Class / Patent application number | Description | Number of patent applications / Date published |
540575000 | The nitrogens are in the 1,4-positions of the hetero ring | 61 |
20080249301 | Regioselective Process for Preparing Benzimidazole Thiophenes - The present invention provides a process for preparing benzimidazole thiophene compounds of formula (I). | 10-09-2008 |
20080306258 | Cyclopropane 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 cyclopropane compound of formula (1): | 12-11-2008 |
20090043091 | ATM INHIBITORS - A compound of formula I: | 02-12-2009 |
20090143575 | VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS - Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders. | 06-04-2009 |
20090264646 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-22-2009 |
20090264647 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-22-2009 |
20090264648 | SYNTHESIS OF PYRAZOLES - 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 system. | 10-22-2009 |
20090270613 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-29-2009 |
20090275748 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 11-05-2009 |
20090281307 | Benzoimidazole compounds - Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 11-12-2009 |
20090286974 | Derivative having ppar agonistic activity - A compound of the formula (I): | 11-19-2009 |
20090318684 | ROCK INHIBITORS AND USES THEREOF - The subject invention concerns compositions and methods for blocking cancer cell growth or proliferation and/or inducing cancer cell death. Compositions of the present invention are compounds that inhibit Rho-protein associated kinase function. Compounds of the invention include piperazinyl pyridines, piperazinylmethyl pyridines, piperazinyl ureas and carbamates, piperazinyl pyridines and quinoilines (including isoquinliones) as well as piperazinyl (including piperazinylmethyl) pyridines and quinolines (including isoquinolines). Compounds of the invention disrupt Rho-kinase activation and function and significantly inhibit tumor cell growth and induce tumor cell death. | 12-24-2009 |
20100004438 | DIARYLETHER DERIVATIVES AS ANTITUMOR AGENTS - An object of the present invention is to provide a medicinal drug much improved in anti tumor activity and excellent in safety. According to the present invention, there is provided a medicinal drug containing a compound represented by the following general formula (1) or a salt thereof as an active ingredient: [Formula 1] wherein X | 01-07-2010 |
20100069628 | Multidentate AZA Ligands Able to Complex Metal Ions And The Use Thereof In Diagnostics And Therapy - Compounds of the formula: | 03-18-2010 |
20100093998 | NOVEL ADENINE COMPOUND - A novel adenine compound represented by the formula (1): | 04-15-2010 |
20100105894 | Cyclopropane 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 cyclopropane compound of formula (1): | 04-29-2010 |
20100113772 | 2-Aminobenzoxazole Process - A method for forming an optionally substituted 2-aminobenzoxazole compound includes: contacting an optionally substituted 2-aminophenol compound with (1) an amine of the formula NHR | 05-06-2010 |
20100121049 | INDENOISOQUINOLINONE ANALOGS AND METHODS OF USE THEREOF - The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog. | 05-13-2010 |
20100261898 | IMIDAZOLE COMPOUNDS - Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-14-2010 |
20100261899 | IMIDAZOLE COMPOUNDS - Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H | 10-14-2010 |
20110009620 | 4-Amino-5-cyanopyrimidine derivatives - The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R | 01-13-2011 |
20110028715 | NOVEL ADENINE COMPOUND - A novel adenine compound represented by the formula (1): | 02-03-2011 |
20110082295 | NOVEL CURCUMIN DERIVATIVE - To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: | 04-07-2011 |
20110105747 | QUINOLINE DERIVATIVE AND QUINAZOLINE DERIVATIVE INHIBITING SELF-PHOSPHORYLATION OF HEPATOCYTUS PROLIFERATOR RECEPTOR, AND MEDICINAL COMPOSITION CONTAINING THE SAME - An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: | 05-05-2011 |
20110160451 | 2-Aminopyrimidine modulators of the histamine H4 receptor - 2-Aminopyrimidine compounds are described, which are useful as H | 06-30-2011 |
20110160452 | 2-Aminopyrimidine modulators of the histamine H4 receptor - 2-Aminopyrimidine compounds are described, which are useful as H | 06-30-2011 |
20110166343 | THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY - To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): | 07-07-2011 |
20110172415 | NITROGEN-CONTAINING HETEROCYCLE DERIVATIVES SUBSTITUTED WITH CYCLIC GROUP - It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. | 07-14-2011 |
20110218338 | 2-AMINOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - 2-Aminopyrimidine compounds are described, which are useful as H | 09-08-2011 |
20110237792 | QUINOLINE DERIVATIVES AND THEIR USE AS 5-HT6 LIGANDS - Disclosed are quinoline compounds having affinity for the 5-HT | 09-29-2011 |
20110275800 | 2-SULFONYLAMINO-4-HETEROARYL BUTYRAMIDE ANTAGONISTS OF CCR10 - This invention relates to a compound of formula (I) and the pharmaceutically acceptable salts thereof wherein R | 11-10-2011 |
20120029189 | PROCESS FOR THE PREPARATION OF HISTAMINE H3 RECEPTOR MODULATORS - The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders. | 02-02-2012 |
20120116075 | Acrylamide Derivative And Use Thereof In Manufacture Of Medicament - An acrylamide derivative represented by formula (I), pharmaceutically acceptable salts and solvates thereof, as well as a medicament containing said acrylamide derivative or its pharmaceutically acceptable salts as the active ingredient, which can be used to treat disorders associated with tyrosine kinase especially Bcr-Abl, including proliferative disorders such as cancers, and inflammation and the like are provided. | 05-10-2012 |
20120190846 | MICHAEL ADDITION REACTION PRODUCT AND ACTIVE ENERGY RAY-CURABLE COMPOSITION - The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor. | 07-26-2012 |
20120238750 | AROMATIC COMPOUND - The compound of the present invention is represented by the following general formula (1): | 09-20-2012 |
20120309963 | 5-CYANO-4- (PYRROLO [2,3B] PYRIDINE-3-YL) -PYRIMIDINE DERIVATIVES 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. | 12-06-2012 |
20130066069 | PROCESSES FOR PREPARING SUBSTITUTED PYRIMIDINES - The present invention provides a facile process for the preparation of tri- and tetra-substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora-mediated diseases or conditions. | 03-14-2013 |
20130102776 | ANTICANCER AGENT - An anticancer agent comprising a compound represented by the formula (I) [R | 04-25-2013 |
20130131338 | SUBSTITUTED DIKETOPIPERAZINES AS OXYTOCIN ANTAGONISTS - A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof. | 05-23-2013 |
20130144054 | NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF - The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base. | 06-06-2013 |
20130150573 | THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability. | 06-13-2013 |
20130158258 | 2-AMINOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - 2-Aminopyrimidine compounds are described, which are useful as H | 06-20-2013 |
20130158259 | 2-AMINOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - 2-Aminopyrimidine compounds are described, which are useful as H | 06-20-2013 |
20130190489 | QUINOLYLPIPERAZINO SUBSTITUTED THIOLACTONE COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF - The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against | 07-25-2013 |
20130231476 | TRANSAMINATION OF NITROGEN-CONTAINING COMPOUNDS TO MAKE CYCLIC AND CYCLIC/ACYCLIC POLYAMINE MIXTURES - A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses. | 09-05-2013 |
20140135492 | MODULATORS OF TOLL-LIKE RECEPTOR 7 - The present application includes a compound of Formula I or II: | 05-15-2014 |
20140163222 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140163223 | Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors - The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer. | 06-12-2014 |
20140343279 | PROCESS FOR THE PREPARATION OF HISTAMINE H3 RECEPTOR MODULATORS - The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders. | 11-20-2014 |
20140350244 | FUSED PYRIDINE, PYRIMIDINE AND TRIAZINE COMPOUNDS AS CELL CYCLE INHIBITORS - Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives. | 11-27-2014 |
20150018542 | 2-ARYLBENZOFURAN-7-FORMAMIDE COMPOUNDS, PREPARATION METHOD AND USE THEREOF - Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, wherein R | 01-15-2015 |
20150045551 | FUSED AZOLE DERIVATIVE - The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia. Specifically, the invention provides fused azole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin 1b receptor: | 02-12-2015 |
20150073136 | PYRAZINONE DERIVATIVES - The present invention relates to pyrazinone derivatives of formula (I): | 03-12-2015 |
20150087823 | TRANS-2-DECENOIC ACID DERIVATIVE AND DRUG CONTAINING SAME - The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): | 03-26-2015 |
20150087824 | NOVEL PRODUCTION METHOD FOR ISOQUINOLINE DERIVATIVES AND SALTS THEREOF - The present invention provides a method capable of industrially producing a target product, i.e., a compound represented by the aforementioned formula (I) or a salt thereof, which is useful for preventing and treating cerebrovascular disorders such as cerebral infarction, cerebral hemorrhage, subarachnoid hemorrhage, and cerebral edema, particularly for preventing and treating glaucoma, at high yield even on a large scale without imposing a negative impact on the environment. The present invention provides a method for producing a compound represented by formula (I) or a salt thereof, wherein the method comprises a step of reacting a compound represented by formula (III) or a salt thereof with a compound represented by formula (II) in the presence of at least one solvent selected from the group consisting of a nitrile solvent, an amide solvent, a sulfoxide solvent, and a urea solvent, and a base. | 03-26-2015 |
20150105550 | PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: | 04-16-2015 |
20150344464 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease. | 12-03-2015 |
20160024116 | Kinase Inhibitors And Their Uses - The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity. | 01-28-2016 |
20160060224 | N-MYRISTOYL TRANSFERASE INHIBITORS - The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors. | 03-03-2016 |
20160168138 | PROCESS FOR THE PREPARATION OF SUVOREXANT AND INTERMEDIATES USEFUL IN THE SYNTHESIS OF SUVOREXANT | 06-16-2016 |
20180022704 | PROCESS FOR THE PREPARATION OF HISTAMINE H3 RECEPTOR MODULATORS | 01-25-2018 |