Entries |
Document | Title | Date |
20080280891 | 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: | 11-13-2008 |
20080280892 | Compounds - Tricyclic nitrogen containing compounds and their use as antibacterials. | 11-13-2008 |
20080293706 | QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives. | 11-27-2008 |
20080300242 | Imidazopyridine Kinase Inhibitors - The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents. | 12-04-2008 |
20080312221 | QUINOLINE DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF-PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME - An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: | 12-18-2008 |
20090018124 | Novel Benzoimidazole Derivatives and Pharmaceutical Composition Comprising the Same - Disclosed herein are novel benzoimidazole derivatives functioning as antagonists to vanilloid receptor-1, and a pharmaceutical composition comprising the same. They are useful in preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraines, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, strokes, bladder hypersensitivity, irritable bowel syndrome, respiratory disorders such as asthma, chronic obstructive pulmonary disease, etc., burns, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases. | 01-15-2009 |
20090029976 | BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES - The present invention relates to compounds of formula I | 01-29-2009 |
20090029977 | DUAL MODULATORS OF 5HT2A AND D3 RECEPTORS - The present invention relates to compounds of the formula (I) | 01-29-2009 |
20090062266 | OXAZOLIDINONE COMPOUNDS, AND COMPOSITIONS AND METHODS RELATED THERETO - The invention provides new oxazolidinone compounds of formula (I) wherein A is certain heterocycles optionally substituted; R | 03-05-2009 |
20090075987 | ALKYLACETYLENE SUBSTITUTED ACYLTRYPTOPHANOLS - The present invention relates to acyltryptophanols of the general formula I, | 03-19-2009 |
20090075988 | CYANOISOQUINOLINE - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 03-19-2009 |
20090111800 | CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula (I): having 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, and other conditions associated with 11β-HSD type 1 activity. | 04-30-2009 |
20090143372 | CHEMICAL COMPOUNDS - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: | 06-04-2009 |
20090156586 | COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - This invention relates to compounds of the Formula (I): | 06-18-2009 |
20090197876 | INDOLINONE DERIVATIVES SUBSTITUTED IN THE 6 POSITION, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula | 08-06-2009 |
20090239853 | Fused heterocycle derivative - A fused heterocycle derivative represented by the general formula (I): | 09-24-2009 |
20090253689 | Organic Compounds - New compounds of the Formula (I): | 10-08-2009 |
20090270376 | HETEROCYCLIC JANUS KINASE 3 INHIBITORS - The present invention provides a compound of formula (I) having an excellent JAK3 inhibition activity and being useful as an active ingredient of an agent for treating and/or preventing various immune diseases including autoimmune diseases inflammatory diseases, and allergic diseases. The compound according to the present invention has an inhibition activity against JAK3 and is thus useful as an active ingredient of an agent for treating or preventing diseases caused by undesirable cytokine signal transmission (e.g., rejection during organ/tissue transplantation, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis, asthma, atopic dermatitis, Alzheimer's disease, and atherosclerotic disease), or diseases caused by abnormal cytokine signal transmission (e.g., cancer and leukemia). | 10-29-2009 |
20090275568 | FUSED QUINOLINE DERIVATIVE AND USE THEREOF - The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) | 11-05-2009 |
20090286772 | 2-(Phenyl or Heterocyclic)-1H-Phenanthro[9,10-D]Imidazoles - The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed. | 11-19-2009 |
20090286773 | Kinase inhibitors - The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed. | 11-19-2009 |
20100004232 | Pharmaceutical Compounds - The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDK1, Chk (e.g. Cbk1 or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c) an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I′), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I′): or a salt, solvate, tautomer or N-oxide thereof wherein R | 01-07-2010 |
20100009978 | Benzoxazoles and Oxazolopyridines Being Useful as Janus Kinases Inhibitors - The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, | 01-14-2010 |
20100022521 | COMPOUNDS - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH | 01-28-2010 |
20100035870 | Pyrimidin-4-yl-3, 4-Dihydro-2H-Pyrrolo[1,2A] Pyrazin-1-one Compounds - The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR | 02-11-2010 |
20100041645 | RHO KINASE INHIBITORS - Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma. | 02-18-2010 |
20100056505 | Substituted Pyrazalones - The invention is related to compounds of formula (I) as antagonists of the TGFβ family type I receptors, Alk5 and/or AIk 4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable. | 03-04-2010 |
20100056506 | SUBSTITUTED 2-AMINO-FUSED HETEROCYCLIC COMPOUNDS - The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R | 03-04-2010 |
20100063037 | 6-SUBSTITUTED BENZOXAZINES - The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) | 03-11-2010 |
20100069375 | Indolone-Acetamide Derivatives, Processes for Preparing Them and Their Uses - The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion. | 03-18-2010 |
20100081653 | 2-[1H-Benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides as kinase inhibitors - 2-[1H-benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and their salts are kinase inhibitors, useful in the treatment of cancer. | 04-01-2010 |
20100093713 | BETA-CARBOLINES USEFUL FOR TREATING INFLAMMATORY DISEASE - This invention provides beta-carboline compounds of formula | 04-15-2010 |
20100105667 | Quinoxaline- and Quinoline-Carboxamide Derivatives - The invention relates to compounds of formula (I) | 04-29-2010 |
20100105668 | Quinazoline derivatives - The present invention concerns the compounds of formula | 04-29-2010 |
20100137294 | COMPOUNDS, COMPOSITIONS AND METHODS FOR CONTROLLING INVERTEBRATE PESTS - The present application discloses the Tv-stp-1 serine/threonine phosphatase gene from | 06-03-2010 |
20100160303 | CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, | 06-24-2010 |
20100179139 | PYRROLOPYRIDINE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR USE AS MEDICAMENTS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I): | 07-15-2010 |
20100184754 | QUINOLINONE DERIVATIVES - Organic compounds having the formulas I and II are provided where the variables have the values described herein. | 07-22-2010 |
20100197673 | INDOLE AND INDAZOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient. | 08-05-2010 |
20100210634 | Certain Chemical Entities, 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. | 08-19-2010 |
20100227856 | 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 piperidines, according to Formula I | 09-09-2010 |
20100240642 | 1H-Indole-2-Carboxylic Acid Derivatives Useful As PPAR Modulators - The present invention relates to certain indole derivatives that are modulators of PPARγ, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. | 09-23-2010 |
20100249118 | COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR - Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. | 09-30-2010 |
20100261716 | INDAZOLE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS - The invention provides novel indazole-carboxamide 5-HT | 10-14-2010 |
20100261717 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula I | 10-14-2010 |
20100261718 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula | 10-14-2010 |
20100267707 | Tyrosine Kinase Inhibitors - The present invention relates to 4-indol-3-yl-N-phenylpyrimidin-2-amine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 10-21-2010 |
20100267708 | GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT - The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient. | 10-21-2010 |
20100267709 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 10-21-2010 |
20100267710 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula I | 10-21-2010 |
20100286133 | Diacyl indazole derivatives as lipase and phospholipase inhibitors - The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: | 11-11-2010 |
20100305112 | PYRIMIDINE INHIBITORS OF KINASE ACTIVITY - Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, | 12-02-2010 |
20100317656 | IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPEUTICS - Compounds of Formula (I): | 12-16-2010 |
20110009396 | TRICYCLIC COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention provides compounds represented by formula 1: | 01-13-2011 |
20110071144 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The invention relates to quinazoline derivatives of formula (1) | 03-24-2011 |
20110077240 | INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY - This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions. | 03-31-2011 |
20110098286 | (3-ARYL-PIPERAZIN-1-YL), (2-ARYL-MORPHOLIN-4-YL) AND (2-ARYL-THIOMORPHOLIN-4-YL) DERIVATIVES OF 6,7-DIALKOXY-QUINAZOLINE, 6,7-DIALKOXYPHTALAZINE AND 6,7-DIALKOXYISOQUINOLINE - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides a process for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 04-28-2011 |
20110118245 | RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF - Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O) | 05-19-2011 |
20110130394 | PHARMACEUTICAL COMPOUNDS - The invention provides kinase inhibitor compounds of the formula (1): | 06-02-2011 |
20110166130 | NOVEL POTASSIUM CHANNEL BLOCKERS AND USES THEREOF - The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation. | 07-07-2011 |
20110178075 | INDOLES, 1H-INDAZOLES, 1,2-BENZISOXAZOLES, 1,2-BENZOISOTHIAZOLES, AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (indazoles and benzothiazoles), which act as ligands for the α7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 07-21-2011 |
20110183969 | ANTIFUNGAL COMBINATION THERAPY - The invention provides pharmaceutical combinations comprising a combination of an antifungal indolizine compound of formula (I) or a pharmaceutically acceptable salt thereof and a second antifungal agent: wherein: R1, R2, R3, R4, R5, R6, R7, X and X | 07-28-2011 |
20110201604 | Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof - Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase. | 08-18-2011 |
20110218193 | NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases. | 09-08-2011 |
20110224197 | PYRIMIDINES AND PYRIDINES USEFUL AS INHIBITORS OF PROTEIN KINASES - The present invention relates to compounds useful as inhibitors of protein kinases, such as inhibitors of GSK-3. The invention provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. The invention provides processes for preparing compounds of the invention. The invention provides methods of identifying compounds useful for treatment of diabetes, diabetic neuropathy, osteoporosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, leukocytopenia, cardiomyocyte hypertrophy, stroke, post-stroke, spinal cord injury, traumatic brain injury, Charcot-Marie-Tooth, peripheral nerve regeneration, and rheumatoid arthritis. | 09-15-2011 |
20110224198 | ARYL METHYL BENZOQUINAZOLININE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 09-15-2011 |
20110251188 | ACENAPHTHO HETEROCYCLE COMPOUNDS, CYCLODEXTRIN INCLUSION COMPOUNDS AND COMPLEXES, AND USES IN THE MANUFACTURES OF BH3 PROTEIN ANALOGUE, BCL-2 FAMILY PROTEIN INHIBITORS THEREOF - The present invention relates to acenaphtho heterocyclic compounds, cyclodextrin inclusion compounds and complexes thereof, and their uses in manufacturing the inhibitors of BH3 analogue, Bcl-2 family proteins. The acenaphtho heterocyclic compounds are obtained by introducing oxo-, thio-, carbonyl, ester or acyl in the 3-, 4- and 6-position of 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile, or further substituting 9-cyano with carboxyl, ester or amide. The compounds can simulate BH3-only protein, competitively binding and antagonizing Bcl-2, Bel-X | 10-13-2011 |
20110263581 | FUSED TRICYCLIC COMPOUNDS AS SERINE-THREONINE PROTEIN KINASE AND PARP MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules. | 10-27-2011 |
20110275620 | Method for preventing or treating a disease related to the glucocorticoid receptor - A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-hydroquinoline compound. | 11-10-2011 |
20110301155 | INDAZOLE COMPOUNDS FOR ACTIVATING GLUCOKINASE - The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. | 12-08-2011 |
20110312949 | PHARMACEUTICAL USE OF SUBSTITUTED AMIDES - The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable. | 12-22-2011 |
20120004218 | NOVEL TETRAHYDRO-QUINOLINE DERIVATIVES - A compound of formula (I) | 01-05-2012 |
20120010201 | NOVEL ANELLATED PYRIDINE COMPOUNDS - The present invention is concerned with novel dual modulators of the 5-HT | 01-12-2012 |
20120035163 | NOVEL FUSED RING COMPOUND AND USE THEREOF - The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): | 02-09-2012 |
20120035164 | CHEMICAL COMPOUNDS - The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: | 02-09-2012 |
20120040972 | DUAL MODULATORS OF 5HT2A AND D3 RECEPTORS - The present invention relates to compounds of the formula (I) | 02-16-2012 |
20120058996 | CARBAZOLE CARBOXAMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, | 03-08-2012 |
20120088760 | GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Disclosed are new compounds of formula (1) exhibiting excellent activity for glucokinase, pharmaceutical compositions having the same as an active ingredient, and a method of using the same as an active ingredient for lowering blood glucose level: | 04-12-2012 |
20120115855 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 05-10-2012 |
20120115856 | AGENT FOR TREATMENT OR PREVENTION OF DISEASES ASSOCIATED WITH ACTIVITY OF NEUROTROPHIC FACTORS - A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. | 05-10-2012 |
20120157449 | BENZOFURANE COMPOUNDS - The present invention is concerned with novel dual modulators of the 5-HT | 06-21-2012 |
20120190673 | PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES - The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R′, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase. | 07-26-2012 |
20120190674 | SULFONAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 07-26-2012 |
20120202801 | METHODS FOR TREATING BREAST CANCER - Methods for treating breast cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment. | 08-09-2012 |
20120214804 | PHARMACEUTICAL COMPOSITION COMPRISING INDOLE COMPOUND - The present invention relates to a pharmaceutical composition comprising a compound of formula (1), (2) or (3) as defined in the specification for the prevention or treatment of diseases associated with oxidative stress, mitochondria dysfunction, hypoxic injury, necrosis and/or ischemic reperfusion injury, and a cosmetic composition comprising an indole compound having an antioxidant effect. | 08-23-2012 |
20120238558 | Kinase inhibitors - The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed. | 09-20-2012 |
20120238559 | NOVEL COMPOUNDS - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): | 09-20-2012 |
20120252798 | INDOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient. | 10-04-2012 |
20120283254 | NOVEL BENZOFURANE-PIPERIDINE COMPOUNDS - The present invention is concerned with novel selective dual modulators of the 5-HT | 11-08-2012 |
20120283255 | UREA DERIVATIVES, METHODS FOR THEIR MANUFACTURE, AND USES THEREFOR - The present invention provides compounds of formula (I): | 11-08-2012 |
20120289500 | POTASSIUM CHANNEL MODULATORS - Disclosed herein are KCNQ potassium channels modulators of formula (I) | 11-15-2012 |
20120309751 | TERTIARY 8-HYDROXYQUINOLINE-7-CARBOXAMIDE DERIVATIVES AND USES THEREOF - New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed. | 12-06-2012 |
20130053375 | AMINO-QUINOLINES AS KINASE INHIBITORS - Disclosed are quinoline compounds having the formula: | 02-28-2013 |
20130065890 | PYRIMIDINE DERIVATIVES - A compound of the following formula: | 03-14-2013 |
20130143874 | FUSED RING PYRIDINE COMPOUND - [Problem] To provide a compound useful as a novel agent which is excellent in preventing and/or treating cannabinoid receptor type 2-related diseases, based on agonist action on a cannabinoid receptor type 2 | 06-06-2013 |
20130158020 | INDAZOLE DERIVATIVES USEFUL AS ERK INHIBITORS - The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. | 06-20-2013 |
20130165432 | Dual Modulators of 5HT2A and D3 Receptors - The present invention relates to compounds of the formula (I) | 06-27-2013 |
20130165433 | Novel Use - The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection. | 06-27-2013 |
20130172330 | Chemokine Receptor Modulators - The invention provides compounds of Formula (I) | 07-04-2013 |
20130184269 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-18-2013 |
20130190303 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-25-2013 |
20130237532 | INDOLE AND INDAZOLE COMPOUNDS AS AN INHIBITOR OF CELLULAR NECROSIS - The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient. | 09-12-2013 |
20130245008 | NITROBENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATIONS THEREOF - The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis. | 09-19-2013 |
20130274252 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 10-17-2013 |
20130289027 | Isoquinoline Compounds And Methods For Treating HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV). | 10-31-2013 |
20130296311 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 11-07-2013 |
20140005182 | Aryl Methyl Benzoquinazolinone M1 Receptor Positive Allosteric Modulators | 01-02-2014 |
20140024643 | BRIDGED HETEROCYCLIC COMPOUNDS AND METHODS OF USE - This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 01-23-2014 |
20140200212 | Substituted Fused Imidazole Derivatives, Pharmaceutical Compositions, and Methods of Use Thereof - Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase. | 07-17-2014 |
20140243324 | USE OF HEMATOPOIETIC GROWTH FACTOR MIMETICS - The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin. | 08-28-2014 |
20140303153 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: | 10-09-2014 |
20140315899 | SULFONAMIDES AS TRPM8 MODULATORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: | 10-23-2014 |
20140364427 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. | 12-11-2014 |
20150038500 | PHARMACEUTICAL COMPOSITION FOR PREVENTING AND TREATING OPHTHALMIC DISORDERS - The invention relates to a pharmaceutical composition for preventing or treating an ophthalmologic disease comprising a compound of formula (1) as defined in the specification, or a pharmaceutically acceptable salt or isomer thereof as an active ingredient. Also, the invention relates to a composition for cleansing or preserving a contact lens comprising the above active ingredient. | 02-05-2015 |
20150038501 | INHIBITORS OF HCV NS5A - Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C. | 02-05-2015 |
20150045354 | Anti-Malarial Agents - The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R | 02-12-2015 |
20150065494 | AMINOSTYRYLBENZOFURAN DERIVATIVES AS INHIBITORS AGAINST BETA-AMYLOID FIBRIL FORMATION, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid. | 03-05-2015 |
20150065495 | SUBSTITUTED- 1H-BENZO[D]IMIDAZOLE SERIES COMPOUNDS AS LYSINE-SPECIFIC DEMETHYLASE 1 (LSD1) INHIBITORS - The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions. | 03-05-2015 |
20150072978 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein. | 03-12-2015 |
20150105380 | METHODS AND USES OF COMPOUNDS FOR TREATING DISEASE - The present invention provides methods for treating polycystic kidney disease by administering a compound or pharmaceutical composition thereof having the general structural formula (I) | 04-16-2015 |
20150119387 | Compound as WNT Signaling Inhibitor, Composition, and Use Thereof - The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways. | 04-30-2015 |
20150133439 | QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS - The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. | 05-14-2015 |
20150297581 | RHO KINASE INHIBITORS - Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds. | 10-22-2015 |
20150344494 | Thienopyranones as Kinase and Epigenetic Inhibitors - The invention relates to methods of treating diseases including but not limited to, cancer non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis, Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of PI3 kinase and/or bromodomain protein binding to substrates composing the administration of a compound(s) of Formula I-IX (or pharmaceutically acceptable salts thereof) as defined herein. | 12-03-2015 |
20160002177 | COMT INHIBITORS - The present invention relates to compounds of formula | 01-07-2016 |
20160002213 | HEPATITIS C INHIBITORS AND USES THEREOF - This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions. | 01-07-2016 |
20160002231 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: | 01-07-2016 |
20160046583 | ISOQUINOLINE DERIVATIVES - The present invention relates to the use of compounds of general formula | 02-18-2016 |
20160068512 | Quinazoline Derivatives Useful as CB-1 Inverse Agonists - The present invention is directed to quinazoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. For example, the compounds of the present invention are useful in the treatment of metabolic disorders. | 03-10-2016 |
20160068531 | NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION - The invention provides novel compounds having the general formula: | 03-10-2016 |
20160158217 | Quinoline Carboxamide and Quinoline Carbonitrile Derivatives as mGluR2-Negative Allosteric Modulators, Compositions, and Their Use - The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) | 06-09-2016 |
20160158218 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein. | 06-09-2016 |
20160159744 | Quinoline Carboxamide and Quinoline Carbonitrile Derivatives as mGluR2-Negative Allosteric Modulators, Compositions, and Their Use - The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) | 06-09-2016 |
20160194313 | INDOLE AMIDE COMPOUND AS INHIBITOR OF NECROSIS | 07-07-2016 |
20160200685 | SUBSTITUTED 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES | 07-14-2016 |
20160200709 | INDOLE COMPOUND AS INHIBITOR OF NECROSIS | 07-14-2016 |
20160251310 | COMPOUNDS AS MODULATORS OF RORC | 09-01-2016 |