Class / Patent application number | Description | Number of patent applications / Date published |
514212060 | Plural ring hetero atoms in the polycyclo ring system | 54 |
20080242658 | Inhibitors of Iap - Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I | 10-02-2008 |
20080255090 | Ceratamines A and B, and Analogues, Syntheses and Pharmaceutical Compositions Thereof - Antimitotic compounds and salts are provided in which the compound has the structure (formula (I)): wherein X and Y are substituted or unsubstituted and are selected from carbon atoms and atoms of groups 15 and 16 of the periodic table; Z is selected from N—R, O and S; U is selected from CR | 10-16-2008 |
20080287422 | Constrained Compounds as CGRP-Receptor Antagonists - The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors. | 11-20-2008 |
20080312211 | Antibacterial Pyrrolopyridines, Pyrrolopyrimidines and Pyrroloazepines-154 - Compounds of formula (I) and their pharmaceutically acceptable salts are described: formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. | 12-18-2008 |
20090005359 | Heterocyclic Compounds Useful as RAF Kinase Inhibitors - The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases. | 01-01-2009 |
20090062255 | TUMOR-TARGETING EVALUATION METHODOLOGY AND COMPOUNDS RELATED THERETO - The invention relates to a method for evaluating a chemotherapeutic potential of a candidate molecule. In evaluating the candidate molecule, the candidate molecule is tested for its ability to inhibit the in vitro growth of a cancer cell; to bind a cellular receptor produced by a cancer cell, wherein said receptor, such as a peripheral benzodiazepine receptor, is produced in a greater amount by said cancer cell than by a normal cell; and to inhibit the activity of at least one protein member of the MAPK pathway. The invention further relates to dibenzodiazepinone analogues and derivatives thereof. | 03-05-2009 |
20090137555 | Compounds and Compositions as Protein Kinase Inhibitors - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases and disorders associated with kinase activity, particularly diseases associated with the activity of CDK1, CDK2, CDK4, CDK5, GSK3β, Bcr-abl, Flt-3, c-Kit, PDGFRβ, Src, Mek1 and CK1. | 05-28-2009 |
20090264411 | FUSED THIOPHENE DERIVATIVES AS MEK INHIBITORS - A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. | 10-22-2009 |
20090281080 | Spirohydantoin Tricyclic CGRP Receptor Antagonists - Compounds of formula I: | 11-12-2009 |
20090281081 | CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR - Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: | 11-12-2009 |
20090281082 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 11-12-2009 |
20090291941 | Tyrosine Kinase Inhibitors - The present invention relates to pyrido[3,2-c]benzazocinone derivatives and related compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 11-26-2009 |
20090306045 | Inhibition of Glycogen Synthase Kinase and Methods of Treating Autoimmune or Immune Inflammatory Disease - The present invention relates to the use of glycogen synthase kinase 3(GSK3) inhibitors, especially inhibitors of GSK-3α, GSK-3β and GSK-3β2, preferably, inhibitors of GSK-3β, in patients having autoimmune diseases and/or immune dysfunction/dysregulation to induce immune tolerance. Inhibition of GSK leads to activation of a pathway of dendritic cell maturation which leads to a dendritic phenotype which attenuates, rather than induces, immune responses. The immune responses and mature dendritic cells produced by the method of the present invention redirect or attenuate the immune response in individuals, thus leading to effective therapies for a number of autoimmune diseases and/or diseases of immune dysfunction/dysregulation (immune inflammatory diseases), including systemic lupus erythematosus (SLE), autoimmune diabetes (type I diabetes mellitus), asthma, rheumatoid arthritis, inflammatory bowel disease, among numerous others. | 12-10-2009 |
20100056495 | DIMERIC IAP INHIBITORS - Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases. | 03-04-2010 |
20100069360 | ORGANIC COMPOUNDS - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: | 03-18-2010 |
20100075952 | PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIES,THE PREPARATION AND THE PHARMCETICAL USE THEEOF - The invention provides new pyrrolo-nitrogenous heterocyclic derivatives represented by formula (I) or their salts, the preparation thereof, pharmaceutical compositions containing such derivatives and the use of such derivatives as therapeutic agents, especially as protein kinase inhibitors, wherein each substituent in formula (I) is same as defined in the description. | 03-25-2010 |
20100130475 | PREVENTIVE OR THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASES - The present invention relates to a pharmaceutical composition for preventing or treating inflammatory bowel diseases, which comprises 7,8-dimethoxy-4(5H),10-dioxo-1H-1,2,3-triazolo[4,5-c][1]benzoazepine, a prodrug thereof, preferably 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzoazepine as a prodrug, or a pharmaceutically acceptable salt thereof. The pharmaceutical composition according to the present invention is effective in the prophylaxis and therapy of the inflammatory bowel diseases and has few side effects. Particularly, the pharmaceutical composition according to the present invention may exhibit strong prophylactic and therapeutic effects even on severe cases having resistance to the conventional therapeutics. | 05-27-2010 |
20100137283 | INHIBITORS OF THE HIV INTEGRASE ENZYME - The present invention is directed to compounds of formula (I), | 06-03-2010 |
20100179126 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 07-15-2010 |
20100190773 | Anti-Cytokine Heterocyclic Compounds - Heterocyclic compounds and analogues thereof and their use as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors. | 07-29-2010 |
20100249102 | 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. | 09-30-2010 |
20100280004 | SMALL MOLECULE CORRECTORS OF DELTAF508 CFTR TRAFFICKING - This invention provides compounds of Formula I. The compounds are correctors of ΔF508 CFTR trafficking. Also provided are uses of compounds of Formula I for treatment, as well as methods of treatment, of cystic fibrosis. | 11-04-2010 |
20110003793 | AZINONE-SUBSTITUTED AZEPINO[b]INDOLE AND PYRIDO-PYRROLO-AZEPINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF - Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention. | 01-06-2011 |
20110034438 | STRUCTURAL MIMETICS OF PROLINE-RICH PEPTIDES AND THE PHARMACEUTICAL USE THEREOF - The invention relates to compounds of general formula (I), which can be used particularly as structural mimetics of proline-rich peptides and are therefore capable of binding PRM binding domains (proline-rich motif binding domains) of proteins. The invention also relates to the use of said compounds as pharmaceutical active agents and the use of these pharmaceutical active agents for treating bacterial diseases, neurodegenerative diseases and tumours. | 02-10-2011 |
20110136788 | THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME - [Problem] The present invention aims to provide an agent for the prophylaxis or treatment of irritable bowel syndrome. | 06-09-2011 |
20110257157 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 10-20-2011 |
20120172348 | STEROL DERIVATIVE - The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; X | 07-05-2012 |
20120178739 | LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 07-12-2012 |
20120184530 | Dimeric IAP Inhibitors - Compounds, compositions, and methods of using such compounds to modulate apoptosis including IAP antagonists are provided herein. Compositions including mimetics of the invention and, optionally, secondary agents, may be used to treat proliferative disorders such as, cancer and autoimmune diseases. | 07-19-2012 |
20120214794 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula I-A or I-B: | 08-23-2012 |
20120258955 | BICYCLIC THIAZOLES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - The present invention relates to novel bicyclic thiazoles which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (“mGluR5”) and which are useful for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which mGluR5 is involved. | 10-11-2012 |
20120270857 | 5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF | 10-25-2012 |
20120295887 | PHARMACEUTICALLY ACCEPTABLE SALTS OF PYRROLO-NITROGENOUS HETEROCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USE THEREOF - Pharmaceutically acceptable salts of pyrrolo-nitrogenous heterocyclic derivatives, preparation method and medical use thereof are disclosed. More specifically, pharmaceutically acceptable salts of (R,Z)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-methylene)-5-(2-hydroxy-3-morpholinyl-4-yl-propyl)-3-methyl-5,6,7,8-tetrahydro-1H-pyrrolo[3,2-c]azepin-4-one presented by formula (I), the preparation method and the use thereof as therapeutic agents, especially as protein kinase inhibitors, are disclosed. | 11-22-2012 |
20120302550 | SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE - The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro- | 11-29-2012 |
20120302551 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 11-29-2012 |
20120309743 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 12-06-2012 |
20120316154 | FUSED TRICYCLIC COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS - The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X | 12-13-2012 |
20130029972 | NOTCH PATHWAY SIGNALING INHIBITOR COMPOUND - The present invention provides a compound, or a pharmaceutically acceptable salt or hydrate, and a pharmaceutical composition containing said compound, or a pharmaceutically acceptable salt or hydrate, useful as a Notch pathway signaling inhibitor for the treatment of cancer. | 01-31-2013 |
20130252943 | BICYCLIC OXAZOLE LACTAMS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS - In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 09-26-2013 |
20130267498 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 10-10-2013 |
20130303518 | Methods of Inhibiting the Catalytic Activity of a Protein Kinase and of Treating a Protein Kinase Related Disorder - The invention provides a method of inhibiting the catalytic activity of a protein kinase comprising contacting said protein kinase with a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, and also provides a method of treating a protein kinase related disorder comprising a step of administering to a patient in need thereof a therapeutically effective amount of the compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, wherein each substituent in formula (I) is same as defined in the description. | 11-14-2013 |
20130310366 | 5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF | 11-21-2013 |
20140194410 | THIOLACTAMS AND USES THEREOF - This invention provides compounds of formula I: | 07-10-2014 |
20140243318 | SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE - The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. | 08-28-2014 |
20140256710 | BROMODOMAIN INHIBITORS - The present invention provides for compounds of formula (I) | 09-11-2014 |
20140275033 | INHIBITORS OF KINASES AND CANCER STEM CELLS, AND METHODS OF PREPARATION AND USE THEREOF - The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions. | 09-18-2014 |
20150148334 | HETEROARYLS AND USES THEREOF - This invention provides compounds of formula I-A or I-B: | 05-28-2015 |
20160010159 | GENE SIGNATURE TO PREDICT HOMOLOGOUS RECOMBINATION (HR) DEFICIENT CANCER | 01-14-2016 |
20160031888 | 3-(ARYL OR HETEROARYL) METHYLENEINDOLIN-2-ONE DERIVATIVES AS INHIBITORS OF CANCER STEM CELL PATHWAY KINASES FOR THE TREATMENT OF CANCER - The invention provides compounds of Formula I as inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, wherein i.a. R | 02-04-2016 |
20160051561 | High Dosage Strength Tablets of Rucaparib - A tablet including high dosage of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one camsylate salt has been disclosed. | 02-25-2016 |
20160068532 | NOVEL COMPOUNDS THAT ARE ERK INHIBITORS - Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). | 03-10-2016 |
20160106754 | USE OF CONDENSED BENZO[B]THIAZINE DERIVATIVES AS CYTOPROTECTANTS - The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters,pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds. | 04-21-2016 |
20170233405 | MAX BINDERS AS MYC MODULATORS AND USES THEREOF | 08-17-2017 |
20190144466 | MAX BINDERS AS MYC MODULATORS AND USES THEREOF | 05-16-2019 |