Entries |
Document | Title | Date |
20080207635 | Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders - The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use. | 08-28-2008 |
20080214563 | Benzimidazole Thiophene Compounds As Plk Modulators - The present invention provides 5-heteroaryl substituted benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. | 09-04-2008 |
20080242675 | Indolylmaleimide Derivatives as Pkc Inhibitors - This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation. | 10-02-2008 |
20080261995 | Pharmaceutical Combination of a Pde-5 Inhibitor and a 5-Alpha Reductase Inhibitor - This invention relates to the combined use of a PDE5 inhibitor and a 5-alpha reductase antagonist in the treatment of lower urinary tract symptoms (LUTS), such as urgency, frequency, nocturia and urge incontinence. | 10-23-2008 |
20080269244 | Kinase Inhibitors - The present invention provides kinase inhibitors of Formula (I). Wherein R | 10-30-2008 |
20080306086 | PROLINAMIDE DERIVATIVES AS NK3 ANTAGONISTS - The present invention relates to a compound of formula I | 12-11-2008 |
20080312253 | Pharmaceutical compositions containing pyrazole derivatives for treating as serotonin antagonist - The present invention relates to a pharmaceutical composition containing a pyrazole derivative as an active ingredient, which has antagonistic activity against serotonin 5-HT | 12-18-2008 |
20090005397 | Substituted Oxindol Derivatives and Medicaments Containing the Same - The invention relates to novel oxindol derivatives of general formula (1) wherein the substituents A, B, R | 01-01-2009 |
20090036466 | AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION - The present invention concerns amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula | 02-05-2009 |
20090111830 | SUBSTITUTED ISOINDOLONES AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS - The present invention is directed to compounds of formula I: | 04-30-2009 |
20090149470 | Novel aminopyridine derivatives having aurora a selective inhibitory action - The present invention relates to a compound represented by the general formula (I): | 06-11-2009 |
20090186904 | Substituted Oxindole Derivatives, Medicaments Containing the Latter and Use Thereof - The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R | 07-23-2009 |
20090209552 | Organic Compounds - There are provided according to the invention compounds of formula (I) | 08-20-2009 |
20090258883 | 1H-Indole-Pyridinecarboxamide and 1H-Indole-Piperidinecarboxamide Compounds - Compounds of formula (I): | 10-15-2009 |
20090286804 | METABOLITES OF 1-[6-(1-ETHYL-1-HYDROXY-PROPYL)-PYRIDIN-3-YL]-3-[2-(4-METHYL-PIPERAZIN-1-- YL)-BENZYL]-PYRROLIDIN-2-ONE AS SERATONIN RECEPTOR ANTAGONISTS - Metabolites of 1-[6-(1-ethyl-1-hydroxy-propyl)-pyridin-3-yl]-3-[2-(4-methyl-piperazin-1-yl)-benzyl]-pyrrolidin-2-one, and use of same. Metabolites of the present invention are as shown in Formula (II): (II) wherein R | 11-19-2009 |
20090291965 | Histone Deacetylase Inhibitors With Aryl-Pyrazolyl-Motifs - The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo. | 11-26-2009 |
20090318467 | NOVEL HETEROARYL CARBOXAMIDE DERIVATIVES - The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), | 12-24-2009 |
20100004263 | MTP INHIBITING ARYL PIPERIDINES OR PEPERAZINES SUBSTITUTED WITH5-MEMBERED HETEROCYCLES - The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. | 01-07-2010 |
20100035895 | 2-AMINOCARBONYL-PYRIDINE DERIVATIVES - The present invention relates to 2-aminocarbonyl-pyridine derivatives of Formula (I) and their use as P2Y | 02-11-2010 |
20100113475 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 05-06-2010 |
20100144752 | Heterocyclylamide-substituted thiazoles, pyrroles and thiophenes - The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and to processes for preparing them, to their use for the treatment and/or prophylaxis of diseases, and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, particularly for use as antiviral agents, especially against cytomegaloviruses. | 06-10-2010 |
20100152200 | ALPHAVIRUS INHIBITORS AND USES THEREOF - The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as inhibitors of alphaviruses. | 06-17-2010 |
20100190802 | CARBOXAMIDE COMPOUNDS AND METHODS FOR USING THE SAME - Disclosed are carboxamide compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 07-29-2010 |
20100234394 | SUBSTITUTED BENZIMIDAZOLES AND METHODS OF THEIR USE - New substituted benzimidazole 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. | 09-16-2010 |
20100261731 | Method for Treating a Disease, Disorder or Adverse Effect Caused by an Elevated Serum Concentration of an UGT1A1 Substrate - The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate comprising the step of administering to a subject an effective amount of ritonavir. In particular, the present invention is directed to a method of treating unconjugated hyperbilirubinemia by UGT1A1 induction comprising the step of administering to a subject an effective amount of ritonavir. | 10-14-2010 |
20100286165 | SUBSTITUTED OXINDOLE COMPOUNDS - The present invention relates to compounds of the general formula (I) | 11-11-2010 |
20100305137 | PIPERAZINE DERIVATIVES AND METHODS OF USE - The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility. | 12-02-2010 |
20110015206 | METHOD OF STABILIZING LIPID-RICH PLAQUE AND METHOD OF PREVENTING RUPTURE THEREOF - A method of stabilizing lipid-rich plaques and method of preventing the rupture thereof, characterized in that an effective amount of 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, its acid adduct salt or a hydrate thereof is administered to patients with lipid-rich plaques. Prevention of plaque rupture and stabilization of plaques can be attained by reducing the occupancy of macrophages in lipid-rich plaques being unstable and tending to rupture among plaques being a lesion from a seat of atherosclerosis and simultaneously increasing the occupancy of collagen therein. | 01-20-2011 |
20110046152 | Amide Compounds, Preparation Methods and Uses Thereof - Amide compounds, preparation methods and uses thereof. The structure of the compounds is represented as the general formula (I), in which the definitions of substituents are illuminated as description. | 02-24-2011 |
20110059983 | USE OF SUBSTITUTED OXINDOLE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF PAIN - The present invention relates to the use of substituted oxindole derivatives of formula I as defined in the claims and description for the treatment or prophylaxis of pain. | 03-10-2011 |
20110065720 | CARBAMATE-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT DISEASES - The present invention relates to novel carbamate-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. | 03-17-2011 |
20110077253 | AMIDOMETHYL-SUBSTITUTED OXINDOLE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES - The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. | 03-31-2011 |
20110092516 | 5-HALOGEN-SUBSTITUTED OXINDOLE DERIVATIVES AND USE THEREOF FOR TREATING VASOPRESSIN-DEPENDENT DISEASES - The present invention relates to novel 5-halogen-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. | 04-21-2011 |
20110118280 | INDOL-2-ONE DERIVATIVES DISUBSTITUTED IN THE 3-POSITION, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The present invention relates to 3-disubstituted indol-2-one derivatives, to their preparation and to their therapeutic application. | 05-19-2011 |
20110124658 | SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS - The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. | 05-26-2011 |
20110172244 | COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY - The invention provides compounds, of Formula I: pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119. | 07-14-2011 |
20110207742 | METHOD FOR REDUCTION, STABILIZATION AND PREVENTION OF RUPTURE OF LIPID RICH PLAQUE - There is to provide is an agent for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion comprising an effective amount of 2-[4-[2-(benzimidazole-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-p yridyl]acetamide (hereinafter, referred to as compound 1), its pharmaceutically acceptable salt or a hydrate thereof and Pitavastatin, and a pharmaceutically acceptable carrier, wherein the agent is intended to be simultaneously administered, or separately administered with interval of time to a patient in need thereof There is also to provide a method for reduction of a lipid rich plaque, stabilization of a lipid rich plaque and/or prevention of rupture of a lipid rich plaque in an atherosclerotic lesion, comprising simultaneously administering, or separately administering with interval of time an effective amount of the compound 1, its pharmaceutically acceptable salt or a hydrate thereof and an effective amount of Pitavastatin to a patient in need thereof. | 08-25-2011 |
20110207743 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 08-25-2011 |
20110245269 | Inhibitors of Advanced Glycation End Products - The present invention provides compounds of the formula, | 10-06-2011 |
20110257194 | SUBSTITUTED OXINDOL DERIVATIVES AND MEDICAMENTS CONTAINING THE SAME - The present invention relates to novel oxindole derivatives of the general formula (I), | 10-20-2011 |
20110269774 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 11-03-2011 |
20110312969 | COMPOUNDS FOR TREATING CANCER - Compounds of general formula (I): wherein R | 12-22-2011 |
20120022078 | ARYL INDOLE DERIVATIVES - A novel aryl indole derivative is provided that is effective as a preventive or remedy for various diseases. A compound represented by a formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R | 01-26-2012 |
20120046301 | Substituted Cyclic Carboxamide and Urea Derivatives as Ligands of the Vanilloid Receptor - Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and/or inhibition of pain and other conditions mediated by the vanilloid receptor 1. | 02-23-2012 |
20120088778 | AZOLE DERIVATIVES AND FUSED BICYCLIC AZOLE DERIVATIVES AS THERAPEUTIC AGENTS - This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis. | 04-12-2012 |
20120157471 | BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 06-21-2012 |
20120208826 | HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS - The present invention relates to heterocyclic amide derivatives of Formula (I): Formula (I) wherein the variables are as defined in the specification. The present invention further relates to compositions comprising said heterocyclic amide derivatives of formula (I) and methods for using said heterocyclic amide derivatives of formula (I) for treating or preventing a disease or disorder related to the activity of a protein kinase, in particular, a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal infection. | 08-16-2012 |
20120289517 | SOLID PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION - The present invention relates to a solid pharmaceutical composition for oral administration, containing the following components (A) and (B): (A) | 11-15-2012 |
20120322808 | Alpha 4 Beta 2 NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to novel α | 12-20-2012 |
20120322809 | SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS - The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. | 12-20-2012 |
20130012521 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 01-10-2013 |
20130035344 | PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION - The present invention relates to a solid pharmaceutical composition for oral administration, containing the following components (A) and (B): 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide (compound a) or an acid addition salt thereof, and (B) citric acid. An improvement is achieved in the dissolubility of the compound a, which is useful as a therapeutic agent for hypercholesterolemia, arteriosclerosis, and the like. | 02-07-2013 |
20130040961 | OLIGOMER MODIFIED DIAROMATIC SUBSTITUTED COMPOUNDS - Disclosed are compounds comprising diaromatic substituted compound residues, namely the anti-viral (anti-HIV) drug delavirdine, covalently attached via a linkage to water-soluble, non-peptidic oligomers, specifically to poly(ethylene glycol) PEG) oligomers. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds. | 02-14-2013 |
20130040962 | P38 MAP Kinase Inhibitors - There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis. | 02-14-2013 |
20130053397 | INDOLES - Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful in treating cancer. | 02-28-2013 |
20130123273 | METHODS OF TARGETING PTEN MUTANT DISEASES AND COMPOSITIONS THEREFOR - Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present. | 05-16-2013 |
20130131078 | Carboxamide Compounds And Methods For Using The Same - Disclosed are carboxamide compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 05-23-2013 |
20130178480 | Inhibitors of Advanced Glycation End Products - The present invention provides compounds of the formula, | 07-11-2013 |
20130245038 | Method For Selecting Or Identifying A Subject For V1B Antagonist Therapy - Provided herein is a method for detecting an HPA axis function marker in a biological sample. The method may be used to determine whether a patient is a suitable candidate for treatment with a V | 09-19-2013 |
20140011816 | NOVEL SUBSTITUTED TRIAZOLYL PIPERAZINE AND TRIAZOLYL PIPERIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) | 01-09-2014 |
20140018370 | APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 01-16-2014 |
20140107131 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 04-17-2014 |
20140155410 | PYRAZOLYLAMINOPYRIDINES AS INHIBITORS OF FAK - The present invention relates to a compound of formula (I): | 06-05-2014 |
20140194440 | 5,6-DISUBSTITUTED OXINDOLE-DERIVATIVES AND USE THEREOF FOR TREATING VASOPRESSIN-DEPENDENT DISEASES - The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament. | 07-10-2014 |
20140194441 | 3-(BENZOIMIDAZOL-2-YL)-INDAZOLE INHIBITORS OF THE WNT SIGNALING PATHWAY AND THERAPEUTIC USES THEREOF - Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 07-10-2014 |
20140221390 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS - Provided is a compound useful in the prevention and treatment of non-alcoholic steatohepatitis. A prophylactic and/or therapeutic agent for non-alcoholic steatohepatitis which contains, as the active ingredient, 2-[4-[2-(benzimidazol-2-ylthio)ethyl]piperazin-1-yl]-N-[2,4-bis(methylthio)-6-methyl-3-pyridyl]acetamide, an acid-addition salt thereof, or a solvate of the same. | 08-07-2014 |
20140256739 | METHOD OF TREATMENT - The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof. | 09-11-2014 |
20140275110 | AMIDOMETHYL-SUBSTITUTED OXINDOLE DERIVATIVES AND THE USE THEREOF FOR THE TREATMENT OF VASOPRESSIN-DEPENDENT ILLNESSES - The present invention relates to novel amidomethyl-substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-dependent disorders. | 09-18-2014 |
20140296252 | 1,2,4-TRIAZOL-5-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 10-02-2014 |
20140315917 | IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 10-23-2014 |
20140315918 | Oxindole Derivatives Carrying An Oxetane Substituent and Use Thereof For Treating Vassopressin-Related Diseases - The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders. | 10-23-2014 |
20140336201 | BIPYRIDYL DERIVATIVES - The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. | 11-13-2014 |
20140343074 | Oxindole Derivatives Carrying An Oxetane Substituent and use thereof for Treating Vasopressine-Related Diseases - The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders. | 11-20-2014 |
20140343075 | PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS - The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers. | 11-20-2014 |
20140378470 | METHODS OF TREATING CANCER - This invention relates to methods of treating cancer in a subject such as a human and determining at least one of the following in a sample from the subject, such as a human: (a) the presence or absence of a mutation at the alanine 677 (A677) residue in EZH2; or (b) the presence or absence of a mutation at the tyrosine 641 (Y641) residue in EZH2; or (c) the presence or absence of an increased level of H3K27me3 as compared to a control, and administering to said human an effective amount of an EZH2 inhibitor or a pharmaceutically acceptable salt thereof if at least one of the A677 mutation, Y641 mutation, or increased level of H3K27me3 is present in the sample. | 12-25-2014 |
20150051219 | TREATMENT OF ORGANOPHOSPHATE EXPOSURE WITH TETRAHYDROINDOLONE ARYLPIPERAZINE COMPOUNDS - A method of treating exposure to organophosphate agents through the use of compounds comprising tetrahydroindolone and arylpiperazine moieties. | 02-19-2015 |
20150141436 | INDOLES - Herein are disclosed indoles of formula (I) | 05-21-2015 |
20150315197 | SUBSTITUTED 4-PHENYLPIPERIDINES, THEIR PREPARATION AND USE - The present invention provides a compound having the structure: | 11-05-2015 |
20150344459 | 1,4-PYRIDONE BICYCLIC HETEROARYL COMPOUNDS - The present invention relates to 1,4-pyridone bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes. | 12-03-2015 |
20150352110 | SUBSTITUTED OXINDOLE DERIVATIVES AND THEIR USE AS VASOPRESSIN RECEPTOR LIGANDS - The present invention relates to novel oxindole derivatives of the general formula (I) to medicaments comprising them and to their use for the prophylaxis and/or treatment of diseases vasopressin dependent. | 12-10-2015 |
20160046619 | IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Described are compounds of Formula I | 02-18-2016 |
20160074394 | METHOD OF TREATMENT - The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof. | 03-17-2016 |
20160095858 | Modulators of Cystic Fibrosis Transmembrane Conductance Regulator - The present invention features a compound of formula I: | 04-07-2016 |
20160122302 | Mammalian and Bacterial Nitric Oxide Synthase Inhibitors - Compounds and related methods for inhibition of mammalian and bacterial nitric oxide synthase. | 05-05-2016 |
20160130263 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 05-12-2016 |
20160143904 | OLIGOMER MODIFIED DIAROMATIC SUBSTITUTED COMPOUNDS - The invention relates to (among other things) oligomer modified diaromatic substituted compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over non-oligomer modified diaromatic substituted compounds. | 05-26-2016 |
20160152604 | SUBSTITUTED 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS | 06-02-2016 |
20160159772 | ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 06-09-2016 |
20160168135 | OXINDOLE DERIVATIVES CARRYING AN OXETANE SUBSTITUENT ANDUSE THEREOF FOR TREATING VASOPRESSIN-RELATED DISEASES | 06-16-2016 |
20220135541 | CRYSTALLINE FORMS OF PIPERAZINE-1,4-DIYLBIS((6-(1H-BENZO[D]IMIDAZO-2-YL)PYRIDIN-2YL)METHANONE) - Crystalline forms of piperazine-1,4-diylbis((6-(1H-benzo[d]imidazo-2-yl)pyridine-2-yl)methanone), compositions containing one or more crystalline forms of piperazine-1,4-diylbis((6-(1H-benzo[d]imidazo-2-yl)pyridine-2-yl)methanone), processes for preparing crystalline forms of piperazine-1,4-diylbis((6-(1H-benzo[d]imidazo-2-yl)pyridine-2-yl)methanone), and methods of using crystalline forms of piperazine-1,4-diylbis((6-(1H-benzo[d]imidazo-2-yl)pyridine-2-yl)methanone). | 05-05-2022 |