Entries |
Document | Title | Date |
20080200460 | Chemical Compounds - Compounds of formula (I): | 08-21-2008 |
20080221100 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are urea compounds, stereoisomer, or pharmaceutical acceptable salt thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases. | 09-11-2008 |
20080221101 | Calcium receptor modulating agents - The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes. | 09-11-2008 |
20080221102 | Composition and methods for modulating a kinase cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. | 09-11-2008 |
20080227780 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are urea compounds, stereoisomer, or pharmaceutical acceptable salt thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases. | 09-18-2008 |
20080227781 | IMIDAZOLE COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - The present invention relates to compounds of the Formula I | 09-18-2008 |
20080234270 | Pyrrole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 09-25-2008 |
20080234271 | Arylphenylamino- and Arylphenylether-Sulfide Derivatives, Useful For the Treatment of Inflammatory and Immune Diseases, and Pharmaceutical Compositions Containing Them - The present invention relates in part to compounds of formulas (I) and (III): and pharmaceutically-acceptable salts and prodrugs thereof. These compounds can be useful for treating diseases such as inflammatory and immune diseases. The present invention also relates to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a subject. | 09-25-2008 |
20080261976 | NOVEL PIPERIDINECARBOXAMIDE DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME - The invention relates to compounds of formula (I): | 10-23-2008 |
20080269214 | Pyrrole Derivatives as Dna Gyrase and Topoisomerase Inhibitors - Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 10-30-2008 |
20080269215 | Bisamide Inhibitors of Hedgehog Signaling - The invention provides inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: | 10-30-2008 |
20080275043 | Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1 - The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia. | 11-06-2008 |
20080275044 | Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them and use thereof for treating pain and other conditions - Compounds corresponding to formula I: | 11-06-2008 |
20080280901 | Pharmaceutical Composition for Preventing and Treating Metabolic Bone Diseases Containing Alpha-Arylmethoxyacrylate Derivatives - The present invention relates to a use of a specific alpha-arylmethoxyacrylate derivative, or its pharmacologically acceptable salt or solvate for preventing and treating metabolic bone diseases. | 11-13-2008 |
20080280902 | Inhibitors of Checkpoint Kinases - The instant invention provides for compounds which comprise substituted quinolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 11-13-2008 |
20080280903 | Apoptosis Inhibitors - The present invention provides compounds that act as selective agents to protect against unintentional cell death or tissue damage and can relieve side effects of cancer treatment such as, for example, oral mucositis, hair loss, diarrhea due to damage to the gastrointestinal epithelium, and myelosuppression. In addition, these compounds can be used to prevent premature cell death when the cell death is caused by signals from damaged cells, for example, signals generated as the result of a traumatic incident or an ischemic episode. | 11-13-2008 |
20080280904 | N-Substituted Pyridinone or Pyrimidinone Compounds Useful as Soluble Epoxide Hydrolase Inhibitors - Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same. | 11-13-2008 |
20080280905 | UREA ANTAGONISTS OF P2Y1 RECEPTOR USEFUL IN THE TREATMENT OF THROMBOTIC CONDITIONS - The present invention provides novel pyridyl or phenyl ureas and analogues thereof, which are selective inhibitors of the human P2Y | 11-13-2008 |
20080287436 | Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. | 11-20-2008 |
20080293716 | Chemical Compounds - There is provided a compound of Formula (I) or a salt, solvate, or physiologically functional derivative thereof: | 11-27-2008 |
20080293717 | ARYL SULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 11-27-2008 |
20080306065 | Metalloproteinase Inhibitors - Compounds of the formula (I) wherein z is SO | 12-11-2008 |
20080318953 | Substituted Pyridine Derivatives - The present invention relates to pyridine derivatives of the general formula (I) and their use as openers of the KCNQ family potassium ion channels for the treatment of CNS disorders. | 12-25-2008 |
20090023730 | SUBSTITUTED ARYL ACYLTHIOUREAS AND RELATED COMPOUNDS; INHIBITORS OF VIRAL REPLICATION - The invention provides compounds and pharmaceutically acceptable salts of Formula I | 01-22-2009 |
20090023731 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases. | 01-22-2009 |
20090023732 | Citrate Salt of an Indole Derivative and its Pharmaceutical Use - The salt, the 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a process for its preparation, pharmaceutical formulations containing it and the use of it in therapy, and particularly in the therapy of GSK3 related conditions and disorders. | 01-22-2009 |
20090023733 | Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them - The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state. | 01-22-2009 |
20090036447 | Compounds, Compositions and Methods - Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 02-05-2009 |
20090042883 | ANTITUMOR AGENT - The present invention provides a therapeutic agent for a tumor selected from a hematopoietic tumor and a solid tumor which comprises, as an active ingredient, a benzoyl compound represented by General Formula (I): | 02-12-2009 |
20090048255 | PHOSPHODIESTERASE 4 INHIBITORS, INCLUDING N-SUBSTITUTED ANILINE AND DIPHENYLAMINE ANALOGS - PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: | 02-19-2009 |
20090054435 | Phenoxyalkanoic Acid Compound - The present invention provides a compound represented by the formula: | 02-26-2009 |
20090054436 | MONOCYCLIC HETEROCYCLES AS KINASE INHIBITORS - The present invention is directed to compounds having the formula | 02-26-2009 |
20090069322 | N-FORMYL HYDROXYLAMINE DERIVATIVES AS INHIBITORS OF BACTERIAL POLYPEPTIDE FORMYLASE FOR TREATING MICROBIAL INFECTIONS - Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(═O) or formula C(═O)NH(OH); R | 03-12-2009 |
20090069323 | 11beta-hsdi inhibitors - The invention relates to compounds of formula (I) | 03-12-2009 |
20090069324 | CHEMICAL INHIBITORS OF BFL-1 AND RELATED METHODS - Compounds that bind to Bfl-1 as well as conjugates of such compounds are provided. Various embodiments additionally provide methods of using such compounds to identify additional anti-apoptotic Bfl-1 binding compounds. Methods of using such compounds to increase apoptosis in a cell are also provided. | 03-12-2009 |
20090069325 | Piperidine Derivatives Useful as Modulators of Chemokine Receptor Activity - The present invention relates to the compounds of formula (I): | 03-12-2009 |
20090069326 | SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity. | 03-12-2009 |
20090082350 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are heterocylic or heteroaryl compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases. | 03-26-2009 |
20090088430 | PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: | 04-02-2009 |
20090093479 | ANTI-CANCER AGENTS AND USES THEREOF - The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: | 04-09-2009 |
20090099181 | SULFOXIMINES AS KINASE INHIBITORS - The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | 04-16-2009 |
20090099182 | INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: | 04-16-2009 |
20090105249 | 4-phenylsulfonamidopiperidines as calcium channel blockers -
The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R | 04-23-2009 |
20090111808 | NOVEL HISTAMINE H3-RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS - The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease. | 04-30-2009 |
20090111809 | INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity. | 04-30-2009 |
20090118283 | Amide Derivatives as Kinase Inhibitors - The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar | 05-07-2009 |
20090124618 | 2-MORPHOLINO-4-PYRIMIDONE COMPOUND - A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C | 05-14-2009 |
20090124619 | NOVEL COMPOUNDS - This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted morpholines and piperidines, according to Formula I | 05-14-2009 |
20090131433 | HISTAMINE-3 RECEPTOR ANTAGONISTS - This invention is directed to a compound of the formula Ia or Ib, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above. | 05-21-2009 |
20090131434 | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action. | 05-21-2009 |
20090131435 | HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE - Disclosed are compounds of the Formula | 05-21-2009 |
20090137587 | Phenylpyridone Derivative - A compound represented by the formula (I) is contained as an active ingredient: | 05-28-2009 |
20090143383 | ARYLOXYETHYLAMINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR - The present invention relates to aryloxyethylamine compounds of the formula I | 06-04-2009 |
20090149461 | METHOD OF TREATING CANCER - Methods of treating cancer using N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide are disclosed. | 06-11-2009 |
20090163496 | ANTIBACTERIAL AGENTS - Antibacterial compounds of formula I are provided: | 06-25-2009 |
20090163497 | Compounds Useful as Antagonists of CCR2 -
The present invention provides compounds of general formula (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R | 06-25-2009 |
20090163498 | Aryl Sulfonamides - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 06-25-2009 |
20090170850 | Cycloalkyl derivatives of 3-hydroxy-4-pyridinones - The present invention provides an cycloalkyl derivative of 3-hydroxy-4-pyridinone which is useful for the chelation of metal ions such as iron. Its preparation and use is described. In particular, the invention concerns the removal of iron in chemical and biological systems including chelating agents having the formula I | 07-02-2009 |
20090176781 | Acetylenic Heteroaryl Compounds - This invention relates to compounds of the general formula: | 07-09-2009 |
20090176782 | INHIBITORS OF TACE - The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases. | 07-09-2009 |
20090176783 | INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids. | 07-09-2009 |
20090186894 | N-Substituted-Heterocycloalkyloxybenzamide Compounds and Methods of Use - The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure | 07-23-2009 |
20090192158 | Methods for Treating or Preventing Neoplasias - The present invention is directed to a method for treating or preventing a neoplasia in a human patient in need of such treatment comprising administering to the patient a compound that inhibits microsomal prostaglandin E synthase-1 in an amount that is effective for treating or preventing the neoplasia. | 07-30-2009 |
20090192159 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - Disclosed herein is a compound represented by the formula: | 07-30-2009 |
20090197884 | Compounds Useful as Antagonists of CCR2 - The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions. | 08-06-2009 |
20090203694 | INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE - The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions comprising these compounds and methods of using these compounds for treating bacterial disease, such as bacterial infection. | 08-13-2009 |
20090209538 | THERAPEUTIC SUBSTITUTED LACTAMS - Herein are described compounds having a structure | 08-20-2009 |
20090215775 | Sulphonamido-Substituted Cyclohexyl Sulphones for Treatment of Cancer - Compounds of formula (I) are disclosed for treatment of cancer. | 08-27-2009 |
20090215776 | Organic compounds - Compounds of formula I | 08-27-2009 |
20090221577 | COMPOUNDS HAVING MORPHOLINYL AND PIPERIDINYL GROUPS FOR USE AS GLYT1 INHIBITORS - The invention provides a compound of formula (I) or a salt or solvate thereof: | 09-03-2009 |
20090221578 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 09-03-2009 |
20090247521 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS FOR THE TREATMENT OF ENDOTHELIAL DYSFUNCTION - The present invention generally relates to methods useful for a therapy using a class of urea or amide compounds and related compositions, wherein the compound is a soluble epoxide hydrolase inhibitor, for treating and ameliorating the symptoms of diseases related to endothelial dysfunction. | 10-01-2009 |
20090247522 | Hsp90 FAMILY PROTEIN INHIBITORS - The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): | 10-01-2009 |
20090264428 | Renin Inhibitors - Described are compounds of the formula (I) which are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof. | 10-22-2009 |
20090270392 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - Therapeutic compounds, compositions, medicaments, and methods are disclosed herein. | 10-29-2009 |
20090270393 | Iminopyridine Derivatives and Use Thereof - The present invention aims to provide an iminopyridine derivative compound having an α | 10-29-2009 |
20090270394 | CYCLYLAMINE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type and/or T-type calcium channel activity are disclosed. Specifically, a series of compounds of substituted or unsubstituted cyclylamine derivatives as shown in formulas (1). | 10-29-2009 |
20090275581 | RENIN INHIBITORS - Disclosed are compounds according to Formula I: | 11-05-2009 |
20090286786 | Compounds having a 4-pyridylalkylthio group as a substituent - A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: | 11-19-2009 |
20090286787 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - A compound comprising | 11-19-2009 |
20090286788 | Active agent combinations with insecticidal and acaricidal properties - The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing
| 11-19-2009 |
20090298828 | Alkoxyalkyl-Substituted Cyclic Keto-Enols - The invention relates to new alkoxyalkyl-substituted cyclic ketoenols of the formula (I) | 12-03-2009 |
20090298829 | MELANOCORTIN RECEPTOR AGONISTS - The present invention relates to a compound of the following formula 1, pharmaceutically acceptable salt and isomer thereof effective as agonist of melanocortin receptor, and an agonistic composition of melanocortin receptor comprising the same as active ingredient. | 12-03-2009 |
20090306075 | CHEMICAL COMPOUNDS - Compounds of formula (I): | 12-10-2009 |
20090318447 | N-[6-(4-MORPHOLINYL)-3-PYRIDINYL]-2-(TETRAHYDRO-2H-PYRAN-4-YL)-N-[(1--4-PI- PERIDINYL) METHYL] ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS GLYT1 TRANSPORT INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS SUCH AS SCHIZOPHRENIA - The invention provides a compound of formula (I) or a salt or solvate thereof: | 12-24-2009 |
20090318448 | Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: | 12-24-2009 |
20090318449 | THERAPEUTIC LACTAMS - Compounds comprising | 12-24-2009 |
20090318450 | COMPOSITIONS FOR MODULATING A KINASE CASCADE AND METHODS OF USE THEREOF - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 12-24-2009 |
20090318451 | MORPHOLINE DOPAMINE AGONISTS FOR THE TREATMENT OF PAIN - The present invention relates to use of a compound of formula (I), (Ia), or (Ib): | 12-24-2009 |
20090325956 | Aromatic amine derivative and use thereof - The present invention provides a novel SCD inhibitor. An SCD inhibitor containing a compound represented by the formula [I] | 12-31-2009 |
20100004241 | NON-IMIDAZOLE ARYLOXYALKYLAMINES - Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. | 01-07-2010 |
20100016315 | Iminopyridine Derivative and Use Thereof - Provided are an iminopyridine derivative having a selective α | 01-21-2010 |
20100029647 | 3,4,(5)-SUBSTITUTED TETRAHYDROPHYRIDINES - 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)-substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. | 02-04-2010 |
20100035879 | N-SULFONYLCARBOXIMIDAMIDE APOPTOSIS PROMOTERS - Compounds having the formula | 02-11-2010 |
20100035880 | SUBSTITUTED SULFONYLAMINOARYLMETHYL CYCLOPROPANECARBOXAMIDE AS VR1 RECEPTOR ANTAGONISTS - This invention provides a compound of the formula (I): | 02-11-2010 |
20100041653 | COMPOSITION AND METHODS FOR THE DESIGN AND DEVELOPMENT OF METALLO-ENZYME INHIBITORS - The present disclosure provides compounds having the general structure A or pharmaceutically acceptable salts thereof: | 02-18-2010 |
20100056522 | INTRAOCULAR PRESSURE-LOWERING AGENT COMPRISING COMPOUND HAVING HISTONE DEACETYLASE INHIBITOR EFFECT AS ACTIVE INGREDIENT - An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension. | 03-04-2010 |
20100069386 | Modulators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto - The present invention makes available methods and reagents for inhibiting aberrant growth states resulting form hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. Such methods and reagents may also inhibit the hedgehog pathway in normal cells, e.g., where normal levels of hedgehog signalling are unwanted. | 03-18-2010 |
20100087432 | PYRROLE DERIVATIVES HAVING CRTH2 RECEPTOR ANTAGONIST ACTIVITY - There are provided according to the invention compounds of formula (I) as CRTh2 antagonists. In free or salt form, wherein R | 04-08-2010 |
20100087433 | Methods of inhibiting tryptophan hydroxylase - Compounds, compositions and methods of treating serotonin-mediated diseases and disorders are disclosed. | 04-08-2010 |
20100087434 | NK-1 and Serotonin Transporter Inhibitors - The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both. | 04-08-2010 |
20100087435 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 04-08-2010 |
20100093728 | NOVEL SUBSTITUTED BIPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE RECEPTOR LIGANDS - The present invention relates to novel substituted 2,4′- and 3,4′-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders. | 04-15-2010 |
20100093729 | SUBSTITUTED GAMMA LACTAMS AS THERAPEUTIC AGENTS - A compound comprising or a pharmaceutically acceptable salt, prodrug, or a metabolite thereof is disclosed herein. Y, A, and B are as described herein. Methods, compositions, and medicaments related to these compounds are also disclosed. | 04-15-2010 |
20100093730 | NOVEL COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - The present application relates to calcium channel inhibitors containing compounds of formula (I) | 04-15-2010 |
20100099675 | NOVEL PYRROLE DERIVATIVE HAVING UREIDO GROUP AND AMINOCARBONYL GROUP AS SUBSTITUENTS - Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; R | 04-22-2010 |
20100130495 | COMPOUNDS 563 - The present invention relates to novel compounds of formula I and therapeutically acceptable salts thereof, their pharmaceutical compositions, processes for making them and their use as therapeutic methods for treatment and/or prevention of various diseases. In particular the invention relates to compounds, which inhibit the Aβ40 and Aβ42 production, increase the Aβ37 and Aβ38 production and maintain the Notch signaling and will be used for treatment and/or prevention of Aβ-related pathologies such as Alzheimer's disease, Downs syndrome and β-amyloid angiopathy, such as but not limited to cerebral amyloid angiopathy, hereditary cerebral hemorrhage, disorders associated with cognitive impairment, such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. | 05-27-2010 |
20100160319 | HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES - The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. (Formula I) | 06-24-2010 |
20100160320 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 06-24-2010 |
20100168102 | Amide Derivatives as Kinase Inhibitors - The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar | 07-01-2010 |
20100168103 | DIARYL PIPERIDINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of diaryl piperidine compounds are disclosed of the general formula (I) where X is a linker and Y may be C, O, S or N. | 07-01-2010 |
20100173908 | SUBSTITUTED N-PHENYL-BIPYRROLIDINE UREAS AND THERAPEUTIC USE THEREOF - The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I). | 07-08-2010 |
20100184764 | CYCLOALKYL LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses compounds of Formula I: (I) having 11beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia. | 07-22-2010 |
20100190788 | Amide derivatives as kinase inhitors - The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar | 07-29-2010 |
20100204228 | Aryl Sulfonamides Useful for Modulation of the Progesterone Receptor - In one embodiment, compounds of the following structure are described, wherein R | 08-12-2010 |
20100222350 | PHENYL, PYRIDINE, QUINOLINE, ISOQUINOLINE, NAPHTHYRIDINE AND PYRAZINE DERIVATIVES - This invention is concerned with compounds of the formula | 09-02-2010 |
20100227864 | 5-MEMBERED HETEROCYCLIC 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 5-membered heterocyclic 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, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH | 09-09-2010 |
20100240652 | Pyridine Derivatives as Sodium Channel Modulators - The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain. | 09-23-2010 |
20100240653 | BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like. | 09-23-2010 |
20100240654 | HYDRAZIDE DERIVATIVES - A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. | 09-23-2010 |
20100249129 | COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - Disclosed herein are compounds of formula (I) | 09-30-2010 |
20100261721 | Novel Sulphonylpyrroles - Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors. | 10-14-2010 |
20100267721 | Heterocyclic H3 Antagonists - Compound of formula (I) wherein W, X, Y, Z is —C(R′)═ or N; R | 10-21-2010 |
20100267722 | NOVEL PROLINE DERIVATIVES - The invention relates to a compound of formula (I) | 10-21-2010 |
20100286145 | ISOPHTHALAMIDE DERIVATIVES INHIBITING BETA-SECRETASE ACTIVITY - The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. | 11-11-2010 |
20100286146 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS - The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 11-11-2010 |
20100298325 | PYRIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein X and Y are independently NR | 11-25-2010 |
20100305123 | CLASS OF HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH | 12-02-2010 |
20100305124 | Acylated Aminopyridine and Aminopyridazine Insecticides - The present invention relates to aminopyridine and aminopyridazine derivatives of the general formula (I) | 12-02-2010 |
20100317663 | ANILINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 12-16-2010 |
20110003811 | SUBSITUTED PYRIDINE DERIVATIVES - The present invention relates to pyridine derivatives of the general formula (I) and their use as openers of the KCNQ family potassium ion channels for the treatment of CNS disorders. | 01-06-2011 |
20110009407 | PYRIDINONE ANTAGONISTS OF ALPHA-4 INTEGRINS - The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: | 01-13-2011 |
20110021523 | ARYL SULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists. | 01-27-2011 |
20110028476 | PROTON PUMP INHIBITORS - A proton pump inhibitor containing a compound represented by the formula (I) | 02-03-2011 |
20110034463 | TYPE III SECRETION INHIBITORS, ANALOGS AND USES THEREOF - The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as | 02-10-2011 |
20110034464 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α | 02-10-2011 |
20110039846 | IMINOPYRIDINE DERIVATIVES AND USE THEREOF - The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof. | 02-17-2011 |
20110053938 | Compounds and Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 03-03-2011 |
20110053939 | NOVEL AROMATIC NITRO COMPOUNDS - Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding. | 03-03-2011 |
20110053940 | 3,4-SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS - The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency. | 03-03-2011 |
20110059968 | CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS - The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. | 03-10-2011 |
20110065705 | Compositions and Methods of Treating Cell Proliferation Disorders - The invention relates to compounds and methods for treating cell proliferation disorders. | 03-17-2011 |
20110077247 | CLASS OF HISTONE DEACETYLASE INHIBITORS - New histone deacetylase inhibitors according to the general formula (I) | 03-31-2011 |
20110086854 | NOVEL N-SUBSTITUTED-PYRROLIDINES AS INHIBITORS OF MDM2-P-53 INTERACTIONS - There are provided compounds of the formula | 04-14-2011 |
20110092505 | ORGANIC COMPOUNDS - The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof. | 04-21-2011 |
20110098298 | New Pyridin-3-Amine Derivatives - This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) | 04-28-2011 |
20110098299 | SPIROLACTAM DERIVATIVES AND USES OF SAME - The present invention provides spirolactam derivatives of formula (I): | 04-28-2011 |
20110098300 | Compounds Comprising A Cyclobutoxy Group - The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals, useful for the treatment and prevention of diseases or pathological conditions of the central nervous system including mild-cognitive impairments, Alzheimer's disease, learning and; memory disorders, cognitive disorders, attention deficit disorder, attention-deficit hyperactivity disorder, Parkinson's disease, schizophrenia, dementia, depression, epilepsy, seizures, convulsions, sleep/wake and arousal/vigilance disorders such as hypersomnia and narcolepsy, pain and/or obesity. | 04-28-2011 |
20110105503 | ARALKYL PIPERIDINE DERIVATIVES AND THEIR USES AS ANTALGIC OR ATARACTIC AGENT - The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects. | 05-05-2011 |
20110118261 | BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS - The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes. | 05-19-2011 |
20110118262 | Pyrrolidinyl and Piperidinyl Compounds Useful as NHE-1 Inhibitiors - Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same. | 05-19-2011 |
20110144107 | COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA - The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria. | 06-16-2011 |
20110144108 | SUBSTITUTED PIPERIDINE COMPOUNDS AND METHODS OF THEIR USE - Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors. | 06-16-2011 |
20110144109 | Derivatives of 1--4-methylpiperazine, synthesis process and uses thereof - The present invention concerns pyrrole compounds, derivatives of 1-{[1,5-bis(4-chlorophenyl)-2-methyl-1H-pyrrol-3-yl]methyl}-4-methylpiperazine (BM212). The invention concerns the use of the described compounds as antitubercular agents having high activity and low toxicity and process to obtain intermediates and final compounds. | 06-16-2011 |
20110144110 | Novel Pyrrole Inhibitors of S-Nitrosoglutathione Reductase as Therapeutic Agents - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 06-16-2011 |
20110152261 | Organic compounds - There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF | 06-23-2011 |
20110172229 | MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS - Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention. | 07-14-2011 |
20110178085 | Salts of N-[6-cis-2,6-Dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4'-(t- rifluoromethoxy)[1,1'-biphenyl]-3-carboxamide - Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide are prepared and characterized. | 07-21-2011 |
20110178086 | ADAMANTYL DIAMIDE DERIVATIVES AND USES OF SAME - The present invention provides adamantyl-diamide derivatives of formula (I): | 07-21-2011 |
20110178087 | Compositions and Their Use as Anti-Tumor Agents - The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas. | 07-21-2011 |
20110190295 | COMPOSITIONS AND METHODS FOR INHIBITION OF HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET SIGNALING - Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided. | 08-04-2011 |
20110190296 | Substituted Pyrrole Derivatives and Their Use as HMG-CO Inhibitors - The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms. | 08-04-2011 |
20110190297 | PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER - The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer. | 08-04-2011 |
20110201609 | PROTEASOME INHIBITORS FOR SELECTIVELY INDUCING APOPTOSIS IN CANCER CELLS - The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: | 08-18-2011 |
20110201610 | ARYL SULFONAMIDES - The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases. | 08-18-2011 |
20110201611 | Process for the Preparation of Compositions for Modulating a Kinase Cascade and Methods of Use Thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. | 08-18-2011 |
20110201612 | Compositions for Modulating a Kinase Cascade and Methods of Use Thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 08-18-2011 |
20110218199 | PYRIDONEAMIDE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS - Compounds of formula I | 09-08-2011 |
20110224209 | 4,4-DISUBSTITUTED PIPERIDINE DERIVATIVES USEFUL AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-1 (DPP-1) - The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1. | 09-15-2011 |
20110224210 | NOVEL BIS-AMIDES AS ANTI-MALARIAL AGENTS - The invention relates to novel bis-amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria. | 09-15-2011 |
20110281871 | TAAR1 LIGANDS - The invention relates to a compound of formula | 11-17-2011 |
20110288092 | Heterocyclic Inhibitors of MEK and Methods of Use Thereof - Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V | 11-24-2011 |
20110306614 | N-Hydroxylsulfonamide Derivatives as New Physiologically Useful Nitroxyl Donors - The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives. | 12-15-2011 |
20110312962 | NOVEL 2-MORPHOLINO-3-AMIDO-PYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application discloses novel 2-morpholino-3-amido-pyhcline derivatives and their use as modulators of the voltage gated K | 12-22-2011 |
20120004225 | BUMETANIDE, FUROSEMIDE, PIRETANIDE, AZOSEMIDE, AND TORSEMIDE ANALOGS, COMPOSITIONS AND METHODS OF USE - The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na | 01-05-2012 |
20120004226 | Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 01-05-2012 |
20120004227 | CYCLOHEXANE DERIVATIVE HAVING NPY Y5 RECEPTOR ANTAGONISM - The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: | 01-05-2012 |
20120004228 | Bis Aromatic Compounds for Use as LTC4 Synthase Inhibitors - There is provided compounds of formula I, | 01-05-2012 |
20120015942 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 01-19-2012 |
20120015943 | SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 01-19-2012 |
20120035174 | Salts of N-[6-cis-2,6-Dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4'-(t- rifluoromethoxy)[1,1'-biphenyl]-3-carboxamide - Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide are prepared and characterized. | 02-09-2012 |
20120046288 | Hydrazonamide Compounds That Modulate Hsp90 Activity - The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hsρ90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound. | 02-23-2012 |
20120059004 | Compounds And Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 03-08-2012 |
20120077812 | BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds. | 03-29-2012 |
20120101097 | ARYL SULFONAMIDES - The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases. | 04-26-2012 |
20120101098 | 3,28-DISUBSTITUTED BETULINIC ACID DERIVATIVES AS ANTI-HIV AGENTS - Compounds according to Formula (I) are described along with compositions containing the same and methods of use thereof for the treatment of viral infections. | 04-26-2012 |
20120115867 | NEW CLASS OF HISTONE DEACETYLASE INHIBITORS - This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH | 05-10-2012 |
20120122866 | TOPICAL PHARMACEUTICAL COMPOSITION INCLUDING REL-N-[6-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-3-PYRIDINYL]-2-METHYL-4'-(T- RIFLUOROMETHOXY)-[1,1'-BIPHENYL]-3-CARBOXAMIDE - The present invention relates to pharmaceutical compositions of 2-Methyl-4′-trifluoromethoxy-biphenyl-3-carboxylic acid [6-(cis-2,6-dimethyl-morpholin-4-yl)-pyridin-3-yl]-amide, to the use of such compositions in therapeutic applications and to methods for manufacturing such compositions. | 05-17-2012 |
20120142688 | PREPARATION OF 1-(SUBSTITUTED ARYL)-5-TRIFLUOROMETHYL-2-(1H)PYRIDONE COMPOUNDS AND SALTS THEREOF AND THEIR APPLICATIONS - A 1-(substituted aryl)-5-trifluoromethyl-2-(1H)pyridone compounds and pharmaceutical acceptable salts, preparation methods and uses for preparing the drugs for treating fibrosis thereof. | 06-07-2012 |
20120157455 | Compounds And Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 06-21-2012 |
20120172358 | GPCR Agonists - Compounds of formula (I): | 07-05-2012 |
20120172359 | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders - The invention relates to novel heterocyclic compounds of the formula | 07-05-2012 |
20120184549 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula Ik, Im | 07-19-2012 |
20120184550 | SUBSTITUTED NICOTINAMIDES AS KCNQ2/3 MODULATORS - Substituted nicotinamides, processes for their preparation, medicaments comprising these compounds and methods of using these compounds to treat pain, epilepsy, urinary incontinence, anxiety, dependency, mania, bipolar disorders, migraine, cognitive diseases, and/or dystonia-associated dyskinesias. | 07-19-2012 |
20120196857 | Modulators of Muscarinic Receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 08-02-2012 |
20120196858 | METHOD OF PROMOTING APOPTOSIS AND INHIBITING METASTASIS - The invention provides a method of promoting apoptosis in tumor cells, which can result in inhibiting tumor growth, or inhibiting tumor metastasis, or promoting tumor apoptosis, or any combination thereof, by administration of an effective amount of a focal adhesion kinase (FAK) inhibitor. The inhibitor is a small molecule organic compound. Accordingly, the focal adhesion kinase inhibitor can be used in the treatment of tumors, such as malignant cancer. For example, administration of effective amounts of the FAK inhibitor PND-1186 has been found to inhibit tumor cells in murine models for breast and ovarian cancer. | 08-02-2012 |
20120208815 | PIM KINASE INHIBITORS AND METHODS OF THEIR USE - New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer. | 08-16-2012 |
20120214807 | COMPOUNDS USEFUL AS ANTAGONISTS OF CCR2 - The present invention provides compounds of general formula I: | 08-23-2012 |
20120214808 | Aryl Urea Derivatives for Treating Obesity - A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment. | 08-23-2012 |
20120214809 | Aminoindane Compounds and Use Thereof in Treating Pain - The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine. | 08-23-2012 |
20120214810 | Salts of N-[6-cis-2,6-Dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4'-(t- rifluoromethoxy)[1,1'-biphenyl]-3-carboxamide - Salts of N-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2-methyl-4′-(trifluoromethoxy)[1,1′-biphenyl]-3-carboxamide are prepared and characterized. | 08-23-2012 |
20120220590 | NOVEL COMPOUNDS AS MODULATORS OF GLUCOCORTICOID RECEPTORS - Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described. | 08-30-2012 |
20120225877 | SUBSTITUTED 1, 4-DIOXA-8-AZASPIRO[4,5]DECANES USEFUL AS FUNGICIDES AND A PROCESS FOR THE PREPARATION THEREOF - This invention relates provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol-1-yl and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity. | 09-06-2012 |
20120238574 | (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS - The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis. | 09-20-2012 |
20120252809 | SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to compounds of the formula I, | 10-04-2012 |
20120252810 | FATTY ACID NON-FLUSHING NIACIN DERIVATIVES AND THEIR USES - The invention relates to fatty non-flushing acid niacin derivatives; compositions comprising an effective amount of a fatty acid non-flushing niacin derivative; and methods for treating or preventing an metabolic disease comprising the administration of an effective amount of a fatty acid non-flushing niacin derivative. | 10-04-2012 |
20120270873 | ADAMANTYL DIAMIDE DERIVATIVES AND USES OF SAME - The present invention provides adamantyl-diamide derivatives of formula (I): | 10-25-2012 |
20120270874 | Biaryl Compositions and Methods for Modulating a Kinase Cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: | 10-25-2012 |
20120289506 | 5-MEMBERED NITROGEN CONTAINING HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - 5-membered heterocyclic derivatives represented by 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, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH | 11-15-2012 |
20120295905 | NEW ANTI-MALARIAL AGENTS - The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation. | 11-22-2012 |
20120295906 | PYRIDYL-AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE-AND FURANE-DERIVATIVES AS KINASE INHIBITORS - The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R | 11-22-2012 |
20120322801 | HETEROCYCLIC AMIDES AS 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. | 12-20-2012 |
20120329798 | METHODS AND COMPOSITIONS FOR TREATING LUEKEMIA - A combination of a BCR-ABL inhibitor and a hedgehog pathway inhibitor for the treatment of leukemia. | 12-27-2012 |
20130045977 | TGF-beta SIGNAL TRANSDUCTION INHIBITOR - The present invention provides a compound represented by the following formula (I) or a physiologically acceptable salt thereof, and use thereof for the prophylaxis or treatment of TGF-β-related diseases: | 02-21-2013 |
20130053385 | METHOD OF COMBATING AND CONTROLLING PESTS - The use of a compound of formula I | 02-28-2013 |
20130109689 | Novel Methods for Preparation of (+)-1-ethyl-4-[2-(4-morpholinyl)ethyl)-3,3-diphenyl-2-pyrrolidinone | 05-02-2013 |
20130137687 | NOVEL PYRROLIDINE DERIVATIVES - The invention relates to a compound of formula (I) | 05-30-2013 |
20130172347 | C5AR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 07-04-2013 |
20130184277 | ADAMANTYL DIAMIDE DERIVATIVES AND USES OF SAME - The present invention provides adamantyl diamide derivatives of formula (I): | 07-18-2013 |
20130196992 | 1',3'-DISUBSTITUTED-4-PHENY-3,4,5,6-TETRAHYDRO-2H,1'H-[1,4']BIPYRIDINYL-2'- -ONES - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 08-01-2013 |
20130203757 | Compounds And Compositions For Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 08-08-2013 |
20130210822 | Compositions for Modulating a Kinase Cascade and Methods of Use Thereof - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning calorimetry profile, as well as a unique crystalline structure. | 08-15-2013 |
20130217686 | NOVEL METHYLCYCLOHEXANE DERIVATIVES AND USES THEREOF - A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain. | 08-22-2013 |
20130237539 | Compounds and Compositions for Treating Cancer - The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed. | 09-12-2013 |
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: | 09-26-2013 |
20130267516 | SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS - Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds. | 10-10-2013 |
20130281452 | SUBSTITUTED 4-AMINOBENZAMIDES AS KCNQ2/3 MODULATORS - Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders. | 10-24-2013 |
20130281453 | ANTI-CANCER SERINE HYDROLASE INHIBITORY CARBAMATES - Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC | 10-24-2013 |
20130310377 | NOVEL MODULATORS OF CALCIUM RELEASE-ACTIVATED CALCIUM CHANNEL - Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer. | 11-21-2013 |
20130310378 | 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS - The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R | 11-21-2013 |
20130310379 | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF - Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein. | 11-21-2013 |
20130317027 | COMPOUNDS AND THERAPEUTIC USES THEREOF - The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders. | 11-28-2013 |
20130317028 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 11-28-2013 |
20130324530 | 3-(AMINOARYL)-PYRIDINE COMPOUNDS - The present invention provides a compound of formula (I): | 12-05-2013 |
20130324531 | SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES - There are provided compounds of the formula | 12-05-2013 |
20140038963 | Multifunctional Radical Quenchers For The Treatment Of Mitochondrial Dysfunction - The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation. | 02-06-2014 |
20140051702 | Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial Cystitis - The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient. | 02-20-2014 |
20140057909 | Novel Indole Derivative or Pharmaceutically Acceptable Salt Thereof, Preparation Method Thereof, and Pharmaceutical Composition for Preventing or Treating Metabolic Diseases Containing Same as Active Ingredient - The present invention relates to an indole derivative, The indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (DGAT) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease. | 02-27-2014 |
20140066445 | Composition and Methods for Modulating a Kinase Cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention also relates to substantially pure compound 1 and substantially pure compound 1 salt (e.g., compound 1 hydrochloride salt and compound 1 benzenesulfonate salt). The invention further relates to methods of preparing substantially pure compound 1 and compound 1 salts. | 03-06-2014 |
20140080832 | IRE-1alpha INHIBITORS - Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies. | 03-20-2014 |
20140088105 | Cyclohexyl Amide Derivatives and Their Use as CRF-1 Receptor Antagonists - There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF | 03-27-2014 |
20140094461 | BIOMARKERS FOR HEDGEHOG INHIBITOR THERAPY - A method of selecting a subject having cancer for treatment with a Hedgehog signaling inhibitor by determining the level of expression of at least one biomarker in a biological sample derived from the subject. | 04-03-2014 |
20140107122 | Substituted Benzene Compounds - The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 04-17-2014 |
20140128393 | Methods of Treating Cancer - The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 05-08-2014 |
20140135328 | SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to compounds of the formula I, | 05-15-2014 |
20140142103 | Methods and Compositions for Modulating Rad51 and Homologous Recombination - The present invention concerns methods and compositions involving inhibitors and enhancers of RAD51, a protein involved in homologous recombination. In some embodiments, the present invention concerns methods for stimulating homologous recombination, which has a number of significant research and clinical applications. In certain other embodiments, there are methods for protecting cells using a compound that enhances RAD51 activity. Such enhancers may also be employed to prevent or reduce damage to cells that may be caused by DNA damaging agents. In other embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 enhancer or inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation. | 05-22-2014 |
20140155400 | METHODS AND COMPOSITIONS FOR TYPING MOLECULAR SUBGROUPS OF MEDULLOBLASTOMA - Immunohistochemical methods and compositions for the typing of molecular subgroups of medulloblastomas are provided. The methods comprise determining a protein expression profile for a sample obtained from a medulloblastoma by detecting expression of GAB 1, filamin A, or at least two biomarker proteins selected from the group consisting of β-catenin, YAP1, GAB1, and filamin A, and typing the medulloblastoma as a WNT pathway tumor, a SHH pathway tumor, or a non-WNT/non-SHH tumor based on this protein expression profile. Kits for typing a medulloblastoma according to these three molecular subgroups are provided. The kits comprise at least two antibodies, wherein each of said antibodies specifically binds to a distinct biomarker protein selected from the group consisting of β-catenin, YAP1, GAB1, and filamin A, and can optionally comprise one or more of instructions for use, reagents for detecting antibody binding to one or more of said biomarker proteins, and one or more positive control samples. | 06-05-2014 |
20140155401 | NOVEL SUBSTITUTED BIPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE RECEPTOR LIGANDS - The present invention relates to novel substituted 2,4′- and 3,4′-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders. | 06-05-2014 |
20140187554 | MODULATORS OF THE NUCLEAR HORMONE RECEPTOR ROR - The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as RORα, RORβ, or RORγ. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided. | 07-03-2014 |
20140187555 | NOVEL SOFT PDE4 INHIBITORS - The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 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 soft PDE4 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 inflammatory diseases. | 07-03-2014 |
20140194424 | SPIROLACTAM DERIVATIVES AND USES OF SAME - The present invention provides spirolactam derivatives of formula (I): | 07-10-2014 |
20140194425 | Novel Pyrrole Inhibitors of S-Nitrosoglutathione Reductase as Therapeutic Agents - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 07-10-2014 |
20140206690 | COMPOUNDS FOR USE AS THERAPEUTIC AGENTS AFFECTING P53 EXPRESSION AND/OR ACTIVITY - The present invention relates to compound (I) | 07-24-2014 |
20140213587 | Biaryl Compositions and Methods for Modulating a Kinase Cascade - The invention relates to compounds and methods for modulating one or more components of a kinase cascade. | 07-31-2014 |
20140213588 | PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS - The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds. | 07-31-2014 |
20140221373 | ARYLPYRAZOLE ETHERS AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE - The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A | 08-07-2014 |
20140235635 | SYNTHESIS AND USE OF KINASE INHIBITORS - An improved synthesis of a class of inhibitor of Focal Adhesion Kinase (FAK) is provided, wherein use of an expensive palladium-based catalyst is reduced and reaction yields and product purities are improved. Two key reactions of coupling of aryl halides with anilines are optimized with the surprising discovery that the palladium-based catalyst can be dispensed with entirely in one of the reactions. The invention also provides the use of the FAK-inhibitory compounds in the treatment of inflammatory and immune disorders and of arthritis. | 08-21-2014 |
20140235636 | N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES - The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. | 08-21-2014 |
20140235637 | COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS - Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system. | 08-21-2014 |
20140243334 | SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 08-28-2014 |
20140243335 | SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF - This invention provides compounds of formula (I): | 08-28-2014 |
20140243336 | 2-Pyridyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors - The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 08-28-2014 |
20140243337 | Phenyl Carboxamide-Containing Spleen Tyrosine Kinase (SYK) Inhibitors - The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase. | 08-28-2014 |
20140249149 | Compounds with Nematicidal Activity - The present invention relates to the use of known pyridyl carboxamide derivatives and novel pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes. | 09-04-2014 |
20140275079 | PYRROLE AMIDE INHIBITORS - The present invention provides for compounds of formula (I) | 09-18-2014 |
20140275080 | N-Acyl-N'-(pyridin-2-yl) Ureas and Analogs Exhibiting Anti-Cancer and Anti-Proliferative Activities - Described are compounds of Formula I | 09-18-2014 |
20140275081 | INHIBITORS OF HUMAN EZH2, AND METHODS OF USE THEREOF - The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject. | 09-18-2014 |
20140296237 | PICOLINAMIDE DERIVATIVES AS TTX-S BLOCKERS - The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. | 10-02-2014 |
20140309225 | NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF - The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, | 10-16-2014 |
20140315903 | 1, 4-Disubstituted 3-Cyano-Pyridone Derivatives and Their Use As Positive Allosteric Modulators of MGLUR2-Receptors - The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) | 10-23-2014 |
20140323483 | TYPE III SECRETION INHIBITORS, ANALOGS AND USES THEREOF - The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as | 10-30-2014 |
20140350015 | PYRIDINE AND PYRIMIDINE BASED COMPOUNDS AS WNT SIGNALING PATHWAY INHIBITORS FOR THE TREATMENT OF CANCER - The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer. | 11-27-2014 |
20150025073 | MORPHOLINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 01-22-2015 |
20150025074 | METHODS AND COMPOSITIONS FOR TREATING SOLID TUMORS AND OTHER MALIGNANCIES - A combination of a kinase inhibitors of mTOR and downstream effector and a hedgehog pathway inhibitor for the treatment of cancer. | 01-22-2015 |
20150045363 | Hedgehog Pathway Inhibition for Cartilage Tumor and Metachondromatosis Treatment - Hedgehog pathway inhibitors, such as small molecules, are used to prevent, slow, block the formation of cartilage tumors as well as exostosis or enchondromas. | 02-12-2015 |
20150057279 | HETEROARYL COMPOUNDS WITH A-CYCLIC BRIDGING UNIT - This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds. | 02-26-2015 |
20150065503 | SALT FORM OF A HUMAN HISTONE METHYLTRANSFERASE EZH2 INHIBITOR - Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound. | 03-05-2015 |
20150065504 | ANTIVIRAL COMPOUNDS - Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV). | 03-05-2015 |
20150099747 | Methods and Compositions For Detecting Mutation in the Human EZH2 Gene - The invention comprises reagents and methods for detecting cancer-associated mutations in the human EZH2 gene. Further, a method of detecting the mutations and a method of treatment are disclosed. | 04-09-2015 |
20150105386 | 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS - The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R | 04-16-2015 |
20150141425 | C5aR ANTAGONISTS - Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors. | 05-21-2015 |
20150290182 | USE OF AMINOINDANE COMPOUNDS IN TREATING OVERACTIVE BLADDER AND INTERSTITIAL CYSTITIS - The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient. | 10-15-2015 |
20150290203 | TREATMENT AND/OR PROPHYLAXIS OF TSPO MEDIATED DISEASES AND/OR DISORDERS - The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity. | 10-15-2015 |
20150299125 | PRODRUG BIPYRIDYLAMINOPYRIDINES AS SYK INHIBITORS - The present invention provides compounds of Formula (I), which are prodrugs of trans-4-[(1R)-(6-{[4-(difluoromethyl)pyridin-2-yl]amino}-4-methyl-2,3′-bipyridin-6′-yl)-1-hydroxyethyl]cyclohexanecarboxylic acid, a potent inhibitor of Syk. The compounds are useful in the treatment and prevention of diseases mediated by the enzyme, such as asthma, COPD, rheumatoid arthritis and cancer. | 10-22-2015 |
20150306069 | METHODS AND COMPOSITIONS INVOLVING RAD51 INHIBITORS - The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation. | 10-29-2015 |
20150307480 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 10-29-2015 |
20150313906 | COMBINATION - The present invention relates to a method of treating cancer and pre-cancerous syndromes in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering:
| 11-05-2015 |
20150315147 | COMPOSITIONS FOR MODULATING A KINASE CASCADE AND METHODS OF USE THEREOF - The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxyl)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. | 11-05-2015 |
20150335652 | USP14 Inhibitors for Treating or Preventing Viral Infections - Disclosed herein are methods of treating or preventing a viral infection resulting from infection by a flavivirus, comprising administering to a subject a small molecule inhibitor of USP14, represented by Formula (I) or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, chemically-protected form, enantiomer or stereoisomer thereof, and pharmaceutical compositions comprising an effective amount of a compound of Formula (I) for use in the method. | 11-26-2015 |
20150344427 | 1,4-PYRIDONE COMPOUNDS - The present invention relates to 1,4-pyridone compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 12-03-2015 |
20150352119 | SUBSTITUTED BENZENE COMPOUNDS - The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 12-10-2015 |
20150353548 | 2-AMINOPYRIDINE COMPOUNDS - The invention provides novel substituted 2-aminopyridine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases. | 12-10-2015 |
20150376130 | N-PROP-2-YNYL CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS - Compounds of formula I, wherein A, B, X, Z and R | 12-31-2015 |
20160002156 | N-HYDROXYLSULFONAMIDE DERIVATIVES AS NEW PHYSIOLOGICALLY USEFUL NITROXYL DONORS - The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives. | 01-07-2016 |
20160008369 | ORAL FORMULATION AND SUSPENSION OF AN ONCOLOGY DRUG | 01-14-2016 |
20160016946 | Methods, Compounds, and Compositions for the Treatment of Angiotensin-Related Diseases - Disclosed are small molecule non-peptidic compounds, as well as methods and compositions for the treatment of angiotensin-related diseases and disorders, including cardiovascular diseases, metabolic diseases, gastrointestinal diseases, renal diseases, inflammatory/autoimmune diseases, neurological diseases, bone marrow diseases and cancer. | 01-21-2016 |
20160022693 | ARYL- OR HETEROARYL-SUBSTITUTED BENZENE COMPOUNDS - The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 01-28-2016 |
20160039752 | BENZYLAMINE DERIVATIVES - The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R3, R5 to R9, A, P, V, W, X, Y and Z are as defined herein. | 02-11-2016 |
20160039774 | HETEROARYL ACID MORPHOLINONE COMPOUNDS AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER - The present invention provides MDM2 inhibitor compounds of Formula (I), or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor of Formula (I). | 02-11-2016 |
20160046570 | N-ACYLOXYSULFONAMIDE AND N-HYDROXY-N-ACYLSULFONAMIDE DERIVATIVES - The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. | 02-18-2016 |
20160096804 | NOVEL HISTONE DEACETYLASE INHIBITORS - The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors. | 04-07-2016 |
20160102083 | ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS - This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers. | 04-14-2016 |
20160129007 | Method for Preventing and/or Treating Chronic Traumatic Encephalopathy - IV - The present invention relates to a method of preventing and/or treating chronic traumatic encephalopathy by administering to a subject 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide. | 05-12-2016 |
20160136174 | SALTS AND SOLID FORMS OF (S)-3-(4-((4-(MORPHOLINOMETHYL)BENZYL)OXY)-1-OXOISOINDOLIN-2-YL)PIPERIDIN- E-2,6-DIONE AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed. | 05-19-2016 |
20160159773 | HETEROCYCLIC COMPOUND - The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. | 06-09-2016 |
20160166553 | ANTIMETASTATIC COMPOUNDS | 06-16-2016 |
20160168093 | PIPERIDINE DERIVATIVES AS HDAC1/2 INHIBITORS | 06-16-2016 |
20160194284 | ALLOSTERIC MODULATORS OF THE CANNABINOID 1 RECEPTOR | 07-07-2016 |
20180022702 | PIPERIDINE DERIVATIVES AS HDAC1/2 INHIBITORS | 01-25-2018 |
20190144437 | SUBSTITUTED 2, 4-DIAMINO-QUINOLINE DERIVATIVES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES | 05-16-2019 |