducing a skin wrinkle. In some embodiments, the polysaccharide comprises disaccharides. In some embodiments, the average molecular weight of a disaccharide unit of the polysaccharide is between about 345 D and about 1,000 D. | 11-07-2013 |
20130316962 | Muteins of hNGAL and related proteins with affinity for a given target - The present invention relates to novel muteins derived from human lipocalin 2 (hNGAL) and related proteins that bind a given non-natural ligand with detectable affinity. The invention also related to corresponding nucleic acid molecules encoding such a mutein and to a method for their generation. The invention further relates to a method for producing such a mutein. Furthermore, the invention is directed to a pharmaceutical composition comprising such a lipocalin mutein as well as to various uses of the mutein. | 11-28-2013 |
20130324483 | MAMMALIAN CELL SURFACE ANTIGENS; RELATED REAGENTS - Purified genes encoding a T cell surface antigen from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this antigen are provided. Methods of using said reagents and diagnostic kits are also provided. | 12-05-2013 |
20130345152 | COMPOSITIONS COMPRISING RECOMBINANT COWPOX VIRUS PROTEIN CPXV014 - Disclosed herein are expression vectors that encode cowpox virus protein CPXV014 and homologs thereof that are useful in inhibiting CD3/CD28 mediated T cell stimulation. Further disclosed are polypeptide compositions comprising CPXV014 and homologs thereof as well as methods of inhibiting CD3/CD28 mediated T cell stimulation using the polypeptide compositions. | 12-26-2013 |
20130345153 | TOPICAL PREVENTATIVE MEDICAMENT AGAINST BURNS-RELATED SYSTEMIC INFLAMMATORY RESPONSE SYNDROME - A topical preventative medicament against burns-related systemic inflammatory response syndrome containing a low-molecular-weight chaperone as the main active ingredient. | 12-26-2013 |
20140038908 | Polynucleotides and Polypeptides Associated with Trophoblast Cell Death, Differentiation, Invasion and/or Cell Fusion and Turnover - The invention relates to polypeptides and polynucleotides associated with trophoblast cell death, differentiation, invasion, and/or cell fusion and turnover, and uses of same in the prevention, diagnosis and treatment of conditions requiring regulation of trophoblast cell death, differentiation, invasion, and/or cell fusion and turnover. In particular aspects, diagnostic methods are disclosed for evaluating conditions such as preeclampsia utilizing matador polypeptides and polynucleotides encoding same. | 02-06-2014 |
20140045775 | SHORT-FORM HUMAN MD-2 AS A NEGATIVE REGULATOR OF TOLL-LIKE RECEPTOR 4 SIGNALING - The present invention is based on a novel, alternatively spliced human isoform of MD-2 (MD-2s). In addition, the present invention relates to modified MD-2 proteins, wherein one or more tyrosine residues have been mutated to phenylalanine. In various embodiments, the invention relates to methods and kits for preventing, reducing the likelihood of developing and/or treating various conditions using MD-2s. The invention also describes methods of determining the risk of a subject to various conditions. | 02-13-2014 |
20140051645 | MUTEINS OF HUMAN LIPOCALIN 2 WITH AFFINITY FOR CTLA-4 - The present invention relates to novel, specific-binding therapeutic and/or diagnostic proteins directed against Cytotoxic T-Lymphocyte Antigen 4 (CTLA-4) also known as CD152, which proteins preferably are muteins of a lipocalin protein, more preferably of lipocalin 2 (Lcn2 or NGAL). The invention also relates to nucleic acid molecules encoding such proteins and to methods for generation and use of such proteins and nucleic acid molecules. Accordingly, the invention also is directed to pharmaceutical and/or diagnostic compositions comprising such lipocalin proteins, including uses of these proteins. | 02-20-2014 |
20140057858 | METHOD FOR INCREASING EMBRYO IMPLANTATION RATE IN MOTHER'S UTERUS IN MAMMALS, USE OF AN EFFECTIVE AMOUNT OF BETA-GALACTOSIDE-BINDING LECTIN OR DERIVATIVES THEREOF, BETA-GALACTOSIDE-BINDING LECTIN OR DERIVATIVES AND PRODUCT - The present invention relates to a method for increasing embryo implantation rate in mother's uterus in mammals by administering to the uterus of a mammal an effective amount of beta-galactoside-binding lectin or derivatives thereof, as well as to a product comprising said lectin. | 02-27-2014 |
20140107042 | COMPOSITIONS, METHODS AND USES FOR RADIOPROTECTANTS - Embodiments herein report methods and compositions for treating or preventing adverse effects of radiation therapies. In certain embodiments, compositions and methods relate to reducing or inhibiting damage due to acute, periodic or chronic radiation exposure. | 04-17-2014 |
20140113873 | CHITIN BINDING PROTEINS AND METHODS OF USE - Disclosed herein are methods of increasing epithelial cell proliferation (such as intestinal epithelial cell proliferation) by contacting epithelial cells with one or more CBPs. In some examples, the methods include administering the CBP to a subject, such as a subject in need of increased epithelial cell proliferation. Also disclosed herein are methods of identifying a subject having or at risk of developing hyperproliferation of epithelial cells (such as intestinal epithelial cells). Further disclosed are methods of decreasing epithelial cell proliferation by decreasing expression and/or activity of a CBP and methods of identifying inhibitors of epithelial cell proliferation and/or CBP activity. | 04-24-2014 |
20140121171 | TREATMENT FOR MUSCULAR DYSTROPHIES - miRNA-21 inhibitors and pharmaceutical compositions including an miRNA-21 inhibitor together with pharmaceutical excipients and carriers for use in the treatment of a muscular dystrophy and/or a muscular dystrophy-like myopathy. Particularly, the miRNA-21 inhibitors and pharmaceutical compositions including the same are for use in the regeneration of skeletal muscle in muscular dystrophy and/or a muscular dystrophy-like myopathy patients. | 05-01-2014 |
20140135275 | MITOCHONDRIAL TARGETING AND THERAPEUTIC USE THEREOF - The present invention provides, among other things, compositions and methods for treatment of Friedrich's Ataxia based on effective targeting of a therapeutic moiety to mitochondria that can substitute for natural FXN protein activity or rescue one or more phenotypes or symptoms associated with frataxin-deficiency. In some embodiments, the present invention provides a targeted therapeutic comprising a therapeutic moiety, which is a polypeptide having an N-terminus and a C-terminus, a mitochondrial targeting sequence associated with the therapeutic moiety at the N-terminus, and a mitochondrial membrane-penetrating peptide associated with the therapeutic moiety at the C-terminus, wherein the therapeutic moiety is targeted to mitochondria upon cellular entry. | 05-15-2014 |
20140142048 | FIBROUS PROTEIN FUSIONS AND USE THEREOF IN THE FORMATION OF ADVANCED ORGANIC/INORGANIC COMPOSITE MATERIALS - The claimed invention provides a fusion polypeptide comprising a fibrous protein domain and a mineralization domain. The fusion is used to form an organic-inorganic composite. These organic-inorganic composites can be constructed from the nano- to the macro-scale depending on the size of the fibrous protein fusion domain used. In one embodiment, the composites can also be loaded with other compounds (e.g., dyes, drugs, enzymes) depending on the goal for the materials, to further enhance function. This can be achieved during assembly of the material or during the mineralization step in materials formation. | 05-22-2014 |
20140148396 | COMPOUNDS FOR TREATING CARDIAC DAMAGE AFTER ISCHAEMIA/REPERFUSION - The present invention relates to the use of an EMMPRIN inhibitor for preventing and/or treating cardiac damage arising after an ischemic process followed by reperfusion. The authors of the present invention have observed that EMMPRIN expression increases in subjects who have suffered ischemia/reperfusion, ascertaining that an EMMPRIN inhibitor is capable of reducing the cardiac damage caused after ischemia followed by reperfusion, both in vitro and in vivo. | 05-29-2014 |
20140187502 | PEPTIDE LINKERS FOR POLYPEPTIDE COMPOSITIONS AND METHODS FOR USING SAME - Disclosed herein are novel peptide linkers and polypeptide compositions comprising the linkers (e.g., chimeric polypeptides) and methods of using the polypeptide compositions. The compositions and methods are particularly useful for targeting/delivering a polypeptide or protein of interest (e.g., a therapeutic polypeptide) to a cell, tissue or organ of interest in order to treat various diseases or disorders (e.g., lysosomal storage disorders). | 07-03-2014 |
20140194370 | SILK-ELASTIN LIKE PROTEIN POLYMERS FOR EMBOLIZATION AND CHEMOEMBOLIZATION TO TREAT CANCER - A chemoembolic agent is disclosed that includes an injectable, recombinantly synthesized silk-elastin like protein copolymer and one or more chemotherapeutic agents. Upon injection, the chemoembolic agent blocks the tumor vasculature, including the capillary bed, and may optionally release chemotherapeutic agents. The chemoembolic agent may be used to treat cancer, including hepatocellular carcinoma. | 07-10-2014 |
20140200187 | Cell-Permeable Peptide Inhibitors of the JNK Signal Transduction Pathway - The present invention refers to protein kinase inhibitors and more specifically to inhibitors of the protein kinase c-Jun amino terminal kinase. Additionally, the present invention provides JNK inhibitor sequences, chimeric peptides, nucleic acids encoding same as well as pharmaceutical compositions for treating pathophysiologies associated with JNK signaling. | 07-17-2014 |
20140249093 | Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages - The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (α-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs. | 09-04-2014 |
20140249094 | SENSATION-IMPROVING AGENT - An object of the present invention is to provide a safety sensation-improving agent that can improve dulled peripheral sensations through daily ingestion or application to the skin. Another object of the present invention is to provide a sensation-improving food, beverage, feed, or cosmetics that can improve dulled peripheral sensations through oral ingestion or application to the skin. A sensation-improving agent containing a milk-derived protein and/or a hydrolysate therefrom as an active ingredient is provided. The milk-derived protein and/or the hydrolysate therefrom can be orally ingested or applied direct to the skin to improve dulled sensations, particularly peripheral sensations, and be formed into a sensation-improving food, beverage, feed, or cosmetics. | 09-04-2014 |
20140256652 | Polypeptides Involved In Immune Response - Novel polypeptides which comprise a receptor-ligand pair involved in T-cell activation are disclosed. Nucleic acid molecules encoding said polypeptides, and vectors and host cells for expressing same are also disclosed. The polypeptides, or agonists and antagonists thereof, are used to treat T-cell mediated disorders. | 09-11-2014 |
20140256653 | WHEY PROTEIN MICELLES TO ENHANCE MUSCLE MASS AND PERFORMANCE - The present invention relates to a non-therapeutic use of whey protein micelles to enhance muscle protein synthesis in a subject. Further aspects of the invention are food compositions comprising whey protein micelles to be administered to children, athletes or elderly persons. | 09-11-2014 |
20140274915 | Methods of Use for Recombinant Human Secretoglobins - Methods of synthetically producing, formulating and using secretoglobins SCGB1A1, SCGB3A2, and SCGB3A1 are provided. Methods of using secretoglobins SCGB1A1, SCGB3A2, and SCGB3A1 as therapeutic agents to affect long term patient outcomes, such as preventing severe respiratory exacerbations of underlying conditions that require medical intervention, including hospitalization are provided. Methods of producing recombinant human secretoglobins, analytical methods, pharmaceutical compositions, and methods of use to prevent the long term sequelae of acute and chronic respiratory conditions are provided. | 09-18-2014 |
20140288008 | NOVEL BINDING PROTEINS FOR PCSK9 - The present disclosure relates to novel lipocalin muteins which bind to PCSK9. The disclosure also provides corresponding nucleic acid molecules encoding lipocalin muteins and methods for producing lipocalin muteins as well as their encoding nucleic acid molecules. | 09-25-2014 |
20140288009 | Collagen-like Silk Genes - The present invention relates to silk proteins which can be used to produce silk with a collagen-like structure, as well as nucleic acids encoding such proteins. The present invention also relates to recombinant cells and/or organisms which synthesize silk proteins. Silk proteins of the invention can be used for a variety of purposes such as in the production of personal care products, plastics, textiles, and biomedical products. | 09-25-2014 |
20140296162 | Whey Protein Composition with a Reduced Astringency - The invention relates to a sterilized liquid or semi-solid acid enteral composition comprising per 100 ml 9 to 20 g of non-hydrolysed globular proteins, fat and at least 100 mg of divalent metal cations and having a pH ranging between 3 and 5. The invention further relates to a method for preparing a composition according to the invention, comprising a step wherein at least the non-hydrolysed globular proteins are subjected to a direct steam injection (DSI) at specific holding values, such as a holding temperature of 100 to 140° C. during a holding time of about 0.5 to 10 seconds, followed by a homogenization step and a sterilization step The composition according to the invention has a reduced astringency and can be used for medical purposes, such as for stimulating muscle protein synthesis in a mammal, in particular for treating sarcopenia, and for specific groups of people, such as elderly and sportsman. | 10-02-2014 |
20140303093 | MICRO-UTROPHIN POLYPEPTIDES AND METHODS - Described herein are polypeptides, polynucleotides and methods involving a μ-utrophin region or an anti-dystrophinopathic fragment thereof operationally linked to a second region effective to transduce the fusion protein into mammalian muscle cells. | 10-09-2014 |
20140303094 | COMPOSITION AND USE THEREOF IN THE TREATMENT OF ANAL RHAGADES - The present invention relates to a composition comprising at least one protein extract of hibiscus and/or at least one beta glucan or a salt thereof. Furthermore, the present invention relates to the use of said composition for the treatment of anal rhagades. | 10-09-2014 |
20140309177 | COMPOSITIONS AND METHODS FOR THE INDUCTION AND TUNING OF GENE EXPRESSION - Disclosed herein are compositions of transcription activator-like effectors transcription factors and methods of using said compositions for inducing gene expression of mammalian genes. | 10-16-2014 |
20140315830 | RICE-PROTEIN COMPOSITION AND METHOD FOR MANUFACTURING SAME - The objective of the present invention is to provide a high-purity rice-protein composition with improved tongue feel and a melt-in-the-mouth quality, and a method for manufacturing the composition. The rice-protein composition comprises glutelin and prolamine, the protein content with respect to the solid content being at least 90%. Rice protein extracted by an alkaline solution from rice or rice flour is neutralized and coagulated at a temperature no lower than 40 80 DEG C., or is coagulated by adding a divalent metal ion and then neutralized, or glucono-delta-lactone is added and the solution is heated to gel the protein; by therein keeping the pH of the rice-protein composition no lower than 7.0 or no higher than 4.0, a rice-protein composition with extremely good dispersibility and tongue feel can be obtained. Further, by heating to at least 80 DEG C. after adjusting pH, a composition with high water absorbency is achieved. | 10-23-2014 |
20140323413 | METHODS OF DIAGNOSING AND TREATING VASCULAR ASSOCIATED MACULOPATHY AND SYMPTOMS THEREOF - Disclosed herein are methods and compositions for the diagnosis and treatment of Vascular Associated Maculopathy, or a symptom thereof, in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of one or more symptoms associated with Vascular Associated Maculopathy Disclosed in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of severe maculopathy or last stage maculopathy in a subject. Disclosed herein are methods and compositions for the diagnosis and treatment of resolving aberrant choriocapillaris lobules in a subject. | 10-30-2014 |
20140329764 | NOVEL METHODS OF USE OF HSP70 FOR INCREASED PERFORMANCE OR TREATMENT OF HSP70 RELATED DISORDERS - The present invention relates to novel therapies that utilize exogenous HSP70 for the treatment of disorders or conditions regulated by HSP70 through administration of exogenous HSP70. | 11-06-2014 |
20140336133 | METHODS AND COMPOSITIONS FOR TREATING HUNTINGTON'S DISEASE - Disclosed herein are methods and compositions for treating or preventing Huntington's Disease. | 11-13-2014 |
20140357576 | METHODS FOR ENHANCEMENT OF MUSCLE PROTEIN SYNTHESIS - The present disclosure provides methods for enhancing muscle protein synthesis in an individual in need of same. Specifically, the present disclosure provides methods for enhancing muscle protein synthesis by enhancing myofibrillar muscle protein synthesis. The method includes administering to the individual a mixed macronutrient composition having (i) an amount of whey protein that is not capable of enhancing myofibrillar protein synthesis when ingested by itself and (ii) free leucine. The composition comprises at least about 5.0 g total leucine per dose. | 12-04-2014 |
20150011482 | Nutritive Fragments, Proteins and Methods - Nutritive proteins are provided. In some embodiments the nutritive proteins comprise a first polypeptide sequence comprising a fragment of a naturally-occurring nutritive protein. In some embodiments the fragment comprises at least one of a) an enhanced ratio of branch chain amino acid residues to total amino acid residues present in the nutritive protein; b) an enhanced ratio of leucine residues to total amino acid residues present in the nutritive protein; and c) an enhanced ratio of essential amino acid residues to total amino acid residues present in the nutritive protein. In some embodiments, the fragment comprises at least one of a) a ratio of branch chain amino acid residues to total amino acid residues present in the nutritive protein; b) a ratio of leucine residues to total amino acid residues present in the nutritive protein; and c) a ratio of essential amino acid residues to total amino acid residues present in the nutritive protein, that is equal to or greater than the corresponding ratio present in a benchmark protein such as whey, egg or soy protein. Also provided are nucleic acids encoding the proteins, recombinant microorganisms that make the proteins, methods of making the proteins using recombinant microorganisms, compositions that comprise the proteins, and methods of using the proteins, among other things. | 01-08-2015 |
20150025022 | NOVEL IL-17R-ECD MUTANTS - Provided are engineered soluble hIL-17RA receptors with high affinity to hIL-17 that inhibit downstream IL17A induced signaling events in cells. Also provided are methods of inhibiting hIL-17A induced secretion of CXCL1 and/or IL-6 in cells, as well as methods of treating inflammation and/or inflammatory disorders in a subject. | 01-22-2015 |
20150051158 | CTLA4 PROTEINS AND THEIR USES - The present disclosure relates to CTLA4 proteins and uses of such proteins, for example to treat diseases associated with the dysregulation of immune responses. | 02-19-2015 |
20150087602 | Nutritive Proteins and Methods - Nutritive proteins are provided. In some embodiments the nutritive proteins comprise at least one of a level of a) a ratio of branch chain amino acid residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of branch chain amino acid residues to total amino acid residues present in whey protein; b) a ratio of leucine residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of leucine residues to total amino acid residues present in whey protein; and c) a ratio of essential amino acid residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of essential amino acid residues to total amino acid residues present in whey protein. Also provided are nucleic acids encoding the proteins, recombinant microorganisms that make the proteins, methods of making the proteins using recombinant microorganisms, compositions that comprise the proteins, and methods of using the proteins, among other things. | 03-26-2015 |
20150099708 | WNT COMPOSITIONS AND THERAPEUTIC USES OF SUCH COMPOSITIONS - The invention provides novel Wnt polypeptides that have improved production characteristics, solubility, systemic delivery, and tissue uptake, and polynucleotides encoding the Wnt polypeptides of the invention. The Wnt polypeptides of the invention can be used therapeutically, such as, for example, in methods of preventing or treating muscle loss and/or promoting muscle hypertrophy and growth. | 04-09-2015 |
20150119339 | USE OF HMB TO IMPROVE HEALTH OUTCOMES FOR HOSPITALIZED PATIENTS - A method of care is described that includes administering an effective amount of β-hydroxy-β-methylbutyrate (HMB) to an adult or elderly patient to decrease the risk of an adverse health event during or subsequent to hospitalization of the patient. | 04-30-2015 |
20150126459 | PLANT PROFILIN POLYPEPTIDES FOR USE IN NON-SPECIFIC ALLERGY IMMUNOTHERAPY - The invention relates to the treatment of a hypersensitivity immune response caused by a non-profilin allergen of a profilin-containing plant material (e.g. grass or tree pollen) by bystander suppression with a plant profilin (e.g. Phl p 12, Bet v 2, or Ole e 2) or a variant thereof. Also the invention features a particular variant of Phl p 12 with two of its cysteine residues replaced with another amino acid to increase its pharmaceutical properties. | 05-07-2015 |
20150306177 | THERAPY FOR RADIATION-INDUCED LUNG INJURY - Methods are disclosed for therapy of radiation-induced lung injury and other lung diseases using R-spondin | 10-29-2015 |
20150329601 | Methoxypolyethyleneglycol succinimidyl propionate modified recombinant Ganoderma Lucidum immunoregulatory protein, preparing method and application thereof - Methoxypolyethyleneglycol succinimidyl propionate modified recombinant | 11-19-2015 |
20150335706 | FORMULATION FOR BISPECIFIC T-CELL ENGAGERS (BITES) - The present invention relates to stable pharmaceutical compositions which contain polypeptides having at least two antigen-binding domains and are especially suited for subcutaneous administration. The invention provides liquid compositions which minimize the formation of undesired polypeptide aggregates (dimers and/or multimers). The present invention further provides a method for minimizing the aggregation of polypeptides having antigen-binding domains in liquid compositions. | 11-26-2015 |
20150344538 | NOVEL SPECIFIC-BINDING PROTEINS AND USES THEREOF - The present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q16552 and novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q9NPF7. In addition, the present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against one or both of Swiss Prot Q16552 and Swiss Prot Q9NPF7. The invention also relates to nucleic acid molecules encoding such polypeptides and to methods for generation of such polypeptides and nucleic acid molecules. In addition, the invention is directed to compositions comprising the polypeptides, and therapeutic and/or diagnostic uses of these polypeptides. | 12-03-2015 |
20150366937 | METHODS TO TREAT INFLAMMATION OF THE LUNG - The present invention provides pharmaceutical compositions comprising leukotoxin for the treatment of lung inflammation. | 12-24-2015 |
20150368318 | MUTANTS OF INTERLEUKIN-1 RECEPTOR ANTAGONIST AND USES THEREOF - The invention provides an isolated polypeptide comprising a variant amino acid sequence of SEQ ID NO: 1, or a fusion or derivative of said polypeptide, or a fusion of a said derivative thereof, wherein the polypeptide, fusion or derivative retains a biological activity of wild type IL-IRa. In one embodiment, the isolated polypeptide, fusion or derivative is or comprises a polypeptide variant of amino acid sequence SEQ ID NO: 1 comprising or consisting of substitutions at one or more of the following amino acid mutations of SEQ ID NO: 1: Q29K, P38Y, P38R, L42W, D47N, E52R, H54R, E90Y, Q129L, Q129N, M136N, M136D and Q149K. Also provided are pharmaceutical compositions of the above polypeptide, fusion or derivative, as well as uses of the same for treating a disease or condition capable of being treated by an agent which inhibits the function of IL-1 receptors. | 12-24-2015 |
20150376241 | FLAGELLIN RELATED POLYPEPTIDES AND USES THEREOF - The use of flagellin and flagellin related polypeptides for the protection of mammals from the effects of apoptosis is described. | 12-31-2015 |
20150376246 | HIGH AFFINITY DIGOXIGENIN BINDING PROTEINS - Isolated polypeptides with steroid binding activity and methods for their use as therapeutics and detection agents are disclosed herein. | 12-31-2015 |
20160008437 | METHOD OF TREATMENT OF HYPOXIA INDUCIBLE FACTOR (HIF)-RELATED CONDITIONS | 01-14-2016 |
20160022696 | Therapeutic and Method of Use - The present invention is a compound comprising an anti-inflammatory drug component consisting preferably of at least one of an NSAID portion and a cannabis portion and at least one of a progestin component and a progesterone component. The compound may take for instance the form of a pill or pellet (for oral internal use or for subdermal implantation), an injectable solution, or a suppository. The compound is intended for use in treating subjects having or being at increased risk—especially genetically determined risk—of developing endometriosis. The compound may also be used for treating other disorders or as a contraceptive. | 01-28-2016 |
20160024162 | Promoting Apoptosis Of Differentiated Adipocytes And Increasing Endogenous Expression Of sFRP-5 Peptide By Adipocytes By Administration Of sFRP-5 Peptide - Disclosed is a method of reducing the amount of adipose tissue in a subject comprising administering to the subject an amount of an sFRP-5 peptide effective to reduce the amount of adipose tissue, or an amount of a molecule effective to stimulate expression of the sFRP-5 peptide in the subject. Also disclosed is a screen for molecules that can reduce the amount of adipose tissue in a subject. | 01-28-2016 |
20160024172 | Compositions Comprising Receptor-Associated Protein (RAP) Variants Specific for CR-Containing Proteins and Uses Thereof - The present invention relates generally to receptor-selective variants of the low-density lipoprotein receptor-associated protein (RAP) and compositions thereof, methods of generating such variants and methods of using such receptor-selective RAP variant compositions for therapeutic purposes. | 01-28-2016 |
20160030511 | NEUROTOXINS EXHIBITING SHORTENED BIOLOGICAL ACTIVITY - The present invention relates to the pharmaceutical field. Specifically, it contemplates a polynucleotide encoding a Neurotoxin polypeptide exhibiting a reduced duration of biological effect in a subject, wherein the polypeptide comprises at least one degradation signal in the light chain as well as vectors and host cells comprising the polynucleotide, polypeptides encoded thereby and antibodies specifically binding to the polypeptides. Moreover, the invention relates to medicaments comprising the polynucleotides and polypeptides as well as specific therapeutic applications thereof. Furthermore, the present invention contemplates methods for the manufacture of the polypeptides and medicaments. | 02-04-2016 |
20160031958 | METHODS AND COMPOSITIONS USEFUL IN MANIPULATING THE STABILITY OF RE1 SILENCING TRANSCRIPTION FACTOR - Disclosed are methods of screening for compounds that promote REST degradation by inhibiting the activity of the CDTSP1 phosphorylase including fluorescent and antibody based screens. Also disclosed are peptides that promote REST stabilization as well as antibodies that recognize REST phosphorylated at serine 861 and serine 864. | 02-04-2016 |
20160051626 | COMPOSITIONS COMPRISING COMPLEXES OF PROANTHOCYANIDINS WITH VEGETABLE PROTEINS - Disclosed is a complex of pea protein and proanthocyanidins for use in the treatment of disorders caused by alterations of the intestinal epithelial tissue. | 02-25-2016 |
20160051677 | PROCESS FOR PURIFYING RECOMBINANT PLASMODIUM FALCIPARUM CIRCUMSPOROZOITE PROTEIN - The present invention relates to processes for purifying high-quality recombinant | 02-25-2016 |
20160068580 | METHOD FOR TREATMENT OF GM1 GANGLIOSIDOSIS - The present invention relates to a method for preparing a GM1 gangliosidosis human cell model based on induced pluripotent stem cells (iPSCs) and iPSCs originated neural progenitor cells, and a use of the GM1 model above for the development of a GM1 gangliosidosis treating agent. The iPSCs originated from GM1 patient fibroblasts can be differentiated into neural progenitor cells (NPCs) and neurosphere cells that can emulate the characteristics shown in GM1 patient, so that the said cells can be efficiently used for the investigation of intracellular GM1 symptoms such as the GM1 gangliosidosis and lysosome accumulation and the gene expression pattern change. So, the GM1 cell model of the present invention can be efficiently used for the study of GM1 development mechanism and the study for the development of a therapeutic agent for the disease. The present inventors also established the inflammasome inhibitor rhIL1RA or Z-YVAD-FMK by using the above GM1 cell model and further confirmed that it can be efficiently used as a relieving/treating agent of GM1 gangliosidosis. | 03-10-2016 |
20160075767 | CAPPING MODULES FOR DESIGNED ANKYRIN REPEAT PROTEINS - Improved N-terminal capping modules for designed Ankyrin repeat proteins (DARPins) conferring improved thermal stability to the DARPins are described, as well as nucleic acids encoding such proteins, pharmaceutical compositions comprising such proteins and the use of such proteins in the treatment of diseases. | 03-17-2016 |
20160082116 | ENGINEERED MICROGELS - Microparticles containing heparin or a heparin-like polymer and a biocompatible polymer are described. The heparin or the heparin-like polymer and the biocompatible polymer can be indirectly linked together by a coupling agent, which can have a structure represented by Formula I, (A) | 03-24-2016 |
20160158313 | CLATHRIN THERAPEUTIC FOR INFECTIOUS DISEASES - The invention in suitable embodiments is directed to purified clathrin protein therapeutics. In one aspect, one or more purified clathrin protein therapeutic, formed in whole or in part from isolated, synthetic and or recombinant amino acid residues comprising in whole or in part one or more clathrin heavy chain protein and isoforms thereof, forms one or more type of therapeutic agent for treating an infectious disease, condition, or disorder in vivo or in vitro. | 06-09-2016 |
20160176933 | MUTANT CHANNELRHODOPSINS WITH ALTERED ION SELECTIVITY | 06-23-2016 |
20160199445 | USE OF ARPIN A NEW INHIBITOR OF THE ARP2/3 COMPLEX FOR THE DIAGNOSIS AND TREATMENT OF DISEASES | 07-14-2016 |
20160376343 | NOVEL IL-17R-ECD MUTANTS - A protein comprising an amino acid sequence having at least 97% homology to SEQ ID NO: 1. The amino acid sequence comprises valine at position 60, glycine at position 123 and lysine at position 109 and the protein binds hIL17A. | 12-29-2016 |
20190142843 | THERAPEUTIC AND METHOD OF USE | 05-16-2019 |
20080242654 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present application relates to thiazolylidene containing compounds of formula (I) | 10-02-2008 |
20080255083 | NEW PYRIDONE DERIVATES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS - The present invention relates to compounds of general formula I | 10-16-2008 |
20080261940 | N-(1-Arylpyrazol-4L) Sulfonamides and their Use as Parasiticides - The invention relates to a sulfonamide compound of formula (I) or a pharmaceutically, veterinarily or agriculturally acceptable salt or solvate thereof, where the groups R | 10-23-2008 |
20080261941 | Biaryl Ether Urea Compounds - The present invention relates to compounds of Formula (I) | 10-23-2008 |
20080280868 | Pyridine Derivatives and Their Use as Cb2 Receptor Modulators - The present invention relates to novel pyridine derivatives such as compounds of the formula (I): | 11-13-2008 |
20080287409 | PHENYL AND PYRIDINYL-1,2,4-OXADIAZOLONE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention comprises phenyl and pyridinyl 1,2,4-oxadiazolone compounds their physiologically acceptable salts and physiologically functional derivatives that exhibit peroxisome proliferator activator receptor (PPAR) delta agonist activity. Also described and claimed are processes for their preparation and their use as pharmaceuticals. These are compounds of formula I, | 11-20-2008 |
20080287410 | PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA - Disclosed are novel compounds of formula (I): | 11-20-2008 |
20080287411 | Optically active dihydropyridine derivative - The optically active compound (R)-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl) ester 5-isopropyl ester or a pharmacologically acceptable salt thereof, and a method using the compound or its salt to treat circulatory diseases. | 11-20-2008 |
20080293687 | Benzamide Compounds - The invention concerns benzamide compounds of Formula (I), wherein R | 11-27-2008 |
20080300232 | N-Piperidine Derivatives as Ccr3 Modulators - Compounds of formula I, processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders and to pharmaceutical compositions containing them. | 12-04-2008 |
20080312206 | Chemical Compounds-149 - The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula which possess CSF 1R kinase inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man. | 12-18-2008 |
20090005353 | Non-Anilinic Derivatives of Isothiazol-3(2H)-one 1,1-Dioxides as Liver X Receptor Modulators - The present invention relates to certain novel compounds of the formula (I) | 01-01-2009 |
20090005354 | New Amino Derivatives and Their Use as Pharmaceuticals - The present invention provides for compounds of formula (I): | 01-01-2009 |
20090029963 | PYRAZOL DERIVATIVES - The invention is concerned with novel pyrazol derivatives of formula (I), | 01-29-2009 |
20090036419 | COMPOUNDS USEFUL AS RAF KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases. | 02-05-2009 |
20090036420 | BENZAMIDE DERIVATIVES AND THEIR USE FOR TREATING CNS DISORDERS - The present invention relates to methods of treating CNS disorders with a compound of formula I | 02-05-2009 |
20090036421 | Pyrrole Derivative or Salt Thereof - [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT | 02-05-2009 |
20090042852 | Novel Pyridine Compounds - The present invention relates to certain novel pyridin compounds of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, and processes for their preparation, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them. | 02-12-2009 |
20090048225 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES -
The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. | 02-19-2009 |
20090054392 | NAPHTHYLPYRIMIDINE, NAPHTHYLPYRAZINE AND NAPHTHYLPYRIDAZINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM - The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog. | 02-26-2009 |
20090069282 | ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS - The present invention relates to alkyne compounds of general formula I | 03-12-2009 |
20090069283 | Potassium Channel Inhibitors - The present invention relates to pyridine substituted ethanol compounds and derivatives thereof having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. | 03-12-2009 |
20090069284 | Substituted 3-alkyl and 3-alkenyl azetidine derivatives - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver. | 03-12-2009 |
20090075968 | CETP inhibitors - The present invention relates to a compound of formula | 03-19-2009 |
20090124592 | PHARMACEUTICAL COMPOSITION FOR TREATING AND/OR PREVENTING A PATHOLOGY ASSOCIATED WITH AN OBSESSIONAL BEHAVIOR OR WITH OBESITY - This invention relates to the use of a ligand of the 5-HT | 05-14-2009 |
20090131397 | ESTROGEN MODULATORS - The present application is directed to a new class of isoxazoles and their use as estrogen modulators. | 05-21-2009 |
20090137545 | Compounds - The present invention relates to compounds of general formula I | 05-28-2009 |
20090137548 | 1,3-Oxazolidin-2-One Derivatives Useful as Cetp Inhibitors - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B. | 05-28-2009 |
20090149438 | Pyrimidines as PLK inhibitors - The present invention encompasses compounds of general formula (1), | 06-11-2009 |
20090156571 | BIPHENYL AMIDE LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β-HSD type 1 activity. | 06-18-2009 |
20090156573 | N-(Aminoheteroaryl)-1H-indole-2-carboxamide derivatives, and preparation and therapeutic application thereof - The invention concerns compounds of general formula (I): | 06-18-2009 |
20090156574 | 2-ACYLAMINO-4-PHENYLTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF - The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): | 06-18-2009 |
20090163462 | BIARYL SUBSTITUTED HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION - The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders. The compounds have general formula Ψ: | 06-25-2009 |
20090163463 | Organic Compounds - The present invention concerns a compound of formula (I) | 06-25-2009 |
20090163464 | BENZOTHIAZOLE AND BENZOOXAZOLE DERIVATIVES AND METHODS OF USE - Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds. | 06-25-2009 |
20090163465 | Pyrimidines as PLK inhibitors - The present invention encompasses compounds of general formula (1), | 06-25-2009 |
20090170826 | Acid Addition Salt of Optically Active Dihydropyridine Derivative - There is provided an excellent medicine for treating or preventing hypertension or the like. A specific acid addition salt of (R)-2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenyl-methylazetidin-3-yl) ester 5-isopropyl ester is useful as a medicine for treating or preventing hypertension or the like. | 07-02-2009 |
20090170827 | Acid Addition Salt of Dihydropyridine Derivative - There is provided an excellent medicine for treating or preventing hypertension or the like. A specific acid addition salt of 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-(1-diphenylmethylazetidin-3-yl)ester 5-isopropyl ester is useful as a medicine for treating or preventing hypertension or the like. | 07-02-2009 |
20090170828 | Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase - Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I) | 07-02-2009 |
20090170829 | Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 07-02-2009 |
20090192134 | Compounds - A compound of formula (1), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof: and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 07-30-2009 |
20090192136 | BENZOYL-PIPERAZINE DERIVATIVES - A compound of formula | 07-30-2009 |
20090197859 | Pyridinyl Amides for the Treatment of CNS and Metabolic Disorders - The present invention relates to novel pyridinyl derivatives of Formula | 08-06-2009 |
20090209511 | Benzofuran Derivatives - The present invention provides a benzofuran derivative of the formula [1]: | 08-20-2009 |
20090233896 | Inhibitors of checkpoint kinases - The instant invention provides for compounds which comprise substituted pyridyl aminothiazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 09-17-2009 |
20090247500 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are compounds of formula (I) | 10-01-2009 |
20090253671 | TRICYCLIC DERIVATIVES OF AZETIDINE AND PYRROLE WITH ANTIBACTERIAL ACTIVITY - Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 10-08-2009 |
20090253673 | Substituted Pyrazoles as Ghrelin Receptor Antagonists - Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome. | 10-08-2009 |
20090253674 | Substituted Triazole Derivatives As Oxytocin Antagonists - The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction. | 10-08-2009 |
20090258851 | DIARYL SUBSTITUTED ALKANES - The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. | 10-15-2009 |
20090264400 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to formula I: | 10-22-2009 |
20090264401 | SUBSTITUTED PYRIMIDIN-5-CARBOXAMIDES 281 - A compound of formula (I): | 10-22-2009 |
20090275550 | Pyridyl Amide T-Type Calcium Channel Antagonists - The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 11-05-2009 |
20090291936 | OXIME DERIVATIVE AND PREPARATIONS THEREOF - The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: | 11-26-2009 |
20090298806 | FACTOR XA INHIBITORS - The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. | 12-03-2009 |
20090298807 | Compounds - The present invention relates to spirocyclic amide derivatives of the formula I, | 12-03-2009 |
20090306038 | 2-Aminopyrimidine derivatives as modulators of the histamine H4 receptor activity - 2-Aminopyrimidine derivatives of formula (I) that are useful as modulators of the H | 12-10-2009 |
20090306039 | COMPOUNDS AND COMPOSITIONS AS ITPKB INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb). | 12-10-2009 |
20090318405 | 4-PYRAZOLYL-N-ARYLPYRIMIDIN-2-AMINES AND 4-PYRAZOLYL-N-HETEROARYLPYRIMIDIN-2-AMINES AS JANUS KINASE INHIBITORS - The present invention provides substituted bicyclic heteroaryl compounds, including, for example, 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines that modulate the activity of kinases and are useful in the treatment of diseases related to activity of kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 12-24-2009 |
20090325923 | NEW METHOD FOR THE TREATMENT OF INFLAMMATORY DISEASES - The present invention relates to the use of an inhibitor of the formation of nicotinamide adenyl dinucleotide for the preparation of a medicament used in the treatment of inflammatory diseases such as rheumatoid arthritis and endotoxemia. | 12-31-2009 |
20100004219 | MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-KAPPABETA ACTIVITY AND USE THEREOF - Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R | 01-07-2010 |
20100009956 | NOVEL SUBSTITUTED PYRIMIDINES AS CYSTEINE PROTEASE INHIBITORS - Substituted heteroaryl nitrile salts of Formula I, | 01-14-2010 |
20100016275 | NOVEL COMPOUND 395 - A compound of formula (1) | 01-21-2010 |
20100022502 | AMINOPYRIDINES AND AMINOPYRIMIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 01-28-2010 |
20100022503 | AMINOPYRAZOLE KINASE INHIBITORS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents. | 01-28-2010 |
20100029605 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases. | 02-04-2010 |
20100029606 | MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF - The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system. | 02-04-2010 |
20100029608 | Histamine H3 Receptor Agents, Preparation and Therapeutic Uses - The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-113 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. | 02-04-2010 |
20100056489 | TREATMENT OF NEUROPATHIC PAIN - A method for treating a patient suffering from neuropathic pain, comprising administering to a patient in need of such treatment an effective amount of an agonist drug capable of binding to the neuronal nicotinic receptor (NNR) but which does not readily cross the blood-brain barrier. | 03-04-2010 |
20100063022 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present application relates to cannabinoid receptor ligands of formula (I) | 03-11-2010 |
20100069346 | New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases - The application relates to new piperazine- or morpholine-substituted azetidine derivatives of formula I. These compounds are antagonists at the neurokinin receptor and can be used for the treatment of gastrointestinal diseases. The application also relates to processes for the preparation of the compounds and to intermediates in said preparation. | 03-18-2010 |
20100069348 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are cannabinoid receptor ligands of formula (I) | 03-18-2010 |
20100069349 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are cannabinoid receptor ligands of formula (I) | 03-18-2010 |
20100075942 | N-PHENYL-4-PYRIDIN-2-YL-BENZAMIDE DERIVATIVES AS HISTONE DEACYLASE (HDAC) INHIBITORS FOR THE TREATMENT OF CANCER - The invention concerns benzamide derivatives of Formula (I) wherein R | 03-25-2010 |
20100075944 | NOVEL PYRIDINE DERIVATIVES AND PYRIMIDINE DERIVATIVES (3) - A compound represented by the following formula, or a salt thereof or a hydrate of the foregoing, has excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity, and cancer metastasis inhibitory activity. | 03-25-2010 |
20100081641 | IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R | 04-01-2010 |
20100081642 | CB-1 RECEPTOR MODULATOR PHARMACEUTICAL FORMULATIONS - The present invention relates to pharmaceutical compositions that stabilize and improve the bioavailability of 3-[(1S)- 1-(1-{(S)-(4-chlorophenyl)[3-(5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)phenyl]methyl}azetidin-3-yl)-2-fluoro-2-methylpropyl]-5-fluorobenzonitrile. In particular, the present invention relates to pharmaceutical compositions that include 3-[(1S)-1-(1-{(S)-(4-chlorophenyl)[3 -(5-oxo-4,5-dihydro- 1,3,4-oxadiazol-2-yl)phenyl]methyl}azetidin-3-yl)-2-fluoro-2-methylpropyl]-5-fluorobenzonitrile and at least one pharmaceutical acceptable excipient, such as a mono-, di- or triglyceride. | 04-01-2010 |
20100081644 | Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 04-01-2010 |
20100093689 | HETEROARYL COMPOUNDS AS P2Y1 RECEPTOR INHIBITORS - The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y | 04-15-2010 |
20100093690 | 5-PHENYLTHIAZOLE DERIVATIVES AND USE AS PI3 KINASE INHIBITORS - Compounds of formula I | 04-15-2010 |
20100099658 | DI(ARYLAMINO)ARYL COMPOUND - The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. | 04-22-2010 |
20100105650 | Substituted isoquinoline and isoquinolinone derivatives - The invention relates to 6-substituted isoquinoline and isochinolone derivatives of the formula (I) | 04-29-2010 |
20100130464 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR | 05-27-2010 |
20100130465 | 2-AMINOTHIAZOLE-4-CARBOXYLIC AMIDES AS PROTEIN KINASE INHIBITORS - The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase. | 05-27-2010 |
20100130466 | TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS - The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer. | 05-27-2010 |
20100137274 | SUBSTITUTED OXAZOLIDINONES AND THEIR USE IN THE FIELD OF BLOOD COAGULATION - The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) | 06-03-2010 |
20100137275 | TRIAMINOPYRIMIDINE DERIVATIVES AS INHIBITORS OF CDC25 PHOSPHATASE - The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synthesizing these compounds and also to therapeutic compositions containing these products and to the use thereof as medicaments. | 06-03-2010 |
20100144695 | 4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS OF CCR2 - The present invention comprises compounds of Formula (I). | 06-10-2010 |
20100144697 | Stabilized pharmaceutical compositions containing a calcium channel blocker - The present invention provides a pharmaceutical composition containing a calcium channel blocker of the following formula or a pharmacologically acceptable salt thereof and a pharmacologically acceptable alkaline material which is added to an extent such that an aqueous solution or dispersion solution of said pharmaceutical composition containing a calcium channel blocker has a pH of at least 8: | 06-10-2010 |
20100152155 | Histone Deacetylase Inhibitors - Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical. | 06-17-2010 |
20100160280 | AMINOPYRIDINE AND CARBOXYPYRIDINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS - Pyridine and pyrimidine compounds: | 06-24-2010 |
20100168076 | DIPHENYL SUBSTITUTED ALKANES - The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. | 07-01-2010 |
20100168077 | Novel Pyridine Derivatives, Processes for Preparing Them, Pharmaceutical Compositions Thereof - The present invention concerns 2-amino pyridine derivatives of formula 1 processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 07-01-2010 |
20100173886 | BICYCLIC ARYL AND HETEROARYL COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful for the treatment of metabolic disorders including obesity. | 07-08-2010 |
20100179118 | CYCLIC AMINOALKYLCARBOXAMIDE DERIVATIVE - The present invention relates to a compound represented by the following formula (I), which is useful as an antiallergic agent and/or an anti-inflammatory agent, or a physiologically acceptable salt thereof and the like: | 07-15-2010 |
20100184737 | IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS - The present invention relates to compounds of Formula I | 07-22-2010 |
20100190761 | DIPHENYL SUBSTITUTED ALKANES - The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents. | 07-29-2010 |
20100190762 | TRIAZOLYL PHENYL BENZENESULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists. | 07-29-2010 |
20100197652 | PYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 08-05-2010 |
20100204196 | 2-[2--1H-Pyrrolo[2,3-D]Pyrimidin-4-YL)Amino] Benzamide Derivatives As IGF-1R Inhibitors For The Treatment Of Cancer - Novel pyrrolopyrimidines as shown in formula (I): | 08-12-2010 |
20100210617 | Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors - The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y | 08-19-2010 |
20100216758 | Pyridone Compounds - An active ingredient is a compound represented by the general formula [I]: | 08-26-2010 |
20100216760 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are cannabinoid receptor ligands of formula (I) | 08-26-2010 |
20100222317 | Azetidine Derivatives as GlyT1 Inhibitors - The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders. | 09-02-2010 |
20100222318 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 09-02-2010 |
20100222319 | NICOTINAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I): | 09-02-2010 |
20100227845 | SUBSTITUTED 1,2,4-OXADIAZOLES AND ANALOGS THEREOF AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES - The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases. | 09-09-2010 |
20100234341 | SUBSTITUTED PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS - Compounds of formula (I) including pharmaceutically acceptable salts, esters, solvates and stereoisomers thereof, R | 09-16-2010 |
20100234343 | INHIBITORS OF ION CHANNELS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 09-16-2010 |
20100249084 | SUBSTITUTED PYRIMIDINES AS ADENOSINE RECEPTOR ANTAGONISTS - Compounds of formula (I): wherein R | 09-30-2010 |
20100249085 | HETEROARYL SUBSTITUTED PYRAZOLE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures. | 09-30-2010 |
20100249086 | Compounds As Cannabinoid Receptor Ligands - Cannabinoid receptor ligands of formula (I) | 09-30-2010 |
20100249087 | COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are cannabinoid receptor ligands of formula (I) | 09-30-2010 |
20100249088 | AZOLECARBOXAMIDE COMPOUND OR SALT THEREOF - [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action. | 09-30-2010 |
20100249089 | ABCG2 INHIBITOR - The present invention relates to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. | 09-30-2010 |
20100261697 | 2-(HETEROCYCLYLBENZYL)PYRIDAZINONE DERIVATIVES - Compounds of the formula (I) in which R | 10-14-2010 |
20100261699 | N-PYRAZOLE-2-PYRIDINE CARBOXAMIDE DERIVATIVE - The present invention relates to a compound represented by the formula: | 10-14-2010 |
20100273764 | INHIBITORS OF PI3 KINASE AND/OR MTOR - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; | 10-28-2010 |
20100279999 | INSECTICIDAL COMPOUNDS - A compound of formula (I), wherein A | 11-04-2010 |
20100286110 | AZETIDINYL G-PROTEIN COUPLED RECEPTOR AGONISTS - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome. | 11-11-2010 |
20100298284 | BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA - Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. | 11-25-2010 |
20100305085 | SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES - The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds. | 12-02-2010 |
20100305086 | Pharmaceutical Compositions for the Treatment of Pain - This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype α4β2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject. | 12-02-2010 |
20100305088 | INHIBITORS OF THE CHEMOKINE RECEPTOR CxCR3 - This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR | 12-02-2010 |
20100317641 | THIAZOLES AND PYRAZOLES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 12-16-2010 |
20100317644 | Substituted Sulfonamide Compounds - Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states. | 12-16-2010 |
20100324009 | Substituted Sulfonamide Compounds - Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states. | 12-23-2010 |
20110009377 | AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY - The invention relates to azetidine derivatives having the formula (I): | 01-13-2011 |
20110021486 | VIRAL POLYMERASE INHIBITORS - Compounds of formula I: | 01-27-2011 |
20110021487 | CYCLOALKOXY-SUBSTITUTED 4-PHENYL-3,5-DICYANOPYRIDINES AND THEIR USE - The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders. | 01-27-2011 |
20110021488 | New Compounds - The present invention relates to compounds of general formula I | 01-27-2011 |
20110039817 | 4-AMINOPYRIMIDINE DERIVATIVES AS HISTAMINE H4 RECEPTOR ANTAGONISTS - 4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists. | 02-17-2011 |
20110046104 | AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 02-24-2011 |
20110046106 | ARYL SULFONAMIDES AS EFFECTIVE ANALGESICS - The present invention relates to compounds of general formula I | 02-24-2011 |
20110059937 | IL-8 RECEPTOR ANTAGONISTS - This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). | 03-10-2011 |
20110059938 | NEW CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1) | 03-10-2011 |
20110071125 | SUBSTITUTED PHENYLAMINO-BENZENE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH MITOGEN EXTRACELLULAR KINASE ACTIVITY - This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients. | 03-24-2011 |
20110071126 | INHIBITORS OF BETA-SECRETASE - The present invention is directed to a compound represented by the following structural formula | 03-24-2011 |
20110071127 | Compounds Which Modulate the CB2 Receptor - Compounds of formula (I) | 03-24-2011 |
20110086832 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present application relates to thiazolylidene containing compounds of formula (I) | 04-14-2011 |
20110092474 | Diamino-pyridine, pyrimidine, and pyrazine modulators of the histamine H4 receptor - Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H | 04-21-2011 |
20110098267 | TOPICAL FORMULATIONS FOR THE TREATMENT OF PSORIASIS - The invention relates to a topical composition and a method for treating psoriasis. The topical composition comprises one or more compound that inhibits the production of IL-12 and IL-23. | 04-28-2011 |
20110098268 | SPIROCYCLIC COMPOUNDS - The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo. | 04-28-2011 |
20110098269 | Substituted Pyridazinone Derivatives as Histamine-3 (H3) Receptor Ligands - The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII: | 04-28-2011 |
20110105454 | SUBSTITUTED OXINDOLE-DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES - The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses. | 05-05-2011 |
20110105456 | 3-PHENYL-PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT | 05-05-2011 |
20110112060 | 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. | 05-12-2011 |
20110112061 | PYRIDAZINONES, THE PREPARATION AND THE USE THEREOF - The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer. | 05-12-2011 |
20110112062 | Carbamate And Urea Inhibitors Of 11Beta-Hydroxysteroid Dehydrogenase 1 - This invention relates to novel compounds of the Formula I, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell. | 05-12-2011 |
20110112064 | Pyridyl Amide T-Type Calcium Channel Antagonists - The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved. | 05-12-2011 |
20110124618 | SUBSTITUTED (PYRAZOLYLCARBONYL)IMIDAZOLIDINONES AND THEIR USE - The present invention relates to novel substituted (pyrazolylcarbonyl)imidazolidinones, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals. | 05-26-2011 |
20110124619 | Pyrimidine Sulphonamide Derivatives as Chemokine Receptor Modulators - A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders. | 05-26-2011 |
20110130377 | SUBSTITUTED ARYLOXAZOLES AND THEIR USE - The present application relates to novel substituted aryloxazole derivatives, a method for the production thereof, the use thereof for the treatment and/or prophylaxis of diseases and the use thereof for the production of drugs for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders. | 06-02-2011 |
20110130379 | PIPERAZINE DERIVATIVES USED AS CAV2.2 CALCIUM CHANNEL MODULATORS - The present invention relates to novel piperazine derivatives (I); to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca | 06-02-2011 |
20110144080 | PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS - The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R | 06-16-2011 |
20110152232 | SULFONAMIDE COMPOUNDS AND USES THEREOF - Compounds that modulate GHS-R are described, for examples compounds formula (I) | 06-23-2011 |
20110152234 | Novel Compounds - The invention relates to thiophene carboxamides of formula (I), wherein A, R | 06-23-2011 |
20110152235 | Aminopyrimidine Kinase Inhibitors - Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. | 06-23-2011 |
20110152236 | AZETIDINE POLYSUBSTITUTED COMPOUNDS, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF - The invention relates to compounds of the formula (I) where: R is a (C | 06-23-2011 |
20110160176 | HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH | 06-30-2011 |
20110166116 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO - New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): | 07-07-2011 |
20110166117 | Novel Compounds - The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation. | 07-07-2011 |
20110178054 | Heterocyclic GPCR Agonists - Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity. | 07-21-2011 |
20110178055 | DUAL NK1/NK3 RECEPTOR ANTAGONISTS - The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula | 07-21-2011 |
20110183952 | NEW CHEMICAL COMPOUNDS - The present invention encompasses compounds of general formula (1), wherein the groups R | 07-28-2011 |
20110183953 | SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 07-28-2011 |
20110183954 | TRICYCLIC 2,4-DIAMINO-L,3,5-TRIAZINE DERIVATIVES USEFUL FOR THE TREATMENT OF CANCER AND MYELOPROLIFERATIVE DISORDERS - The present invention relates to compounds of Formula (I): (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer. | 07-28-2011 |
20110183955 | 2-Aminocarbonyl Substituted Piperazine or Diaza-Cyclic Compounds as Apoptosis Protein Inhibitors (Iap) Modulators - The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases. | 07-28-2011 |
20110183957 | CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. | 07-28-2011 |
20110183958 | AZETIDINE DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis. | 07-28-2011 |
20110190255 | HETEROCYCLIC COMPOUNDS - Disclosed are compounds of Formula (I) | 08-04-2011 |
20110190256 | Amine and Ether Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain. | 08-04-2011 |
20110201589 | NEW BRADYKININ B1 ANTAGONISTS - The invention relates to compounds of formula (I) wherein R | 08-18-2011 |
20110201590 | SUBSTITUTED AMINOINDANES AND ANALOGS THEREOF, AND THE PHARMACEUTICAL USE THEREOF - The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders. | 08-18-2011 |
20110201591 | ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 08-18-2011 |
20110224185 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 09-15-2011 |
20110230458 | PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF - The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof | 09-22-2011 |
20110230459 | LACTAM ACETAMIDES AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors containing compounds of formula (I) | 09-22-2011 |
20110245220 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 10-06-2011 |
20110245221 | ARYL ISOXAZOLE COMPOUNDS WITH ANTITUMOURAL ACTIVITIES - The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds. | 10-06-2011 |
20110245222 | Methods for Using Carboxamide, Sulfonamide and Amine Compounds - Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein. | 10-06-2011 |
20110251168 | 3-AMINOPYRROLIDINE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS - The present invention relates to 3-aminopyrrolidine derivatives of the formula I: | 10-13-2011 |
20110263557 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119; such as, but not limited to, diabetes, obesity and associated metabolic disorders. Formula (I) is a compound, in which A can have up to 2 ring —CH2- group substituted with —C(O)— and can be partially unsaturated with up to 2 double bonds; Wi and W2 are independently selected from CR10 and N; wherein R10 is selected from hydrogen and C1_6alkyl; Yi is selected from NRn, O and S; wherein Rn is selected from hydrogen and C1_6alkyl; Y2 and Y3 are independently selected from CH and N; Y4 is selected from CH2, OCH2 and NR15; wherein R15 is selected from hydrogen and C1_6alkyl; or the pharmaceutically acceptable salts thereof. | 10-27-2011 |
20110269732 | DRUG DISCOVERY METHODS - The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore. | 11-03-2011 |
20110269733 | Silent Desensitizers of Neuronal nAChR and Methods of Use Thereof - One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. | 11-03-2011 |
20110269734 | PIPERIDINYL GPCR AGONISTS - Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity. | 11-03-2011 |
20110275607 | NUCLEAR TRANSPORT MODULATORS AND USES THEREOF - The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic). | 11-10-2011 |
20110275608 | PIPERIDINE-CONTAINING COMPOUNDS AND USE THEREOF - A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): | 11-10-2011 |
20110281836 | Silent desensitizers of neuronal NACHR and methods of use thereof - One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. | 11-17-2011 |
20110281837 | 3-SUBSTITUTED-6-ARYL PYRIDINES - 3-substituted-6-aryl pyridines of Formula I are provided: | 11-17-2011 |
20110281838 | 5-ALKYNYL-PYRIMIDINES - The present invention encompasses compounds of general Formula (1) wherein R | 11-17-2011 |
20110288066 | PHENOXY ACETIC ACID DERIVATIVES - The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses. | 11-24-2011 |
20110301140 | Pyridine Carboxamide orexin Receptor Antagonists - The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 12-08-2011 |
20110312930 | Aryl compounds with aminoalkyl substituents and their use - The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures. | 12-22-2011 |
20110312931 | GLYCINE TRANSPORTER-1 INHIBITORS, METHODS OF MAKING THEM, AND USES THEREOF - The compounds of the present invention are represented by the following formula (I): | 12-22-2011 |
20110312932 | Therapeutic Uses of Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) | 12-22-2011 |
20110319378 | PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER - The present invention provides MDM2 inhibitor compounds of Formula I, | 12-29-2011 |
20120010182 | Chemical Compounds - The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 01-12-2012 |
20120010183 | Chemical Compounds - The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. | 01-12-2012 |
20120010184 | Therapeutic Uses of Compounds Which Selectively Modulate The CB2 Receptor - Compounds of formula (I) | 01-12-2012 |
20120010185 | NEW PYRIDONE DERIVATES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS - The present invention relates to compounds of general formula I | 01-12-2012 |
20120010186 | HETEROCYCLIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE - Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis. | 01-12-2012 |
20120010187 | BROAD SPECTRUM BENZOTHIOPHENE-NITROTHIAZOLIDE AND OTHER ANTIMICROBIALS - The invention provides FIG. | 01-12-2012 |
20120015927 | CRYSTALLINE FORMS OF N-[2-[[(2,3-DIFLUOROPHENYL)METHYL]THIO]-6--4-PYRIMIDINYL]-1-AZETIDINESULF- ONAMIDE - There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial. | 01-19-2012 |
20120015929 | NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are compounds of formula (I) | 01-19-2012 |
20120028950 | Substituted heterocyclylbenzylpyrazoles and use thereof - The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures. | 02-02-2012 |
20120040948 | AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to aminoindane derivatives of the formula (I) | 02-16-2012 |
20120046266 | RESORCINOL DERIVATIVES AS HSP90 INHIBITORS - The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds. | 02-23-2012 |
20120058983 | Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension - The present invention relates to the use of selective adenosine A | 03-08-2012 |
20120077793 | Compounds for the Treatment of Metabolic Disorders - The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes. | 03-29-2012 |
20120077794 | BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS - The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes. | 03-29-2012 |
20120101079 | SUBSTITUTED 6-AMINO-NICOTINAMIDES AS KCNQ2/3 MODULATORS - Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 04-26-2012 |
20120115837 | Solid Preparation - Provided is a solid preparation comprising (i) a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, (ii) a sugar alcohol, and (iii) a calcium antagonist, which is superior in the dissolution property and stability. | 05-10-2012 |
20120115838 | AMPK-Activating Heterocycloalkyloxy(Hetero)Aryl Carboxamide, Sulfonamide And Amine Compounds And Methods For Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 05-10-2012 |
20120142660 | AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 06-07-2012 |
20120149674 | Diaryl Substituted Alkanes - The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. | 06-14-2012 |
20120157425 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The invention relates to new piperidine derivatives of the formula I | 06-21-2012 |
20120157426 | MUTANT-SELECTIVE EGFR INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-21-2012 |
20120157427 | PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I: | 06-21-2012 |
20120165303 | TRIAZOLYL PHENYL BENZENESULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists. | 06-28-2012 |
20120172345 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: | 07-05-2012 |
20120184520 | GLYCINE COMPOUND | 07-19-2012 |
20120184521 | SUBSTITUTED AMIDE COMPOUND - A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: | 07-19-2012 |
20120196844 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 08-02-2012 |
20120214782 | New compounds, pharmaceutical compositions and uses thereof - The invention relates to new compounds of the formula I | 08-23-2012 |
20120214783 | VIRAL POLYMERASE INHIBITORS - Compounds of formula I: | 08-23-2012 |
20120214784 | SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS - An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines. | 08-23-2012 |
20120220561 | OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compound of formula (I): | 08-30-2012 |
20120220562 | Anti-Viral Compounds - Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection. | 08-30-2012 |
20120225854 | COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES - The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, | 09-06-2012 |
20120238539 | NOVEL PIPERAZINE ANALOGS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS - A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: | 09-20-2012 |
20120245136 | CHROMAN-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to chroman spirocyclic piperidine amide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 09-27-2012 |
20120258946 | Substituted Phenylureas and Phenylamides as Vanilloid Receptor Ligands - Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions. | 10-11-2012 |
20120258947 | SUBSTITUTED 6-AMINO-NICOTINAMIDES AS KCNQ2/3 MODULATORS - Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 10-11-2012 |
20120258948 | N-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents - The present invention is directed to a new class of hydroxamic acid derivatives of formula I, | 10-11-2012 |
20120264728 | AMINO-HETEROARYL DERIVATIVES AS HCN BLOCKERS - The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain. | 10-18-2012 |
20120295881 | TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to tetraline and indane derivatives of the formula (I) | 11-22-2012 |
20120309735 | AMINOPYRIMIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis. | 12-06-2012 |
20120322784 | Compounds, pharmaceutical compositions and uses thereof - The present invention relates to compounds of formula I, | 12-20-2012 |
20120329771 | BENZYLIC OXINDOLE PYRIMIDINES - The present invention encompasses compounds of general formula (I) | 12-27-2012 |
20130005702 | PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS - The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: | 01-03-2013 |
20130018030 | New compounds, pharmaceutical compositions and uses thereofAANM HIMMELSBACH; FrankAACI MittelbiberachAACO DEAAGP HIMMELSBACH; Frank Mittelbiberach DEAANM LANGKOPF; ElkeAACI Biberach an der RissAACO DEAAGP LANGKOPF; Elke Biberach an der Riss DEAANM NOSSE; BerndAACI Biberach an der RissAACO DEAAGP NOSSE; Bernd Biberach an der Riss DE - The present invention relates to compounds of general formula I, | 01-17-2013 |
20130018031 | AMINOALKYLPYRIMIDINE DERIVATIVES AS HISTAMINE H4 RECEPTOR ANTAGONISTS - Aminoalkylpyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H | 01-17-2013 |
20130029961 | Substituted Heterocyclic Aza Compounds - Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders. | 01-31-2013 |
20130029962 | Substituted Heteroaromatic Pyrazole-Containing Carboxamide and Urea Compounds as Vanilloid Receptor Ligands - Substituted heteroaromatic pyrazole-containing carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also to a method of using these compounds for treating and/or inhibiting pain and further diseases and/or disorders. | 01-31-2013 |
20130029963 | 1,2,4-TRIAZINE-4-AMINE DERIVATIVES - According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A | 01-31-2013 |
20130035323 | AMINOCHROMANE, AMINOTHIOCHROMANE AND AMINO-1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) | 02-07-2013 |
20130040926 | NOVEL COMPOUND - There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. | 02-14-2013 |
20130040928 | NITROGEN HETEROCYCLE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN HUMAN THERAPEUTICS - The present invention relates to compounds having general formula I characterised in that | 02-14-2013 |
20130045962 | PEPTIDE DEFORMYLASE INHIBITORS - The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): | 02-21-2013 |
20130065876 | 3-PYRIDINE CARBOXYLIC ACID HYDRAZIDES - The present invention relates to compounds of formula I, | 03-14-2013 |
20130065877 | SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). | 03-14-2013 |
20130072467 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases. | 03-21-2013 |
20130072469 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 03-21-2013 |
20130079320 | Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands - The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 03-28-2013 |
20130079321 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 03-28-2013 |
20130085126 | PYRAZOLE COMPOUNDS - Compounds of formula (I): | 04-04-2013 |
20130085127 | HETEROCYCLIC COMPOUND AND H1 RECEPTOR ANTAGONIST - A heterocyclic compound useful as an antiallergic agent is provided. | 04-04-2013 |
20130096100 | DI(ARYLAMINO)ARYL COMPOUND - The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. | 04-18-2013 |
20130109665 | NOVEL PYRAZINE DERIVATIVES | 05-02-2013 |
20130109667 | Chemical Compounds | 05-02-2013 |
20130116228 | THIAZOLES AND PYRAZOLES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 05-09-2013 |
20130123230 | 2-Thiopyrimidinones - Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions. | 05-16-2013 |
20130131035 | CARBOXAMIDES AS INHIBITORS OF VOLTAGE-GATED SODIUM CHANNELS - The present invention provides compounds that are inhibitors of voltage-gated sodium channels (Nav), in particular Nav 1.7, and are therefore useful for the treatment of diseases treatable by inhibition of these channels, in particular, chronic pain disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 05-23-2013 |
20130131036 | NOVEL TRPV3 MODULATORS - Disclosed herein are modulators of TRPV3 of formula (II): | 05-23-2013 |
20130131037 | 2-(HETEROCYCLYLBENZYL)PYRIDAZINONE DERIVATIVES - Compounds of the formula (I), in which R | 05-23-2013 |
20130137671 | Substituted Triazole Derivatives As Oxytocin Antagonists - The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction. | 05-30-2013 |
20130143860 | GUANIDINE COMPOUND | 06-06-2013 |
20130150339 | Bicyclic Aryl and Heteroaryl Sodium Channel Inhibitors - The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. | 06-13-2013 |
20130157995 | NICOTINE COMPOUNDS AND ANALOGS THEREOF, SYNTHETIC METHODS OF MAKING COMPOUNDS, AND METHODS OF USE - Embodiments of the present disclosure provide for compounds such as those shown in FIG. | 06-20-2013 |
20130172310 | BENZAMIDES AND RELATED INHIBITORS OF FACTOR XA - Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders. | 07-04-2013 |
20130172311 | Substituted heterocyclyl benzyl pyrazoles, and use thereof - The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures. | 07-04-2013 |
20130172312 | Azetidine Derivatives - Azetidine derivatives of which the following is exemplary | 07-04-2013 |
20130184248 | NOVEL COMPOUNDS - This invention relates to compounds of formula I | 07-18-2013 |
20130190286 | B-RAF KINASE INHIBITORS - The present invention encompasses compounds of general formula (1) where in the groups R | 07-25-2013 |
20130190287 | THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE - Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein. | 07-25-2013 |
20130210795 | SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF - The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders. | 08-15-2013 |
20130210796 | TETRAZOLE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca | 08-15-2013 |
20130210797 | ADENOSINE A1 AGONISTS FOR THE TREATMENT OF GLAUCOMA AND OCULAR HYPERTENSION - The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension. | 08-15-2013 |
20130210798 | SOLUBLE GUANYLATE CYCLASE ACTIVATORS - This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver. | 08-15-2013 |
20130225548 | Pyridine Derivative and Medicinal Agent - A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. | 08-29-2013 |
20130231320 | SUBSTITUTED AMIDE COMPOUND - A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: | 09-05-2013 |
20130231321 | 2-SUBSTITUTED-ETHYNYLTHIAZOLE DERIVATIVES AND USES OF SAME - The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): | 09-05-2013 |
20130237514 | PYRROLIDINONE CARBOXAMIDE DERIVATIVES - Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor. | 09-12-2013 |
20130237515 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention relates to compounds of general formula I, | 09-12-2013 |
20130244993 | SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE - The present invention relates to compounds defined by formula I: wherein the variables A | 09-19-2013 |
20130252934 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 09-26-2013 |
20130261100 | PYRIDINE AMIDE DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS - The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 10-03-2013 |
20130267491 | PYRIMIDINE COMPOUNDS AS INHIBITORS OF PROTEIN KINASES IKK EPSILON AND/OR TBK-1, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKε and/or TBK-1: in which: R | 10-10-2013 |
20130267492 | ARYL SULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 10-10-2013 |
20130281426 | PYRIDAZINONES, THE PREPARATION METHOD AND THE USE THEREOF - The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer. | 10-24-2013 |
20130303505 | TGR5 AGONISTS - TGR5 agonists of structural formula VIII(Q), wherein X, R | 11-14-2013 |
20130303506 | AMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 11-14-2013 |
20130303507 | SUBSTITUTED HETERO-BIARYL COMPOUNDS AND THEIR USES - The present invention provides a compound of formula (II): | 11-14-2013 |
20130310357 | Azolyl Urea Compounds and Methods of Use Thereof - Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 11-21-2013 |
20130331370 | CERTAIN KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. | 12-12-2013 |
20140005161 | PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF | 01-02-2014 |
20140031329 | SUBSTITUTED DIHYDROPYRAZOLONES FOR TREATING CARDIOVASCULAR AND HEMATOLOGICAL DISEASES - The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing. | 01-30-2014 |
20140031330 | ARYL SULTAM DERIVATIVES AS RORc MODULATORS - Compounds of the formula I: | 01-30-2014 |
20140031331 | AMINOTETRALINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to aminotetraline derivatives of the formula (I) | 01-30-2014 |
20140051672 | 1,4-DISUBSTITUTED PYRIDAZINE ANALOGS THERE OF AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS - The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; | 02-20-2014 |
20140051673 | AMPK-Activating Heterocycloalkyloxy(Hetero)Aryl Carboxamide, Sulfonamide And Amine Compounds And Methods For Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 02-20-2014 |
20140066421 | OXIMES FOR TREATMENT OF PERIPHERAL AND CENTRAL NERVOUS SYSTEM EXPOSURE TO ACETYL CHOLINESTERASE INHIBITORS - The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates. | 03-06-2014 |
20140073620 | VEGFR3 INHIBITORS - This invention relates to a compound of the formula (I): | 03-13-2014 |
20140073621 | 5-ALKYNYL-PYRIMIDINES - The present invention encompasses compounds of general formula (1) | 03-13-2014 |
20140080798 | VEGFR3 INHIBITORS - This invention relates to compounds of the formula (I): | 03-20-2014 |
20140080799 | Aminopyrimidine Kinase Inhibitors - Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. | 03-20-2014 |
20140080801 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 03-20-2014 |
20140088071 | sGC STIMULATORS - Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed. | 03-27-2014 |
20140100210 | GUANIDINE COMPOUND | 04-10-2014 |
20140107093 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 04-17-2014 |
20140128363 | N-Link Hydroxamic Acid Derivatives Useful As Antibacterial Agents - The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. | 05-08-2014 |
20140135304 | NOVEL COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGANDS - The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. | 05-15-2014 |
20140142081 | COMPOUNDS AND THEIR METHODS OF USE - Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer. | 05-22-2014 |
20140142082 | PYRROLO SULFONAMIDE COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (ROR-GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES - The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof. | 05-22-2014 |
20140142083 | Substituted Benzene Compounds - The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 05-22-2014 |
20140148430 | IMIDAZOPYRIDINES SYK INHIBITORS - Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 05-29-2014 |
20140155370 | NUCLEAR TRANSPORT MODULATORS AND USES THEREOF - The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic). | 06-05-2014 |
20140162997 | SUBSTITUTED PYRAZOLES AS N-TYPE CALCIUM CHANNEL BLOCKERS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 06-12-2014 |
20140162998 | PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF - A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I. | 06-12-2014 |
20140162999 | PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF - PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I. | 06-12-2014 |
20140179662 | PHARMACEUTICALLY ACTIVE DISUBSTITUTED TRIAZINE DERIVATIVES - The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase. | 06-26-2014 |
20140179663 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 06-26-2014 |
20140179664 | Heterocyclyl Pyrimidine Analogues As JAK Inhibitors - The present invention relates to compounds of formula (I) | 06-26-2014 |
20140187529 | AMINOPYRAZINE COMPOUNDS - A compound of formula (I): | 07-03-2014 |
20140187530 | AZA Spiro Alkane Derivatives as Inhibitors of Metalloproteases - The present invention provides a compound of Formula I or Formula II: | 07-03-2014 |
20140187531 | APOPTOSIS PROMOTERS - Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. | 07-03-2014 |
20140194402 | PYRUVATE KINASE ACTIVATORS FOR USE IN THERAPY - Described herein are methods for using compounds that activate pyruvate kinase. | 07-10-2014 |
20140206660 | Phenyl-Heteroaryl Derivatives and Methods of Use Thereof - The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof | 07-24-2014 |
20140213568 | Pyrrolidine derivatives, pharmaceutical compositions and uses thereof - The invention relates to new pyrrolidine derivatives of the formula | 07-31-2014 |
20140213569 | Substituted 6-amino-nicotinamides as KCNQ2/3 modulators - Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 07-31-2014 |
20140213570 | 1,4-DISUBSTITUTED PYRIDAZINE ANALOGS THERE OF AND METHODS FOR TREATING SMN-DEFICIENCY-RELATED CONDITIONS - The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; | 07-31-2014 |
20140221332 | METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS OF USE THEREOF - Compounds that modulate GluR5 activity and methods of using the same are disclosed. | 08-07-2014 |
20140221334 | KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 08-07-2014 |
20140235606 | CRYSTALLINE FORMS OF N-[2-[[(2,3-DIFLUOROPHENYL)METHYL]THIO]-6--4-PYRIMIDINYL]-1-AZETIDINESULF- ONAMIDE - There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial. | 08-21-2014 |
20140235608 | PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. | 08-21-2014 |
20140235609 | CARBAMATE/UREA DERIVATIVES CONTAINING PIPERIDIN AND PIPERAZIN RINGS AS H3 RECEPTOR INHIBITORS - The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for treating diseases connected to tehinhibition of H3 receptor. | 08-21-2014 |
20140243303 | SPIROCYCLIC MOLECULES AS PROTEIN KINASE INHIBITORS - The present invention relates to spirocyclic compounds of formula I, namely spirocyclic (1H-pyrazol-4-yl)-3-(1-(2,6-dichloro-3-fiuorophenyl)ethoxy)pyridin-2-amines having protein kinase inhibitory activity, and methods of synthesizing and using such compounds. Preferred compounds are c-Met and/or ALK inhibitors useful for the treatment of abnormal cell growth, such as cancers. | 08-28-2014 |
20140249127 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 09-04-2014 |
20140249128 | TRIAZINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted triazine carboxamides of Formula I: | 09-04-2014 |
20140256699 | SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula Ia. | 09-11-2014 |
20140275002 | AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS - The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder. | 09-18-2014 |
20140275003 | BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS - The present invention provides compounds of Formula (I) | 09-18-2014 |
20140275005 | SUBSTITUTED PHENYL CYCLOALKYL PYRROLIDINE (PIPERIDINE) SPIROLACTAMS AND AMIDES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). | 09-18-2014 |
20140275006 | AZOLE DERIVATIVE - The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth. | 09-18-2014 |
20140288041 | Aryl- or Heteroaryl-Substituted Benzene Compounds - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 09-25-2014 |
20140303137 | AMINOPYRIMIDINES USEFUL AS KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention. | 10-09-2014 |
20140303138 | SUBSTITUTED OXINDOLE-DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES - The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses. | 10-09-2014 |
20140303139 | PYRIMIDINES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A | 10-09-2014 |
20140315878 | CHEMICAL COMPOUNDS - The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or a pharmaceutically acceptable salt thereof: | 10-23-2014 |
20140315879 | Sulfonamide Derivatives - The present invention relates to sulfonamide derivatives, of formula (I): | 10-23-2014 |
20140323460 | Methods for Using Carboxamide, Sulfonamide and Amine Compounds - Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein. | 10-30-2014 |
20140323461 | Phenyl-Substituted Nicotinic Ligands, and Methods of Use Thereof - Disclosed are compounds and methods of using them to treat a disorder selected from the group consisting of addiction, pain, obesity, schizophrenia, epilepsy, mania and manic depression, anxiety, Alzheimer's disease, learning deficit, cognition deficit, attention deficit, memory loss, Lewy Body Dementia, Attention Deficit Hyperactivity Disorder (ADHD), Parkinson's disease, Huntington's disease, Tourette's syndrome, amyotrophic lateral sclerosis, inflammation, stroke, spinal cord injury, dyskinesias, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, autism, mutism, trichotillomania, hypothermia, and disorders of sleep. | 10-30-2014 |
20140336165 | DIHYDROXY AROMATIC HETEROCYCLIC COMPOUND - Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as, for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. | 11-13-2014 |
20140343029 | Novel Imidazole Amines as Modulators of Kinase Activity - The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 11-20-2014 |
20140343030 | BIPYRAZOLE DERIVATIVES AS JAK INHIBITORS - The present invention provides compounds of Formula I: | 11-20-2014 |
20140343031 | N-Link Hydroxamic Acid Derivatives Useful As Antibacterial Agents - The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections. | 11-20-2014 |
20140349986 | SUBSTITUTED AMINOINDANES AND ANALOGS THEREOF, AND THE PHARMACEUTICAL USE THEREOF - The invention relates to substituted aminoindanes and analogs thereof of formula I | 11-27-2014 |
20140357612 | COMPOUNDS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases and methods for regulating protein kinase pathways are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 12-04-2014 |
20140357613 | Aminoheteroaryl compounds and preparation method and use thereof - The present invention refers to aminoheteroaryl compounds of the following formula (I) as well as the preparation method and use thereof, wherein R | 12-04-2014 |
20140357614 | Diamino-Pyridine, Pyrimidine, and Pyrazine Modulators of the Histamine H4 Receptor - Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H | 12-04-2014 |
20140364408 | Hydrazide Containing Nuclear Transport Modulators And Uses Thereof - The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity. | 12-11-2014 |
20140371195 | INHIBITORS OF HISTONE DEMETHYLASES - The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form | 12-18-2014 |
20140371196 | DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND - Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer. | 12-18-2014 |
20140378428 | 2,5-Disubstituted-Pyridyl Nicotinic Ligands, and Methods of Use Thereof - Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia. | 12-25-2014 |
20140378429 | Carboxamide, Sulfonamide and Amine Compounds and Methods for Using Them - The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein. | 12-25-2014 |
20150011526 | 2-Oxo-Piperidinyl Derivatives - The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals. | 01-08-2015 |
20150018328 | THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE - Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein. | 01-15-2015 |
20150018330 | BROAD SPECTRUM BENZOTHIOPHENE-NITROTHIAZOLIDE AND OTHER ANTIMICROBIALS - The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative | 01-15-2015 |
20150025055 | MUTANT-SELECTIVE EGFR INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 01-22-2015 |
20150031661 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to pyrazine compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 01-29-2015 |
20150038481 | PYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER - Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described. | 02-05-2015 |
20150045339 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR SALT THEREOF - The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL). | 02-12-2015 |
20150051185 | Chemical Compounds 251 - The invention relates to chemical compounds of formula I, | 02-19-2015 |
20150057260 | ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0): | 02-26-2015 |
20150065477 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS V - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R | 03-05-2015 |
20150065478 | Amino-Derivatives As Novel Inhibitors Of Histone Deacetylase - This invention comprises the novel compounds of formula (I) | 03-05-2015 |
20150072970 | BIARYL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME - The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents. | 03-12-2015 |
20150080362 | ANTIBACTERIAL COMPOUNDS AND METHODS FOR USE - The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens. | 03-19-2015 |
20150080363 | SUBSTITUTED 5-,6- AND 7-MEMBERED HETEROCYCLES, MEDICAMENTS CONTAINING SUCH COMPOUNDS, AND THEIR USE - The present invention relates to compounds defined by formula I: wherein the variables A | 03-19-2015 |
20150094294 | COMPOUNDS AND METHODS FOR TREATING MALARIA - The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a | 04-02-2015 |
20150099728 | Substituted Phenylureas and Phenylamides as Vanilloid Receptor Ligands - Substituted phenylureas and phenylamides, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for preparing pharmaceutical compositions. | 04-09-2015 |
20150099729 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I | 04-09-2015 |
20150111866 | CYCLIC AMINE SUBSTITUTED HETEROCYCLIC CETP INHIBITORS - Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. | 04-23-2015 |
20150111867 | Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy - The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) | 04-23-2015 |
20150119375 | PYRAZOLE INDANYL CARBOXAMIDES - The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials. | 04-30-2015 |
20150126484 | AMINOPYRIMIDINE DERIVATIVES FOR USE AS MODULATORS OF KINASE ACTIVITY - The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 05-07-2015 |
20150126485 | BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 - The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers. | 05-07-2015 |
20150133423 | AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS - The invention provides certain azetidinyloxyphenylpyrrolidine compounds, particularly compounds of formula I wherein R is hydrogen or methyl, and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder. | 05-14-2015 |
20150141395 | BENZOFURAN DERIVATIVES FOR THE TREATMENT OF HEPATITIS C - The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 05-21-2015 |
20150291514 | N-Aminosulfonyl Benzamides - The present invention relates to sulfonamide derivatives of formula (I): | 10-15-2015 |
20150291576 | COMPOUNDS AND THEIR METHODS OF USE - Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided. | 10-15-2015 |
20150296787 | SUBSTITUTED AZINES AS PESTICIDES - The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically acceptable salt thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling endoparasites in warm-blooded animals | 10-22-2015 |
20150299165 | PYRIDINE-2-AMIDES USEFUL AS CB2 AGONISTS - The invention relates to CB2 agonists of formula (I) wherein R | 10-22-2015 |
20150299179 | SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS - Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated. | 10-22-2015 |
20150299214 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound represented by the following formula (I), wherein X | 10-22-2015 |
20150307452 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) wherein R | 10-29-2015 |
20150315187 | INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1 - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer. | 11-05-2015 |
20150322040 | 3-ESTER-4 SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 11-12-2015 |
20150342930 | NOVEL FXR (NR1H4) BINDING AND ACTIVITY MODULATING COMPOUNDS - The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds. | 12-03-2015 |
20150344443 | INHIBITORS OF THE USP1/UAF1 DEUBIQUITINASE COMPLEX AND USES THEREOF - Disclosed are inhibitors of the USP1/UAF1 deubiquitinase complex, for example. of formula (I), wherein R | 12-03-2015 |
20150353512 | TRIAZINE CARBOXAMIDES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted triazine carboxamides of Formula I: | 12-10-2015 |
20150376169 | HISTONE DEMETHYLASE INHIBITORS - The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 12-31-2015 |
20160000784 | PYRIMIDINE COMPOUNDS USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY IKKE AND/OR TBK1 MECHANISMS - Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKKε and/or TBK-1 in which one of V and W is N, and the other of V and W is C—H; and R | 01-07-2016 |
20160002218 | 2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF | 01-07-2016 |
20160009662 | PYRAZINE GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES | 01-14-2016 |
20160009686 | VEGFR3 INHIBITORS | 01-14-2016 |
20160015687 | TETRAZOLE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca | 01-21-2016 |
20160016968 | NOVEL PYRIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 01-21-2016 |
20160024021 | NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND THEIR USAGE - The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, | 01-28-2016 |
20160024022 | PYRIMIDINES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A | 01-28-2016 |
20160024050 | NOVEL ACRYLAMIDE DERIVATIVES AS ANTIMALARIAL AGENTS - The invention relates to novel acrylamide derivatives of the formula (I) wherein R | 01-28-2016 |
20160031825 | SUBSTITUTED DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY - Substituted dihydropyrimidinones of formula 1 | 02-04-2016 |
20160031853 | 2-Halo-5-Alkynyl-Pyridyl Nicotinic Ligands - Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia. | 02-04-2016 |
20160031870 | COMPOUNDS FOR THE TREATMENT OF TUBERCULOSIS - Disclosed are compounds that can be used for treating tuberculosis. | 02-04-2016 |
20160031871 | Glycosidase Inhibitors - Compounds of formula (I) | 02-04-2016 |
20160031904 | COMPOUNDS AND USES THEREOF FOR THE MODULATION OF HEMOGLOBIN - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 02-04-2016 |
20160038483 | HEPATITIS C VIRUS INHIBITORS - The invention provides compounds of formula (I): | 02-11-2016 |
20160039771 | DIHYDROXY AROMATIC HETEROCYCLIC COMPOUND - Provided is a compound having a D-amino acid oxidase (DAAO) inhibitory action, and useful as for example, a prophylaxis and/or therapeutic agent for schizophrenia or neuropathic pain. The present inventors have studied a compound that inhibits DAAO, and confirm that a dihydroxy aromatic heterocyclic compound has a DAAO inhibitory action, and completed the present invention. That is, the dihydroxy aromatic heterocyclic compound of the present invention has a good DAAO inhibitory action, and can be used as a prophylaxis and/or therapeutic agent for, for example, schizophrenia or neuropathic pain. | 02-11-2016 |
20160039802 | 3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH - The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R | 02-11-2016 |
20160039804 | NOVEL OXAZOLIDINONE DERIVATIVE AS CETP INHIBITOR, ITS PREPARATION METHOD, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed are a novel oxazolidinone derivative exhibiting inhibitory activity against CETP, a preparation method thereof, and a pharmaceutical composition comprising the same. Exhibiting excellent inhibitory activity against CETP, the oxazolidinone derivative can be effectively applied to the prevention or treatment of various CETP enzyme activity- or HDL cholesterol level-related diseases such as dyslipidemia, atherosclerosis, and coronary heart disease. | 02-11-2016 |
20160039834 | CARM1 INHIBITORS AND USES THEREOF - Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R | 02-11-2016 |
20160052926 | NOVEL PYRIMIDINE AND PYRIDINE COMPOUNDS AND USAGE THEREOF - The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, | 02-25-2016 |
20160102076 | COMPOUNDS AND COMPOSITIONS FOR MODULATING EGFR MUTANT KINASE ACTIVITIES - The present invention provides a new group of protein kinase inhibitors, aminopyrimidine derivatives, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer and immune disease. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefore. The invention also provides useful intermediates generated during the syntheses of the aminopyrimidine derivatives. | 04-14-2016 |
20160106665 | OCULAR DISCOMFORT - Described herein are methods and pharmaceutical formulations for improving ocular discomfort. | 04-21-2016 |
20160107995 | HISTONE DEMETHYLASE INHIBITORS - The present disclosure relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 04-21-2016 |
20160108023 | Novel Compound - There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. | 04-21-2016 |
20160115128 | AROMATIC COMPOUND - Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: | 04-28-2016 |
20160115158 | N-(HETEROARYL)-SULFONAMIDE DERIVATIVES USEFUL AS S100-INHIBITORS - A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders. | 04-28-2016 |
20160122316 | SERINE/THREONINE KINASE INHIBITORS - Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 05-05-2016 |
20160122326 | TRIAZOLE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Aβ-related diseases. | 05-05-2016 |
20160129002 | PYRIMIDINE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS - The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Aβ-related diseases. | 05-12-2016 |
20160130230 | SUBSTITUTED DICYANOPYRIDINES AND USE THEREOF - The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders. | 05-12-2016 |
20160130247 | INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1 - The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer. | 05-12-2016 |
20160130253 | MAP KINASE MODULATORS AND USES THEREOF - The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38α MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising administration of MAP kinase inhibitors or compositions comprising MAP kinase inhibitors. In some embodiments, the disease is Alzheimer's Disease, ALS, Huntington's Disease or Parkinson's Disease. | 05-12-2016 |
20160130258 | SMALL MOLECULE INHIBITORS OF FIBROSIS - Described herein are compounds and compositions for the treatment of a fibrotic disease. | 05-12-2016 |
20160130262 | N-SUBSTITUTED AZETIDINE DERIVATIVES - The present invention relates to novel N-substituted azetidine derivativesto pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERα) antagonistic and—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells. | 05-12-2016 |
20160137609 | PYRAZOLE DERIVATIVES AS ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. Formula (I). | 05-19-2016 |
20160145252 | HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF - The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. | 05-26-2016 |
20160152595 | INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1 | 06-02-2016 |
20160152621 | ARYL LACTAM KINASE INHIBITORS | 06-02-2016 |
20160159782 | INHIBITORS OF EZH2 - The present invention relates to compounds that inhibit activity of the histone lysine N-methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, such as hematologic and solid tumors. | 06-09-2016 |
20160168137 | INHIBITORS OF HUMAN 12/15-LIPOXYGENASE | 06-16-2016 |
20160175314 | 1,2,4-TRIAZINE-4-AMINE DERIVATIVES | 06-23-2016 |
20160185752 | PIPERIDINE AND AZEPINE DERIVATIVES AS PROKINETICIN RECEPTOR MODULATORS - The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof (Formula (I)) in which m, X, R | 06-30-2016 |
20160185797 | ALKYNYL ALCOHOLS AND METHODS OF USE - The invention relates to compounds of Formula (0): | 06-30-2016 |
20160194342 | PHENICOL ANTIBACTERIALS | 07-07-2016 |
20160200705 | BENZAMIDE DERIVATIVES FOR INHIBITING THE ACTIVITY OF ABL1, ABL2 AND BCR-ABL1 | 07-14-2016 |
20160251335 | NEW COMPOUNDS | 09-01-2016 |
20160251341 | SUBSTITUTED TRIAZOLE COMPOUNDS AS SERINE PROTEASE INHIBITORS | 09-01-2016 |
20160376238 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formula (I): | 12-29-2016 |
20160376279 | FXR AGONISTS AND METHODS FOR MAKING AND USING - Novel FXR agonists are disclosed, embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject. | 12-29-2016 |
20170233352 | HSP70 MODULATORS AND METHODS FOR MAKING AND USING THE SAME | 08-17-2017 |
20170233373 | Crystalline (2S)-3-[(3S,4S)-3-[(1R)-1-hydroxyethyl]-4-(4-methoxy-3-phenyl)-3-methylpy- rrolidin-1-yl]-3-oxopropane-1,2-diol | 08-17-2017 |
20170233380 | NOVEL COMPOUNDS AS ROR GAMMA MODULATORS | 08-17-2017 |
20190142814 | Novel FXR (NR1H4) binding and activity modulating compounds | 05-16-2019 |
20190144394 | INHIBITORS OF PROTEASE-ACTIVATED RECEPTOR-2 | 05-16-2019 |
20190144399 | NOVEL 2,4,6-TRISUBSTITUTED S-TRIAZINE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF | 05-16-2019 |
20220135574 | BIARYL DERIVATIVE AS GPR120 AGONIST - The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis. | 05-05-2022 |