Entries |
Document | Title | Date |
20080234233 | MEDICAMENT FOR TREATMENT OF NEURODEGENERATIVE DISEASES - A medicament for preventive and/or therapeutic treatment of neurodegenerative diseases such as Alzheimer's disease or the like which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: | 09-25-2008 |
20080249071 | INFLAMMATORY CYTOKINE RELEASE INHIBITOR - A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: | 10-09-2008 |
20080306029 | Prevention, Treatment, and Amelioration of Radiation Induced Enteritis - The present invention provides a new method of ameliorating and/or treating enteritis induced by radiation therapy, alone or in combination with other therapies, for the treatment of, for example, gastrointestinal malignancies, including colorectal, appendiceal, anal, or small bowel cancers; urogenital malignancies, including prostate, ladder, testicular, or penile cancers; gynecologic malignancies, including cervical, endometrial, ovarian, vaginal, or vulvar cancers; or osteogenic and other sarcomatous malignancies in which pelvic structures are involved, comprising the administration of a therapeutically effective amount of balsalazide to a patient in need thereof. | 12-11-2008 |
20080306030 | Use of a TRPM5 Inhibitor to Regulate Insulin and GLP-1 Release - The present invention is directed to methods of enhancing insulin release, GLP-1 release, and insulin sensitivity, methods of increasing insulin gene expression, methods of decreasing gastric secretion and emptying and glucagons secretion, and methods of inhibiting food intake, and methods of treating diabetes mellitus, insulin resistance syndrome, hyperglycemia, and obesity comprising administering to a subject an effective amount of a TRPM5 inhibitor. | 12-11-2008 |
20080306031 | Methods of Inhibiting Poxvirus Growth - This disclosure ascribes new functions to derivatives of tetralin, anthraquinone, naphthylamine, tri-amino-pyrimidine, xanthen-3-one, and/or cinnamic acid (including, for example, NSC270718R, NSC117285R, NSC170008Y, NSC306711P, NSC119913X, NSC119915Z, NSC119911V, NSC119910U, NSC128437O, NSC125908P, NSC9600Q, or NSC13778J, each obtained from the Structure Diversity Set, National Institutes of Health, National Cancer Institute, Developmental Therapeutics Program). These compounds are shown to be effective inhibitors of viral essential protein kinases (such as poxvirus B1 and/or F10 protein kinases). Exemplary chemical structures for viral protein kinase (VPK) inhibitors are provided, as are methods of using such compounds, for instance, to inhibit VPK activity and/or poxvirus growth, and/or for the treatment of poxvirus infection. Also provided are pharmaceutical compositions including disclosed VPK inhibitors. | 12-11-2008 |
20080312192 | Diaryl Urea Derivatives in the Treatment of Protein Kinase Dependent Diseases - The invention relates to the use of diaryl urea derivatives for the manufacture of pharmaceutical compositions for the treatment of RET dependent disorders, especially RET dependent tumour diseases. The invention further relates to novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives and their use in the treatment of the animal or human body, especially in the treatment of a protein kinase dependent disease, to pharmaceutical compositions comprising such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives and to the use of such novel N-[4-(pyrimidin-4-yloxy)-phenyl]-N′-phenyl-urea derivatives for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as tumour diseases. | 12-18-2008 |
20090082314 | Targeting Prodrugs for the Treatment of Gastrointestinal Diseases - Provided herein are compounds, compositions and methods for decreasing NFκB DNA-binding activity in a patient comprising administering of a therapeutically effective amount of a compound or composition of the application to the patient to reduce, alleviate or treat various gastrointestinal diseases, such as inflammatory bowel disease (IBD). | 03-26-2009 |
20090176746 | THROMBOPOIETIN MIMETICS - Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative. | 07-09-2009 |
20090186860 | Microbicidal Compositions and their Use - A composition comprising a copper salt of N′-hydroxy-N-cyclohexyldiazenium oxide (CuHDO) and a diluent is useful for combating and/or killing bacteria, mould, yeast and algae in industrial materials and or industrial processes. In a preferred embodiment CuHDO is generated in-situ within the application or medium. The composition may additionally include at least one of certain other biocidal active components. | 07-23-2009 |
20090192122 | INFLAMMATORY CYTOKINE RELEASE INHIBITOR -
A medicament having inhibitory activity against NF-κB activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient:
| 07-30-2009 |
20090203654 | COSMETIC AND PHARMACEUTICAL COMPOSITIONS - This invention relates to novel compounds that display retinoid like activities, including HB-EGF (Heparin Binding Epidermal Growth Factor) release from keratinocytes, cell proliferation, and epidermal thickening without the irritation potentials, such as release of interleukin 8 and inhibition of terminal differentiation of keratinocytes. | 08-13-2009 |
20100048517 | ANDROGEN MODULATORS - The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth. | 02-25-2010 |
20100075928 | CANCER TREATMENT METHOD - Invented is a method of treating cancer and pre-cancerous syndromes in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal. | 03-25-2010 |
20100087401 | FORMULATIONS AND USES OF 2-HYDROXY-5-PHENYLAZOBENZOIC ACID DERIVATIVES - A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food. | 04-08-2010 |
20100120725 | Substituted Phenylsulfonamide Inhibitors of Beta Amyloid Production - Compounds of Formula I, | 05-13-2010 |
20100130450 | Methods of Treating Fungal Infections - Methods of identifying compounds that potentiate the activity of antifungal agents, potentiators identified by these methods, and methods of using potentiators are disclosed. | 05-27-2010 |
20100160262 | COMPOSITIONS AND METHODS FOR MODULATING SIRTUIN ACTIVITY - The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide. The present invention further provides active agents that modulate sirtuin activity or expression; and compositions, including pharmaceutical compositions, comprising the active agents. | 06-24-2010 |
20100190754 | AZOLYLMETHYLIDENEHYDRAZINE DERIVATIVE AND USE THEREOF - An azolylmethylidenehydrazine derivative represented by the formula (I) | 07-29-2010 |
20100204185 | PHENAZOPYRIDINE COMPOUNDS - The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine. | 08-12-2010 |
20100234327 | Novel Triazene Compounds For The Treatment Of Cancer - The present invention relates to novel triazene compounds, to a process for their preparation, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans. The novel triazene compounds are distinguished, as compared with the known triazene compounds, by improved activity while at the same time having reduced toxicity, that is to say by fewer side-effects. | 09-16-2010 |
20100240618 | SUBSTITUTED PIPERAZINES - Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists. | 09-23-2010 |
20100311699 | NOVEL CARBOXYLIC ACID 4-PHENYLAZO-PHENYL ESTER DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel carboxylic acid 4-phenylazo-phenyl ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 12-09-2010 |
20100317628 | MicroRNA Modulators and Method for Identifying and Using the Same - The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease. | 12-16-2010 |
20110009370 | METHOD TO ENHANCE TISSUE REGENERATION - The present invention provides for compositions and methods for modulating tissue growth using tissue growth modulators, which are agents that either enhance or inhibit tissue growth as desired by a particular indication by modulating the PG or Wnt signaling pathways, or employing modulators of both PG and Wnt signaling pathways for a synergistic effect or highly selective effect. | 01-13-2011 |
20110046092 | SMALL MOLECULES FOR NEURONAL DIFFERENTIATION OF EMBRYONIC STEM CELLS - A method of preparing neural precursor cells by exposing pluripotent stem cells or neural stem cells to a differentiation agent. The agent is a pyridine analog, which in preferred embodiments is a phenylethynyl-substituted or phenylazo-substituted pyridine. In other embodiments, a method of enhancing neural precursor cell survival is provided in which the survival is enhanced by exposure to the pyridine analog. In further embodiments, a method of preparing neuronal cells is provided in which pluripotent or neural stem cells exposed to the pyridine analog are then incubated without the pyridine analog, resulting in differentiation into neurons, astrocytes and oligodendrocytes. These methods may be used in toxicological screens, e.g., to evaluate the neurotoxicity of a test compound. | 02-24-2011 |
20110059924 | Chemoprevention of Colorectal Cancer by Mesalamine/Sulfasalazine - A method for preventing or treating colorectal cancer in a patient possessing human tropomyocin isoform TC22 is presented. Also presented is a method for evaluating TC22 expression reduction activity of a compound. | 03-10-2011 |
20110065675 | AZO DYE RELATED SMALL MOLECULE MODULATORS OF PROTEIN-PROTEIN INTERACTIONS - Azo dyes and suramin-related small molecules are effective in inhibiting the CD40/CD154 protein-protein interaction, an important co-stimulatory interaction involved in the activation of immune responses mediated by T- and B-cells. The compounds were found to be active as indicated by their IC | 03-17-2011 |
20110118214 | LIGANDS SPECIFIC FOR CANNABINOID RECEPTOR SUBTYPE 2 - A compound of Formula I: (I) has activity as a cannabinoid receptor antagonist. In Formula 1, R1 is unsubstituted or substituted aryl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted heteroaryl; R2 is unsubstituted or substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl; and R3 is unsubstituted or substituted alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted heteroaralkyl; with the proviso that at least one of Ri and R3 is other than unsubstituted aralkyl or R2 is other than unsubstituted aryl. | 05-19-2011 |
20110130368 | DERIVATIVES OF 4- OR 5-AMINOSALICYLIC ACID - The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention/treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention/treatment of colon cancer. | 06-02-2011 |
20110144065 | SELECTIVE HIGH-AFFINITY POLYDENTATE LIGANDS AND METHODS OF MAKING SUCH - This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity. | 06-16-2011 |
20110178045 | Method to induce fatty liver in animal - The present invention discloses a method to induce fatty liver in an animal. The steps of the method comprise: feeding an animal with a high calorie diet, and injecting a mitochondrial inhibitor into the animal to inhibit the mitochondrial activity of the animal, then resulting in fat accumulation and inflammation in the liver of the animal. | 07-21-2011 |
20110190239 | BMI-1 PROTEIN EXPRESSION MODULATORS - The compounds, pharmaceutical compositions, and methods of using such compounds or compositions thereof described herein are useful for treating a disease modulated by B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein expression. | 08-04-2011 |
20110190240 | NUCLEAR FACTOR KAPPA B PATHWAY INHIBITOR COMPOSITION AND USE OF SAME - An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I)a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NFκB pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds. | 08-04-2011 |
20110201576 | Small molecule inhibitors of stat3 with anti-tumor activity - The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents. | 08-18-2011 |
20110201577 | PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF OSELTAMIVIR AND ANALOGS THEREOF - The present application relates to processes for the preparation of oseltamivir and the H | 08-18-2011 |
20110230451 | IDENTIFICATION AND USE OF COMPOUNDS THAT AFFECT THE FIDELITY OF EUKARYOTIC TRANSLATION INITIATION CODON SELECTION - A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed. | 09-22-2011 |
20110263540 | SMALL-MOLECULE INHIBITORS OF PROTEIN SYNTHESIS INACTIVATING TOXINS - Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin. | 10-27-2011 |
20110281826 | STILBENE DERIVATIVES FOR ADP-RIBOSYL CYCLASE INHIBITORS - The present disclosure relates to bisphenyl compounds that are useful for inhibiting the ADP-ribosyl cyclase (ADPR-cyclase). More particularly, the disclosed compounds can be used for treatment and prevention of hypertension, hypertensive cardiac hypertrophy, diabetes, and diabetic nephropathy, in which pathogenesis ADPR-cyclase is involved. The compounds and compositions of the invention can be used for treatment and prevention of cardiovascular disease and related disease states, particularly, hypertension or diabetes related disorders, such as, hypertensive cardiac hypertrophy, diabetic nephropathy, and the like. | 11-17-2011 |
20110312918 | METHOD FOR IDENTIFYING AGENTS FOR INHIBITING CELL MOTILITY AND INVASIVENESS - The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein. | 12-22-2011 |
20110312919 | INHIBITORS OF TYROSINE KINASE RECEPTOR DIMERIZATION - The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner. | 12-22-2011 |
20110312920 | CAVITY INDUCED ALLOSTERIC MODIFICATION OF INTERMOLECULAR INTERACTIONS AND METHODS OF IDENTIFYING COMPOUNDS THAT EFFECT THE SAME - Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed. | 12-22-2011 |
20110319367 | Phenazopyridine Compounds - The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine. | 12-29-2011 |
20120010176 | UTROPHIN PROMOTER ACTIVITY UPREGULATION FOR THE TREATMENT OF MUSCULAR DYSTROPHY - Methods are provided for increasing utrophin promoter activity, utrophin expression or utrophin activity, and treating or reducing the symptoms of muscular dystrophy by administering to a subject in need thereof an effective amount of a composition comprising a utrophin promoter or activity upregulator. Muscular dystrophy includes but is not limited to Duchenne muscular dystrophy, Becker's muscular dystrophy, limb girdle muscular dystrophy, or a disease characterized by mutation or dysregulation of the dystrophin gene or an aberrant or dysfunctional dystrophin. | 01-12-2012 |
20120010177 | MicroRNA Modulators and Method for Identifying And Using The Same - The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease. | 01-12-2012 |
20120015911 | METHOD AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES - Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease. | 01-19-2012 |
20120083473 | TREATMENT OF CONDITIONS BY TOLL-LIKE RECEPTOR MODULATORS - Provided herein are methods for treating certain conditions, including fibrosis, inflammatory, and autoimmune conditions, with conjugated compounds having Toll-like receptor modulatory activity. | 04-05-2012 |
20120094963 | TARGETING PRODRUGS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISEASES - Provided herein are compounds of formula (I) as well as compounds of formula (I) which are prodrugs in which the (R7)a-phenyl-S(O)2NH group represents a sulphonamide-bond compound, compositions and methods for preventing or treating gastrointestinal diseases such as inflammatory bowel disease and colorectal cancer, wherein the method comprises delivering an effective amount of a COX-2 or a similar sulphonamide inhibitor as a prodrug or a derivative thereof to the colon, wherein the COX-2 or similar inhibitor is released in vivo. | 04-19-2012 |
20120115817 | PHTHALIMIDE DERIVATIVES OF NON-STEROIDAL ANTI-INFLAMMATORY COMPOUNDS AND/OR TNF-ALPHA MODULATORS, METHOD FOR PRODUCING SAME, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND USES THEREOF FOR THE TREATMENT OF INFLAMMATORY DISEASES - The present invention relates to phthalimide derivatives of non-steroidal and/or TNF-α modulating anti-inflammatory compounds as well as the process of obtaining the so-called derivatives, pharmaceutical compositions containing such derivatives and their uses, including use in the treatment of inflammatory diseases, especially those related to chronic inflammatory processes, such as rheumatoid arthritis and intestinal inflammatory diseases (for instance, Chron's disease) and the use of the referred to pharmaceutical compositions as antipyretic, analgesic and platelet antiaggregating medications. | 05-10-2012 |
20120172339 | ANGIOGENIC RESORCINOL DERIVATIVES - Novel resorcinol derivatives and methods of preparation and use are presented. These compounds can stimulate angiogenesis as a biological function triggered by the activation of one cannabinoid receptor distinct from CB1 and CB2. Thus, these compounds are specific ligands for one cannabinoid receptor distinct from CB1 and CB2. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions. | 07-05-2012 |
20120178723 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula IA-a or IB-a and subsets thereof: | 07-12-2012 |
20120190651 | ANTI-INFLAMMATORY COMPOUNDS - This invention relates to novel compounds obtained by fermentation of Myxobacteria strain (PM0670013/MTCC 5570). The present invention further relates to the processes for the production of the novel anti-inflammatory compounds, to the culture no. PM0670013 (MTCC 5570), and to pharmaceutical compositions containing compounds of the present invention as an active ingredient and its use in medicines for the treatment of inflammatory diseases or disorders mediated by proinflammatory cytokines such as Tumor Necrosis Factor-alpha (TNF-α) and/or interleukins such as IL-6, having anti-inflammatory activity The invention also includes all stereoisomeric forms of compounds of the present invention. | 07-26-2012 |
20120232039 | PRIMARY AMINE DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES - A compound having the structure | 09-13-2012 |
20130005693 | Method for Reducing Levels of Disease Associated Proteins - The subject invention concerns the reduction of protein aggregation in the neurons of a mammal through the use of a ketogenic treatment such as a ketogenic diet, a physical training regimen and/or administration of agents to increase fatty acid oxidation. Such ketogenic treatment can be useful in the reduction of certain aggregates including amyloid β peptide, polyglutamine containing huntintin protein, polyglutamine containing androgen receptor, polyglutamine containing atrophin-1, polyglutamine containing ataxins, α-synclein, prion protein, tau and superoxide dismutase 1 (SOD1). | 01-03-2013 |
20130023497 | Triazine Derivatives and their Therapeutical Applications - The present invention comprises inter alia triazine compounds as shown in formula (I) and pharmaceutically acceptable salts thereof. | 01-24-2013 |
20130023498 | MicroRNA Modulators and Method for Identifying and Using the Same - The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease. | 01-24-2013 |
20130029941 | 7,11-METHANOCYCLOOCTA [B] QUINOLINE DERIVATIVE AS HIGHLY FUNCTIONALIZABLE ACETYLCHOLINESTERASE INHIBITORS - New highly functionalizable Huprine derivatives of formula I: | 01-31-2013 |
20130029942 | COMPOUNDS AND THERAPEUTICAL USES THEREOF - Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. | 01-31-2013 |
20130040917 | Phenazopyridine Compounds - The present invention is directed to substituted phenazopyridines represented by Formula I. The present invention also relates to the discovery that compounds of Formula I have increased bioavailability as compared to unconjugated phenazopyridine. | 02-14-2013 |
20130053352 | DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES - A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R | 02-28-2013 |
20130059823 | Diazeniumdiolate Cyclohexyl Derivatives - A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R | 03-07-2013 |
20130065862 | FORMULATIONS AND USES OF 2-HYDROXY-5-PHENYLAZOBENZOIC ACID DERIVATIVES - A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food. | 03-14-2013 |
20130065863 | NITROXYL (HNO) RELEASING COMPOUNDS AND USES THEREOF IN TREATING DISEASES - Disclosed is a compound of the formula (I) or a pharmaceutically acceptable salt thereof: (I) in which R | 03-14-2013 |
20130065864 | NOVEL IRIDIUM/RHODIUM ANTI-CANCER COMPOUNDS - The present invention relates to novel iridium and/or rhodium containing complexes for use as a cytotoxic, such as an anti-cancer agent. There is also provided a method of preparing said compounds. | 03-14-2013 |
20130123216 | CYCLIC NITRO COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF AND USES THEREOF - The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease. | 05-16-2013 |
20130150332 | 9-AMINONOSCAPINE AND ITS USE IN TREATING CANCERS, INCLUDING DRUG-RESISTANT CANCERS - 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs. | 06-13-2013 |
20130184241 | Naphthalene Derivative - The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) | 07-18-2013 |
20130203709 | ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME - The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide. | 08-08-2013 |
20130210772 | ANDROGEN INDUCED OXIDATIVE STRESS INHIBITORS - Described herein are pharmaceutical compositions and medicaments, and methods of using such pharmaceutical compositions and medicaments in the treatment of cancer. | 08-15-2013 |
20130210773 | INDOLE COMPOUNDS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC RECEPTOR - In one aspect, the invention relates to indole compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M | 08-15-2013 |
20130210774 | POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS - The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection. | 08-15-2013 |
20130231308 | USE OF AMINOSALICYLATES IN DIARRHOEA-PREDOMINENT IRRITABLE BOWEL SYNDROME - A method for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant irritable bowel syndrome or other non-specific bowel disorder is disclosed comprising administering to a patient in need of such treatment or prophylaxis an effective amount of balsalazide, or a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or a derivative thereof, or a composition comprising balsalazide the modified compound, or a salt or a derivative thereof together with a suitable carrier. Use of balsalazide, a 4-ASA or 5-ASA compound modified to include a 4-ABA side chain, or a salt or derivative thereof, for the manufacture of a medicament for the treatment or prophylaxis of non-inflammatory bowel diseases, diarrhoea-predominant Irritable Bowel Syndrome or other non-specific bowel disorder is also disclosed. | 09-05-2013 |
20130244985 | Drug Depots Having Different Release Profiles for Reducing, Preventing or Treating Pain and Inflammation - Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least analgesic and/or at least one anti-inflammatory agent at or near a target site, one can reduce, prevent or treat inflammation and pain. | 09-19-2013 |
20130289003 | DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES - A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy. | 10-31-2013 |
20130316985 | GPR35 Ligands And Uses Thereof - A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein. | 11-28-2013 |
20140066410 | INHIBITORS OF BROMODOMAINS AS MODULATORS OF GENE EXPRESSION - This disclosure relates generally to compounds and compositions comprising one or more diphenylethylene, diphenylethylyne, and azobenzene analogs. These compounds are useful for treating diseases associated with NF-kB and p53 activity, such as cancer and inflammatory disease. | 03-06-2014 |
20140066411 | PHARMACEUTICAL COMPOSITIONS FOR EXTENDED RELEASE OF AZO-BONDED 5-AMINOSALICYLIC ACID COMPOSITIONS - Gastric retentive dosage forms for sustained release of an azo-bonded prodrug of 5-aminosalicylic acid (5-ASA) are described which may allow once- or twice-daily dosing for both acute and long-term treatment of inflammatory bowel disorders. Methods of treatment using the dosage forms and methods of making the dosage forms are also described. | 03-06-2014 |
20140073609 | Compositions and Methods Including Cell Death Inducers and Procaspase Activation - Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3. | 03-13-2014 |
20140073610 | AROMATIC CARBOXYLIC ACID DERIVATIVES FOR TREATMENT AND PROPHYLAXIS OF GASTROINTESTINAL DISEASES INCLUDING COLON CANCERS - Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease. | 03-13-2014 |
20140088048 | DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES - A compound having the structure | 03-27-2014 |
20140121187 | 1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT - Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. | 05-01-2014 |
20140128350 | Substituted Pyridine Derivatives Useful In The Treatment Of Cancer - The present invention describes compounds of formula (I) | 05-08-2014 |
20140135295 | NONOATE DERIVATIVES AND USES THEREOF - A compound of Formula (I): | 05-15-2014 |
20140142069 | SUBSTITUTED 3-PHENYLPROPIONIC ACIDS AND THE USE THEREOF - The present application relates to novel 3-phenylpropionic acid 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, in particular for the treatment and/or prevention of cardiovascular disorders. | 05-22-2014 |
20140148416 | Agent for Treatment of Eye Diseases - The present invention provides agents effective to treat eye diseases, pharmaceutical compositions comprising them, methods for preparing pharmaceuticals for treatment of eye diseases comprising using the agents, use of the agents in manufacture of pharmaceuticals for treatment of eye diseases and methods for treating eye diseases comprising administering the agents or the pharmaceutical compositions. The eye diseases treated by the present invention include particularly glaucoma, especially normal tension glaucoma, or retinitis pigmentosa. The present invention provides the compound of formula (I) | 05-29-2014 |
20140171395 | Tunable Nitric Oxide-Releasing Macromolecules Having Multiple Nitric Oxide Donor Structures - Provided here are nitric oxide-releasing compounds that include at least two different NO donor functional groups of the same class. In some embodiments, such nitric oxide-releasing compounds are macromolecules such as dendrimer and co-condensed silica. Pharmaceutical compositions, wound dressings, kits and methods of treatments are also provided herein. | 06-19-2014 |
20140221319 | Small Molecule CD38 Inhibitors and Methods of Using Same - The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity. | 08-07-2014 |
20140309196 | PIPERAZINE DERIVATIVES - Disclosed are piperazine derivatives having the general formula: (I) Also disclosed are methods of treating a subject having cancer with this compound or a pharmaceutical composition comprising the compound. | 10-16-2014 |
20140315865 | HYBRID DIAZENIUMDIOLATED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHOD OF TREATING CANCER - Disclosed are hybrid compounds that release both nitric oxide and a moiety that inhibits poly (ADP-ribose) polymerase (PARP), e.g., a compound or a pharmaceutically acceptable salt thereof of formula (I), wherein R | 10-23-2014 |
20150025044 | IDENTIFICATION AND USE OF COMPOUNDS THAT AFFECT THE FIDELITY OF EUKARYOTIC TRANSLATION INITIATION CODON SELECTION - A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed. | 01-22-2015 |
20150065468 | BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF - Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases. | 03-05-2015 |
20150080349 | MODULATION OF BACTERIAL QUORUM SENSING WITH SYNTHETIC LIGANDS - The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups. | 03-19-2015 |
20150290224 | ACTIVATED NITRIC OXIDE DONORS AND METHODS OF MAKING AND USING THEREOF - Described herein are compositions useful in anticancer treatment and prevention. The compositions are composed of (a) an O | 10-15-2015 |
20150315126 | CYCLOPROPYLAMINE DERIVATIVES USEFUL AS INHIBITORS OF HISTONE DEMETHYLASES KDM1A - The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R | 11-05-2015 |
20160000767 | ANTIBACTERIAL COMPOUNDS - Provided are iminosugars having antibacterial properties and methods of treating and/or preventing bacterial infections with such iminosugars. The present disclosure relates to antibacterial compounds and, in particular, to iminosugars having antibacterial activity. One embodiment is a method of treating or preventing a bacterial infection comprising administering to a subject in need thereof an antibacterial effective amount of a compound of the following formula: or a pharmaceutically acceptable salt thereof. | 01-07-2016 |
20160000810 | Method For Treating Eye Diseases - The present invention provides a pharmaceutical composition for removing drusen, suppressing formation of drusen, and/or treating and/or preventing age-related macular degeneration comprising the compound of formula (I) wherein Ra is independently selected from the group consisting of halo, hydroxy, alkyl, halo-substituted alkyl, aryl, halo- or alkyl-substituted aryl, alkoxy, hydroxy- or carboxy-substituted alkoxy, aryloxy, halo- or alkyl-substituted aryloxy, CHO, C(O)-alkyl, C(O)-aryl, C(O)-alkyl-carboxyl, C(O)-alkylene-carboxy ester and cyano, and m is an integer selected from 0 to 4. | 01-07-2016 |
20160008380 | TARGETING GLUTAMINE METABOLISM IN BRAIN TUMORS | 01-14-2016 |
20160022708 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF GLUTAMINE-ADDICTED CANCERS - Provided herein are methods for a novel combination therapy for treating a glutamine-addicted cancer in a subject in need thereof, which comprises the administration of a glutaminase antagonist and a pro-apoptotic compound. Specific glutaminase antagonists and pro-apoptotic compounds are provided. In some embodiments, the glutaminase antagonist is 6-diazo-5-oxo-1-norleucine (DON) and the pro-apoptotic compound is a Bcl-2 family member antagonist. In some embodiments, the pro-apoptotic compound is obatoclax mesylate, navitoclax, or fenretinide. In some embodiments, the glutamine-addicted cancer is a cancer in which Myc is deregulated. In some embodiments, the cancer is a pediatric cancer. | 01-28-2016 |
20160022817 | Photoswitchable HDAC Inhibitors - This invention relates to photoswitchable inhibitors of histone deacetylases and methods of using the same. Provided herein are inhibitors of HDAC having photoswitchable modulators of protein function with short thermal relaxation kinetics. The compounds are diazo compounds including a substituted or unsubstituted aryl or heteroaryl ring, wherein at least one of the rings is substituted with one or more HDAC targeting elements. | 01-28-2016 |
20160024527 | Compositions and Methods for Enhancing Bioenergetic Status in Female Germ Cells - Compositions and methods comprising bioenergetic agents for restoring the quality of aged oocytes, enhancing oogonial stem cells or improving derivatives thereof (e.g., cytoplasm or isolated mitochondria) for use in fertility-enhancing procedures, are described. | 01-28-2016 |
20160052896 | ISOXAZOLE ANALOGS AS MEDIATORS OF TRANSCRIPTIONAL INDUCTION OF E-CADHERIN - In one aspect, the invention relates to N-((arylamino)alkyl)-5-arylisoxazole-3-carboxamide analogs, derivatives thereof, and related compounds, which are useful as mediators of transcriptional induction of E-cadherin; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with E-cadherin activity 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. | 02-25-2016 |
20160083339 | TUNABLE NITRIC OXIDE-RELEASING MACROMOLECULES HAVING MULTIPLE NITRIC OXIDE DONOR STRUCTURES - Provided here are nitric oxide-releasing compounds that include at least two different NO donor functional groups of the same class. In some embodiments, such nitric oxide-releasing compounds are macromolecules such as dendrimer and co-condensed silica. Pharmaceutical compositions, wound dressings, kits and methods of treatments are also provided herein. | 03-24-2016 |
20160120838 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE - The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria. | 05-05-2016 |
20160120839 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASE - The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing inflammatory bowel disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal diseases and inflammation such as inflammatory bowel disease, ulcerative colitis, mild-to-moderate Crohn's disease, rheumatoid arthritis, inflammatory arthritis, psoriatic arthritis, liver cirrhosis and idiopathic urticaria. | 05-05-2016 |
20160120886 | PREVENTION, TREATMENT, AND AMELIORATION OF RADIATION INDUCED ENTERITIS - The present invention provides a new method of ameliorating and/or treating enteritis induced by radiation therapy, alone or in combination with other therapies, for the treatment oil for example, gastrointestinal malignancies, including colorectal, appendiceal, anal, or small bowel cancers; urogenital malignancies, including prostate, bladder, testicular, or penile cancers; gynecologic malignancies, including cervical, endometrial, ovarian, vaginal, or vulvar cancers; or osteogenic and other sarcomatous malignancies in which pelvic structures are involved, comprising the administration of a therapeutically effective amount of balsalazide to a patient in need thereof | 05-05-2016 |
20160168139 | NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF | 06-16-2016 |
20160193234 | EYE DROP COMPOSITION FOR TREATING OCULAR INFLAMMATORY DISEASE AND PREPARATION METHOD THEREFOR | 07-07-2016 |
20160199393 | METHODS OF TREATING BRAIN ISCHEMIA OR HYPOXIA | 07-14-2016 |
20160200695 | Methods and Compositions for Selective and Targeted Cancer Therapy | 07-14-2016 |