Entries |
Document | Title | Date |
20080280881 | MORPHOLINYL CONTAINING BENZIMIDAZOLES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula | 11-13-2008 |
20080287419 | APOPTOSIS PROMOTERS - Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed. | 11-20-2008 |
20090105215 | Heterocyclic compounds, methods for the preparation thereof, and uses thereof - The compounds of the present invention are of formula I: | 04-23-2009 |
20090105216 | 3- (AMINOMETHYLIDEN) 2-INDOLINONE DERIVATES AND THEIR USE AS CELL PROLIFERATION INHIBITORS - The present invention encompasses compounds of general formula (1) wherein R | 04-23-2009 |
20090105217 | 2-PHENYL-5-AMINO-1,3,4-OXADIAZOLES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - Novel oxadiazole derivatives of formula (I) having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of neurological, psychiatric disorders and gastrointestinal disorders through modulation of the nicotinic α7 receptor. | 04-23-2009 |
20090124596 | Chemical Compounds 637 - The present invention provides a compound of a formula (I): | 05-14-2009 |
20090137553 | Thiazepine Oxazolidinones as Antibacterial Agents - The present invention relates to a new class of oxazolidinone derivatives, to their use as antibacterial agents, to pharmaceutical compositions containing these compounds and to methods for their preparation. | 05-28-2009 |
20090143357 | HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHK1 - Substituted urea compounds useful in the treatment of diseases and conditions related to DNA damage or lesions in DNA replication are disclosed. Methods of making the compounds, and their use as therapeutic agents, for example, in treating cancer and other diseases characterized by defects in DNA replication, chromosome segregation, or cell division, also are disclosed. | 06-04-2009 |
20090143358 | INHIBITORS OF ION CHANNELS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 06-04-2009 |
20090197866 | PYRAZOLYLBENZIMIDAZOLE DERIVATIVES, COMPOSITIONS CONTAINING THEM AND USE THEREOF - The disclosure relates to compounds of formula (I): | 08-06-2009 |
20090203666 | COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I. | 08-13-2009 |
20090203667 | PENTADIENAMIDE DERIVATIVES - The present invention provides a pentadienamide derivative represented by the formula (I): | 08-13-2009 |
20090203668 | TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS - Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: | 08-13-2009 |
20090264409 | Bicyclic Heterocyclic p-38 Kinase Inhibitors - Provided are bicyclic heterocycle-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders. | 10-22-2009 |
20090270366 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-29-2009 |
20090281079 | Substituted 4-Amino-Pyrrolotriazine Derivatives Useful for Treating Hyper-Proliferative Disorders and Diseases Associated With Angiogenesis - This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis. | 11-12-2009 |
20090291940 | AMINOPYRROLIDINE COMPOUND - Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC | 11-26-2009 |
20090306044 | QUINAZOLINE DERIVATIVES FOR THE TREATMENT OF CANCER DISEASES - The present invention relates to the use of quinazolines of formula (I), wherein the groups R | 12-10-2009 |
20100009964 | Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 01-14-2010 |
20100016285 | HETEROCYCLIDENE-N-(ARYL) ACETAMIDE DERIVATIVE - The blow-described formula (I)
| 01-21-2010 |
20100022512 | COMPOSITIONS OF CHK1 INHIBITORS AND CYCLODEXTRIN - Compositions containing at least one Chk1 inhibitor and at lease one cyclodextrin are disclosed. Also disclosed are methods of treating a cancer or potentiating a cancer treatment with a composition comprising at least one Chk1 inhibitor and at least one cyclodextrin. | 01-28-2010 |
20100022513 | ORGANIC COMPOUNDS - The invention relates to compounds of formula (I): | 01-28-2010 |
20100041638 | Chemical Compounds 293 - The present invention provides a compound of a formula (I): | 02-18-2010 |
20100056494 | PURINE COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS FOR THE TREATMENT OF PLASMODIUM RELATED DISEASES - The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria. | 03-04-2010 |
20100069357 | PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR). | 03-18-2010 |
20100069358 | USE OF 7-AZAINDOLES IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them. | 03-18-2010 |
20100075951 | Heteroaryls and uses thereof - This invention provides compounds of formula I: | 03-25-2010 |
20100099662 | HYDRAZONE DERIVATIVE - A hydrazone derivative of formula [I]: | 04-22-2010 |
20100130473 | COMPOUNDS - Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where R | 05-27-2010 |
20100130474 | ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS - The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory systems. | 05-27-2010 |
20100152162 | THERAPEUTIC AND/OR PREVENTIVE AGENTS FOR A SLEEP DISORDER - It is intended to provide an agent for treating and/or preventing sleep disorder containing as an active ingredient a thiazole derivative represented by the general formula (I) (in the formula, R | 06-17-2010 |
20100160292 | Kinase Inhibitors, and Methods of Using and Identifying Kinase Inhibitors - Methods of inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, methods of treating patients by inhibiting BTK activity by inhibiting phosphorylation of Y551 of BTK, chemical entities that bind to BTK and inhibited complexes are provided. | 06-24-2010 |
20100168080 | NOVEL COMPOUNDS USEFUL AS CC CHEMOKINE RECEPTOR LIGANDS - The present invention relates to novel morpholine, oxazapane and piperidine derivatives that act as ligands for CC chemokine receptors, such as CCR1. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 07-01-2010 |
20100173891 | HETEROCYCLIC COMPOUNDS, METHODS FOR THE PREPARATION THEREOF, AND USES THEREOF - The compounds of the present invention are of formula I: | 07-08-2010 |
20100179125 | SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients. | 07-15-2010 |
20100184740 | SUBSTITUTED OXAZOLIDINONES AND THEIR USE - The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders. | 07-22-2010 |
20100197659 | BIPHENYLCARBOXAMIDE DERIVATIVES AS HEDGEHOD PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I. | 08-05-2010 |
20100204203 | Chemical Compounds 637: Pyridopyrimidinediones as PDE4 Inhibitors - The present invention provides a compound of a formula (I), 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 PDE4 mediated disease state. | 08-12-2010 |
20100286121 | Water-Immiscible Materials as Vehicles for Drug Delivery - A pharmaceutical composition includes at least one pharmaceutical component and at least one water-immiscible material. The pharmaceutical component is more soluble in the water-immiscible material than in water. The pharmaceutical composition is suitable for ocular administration. | 11-11-2010 |
20100305096 | BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE - Formula I (Ia and Ib) compounds wherein (i) X | 12-02-2010 |
20100305097 | N-BENZYL-4-METHYLENEAMINO-3-HYDROXY-2-PYRIDONES - Compounds of Formula (I) | 12-02-2010 |
20100324021 | (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES - The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I | 12-23-2010 |
20110092484 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR CEREBRAL ANEURYSM - [Problems] To provide a medicament which is effective for treatment and prophylaxis of cerebral aneurysms | 04-21-2011 |
20110098275 | 5-ALKYNYL-PYRIDINES - The present invention encompasses compounds of general formula (1) | 04-28-2011 |
20110098276 | OXYCARBAMOYL COMPOUNDS AND THE USE THEREOF - The invention relates to oxycarbamoyl compounds of Formula I: | 04-28-2011 |
20110112070 | 4-CARBOXAMIDE INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF P13-KINASES - The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity. | 05-12-2011 |
20110118233 | Certain Substituted Amides, Method of Making, and Method of Use Thereof - Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described. | 05-19-2011 |
20110144090 | COMPOUNDS AND METHODS OF USE THEREOF - Indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds. | 06-16-2011 |
20110172207 | SUBSTITUTED PYRAZOLAMIDES AND THEIR USE - The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals. | 07-14-2011 |
20110178062 | INDOLE AND BENZOTHIOPHENE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR - Certain substituted indole and benzothiophene compounds are histamine H | 07-21-2011 |
20110178063 | BENZPYRAZOL DERIVATIVES AS INHIBITORS OF PI3 KINASES - The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity. | 07-21-2011 |
20110195951 | DIAZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE - The invention relates to diazaindole derivatives represented by the general formula (I): where A, E, G, R | 08-11-2011 |
20110207715 | Disubstituted Azepan Orexin Receptor Antagonists - The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 08-25-2011 |
20110245232 | NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS I - The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I | 10-06-2011 |
20110251176 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 10-13-2011 |
20110251177 | 2, 4-PYRIMIDINEDIAMINE COMPOUNDS AND PRODRUGS THEREOF AND THEIR USES - The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I) and (II): | 10-13-2011 |
20110275612 | ALPHA-SUBSTITUTED N-SULFONYL GYLCINE AMIDES ANTAGONISTS OF CCR10, COMPOSITIONS CONTAINING THE SAME AND METHODS FOR USING THEM - Disclosed is a compound of formula (I). Wherein R | 11-10-2011 |
20110312939 | NEW CHEMICAL COMPOUNDS - The present invention relates to new compounds of general formula (I), wherein the groups R | 12-22-2011 |
20120028958 | 5-ALKYNYL-PYRIMIDINES - The present invention encompasses compounds of general formula (1) | 02-02-2012 |
20120046270 | PYRIMIDO [5,4-D] PYRIMIDINE DERIVATIVES FOR THE INHIBITION OF TYROSINE KINASES - The present invention encompasses compounds of general formula (1), wherein the groups R | 02-23-2012 |
20120077801 | Chemical Compounds 637 - The present invention provides a compound of a formula (I): | 03-29-2012 |
20120129837 | Derivatives of Fluorene, Anthracene, Xanthene, Dibenzosuberone and Acridine and Uses Thereof - Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents. | 05-24-2012 |
20120149687 | HETEROCYCLIC COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-14-2012 |
20120157442 | HETEROARYL BTK INHIBITORS - The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same. | 06-21-2012 |
20120157443 | BRUTON'S TYROSINE KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same. | 06-21-2012 |
20120165313 | PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE - Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR). | 06-28-2012 |
20120165314 | SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS - This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis. | 06-28-2012 |
20120196849 | COMPOUNDS AND COMPOSITIONS AS HEDGEHOG PATHWAY MODULATORS - The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I. | 08-02-2012 |
20120225859 | PYRIMIDINE DERIVATIVES USED AS PI-3 KINASE INHIBITORS - Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases. | 09-06-2012 |
20120232058 | SUBSTITUTED PYRIDINE DERIVATIVES AND THEIR MEDICAL USE - The present application relates to novel substituted pyridine derivatives, to their use in therapy, to pharmaceutical compositions comprising the derivatives, to the use of said derivatives in the manufacture of a medicament, and to therapeutic methods comprising the administration of the derivatives. The present derivatives are useful for treating a disorder responsive to activation of K | 09-13-2012 |
20120238547 | 2, 3, 6 - TRIAMINO SUBSTITUTED PYRIDINES AS KV7 (KCNQ) CHANNEL MODULATORS - The present application relates to novel substituted aminopyridine derivatives, to their use in therapy, to pharmaceutical compositions comprising the derivatives, to the use of said derivatives in the manufacture of a medicament, and to therapeutic methods comprising the administration of the derivatives. The present derivatives are useful for treating a disorder responsive to activation of K | 09-20-2012 |
20120238548 | 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention relates to 1,4-Oxazepines of formula I | 09-20-2012 |
20120277212 | Novel Oxime Derivatives and Their Use As Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4. | 11-01-2012 |
20120302549 | SPIRO-[1,3]-OXAZINES AND SPIRO-[1,4]-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - The present invention provides spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines of formula I | 11-29-2012 |
20120309742 | USE OF METABOTROPIC GLUTAMATE RECEPTORS - The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction. | 12-06-2012 |
20130018041 | PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES - This invention is directed to compounds of formula (I): | 01-17-2013 |
20130023519 | 5-ALKYNYL-PYRIDINES - 5-alkynyl-pyridine of general formula (I) | 01-24-2013 |
20130029970 | CB Receptor Agonists - The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders. | 01-31-2013 |
20130029971 | CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula (I): | 01-31-2013 |
20130040936 | 1,4-OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - This invention relates to compounds of the formula | 02-14-2013 |
20130072471 | Inhibitors of Ion Channels - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 03-21-2013 |
20130102587 | New Enzyme Inhibitor Compounds - Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth. | 04-25-2013 |
20130150343 | KINASE INHIBITORS - Compounds of formula (I) and pharmaceutically acceptable salts thereof: | 06-13-2013 |
20130150344 | HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula (1): | 06-13-2013 |
20130196975 | 5-ALKYNYL-PYRIDINES - The present invention encompasses compounds of general formula (1) | 08-01-2013 |
20130203732 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 08-08-2013 |
20130245005 | QUINOLIN-4 (1H) -ONE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASES - Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity. | 09-19-2013 |
20140031339 | INHIBITORS OF LEUKOTRIENE PRODUCTION - The present invention relates to compounds of formula (I): | 01-30-2014 |
20140031340 | 5-Amino-Oxazepine and 5-Amino-Thiazepane Compounds as Beta Secretase Antagonists and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I); wherein variables A | 01-30-2014 |
20140045823 | N-CYCLOPROPYL-N-PIPERIDINYL-AMIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF - The present invention relates to compounds of general formula I, | 02-13-2014 |
20140057898 | COMBINATIONS FOR THE TREATMENT OF DISEASES INVOLVING CELL PROLIFERATION, MIGRATION OR APOPTOSIS OF MYELOMA CELLS, OR ANGIOGENESIS - The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations. | 02-27-2014 |
20140088084 | OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS - The invention relates to novel heterocyclic compounds of the formula | 03-27-2014 |
20140094448 | PYRAZOLOPYRIMIDINES AND RELATED HETEROCYCLES AS CK2 INHIBITORS - The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and have the following general formula: | 04-03-2014 |
20140121200 | SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS - Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R | 05-01-2014 |
20140163010 | PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS, THEIR PREPARATION AND USE AS SIGMA LIGANDS - New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments. | 06-12-2014 |
20140171414 | NOVEL COMPOUNDS - Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated. | 06-19-2014 |
20140179680 | Substituted Imidazopyridines as HDM2 Inhibitors - The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 06-26-2014 |
20140206668 | PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO - This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) | 07-24-2014 |
20140249135 | 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. | 09-04-2014 |
20140296208 | KINASE INHIBITORS - There are provided compounds of formula I, | 10-02-2014 |
20140323469 | 1,4 OXAZEPINES AS BACE1 AND/OR BACE2 INHIBITORS - This invention relates to compounds of the formula | 10-30-2014 |
20140323470 | KINASE INHIBITORS - Compounds of formula (I) and pharmaceutically acceptable salts thereof: | 10-30-2014 |
20140357618 | SUBSTITUTED IMIDAZOPYRIDINES AS HDM2 INHIBITORS - The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. | 12-04-2014 |
20140378438 | MORPHOLINO SUBSTITUTED UREA OR CARBAMATE DERIVATIVES AS MTOR INHIBITORS - The invention relates to compounds of formula (I) | 12-25-2014 |
20150018338 | OXAZINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS - The invention relates to novel heterocyclic compounds of the formula | 01-15-2015 |
20150031678 | SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINES, THEIR PREPARATION AND USE AS MEDICAMENTS - The present invention relates to new substituted pyrazolo[1,5-a]pyridine having a great affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments. | 01-29-2015 |
20150080375 | KINASE INHIBITORS - Compounds of formula (I) and pharmaceutically acceptable salts thereof: | 03-19-2015 |
20150141406 | HETEROCYCLIC COMPOUND - The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. | 05-21-2015 |
20150313873 | Derivatives of Fluorene, Anthracene, Xanthene, Dibenzosuberone and Acridine and Uses Thereof - Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents. | 11-05-2015 |
20150315183 | NOVEL OCTAHYDROPYRIDOQUINAZOLINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USES FOR SAID DERIAVATIVE AND COMPOSITION - [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D | 11-05-2015 |
20150315190 | PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS, THEIR PREPARATION AND USE AS SIGMA LIGANDS - New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments. | 11-05-2015 |
20150344475 | KINASE INHIBITORS - Compounds of formula (I) and pharmaceutically acceptable salts thereof: | 12-03-2015 |
20150353510 | 1,2,3-TRIAZOLE-4-AMINE DERIVATIVES FOR THE TREATMENT OF SIGMA RECEPTOR RELATED DISEASES AND DISORDERS - The present invention relates to new 1,2,3-triazole-amine derivatives, having affinity for sigma receptors, especially sigma-1 receptor, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments for the treatment of sigma receptor related diseases and disorders. | 12-10-2015 |
20150353537 | BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY - The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 12-10-2015 |
20160016966 | FUROPYRIDINES AS BROMODOMAIN INHIBITORS - The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy. | 01-21-2016 |
20160046622 | IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS - The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumour growth. | 02-18-2016 |
20160046651 | TREATMENT OF MALARIA USING INHIBITORS OF THE ISPD ENZYME IN THE NON-MEVALONATE PATHWAY - Compounds are disclosed that inhibit the methylerythritol cytidyltransferase (IspD) enzyme in the non-mevalonate pathway (MEP pathway), which is present in many organisms including the | 02-18-2016 |
20160075709 | PYRAZINO[1,2-a]INDOLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS - The invention refers to compounds of general formula (I) | 03-17-2016 |
20160075719 | THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES - Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. | 03-17-2016 |
20160108040 | DERIVATIVES OF [1, 2, 4] TRIAZOLO [4, 3 - A] PYRIDINE AS P38 - MAP KINASE INHIBITORS - This invention relates to compounds selected in the group consisting of compounds of formula (Ia) to (Id) and compositions, that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract. | 04-21-2016 |
20160176896 | ERK INHIBITORS | 06-23-2016 |
20160251362 | NOVEL COMPOUNDS | 09-01-2016 |
20160376281 | BRUTON'S TYROSINE KINASE INHIBITORS - The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same. | 12-29-2016 |
20180022742 | AUTOTAXIN INHIBITORS | 01-25-2018 |
20180022744 | BENZOTHIAZOLE AND BENZISOTHIAZOLE-SUBSTITUTED COMPOUNDS AS MGLUR4 ALLOSTERIC POTENTIATORS, COMPOSITIONS, AND METHODS OF TREATING NEUROLOGICAL DYSFUNCTION | 01-25-2018 |
20220133737 | CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR TREATING BRONCHIECTASIS - The present disclosure relates to methods for treating bronchiectasis, for example, non-cystic fibrosis bronchiectasis with compositions comprising an effective amount of certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds of Formula (I), including pharmaceutically acceptable salts thereof, | 05-05-2022 |