39th week of 2013 patent applcation highlights part 57 |
Patent application number | Title | Published |
20130252883 | Macrocycles and Their Uses - The present application describes a method of treating a bacterial infection comprising administering to a subject in need thereof a pharmaceutically acceptable amount of a defined macrocycle compound. | 2013-09-26 |
20130252884 | FGF21 ANALOGUES AND DERIVATIVES - Novel analogues of Fibroblast Growth Factor 21 (FGF21), derivatives thereof having a modifying moiety covalently attached thereto, and pharmaceutical use of these analogues and derivatives, in particular, for the treatment of diabetes, dyslipidemia, obesity, cardiovascular diseases, metabolic syndrome, and/or Non Alcoholic Fatty Liver Disease (NAFLD) are described. | 2013-09-26 |
20130252885 | FUSED TRICYCLIC COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONIST - The present disclosure relates to fused tricyclic compounds of formula (I) or its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2A adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2A receptor. Such conditions include, but are not limited to, Parkinsons disease, restless leg syndrome, Alzheimers disease, neurodegenerative disorder, inflammation, wound healing, dermal fibrosis, nocturnal myoclonus, cerebral ischaemia, myocardial ischemia, Huntington's disease, multiple system atrophy, corticobasal degeneration, Wilson's disease or other disorders of basal ganglia which results in dyskinesias, post traumatic stress disorder, hepatic cirrhosis, sepsis, spinal cord injury, retinopathy, hypertension, social memory impairment, depression, neuroprotection, narcolepsy or other sleep related disorders, attention deficit hyperactivity disorder, drug addiction, post traumatic stress disorder and vascular injury and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them. | 2013-09-26 |
20130252886 | METHODS OF DELAYING AND TREATING DIABETES - The present invention provides methods of treating hyperglycemia and delaying the onset of diabetes, comprising administering to a mammal in need thereof a therapeutically effective amount of a GABA receptor agonist at or near a time of an exogenous insulin administration or a meal. | 2013-09-26 |
20130252887 | COMPOSITIONS AND METHODS FOR TREATING ANTIPHOSPHOLIPID SYNDROME - The invention features compositions and methods of using a dimeric inhibitor, e.g., A1-A1, to selectively target β2GPI in β2GPI/antibody complexes. The compositions can be administered to subjects (e.g., a mammal, such as a human) having or likely to develop APS, or one or more symptoms of APS, in order to treat or inhibit the disease or treat or reduce its symptoms. The inhibitors of the invention include two ligand-binding A1 modules, e.g., from ApoER2, connected by a flexible linker. | 2013-09-26 |
20130252888 | USE OF IMP3 AS A PROGNOSTIC MARKER FOR CANCER - Provided herein are methods and compositions for the prognostic evaluation of a patient suspected of having, or having, cancer by assessing the expression of IMP3 in a biological sample of a patient. Methods can be used at the time of initial diagnosis of malignant tumors to identify a group of patients with a high potential to develop progression or metastasis later. Therefore, methods not only are able to provide very useful prognostic information for patients but also can help clinicians to select a candidate patient likely to benefit from early and aggressive cancer therapy. Methods and compositions for the treatment of cancer associated with expression of IMP3 are also provided. | 2013-09-26 |
20130252889 | COMPOSITION COMPRISING VLP AND AMYLOID BETA PEPTIDE - The present invention relates to novel uses of a construct consisting of virus-like particle (VLP) structure chemically coupled to a fragment of the AD-1-42 peptide and its pharmaceutically acceptable salts (hereinafter CONSTRUCT), in particular to dosage regimens, modes of and dosage forms for the administration of a CONSTRUCT for the treatment of patients suffering from dementia. in particular dementia of the A | 2013-09-26 |
20130252890 | 6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, PHARMACEUTICAL PREPARATIONS COMPRISING THEM, AND THE USE THEREOF FOR PRODUCTION OF MEDICAMENTS - The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. | 2013-09-26 |
20130252891 | Therapeutically Active Alpha-MSH Analogues - The invention describes peptide analogues of α-melanocyte-stimulating hormone (α-MSH), which possess an increased efficacy compared to the native α-MSH peptide. The α-MSH analogues exhibit increased anti-inflammatory effects and increased capability to prevent ischemic conditions compared to α-MSH. The invention further discloses use of the peptides for the manufacture of pharmaceutical compositions for the treatment or prophylaxis of a condition in the tissue of one or more organs of a mammal, and moreover pharmaceutical compositions. | 2013-09-26 |
20130252892 | NOVEL OCTAPEPTIDE COMPOUNDS AND THERAPEUTIC USE THEREOF - The present invention relates to novel octapeptide compounds of general formula (I), | 2013-09-26 |
20130252893 | Novel Composition - There is provided according to the invention an aqueous composition having pH between 4 and 7 comprising (i) glucagon at a concentration of 0.05% w/v or more and (ii) a cationic surfactant selected from benzalkonium salts and benzethonium salts as solubilising agent in an amount sufficient to dissolve the glucagon in the composition. | 2013-09-26 |
20130252894 | SUSTAINED DELIVERY OF EXENATIDE AND OTHER POLYPEPTIDES - Described herein are implantable devices, formulations and methods of making implantable devices for the release of a polypeptide from an implantable device, and methods of use thereof. | 2013-09-26 |
20130252895 | PEPTIDES OF SYNDECAN-1 FOR INHIBIT ANGIOGENESIS - The present invention provides a peptide derived from the extracellular domain of syndecan-1 that inhibits angiogenesis. | 2013-09-26 |
20130252896 | TFPI INHIBITORS AND METHODS OF USE - The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound. | 2013-09-26 |
20130252897 | Methods and Compositions Regarding Polychalcogenide Compositions - The present invention concerns the use of polychalcogenide compositions on cells, tissue, organs, and organisms to enhance their survivability. It includes compositions, compounds, methods, articles of manufacture and apparatuses for enhancing survivability and for protecting them from or treating them for injury or damage. In specific embodiments, there are also therapeutic methods and apparatuses for hypoxic/ischemic injury, organ transplantation, hyperthermia, wound healing, hemorrhagic shock, cardioplegia for bypass surgery, neurodegeneration, hypothermia, and cancer using the polychalcogenide compositions described. | 2013-09-26 |
20130252898 | METHOD AND COMPOSITIONS FOR THE TREATMENT AND DETECTION OF ENDOTHELIN-1 RELATED KIDNEY DISEASES - The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1-associated biomarker in a biological sample is also disclosed. | 2013-09-26 |
20130252899 | COLLAGEN HYDROLYSATE FOR USE TO IMPROVE THE HEALTH OF HUMAN SKIN, HAIR AND/OR NAILS - The invention relates to a collagen hydrolysate for use to improve the health of human skin, hair and/or nails, at least 90% by weight of the collagen hydrolysate having a molecular weight of less than 3,500 Da and the collagen hydrolysate comprising at least four characteristic peptides with a molecular weight between 600 and 1,200 Da. | 2013-09-26 |
20130252900 | MICROSPHERES USEFUL FOR THERAPEUTIC VASCULAR EMBOLIZATION - Provided herein, for example, are microspheres comprising a gelatin or gelatin substitute and a copolymer of a N-tris-hydroxymethyl methylacrylamide monomer unit, a diethylaminoethylacrylamide monomer unit and a N,N-methylene-bis-acrylamide monomer unit. Also provided are methods of producing microspheres comprising a gelatin or gelatin substitute and a copolymer of a N-tris-hydroxymethyl methylacrylamide monomer unit, a diethylaminoethylacrylamide monomer unit and a N,N-methylene-bis-acrylamide monomer unit. Further provided herein, for example, are compositions comprising the microspheres and methods of using the microspheres and compositions thereof. | 2013-09-26 |
20130252901 | PEPTIDE COMPOUND USEFUL FOR INHIBITING AMYLOID PLAQUE FORMATION - A peptide compound of the following general formula (I) or (II): | 2013-09-26 |
20130252902 | TYPE A2 BOTULINUM TOXIN PREPARATION - A method for treating a patient who has a neutralizing antibody to a type A1 botulinum toxin. The method includes administering 150 kDa type A neurotoxin from type A2 | 2013-09-26 |
20130252903 | COMPOSITIONS FOR REDUCING OXIDATIVE STRESS AND USES THEREOF - The present invention relates to the use of one or more tripeptides selected from the group consisting of | 2013-09-26 |
20130252904 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The invention relates to compounds, compositions, kits, and methods for the treatment of a cancer. In particular, the invention relates to compounds, compositions, or kits comprising a folate-vinca conjugate, and methods for the treatment of a cancer with a folate-vinca conjugate. | 2013-09-26 |
20130252905 | PLIF MULTIMERIC PEPTIDES AND USES THEREOF - Provided is a multimeric peptide comprising at least two peptide monomers linked to one another, each of the at least two peptide monomers comprising at least 6 consecutive amino acids from the amino acid sequence as set forth in SEQ ID NO: 1, wherein the at least two peptide monomers are each no longer than 30 amino acids, wherein the multimeric peptide is capable of reducing binding of Placenta Immunomodulatory Factor (PLIF) to human leukocytes. | 2013-09-26 |
20130252906 | COMPOUNDS AND METHODS FOR TREATING OR PREVENTING DISEASE CONDITIONS ASSOCIATED WITH ALPHA-1-ANTITRYPSIN - Pharmacological chaperone compounds and methods for the treatment of an individual having, or at risk of having, a disease condition associated with alpha-1-antitrypsin by using said compounds are disclosed. In particular, such methods are useful for the treatment or prevention of lung disorders associated with alpha-1-antitrypsin deficiency as well as liver disorders associated with an excess of alpha-1-antitrypsin. Suitable pharmacological chaperones include peptides and low-molecular weight compounds. Also provided is an assay for determining whether a test compound modulates alpha-1-antitrypsin activity. | 2013-09-26 |
20130252907 | Small Peptides And Methods For Blocking IgE Mediated Activation Of An Immune Cell - Methods for treating cutaneous inflammation, are described. Also described is a method for inhibiting the mucous release into airways of a patient, a method for blocking IgE activation of an immune cell, a method for stabilizing the cell membrane of an immune cell, thereby preventing their further involvement in the increased inflammatory response to an IgE antigen challenge, and a method for inhibiting the migration of T-cells. Such methods involve administering to said patient a therapeutically effective amount of a peptide having the formula f-Met-Leu-X, wherein X is selected from the group consisting of Tyr, Tyr-Phe, Phe-Phe and Phe-Tyr. | 2013-09-26 |
20130252908 | PHARMACEUTICAL COMPOSITION, METHODS FOR TREATING AND USES THEREOF - The invention relates to the treatment of metabolic disorders in an overweight or obese patient characterized in that empagliflozin and one or more antiobesity drugs are administered to the patient. | 2013-09-26 |
20130252909 | TANNIN INHIBITORS OF HIV - The invention provides a method to prevent or treat HIV-infection with synthetic tannins, and pharmaceutical compositions comprising synthetic tannins. | 2013-09-26 |
20130252910 | GLYCOMIMETIC COMPOUNDS AS ANTI-INFECTIOUS AGAINST PATHOGENS LECTINS - The present invention relates to a calixarene-based glycosylated compound (I) having the formula: (I) wherein D is independently selected in the group comprising a —CH | 2013-09-26 |
20130252911 | COMPOSITIONS COMPRISING FLAVONOID-CONTAINING EXTRACTS FROM PLANTS OF THE GENUS CITRUS AND/OR ISOLATED CITRUS FLAVONOIDS AND SPECIFIC CATIONIC SURFACE ACTIVE AGENTS, AND SAID COMPOSITION FOR USE AS AN AGENT FOR TREATING INFESTATIONS WITH HEAD LICE - A composition having anti-lice properties comprising effective amounts of at least one monoalkyl and/or dialkyl quat and/or amidoquat in combination with flavonoid-containing extracts obtained from | 2013-09-26 |
20130252912 | Antibiotic Macrocycle Compounds and Methods of Manufacture and Use Thereof - The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of | 2013-09-26 |
20130252913 | 18-Membered Macrocycles and Analogs Thereof - The present invention relates generally to the 18-membered macrocyclic antimicrobial agents called Tiacumicins, specifically, OPT-80 (which is composed almost entirely of the R-Tiacumicin B), pharmaceutical compositions comprising OPT-80, and methods using OPT-80. In particular, this compound is a potent drug for the treatment of bacterial infections, specifically | 2013-09-26 |
20130252914 | Macrolide Polymorphs, Compositions Comprising Such Polymorphs, and Methods of Use and Manufacture Thereof - The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to | 2013-09-26 |
20130252915 | CRYSTALLINE FORMS OF A MACROLIDE, AND USES THEREFOR - New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein. | 2013-09-26 |
20130252916 | ORAMUCOSAL PHARMACEUTICAL DOSAGE FORM - This invention relates to an oramucosal pharmaceutical dosage form in the form of a wafer. The wafer comprises a porous, hydroscopic, muco-adhesive polymeric matrix with at least one desired pharmaceutically active compound added thereto. The polymer is selected from a number of polymers having different dissolution rates and, in use when taken orally, the matrix adheres to an oramucosal surface to dissolve over a predetermined period of time to release the pharmaceutically active compound. The invention also extends to a method of manufacturing an oramucosal pharmaceutical dosage form in the form of a wafer which involves freeze drying or lyophilisation. | 2013-09-26 |
20130252917 | COMBINATION THERAPY OF 4-(3-(2H-1,2,3-TRIAZO-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO- )PYRIMIDINE-5-CARBOXAMIDE AND FLUDARABINE - The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(3-(2H-1,2,3-triazol-2-yl)phenylamino)-2-(1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma. | 2013-09-26 |
20130252918 | PHOSPHORAMIDITE DERIVATIVES OF GEMCITABINE FOR USE IN THE TREATMENT CANCER - Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR′R″ where R′ is H and R″ is CR | 2013-09-26 |
20130252919 | URIDINE DIPHOSPHATE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISORDERS - This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P | 2013-09-26 |
20130252920 | PHARMACEUTICAL COMBINATIONS COMPRISING A THIONUCLEOTIDE ANALOG - Disclosed herein are pharmaceutical compositions that can include a thionucleotide analog for use in combination therapy with other agents. Also disclosed herein are methods of treating diseases and/or conditions with a pharmaceutical composition that can include a thionucleotide analog in combination therapy with other agents. | 2013-09-26 |
20130252921 | ADHESION BARRIER CONTAINING HYALURONIC ACIDS AND L-ARGININE - The present invention relates to an anti-adhesive agent containing hyaluronic acid and L-arginine, which has increased in vivo residence time and excellent anti-adhesive properties. According to the present invention, adhesion can be prevented from occurring due to surgical operation, infection and trauma. | 2013-09-26 |
20130252922 | SUBSTITUTED PHENOXYPYRIDINES - The present invention relates to substituted phenoxypyridine compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 2013-09-26 |
20130252923 | SKIN-BEAUTIFYING AGENT - A skin-beautifying agent, food, beverage, or feed for skin-beautification which has cosmetic effects such as moisturizing and beautifying the skin as well as preventing skin roughness and wrinkles by oral intake. Also described is a skin-beautifying agent containing a milk-derived phospholipid as an effective ingredient, and to provide food, beverage, or feed for skin- beautification containing the skin-beautifying agent. The milk-derived phospholipid is preferably a composition prepared from milk or milk material containing 40 to 70% by weight of lipid in a total solid content and containing 30% or more by weight of milk-derived phospholipid. | 2013-09-26 |
20130252924 | Compounds and Methods for Treating Pain - The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies. | 2013-09-26 |
20130252925 | PAIN RELIEF COMPOSITIONS, MANUFACTURE AND USES - The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions. | 2013-09-26 |
20130252926 | METFORMIN SALTS OF SALICYLIC ACID AND IT CONGENERS - The present invention relates to compounds, | 2013-09-26 |
20130252927 | TREATING CONDITIONS ASSOCIATED WITH INCREASED EOTAXIN WITH 25-HYDROXYVITAMIN D3 - The present invention relates to treating/preventing conditions associated with an increased level of eotaxin in a human with 25-hydroxyvitamin D3 (calcifediol). Optionally, vitamin D3 may be used together with 25-hydroxyvitamin D3. | 2013-09-26 |
20130252928 | COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS - Combinations comprising (a) a PDE4 Inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases. | 2013-09-26 |
20130252929 | PHARMACEUTICAL COMPOSITION INCLUDING MOMETASONE FUROATE AND AZELASTINE HYDROCHLORIDE FOR NASAL ADMINISTRATION - The present invention provides a pharmaceutical composition for nasal administration comprising mometasone furoate and azelastine hydrochloride, wherein the pharmaceutical composition comprises thaumatin as an agent for reducing bitterness and irritation. | 2013-09-26 |
20130252930 | CYP11B, CYP17, AND/OR CYP21 INHIBITORS - Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z) | 2013-09-26 |
20130252931 | SYNTHETIC BILE ACID COMPOSITIONS AND METHODS - Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties. | 2013-09-26 |
20130252932 | LOCALIZED MODULATION OF TISSUES AND CELLS TO ENHANCE THERAPEUTIC EFFECTS INCLUDING RENAL DENERVATION - Pharmaceutical preparations, compositions, systems, and devices including medical devices and diagnostic or therapeutic agents, and methods to treat disease by modification of local tissue environment to modulate the therapeutic index of locally or systemically delivered therapeutic or diagnostic agents. Improved ability to reduce sympathetic nerve activity in the adventitia and perivascular tissues around arteries and veins in the body. Modulation of the local tissue environment around an artery to enable more effective denervation with or without a therapeutic agent. Modulation may include adjustment of the pH of the tissue. | 2013-09-26 |
20130252933 | Compositions for Delivering Perfume to the Skin - A cleansing composition comprising at least 5% of a surfactant, at least about 25% water, a cyclodextrin complex comprising a perfume, wherein 80% of the plurality of perfume raw materials comprise a FDV of at least 0.69. | 2013-09-26 |
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. | 2013-09-26 |
20130252935 | Monobactams - The present invention is directed to a new class of monobactam derivatives and their use for treating bacterial infections. | 2013-09-26 |
20130252936 | PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGENERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME - Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein. | 2013-09-26 |
20130252937 | NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACIDS - The present invention relates to compounds of general formula I, | 2013-09-26 |
20130252938 | Antibacterial Compounds - The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. | 2013-09-26 |
20130252939 | TRI-CYCLIC PYRAZOLOPYRIDINE 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. | 2013-09-26 |
20130252940 | c-Met Modulators and Method of Use - The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds. | 2013-09-26 |
20130252941 | PYRAZOLOPYRIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention provides compounds of Formula I, stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R | 2013-09-26 |
20130252942 | QUINAZOLINE CARBOXAMIDE AZETIDINES - The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer. | 2013-09-26 |
20130252943 | BICYCLIC OXAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-09-26 |
20130252944 | NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR | 2013-09-26 |
20130252945 | AMORPHOUS BIOINORGANIC IONIC LIQUID COMPOSITIONS COMPRISING PHARMACEUTICALS - An amorphous formulations of a pharmaceutical includes a composition of the formula [A] | 2013-09-26 |
20130252946 | Fluoroquinolone Carboxylic Acid Molecular Crystals - Disclosed herein is a molecular crystal form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1-cyclopropyl-8-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid. The molecular crystal is characterized by at least one of: (a) an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 10.6, 15, 19.7, 21.1, and 22°±0.2°; (b) a DSC melting peak at 288° C.; (c) a | 2013-09-26 |
20130252947 | BMP-2 Upregulating Compounds For Healing Bone Tissue And Screening Methods For Selecting Such Compounds - The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit. | 2013-09-26 |
20130252948 | Substituted piperidines - The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases. | 2013-09-26 |
20130252949 | APREPITANT L-PROLINE COMPOSITION AND COCRYSTAL - A 1:1:1 aprepitant L-proline H | 2013-09-26 |
20130252950 | TARGETING MTOR SUBSTRATES IN TREATING PROLIFERATIVE DISEASES - Provided are over 300 mTOR kinase targets identified by a comprehensive phosphoproteomics assay. Methods of targeting mTOR kinase targets, methods to determine the level of mTOR activity by measuring the level of phosphorylation of an mTOR targeted phosphorylation site, methods for distinguishing different classes of mTOR activity in a cell based on phosphoproteomic analysis of mTOR-targeted proteins are also provided. Also provided is the classification of a hyperproliferative disease based on phosphoproteomic analysis of mTOR-targeted proteins, as well as the personalization of therapeutic methods for the treatment of hyperproliferative disease based on phosphoproteomics. Also provided are therapeutic methods including administering to a subject an mTOR inhibitor, an mTOR inhibitor and an additional kinase inhibitor, or a dual inhibitor of mTOR and an additional kinase based on the phosphorylation levels of mTOR targets determined in the subject. Some aspects of this invention relate to the discovery that GrblO is an mTOR-targeted tumor suppressor gene. | 2013-09-26 |
20130252951 | 7-HYDROXY-PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AND THEIR USE AS CCR2 RECEPTOR ANTAGONISTS - The compounds of formula (I) are antagonists of the CCR2 receptor Wherein R | 2013-09-26 |
20130252952 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) | 2013-09-26 |
20130252953 | Targeting Human Thymidylate Kinase Induces DNA Repair Toxicity in Malignant Tumor Cells - The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers. | 2013-09-26 |
20130252954 | CRYSTAL OF AMIDE COMPOUND - Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms. | 2013-09-26 |
20130252955 | (AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH | 2013-09-26 |
20130252956 | METHODS OF TREATING CANCER - Methods for treating a human having heptocellular carcinoma comprising administering to the human a therapeutically effective amount of Compound A: | 2013-09-26 |
20130252957 | PYRIDINONE ANTAGONISTS OF ALPHA-4 INTEGRINS - The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: | 2013-09-26 |
20130252958 | QUINOLINE COMPOUND COMPOSING 1,2,4-TRIAZINE-DIONE AND USE THEREOF - The present invention relates to a quinoline deravative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R | 2013-09-26 |
20130252959 | NITRIC OXIDE DONORS IN THERAPY OF NITRIC OXIDE DEFICIENCY-INDUCED DISTURBANCES OF CEREBRAL MICROCIRCULATION - The present invention relates to nitric oxide releasing compounds and their use in the prevention, amelioration and/or therapy of nitric oxide (NO) deficiency induced disturbances of the cerebral microcirculation. The NO deficiency induced disturbances of the cerebral microcirculation may be due to an intracranial hemorrhage or stroke and can cause cerebrovascular spasms (or cerebral vasospasms) (CVS) and/or malperfusion of brain parenchyma caused by blood vessel and blood flow dysregulation which, in turn, can cause secondary neurological deficiencies (DIND) and/or brain infarction. Particularly, the present invention relates to the prevention, amelioration and/or therapy of delayed cerebral vasospasm-associated disorders after survived subarachnoidal hemorrhage by applying a NO-donor, most preferably Molsidomine. | 2013-09-26 |
20130252960 | PTERIDINES AND THEIR USE AS AGROCHEMICALS - The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products. More specifically, the invention provides new compounds of the formula (I-A): | 2013-09-26 |
20130252961 | MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES - The invention relates to compounds of formula (Φ) | 2013-09-26 |
20130252962 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. | 2013-09-26 |
20130252963 | PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASE OR CONDITIONS MEDIATED BY LP-PLA2 - The present invention relates to novel compounds that inhibit Lp-PLA | 2013-09-26 |
20130252964 | Compounds And Methods For Treating Candidiasis And Aspergillus Infections - The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a | 2013-09-26 |
20130252965 | COMBINATIONS OF SEROTONIN RECEPTOR AGONISTS FOR TREATMENT OF MOVEMENT DISORDERS - The present invention relates to the use of 5-HT1 agonists in pharmaceutical compositions, compounds and methods for treatment of movement disorders related to neurological dysfunctions. The invention is particularly relevant for treatment of patients suffering from tardive dyskinesia, Parkinson's disease and associated disorders thereof. Kits of parts comprising the 5-HT1 agonist compounds or pharmaceutical compositions according to the present invention, as well as methods of preparation are also provided by the present invention. | 2013-09-26 |
20130252966 | 6-(SULFONYLARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders. | 2013-09-26 |
20130252967 | 8-(SULFONYLBENZYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders. | 2013-09-26 |
20130252968 | ALKYL AMIDES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors. | 2013-09-26 |
20130252969 | Compounds - A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, | 2013-09-26 |
20130252970 | SULFONYL-SUBSTITUTED BICYCLIC COMPOUNDS AS PPAR MODULATORS FOR THE TREATMENT OF NON-ALCOHOLIC STEATOHEPATITIS - Disclosed herein are new methods of treatment of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and other fibrotic diseases of the liver in a subject by modulating PPARδ with sulfonyl-substituted bicyclic compounds and compositions as pharmaceuticals. | 2013-09-26 |
20130252971 | Ophthalmic Formulations of Cetirizine and Methods of Use - The present invention provides stable topical formulations of cetirizine that provide a comfortable formulation when instilled in the eye and is effective in the treatment of allergic conjunctivitis and/or allergic conjunctivitis. The invention further provides methods of treating allergic conjunctivitis and/or allergic rhinoconjunctivitis in a subject in need of such treatment by topical application of the cetirizine formulations of the invention directly to the eye. | 2013-09-26 |
20130252972 | ISOXAZOLE, ISOTHIAZOLE, FURANE AND THIOPHENE COMPOUNDS AS MICROBICIDES - The present invention relates to a compound of formula I: (I) wherein the substituents have the definitions as defined in claim | 2013-09-26 |
20130252973 | Benzofuranyl Derivatives - The present invention provides compounds of Formula (I) | 2013-09-26 |
20130252974 | 5,6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists. | 2013-09-26 |
20130252975 | NOVEL ROCK INHIBITORS - The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. | 2013-09-26 |
20130252976 | POLYMORPHIC FORMS OF (S)-2-(1-(9H-PURIN-6-YLAMINO)PROPYL)-5-FLUORO-3-PHENYLQUINAZOLIN-4(3H)-ON- E - Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. | 2013-09-26 |
20130252977 | Raf Inhibitor Compounds - The present invention provides a pyrido[2,3-d]pyrimidine compound, or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in treating cancer. | 2013-09-26 |
20130252978 | Novel Hydrated Form of Erlotinib Free Base and a Process For Preparation Of Erlotinib Hydrochloride Polymorph Form A Substantially Free of Polymorph Form B - The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D | 2013-09-26 |
20130252979 | PHARMACEUTICAL COMPOSITIONS, DOSAGE FORMS AND NEW FORMS OF THE COMPOUND OF MULA (I), AND METHODS OF USE THEREOF - The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y | 2013-09-26 |
20130252980 | NOVEL GPR 119 AGONISTS - The present invention relates to novel GPR 119 agonists of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. | 2013-09-26 |
20130252981 | PYRIMIDINE COMPOUND AND USE THEREOF FOR PEST CONTROL - A pyrimidine compound of the formula (1): wherein: R | 2013-09-26 |
20130252982 | Biocide Compositions Comprising Alkoxylation Products Of Isoamyl Alcohol Deriatives - Suggested are alkoxylation products of 2-isopropyl-5-methyl-hexan-1-ol in which AO stands for an ethylene oxide, propylene oxide or butylenes oxide unit or their mixtures and n denominates an integer of from 1 to 100. | 2013-09-26 |