Entries |
Document | Title | Date |
20080207592 | Novel 1,4-benzothiazepine-1,1-dioxide derivative having improved properties, method for the production thereof, medicaments containing said compound, and use thereof - The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic. | 08-28-2008 |
20080234250 | Heterocyclic Condensed Compounds Useful as Antidiuretic Agents - The invention concerns compounds according to general formulae 1, wherein G | 09-25-2008 |
20080242656 | N-Substituted-N-Sulfonylaminocyclopropane Compounds and Pharmaceutical Use Thereof - The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) | 10-02-2008 |
20080269192 | Chiral Fused [1,2]Imidazo[4,5-C] Ring Compounds - Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X | 10-30-2008 |
20080293690 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 11-27-2008 |
20090054400 | NEW PROGESTERONE RECEPTOR MODULATORS - The present invention provides new progesterone receptor modulators which are dibenzo[b,f]pyrido[1,2-d]oxazepine-2-amines or dibenzo[b,f]prido[1,2-d]thiazepine-2-amines, and uses thereof. | 02-26-2009 |
20090075973 | BENZO-FUSED HETEROCYCLES - The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. | 03-19-2009 |
20090221551 | SUBSTITUTED FUSED[1,2] IMIDAZO[4,5C] RING COMPOUNDS AND METHODS - [1,2]Imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) substituted with a fused ring containing an oxygen and/or nitrogen atom attached at the 1- and/or 2-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed. | 09-03-2009 |
20090253681 | HIV Integrase Inhibitors - Compounds of Formula I are inhibitors of FHV integrase and inhibitors of FHV replication (I), wherein m, n, X, R | 10-08-2009 |
20090264407 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to formula I: | 10-22-2009 |
20100004222 | Amide Derivatives as Ion-Channel Ligands and Pharmaceutical Compositions and Methods of Using the Same - Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 01-07-2010 |
20100029612 | 2-Aminoethyl Substituted Pyrimidin-2-Ones Cyclopropanes, Pyrazolines, Pyrimidines and Benzothiazepines and Their Uses as Urotensin II and Somatostatin 5 Receptor Ligands - The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor. | 02-04-2010 |
20100069356 | DIBENZOTHIAZEPINE MODULATORS OF DOPAMINE, ALPHA ADRENERGIC, AND SEROTONIN RECEPTORS - The present invention relates to new dibenzothiazepine modulators of D1 receptors, D2 receptors, alpha-1 adrenergic receptors, alpha-2 adrenergic receptors, H1 receptors, 5-HT1A receptors, and/or 5-HT2 receptors, pharmaceutical compositions thereof, and methods of use thereof. | 03-18-2010 |
20100087418 | BENZOXAZEPINE DERIVATIVES AND USE THEREOF - Compounds represented by the general formula (I): | 04-08-2010 |
20100087419 | HIV INTEGRASE INHIBITORS - Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: | 04-08-2010 |
20100087420 | Heterotricyclic Metalloprotease Inhibitors - The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors. | 04-08-2010 |
20100105657 | Compounds, Process for their Preparation, Intermediates, Pharmaceutical Compositions and their use in the Treatment of 5-HT6 Mediated Disorders such as Alzheimer's Disease, Cognitive Disorders, Cognitive Impairment Associated with Schizophrenia, Obesity and Parkinson's Disease - The present invention relates to new compounds of formula (I), or salts, solvates or solvated salts thereof, process for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in the treatment of 5-HT6 mediated disorders such as Alzheimer's disease, cognitive disorders, cognitive impairment associated with schizophrenia, obesity and Parkinson's disease. | 04-29-2010 |
20100120742 | REXINOID COMPOUND HAVING ALKOXY GROUP - Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R | 05-13-2010 |
20100130472 | BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF OBESITY AND DIABETES - Provided herein are methods of utilizing bile acid transport inhibitors for the treatment of obesity and diabetes. | 05-27-2010 |
20100160291 | TRICYCLIC SPIRO-OXINDOLE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R | 06-24-2010 |
20100197657 | 2-ARYL OR HETEROARYL INDOLE DERIVATIVES - The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents. | 08-05-2010 |
20100197658 | PHARMACEUTICAL USE OF FUSED 1,2,4-TRIAZOLES - Methods of using fused 1,2,4-triazoles for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) 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, including type 2 diabetes and metabolic syndrome. | 08-05-2010 |
20100216770 | Inhibitors of the Interaction Between MDM2 and P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: | 08-26-2010 |
20100273770 | 1, 2, 4 -OXADIAZOLE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASES - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 10-28-2010 |
20100273771 | OXADIAZOLE DERIVATIVES ACTIVE ON SPHINGOSINE-1-PHOSPHATE (SIP) - The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders. | 10-28-2010 |
20100273772 | Bisaryl Alkynylamides as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5 (MGLUR5) - Disclosed are compounds of Formula I: | 10-28-2010 |
20100292209 | METHODS FOR IDENTIFYING COMPOUNDS THAT MODULATE NEUROTROPHIC FACTOR SIGNALING - The invention relates to screening for compounds and compositions that modulate neurotrophic factor signaling as reflected by modulation of factor-induced neurite outgrowth. The compounds and compositions are useful in the treatment of a variety of disorders. The invention also provides methods for preparing compounds for treatment of such disorders. | 11-18-2010 |
20100292210 | Novel Compounds for A-Beta-Related Pathologies - The present invention relates to novel compounds of formulae I and II and therapeutically acceptable salts thereof, their pharmaceutical compositions processes for making them and their use in therapeutic methods for treatment and/or prevention of various diseases. In particular, the invention relates to compounds which interfere with γ-secretase and/or its substrate and hence modulate the formation of Aβ peptides. | 11-18-2010 |
20100317651 | PYRAZINOOXAZEPINE DERIVATIVES - Provided is a compound having a serotonin 5-HT | 12-16-2010 |
20110034436 | SPIROCYCLIC AMINOQUINOLNES AS GSK-3 INHIBITORS - Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases. In Formula (I): X | 02-10-2011 |
20110046112 | NOVEL BICYCLIC SULFONAMIDE DERIVATIVES WHICH ARE L-CPT1 INHIBITORS - The invention is concerned with novel heterobicyclic derivatives of formula (I) | 02-24-2011 |
20110086843 | Thiazole Derivatives and Use Thereof - The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries. | 04-14-2011 |
20110092482 | METHODS AND COMPOSITIONS - The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management. | 04-21-2011 |
20110112068 | HUMAN IMMUNODEFICIENCY VIRUS PROTEASE INHIBITORS - The described invention relates to novel human immunodeficiency virus protease inhibitors, pharmaceutical compositions containing at least one such inhibitor, methods of preparing such inhibitors, and methods of utilizing such inhibitors to treat HIV and HIV-related disorders. | 05-12-2011 |
20110136783 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 06-09-2011 |
20110152247 | BENZOXAZEPINE COMPOUNDS, THEIR PREPARATION AND USE - The invention provides a novel benzoxazepine compound of the general formula (I): | 06-23-2011 |
20110237567 | TRICYCLIC SPIRO-OXINDOLE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS - This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R | 09-29-2011 |
20110263569 | RYANODINE CHANNEL BINDERS AND USES THEREOF - Increasing the affinity of calstabin-2 for the cardiac calcium channel RyR2 and thereby stabilizing the channel in the closed state has recently been identified as novel mechanism for treating heart failure, particularly ventricular arrhythmias. JTV-519, a 1,4-benzothiazepine derivative, has been shown to stabilize the calstabin2/RyR2 complex. Novel derivatives of JTV-519 that may be useful in treatment or prevention of heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmias are provided. Synthetic methodology and intermediates in the synthesis of the inventive JTV-519 derivatives are also described. | 10-27-2011 |
20110269743 | PHENYLTHIOPHENYLDIHYDROBENZOTHIAZEPINE INHIBITORS OF STORE OPERATED CALCIUM RELEASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. | 11-03-2011 |
20110294784 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I). | 12-01-2011 |
20110306594 | 1,4-BENZOTHIAZEPINE-1-OXIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION UTILIZING THE SAME - Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I]. | 12-15-2011 |
20110312937 | 2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS - This invention relates to compounds of the formula | 12-22-2011 |
20120028957 | Inhibitors Of The Influenza A Virus M2 Proton Channel - Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein. | 02-02-2012 |
20120083483 | INHIBITORS OF HEPATITIS C VIRUS REPLICATION - The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 04-05-2012 |
20120101085 | Compounds And Methods For Modulating Activity Of Calcium Release Channels - The present teachings provide compounds of Formulae I and II: and pharmaceutically acceptable salts, hydrates, complexes, esters, and prodrugs thereof, wherein R | 04-26-2012 |
20120135980 | GAMMA SECRETASE MODULATORS - This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I). | 05-31-2012 |
20120135981 | NOVEL SUBSTITUTED TRIAZOLE AND IMIDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) | 05-31-2012 |
20120149686 | KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein. | 06-14-2012 |
20120184527 | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved. | 07-19-2012 |
20120184528 | 7-ARYL-1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR | 07-19-2012 |
20120202790 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 08-09-2012 |
20120220567 | BENZO-FUSED OXAZEPINE COMPOUNDS AS STEAROYL-COENZYME A DELTA-9 DESATURASE INHIBITORS - The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 08-30-2012 |
20120220568 | Histamine-3 Receptor Antagonists - This invention is directed to a compound of formula I, | 08-30-2012 |
20120225858 | 1,4 THIAZEPINES/SULFONES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to 1,4 Thiazepines/Sulfones of formula I | 09-06-2012 |
20120232057 | CHIRAL FUSED [1,2]IMIDAZO[4,5-c] RING COMPOUNDS - Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X | 09-13-2012 |
20120258953 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer in which activity against PI3fC-alph mTOR, or both contributes to its pathology and/or symptomatology include breast cancer mantle cell lymphoma, renal cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, NPM/ALK-transformed anaplastic large cell lymphoma, diffu large B cell lymphoma, rhabdomyosarcoma, ovarian cancer, endometrial cancer, cervic cancer, non small cell lung carcinoma, small cell lung carcinoma, adenocarcinoma, col cancer, rectal cancer, gastric carcinoma, hepatocellular carcinoma, melanoma, pancreat cancer, prostate carcinoma, thyroid carcinoma, anaplastic large cell lymphoma, hemangiom glioblastoma, or head and neck cancer. | 10-11-2012 |
20120316153 | BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to benzazepine derivatives of the formula (I) | 12-13-2012 |
20130012494 | CYCLOPROPYL-FUSED-1,3-THIAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I | 01-10-2013 |
20130079333 | OXY-CYCLOHEXYL-4H,6H-5-OXA-2,3,10B-TRIAZA-BENZO[E]AZULENES AS V1A ANTAGONISTS - The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula | 03-28-2013 |
20130090328 | COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS DISEASE - The invention relates to the compounds of formula (I): | 04-11-2013 |
20130116237 | [6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: | 05-09-2013 |
20130237524 | SYNTHESIS OF POLYCYCLIC ALKALOIDS - Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use. | 09-12-2013 |
20130261106 | NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF - The present invention relates to compounds of formula (I): | 10-03-2013 |
20130317005 | NON-HYGROSCOPIC SALTS OF 5-HT2C AGONISTS - Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management. | 11-28-2013 |
20140005172 | Benzoxazepines as Inhibitors of PI3K/M TOR and Methods of Their Use and Manufacture | 01-02-2014 |
20140018347 | BENZOXAZEPINES AS INHIBITORS OF mTOR AND METHODS OF THEIR USE AND MANUFACTURE - The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural Formula (I) wherein the variables are as defined herein. | 01-16-2014 |
20140024637 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 01-23-2014 |
20140045822 | KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME - The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: | 02-13-2014 |
20140066431 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens. | 03-06-2014 |
20140073629 | ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS - The present invention relates to compounds of formula (I): | 03-13-2014 |
20140080810 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture - The invention is directed to Compounds of Formula I: (I) and pharmaceutically acceptable salts or solvates thereof, as well as methods of treating using the compounds, methods for screening for inhibitor compounds and methods for identifying treatment regimens. | 03-20-2014 |
20140107100 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture | 04-17-2014 |
20140135313 | 1,4-BENZOTHIAZEPINE-1-OXIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION UTILIZING THE SAME - Provided are novel compound that is useful as a treatment agent or a prophylactic agent for cardiac failure, cardiac failure due to dystelectasis, left ventricular diastolic impairment, angina or cardiac infarct, hypertension, ischemic cardiac disease, and myocardial relaxation impairment recognized in cardiac failure, atrial fibrillation or ventricular arrhythmia, and a pharmaceutical composition containing the same. The invention pertains to a 1,4-benzothiazepine-1-oxide derivative represented by general formula [I] (In the formula, R represents a hydrogen atom or a hydroxyl group.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same [I]. | 05-15-2014 |
20140155381 | COMPOUNDS AND METHODS - The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ. | 06-05-2014 |
20140163009 | HISTONE DEACETYLASE INHIBITORS AND COMPOSITIONS AND METHODS OF USE THEREOF - Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use. | 06-12-2014 |
20140187536 | AGENTS FOR PREVENTING AND TREATING DISORDERS INVOLVING MODULATION OF THE RYANODINE RECEPTORS - Methods for reducing toxicity or side effects caused by administration of a rycal compound for repairing ryanodine receptor channel leaks when treating a disorder in a subject caused by such leaks. These methods are based upon the selection for administration of those rycal compounds having properties including an EC | 07-03-2014 |
20140200208 | 7-ARYL-1,2,4-TRIAZOLO[4,3-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS - The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved. | 07-17-2014 |
20140349998 | PYRROLOPYRIMIDINES AS JANUS KINASE INHIITORS - The instant invention provides compounds of formula I which are JAK3 inhibitors. Specifically, the compounds of formula I are pyrrolo[2,3-d]pyrimidine derivative compounds. The instant invention also provides methods of treating JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer, by administering the pyrrolo[2,3-d]pyrimidine-derivative compounds of formula I. | 11-27-2014 |
20140378436 | Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their use and Manufacture - The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. | 12-25-2014 |
20140378437 | AGENTS FOR TREATING DISORDERS INVOLVING MODULATION OF RYANODINE RECEPTORS - The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders. | 12-25-2014 |
20150025061 | GABAA RECEPTOR ANTAGONISTS AFFECTING GANGLION CELL FUNCTION AND VISUAL ACUITY - The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABA | 01-22-2015 |
20150352124 | NOVEL THIENOPYRIMIDINE DERIVATIVES, PROCESSES FOR THE PREPARATION THEREOF AND THERAPEUTIC USES THEREOF - The present invention relates to therapeutic uses of the compounds of formula (I): | 12-10-2015 |
20160052938 | SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS - The present invention encompasses compounds of formula (I) | 02-25-2016 |
20160068545 | COMPOUNDS THAT INHIBIT MCL-1 PROTEIN - Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, | 03-10-2016 |
20190144457 | BICYCLIC COMPOUNDS AS AUTOTAXIN (ATX) AND LYSOPHOSPHATIDIC ACID (LPA) PRODUCTION INHIBITORS | 05-16-2019 |