公开(公告)号：EP3020717A4

公开(公告)日：2017-01-25

申请号：EP14822292

申请日：2014-07-11

申请人： NIPPON CHEMIPHAR CO ,  UNIV KYUSHU

发明人： SAKUMA SHOGO ,  KOBAYASHI KUNIO ,  USHIODA MASATOSHI ,  SAITO DAISUKE ,  IMAI TOSHIYASU ,  INOUE KAZUHIDE

IPC分类号： C07D403/10 ,  A61K31/551 ,  A61P25/04 ,  A61P43/00 ,  C07D401/04 ,  C07D403/08

CPC分类号： C07D403/10 ,  C07D401/04 ,  C07D401/14 ,  C07D403/08 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： The present invention relates to a compound represented by the following general formula (II), wherein, in the formula, R 1a to R 6a represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, X a represents C or N, Y a represents N or C(=O), provided that when X a is C, Y a represents N, and when X a is N, Y a represents C(=O), the double line consisting of the solid line and the broken line represents a single bond or double bond, A a represents benzene ring, pyridine ring, and the like, D a represents tetrazole ring, imidazole ring, and the like, E a represents-(CR 9a R 10a ) p -T a -, and G a represents benzene ring, pyridine ring, and the like, which has a P2X4 receptor antagonistic activity.

摘要翻译： 本发明涉及由以下通式（II）表示的化合物，其中，在该式中，R 1a至R 6a表示氢原子，具有1至8个碳原子的烷基等，X a表示C 或N，Y a表示N或C（= O），条件是当X a为C时，Y a表示N，当X a为N时，Y a表示C（= O），由固体 线，虚线表示单键或双键，A a表示苯环，吡啶环等，D a表示四唑环，咪唑环等，E a表示 - （CR 9a R 10a）p -T a - ，G a表示具有P2X4受体拮抗活性的苯环，吡啶环等。

公开(公告)号：EP3020707A4

公开(公告)日：2016-12-07

申请号：EP14822945

申请日：2014-07-11

申请人： NIPPON CHEMIPHAR CO ,  UNIV KYUSHU

发明人： SAKUMA SHOGO ,  KOBAYASHI KUNIO ,  USHIODA MASATOSHI ,  IMAI TOSHIYASU ,  INOUE KAZUHIDE

IPC分类号： C07D243/10 ,  A61K31/551 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14

CPC分类号： C07D243/10 ,  C07D401/12 ,  C07D401/14

摘要： The present invention relates to a compound represented by the following general formula (I), which has a P2X4 receptor antagonistic activity (in the formula, R 1 , R 2 and R 3 represent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, a halogen atom, and the like, X represents C or N, Y represents N or C(=O), provided that when X is C, Y represents N, and when X is N, Y represents C(=O), the double line consisting of the solid line and the broken line represents a single bond or double bond, n represents an integer of 0 to 6, Z represents O, S, or an atomic bond, and A represents benzene ring, pyridine ring, and the like).

摘要翻译： 本发明涉及具有P2X4受体拮抗活性的下述通式（I）表示的化合物（式中，R 1，R 2和R 3表示氢原子，碳原子数为1〜8的烷基） ，碳原子数1〜8的烷氧基，卤素原子等，X表示C或N，Y表示N或C（= O），条件是当X为C时，Y表示N，当X为 N，Y表示C（= O），由实线和虚线构成的双线表示单键或双键，n表示0〜6的整数，Z表示O，S或原子键， A表示苯环，吡啶环等）。

公开(公告)号：EP2803662A4

公开(公告)日：2015-06-03

申请号：EP13736295

申请日：2013-01-10

申请人： NIPPON CHEMIPHAR CO

发明人： USHIODA MASATOSHI ,  KOBAYASHI KUNIO ,  SAITO DAISUKE ,  SAKUMA SHOGO ,  IMAI TOSHIYASU ,  INOUE KAZUHIDE

IPC分类号： C07D243/12 ,  A61K31/551 ,  A61K31/5513 ,  A61P25/04 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D243/10 ,  C07D243/12 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

摘要： The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, R 1 and R 2 represent hydrogen atom and the like, or R 1 and R 2 bind together to form a naphthalene ring and the like together with the benzene ring to which they bind, R 3 and R 4 represent hydrogen atom and the like, R 5 represents hydrogen atom and the like, R 6 and R 7 represent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(=O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(=O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(=O) and the like, D represents an atomic bond and the like, E represents an atomic bond and the like, G represents benzene which may be substituted and the like, and m represents an integer of 0 to 5) or a pharmacologically acceptable salt thereof, and a P2X4 receptor antagonist.

公开(公告)号：EP2597088A4

公开(公告)日：2013-11-20

申请号：EP11806808

申请日：2011-07-13

申请人： NIPPON CHEMIPHAR CO

发明人： SAKUMA SHOGO ,  ARAI MASAHIKO ,  KOBAYASHI KUNIO ,  WATANABE YOSHIKAZU ,  IMAI TOSHIYASU ,  INOUE KAZUHIDE

IPC分类号： C07D243/12 ,  A61K31/551 ,  A61P25/04 ,  A61P43/00 ,  C07D243/10 ,  C07D401/10 ,  C07D403/10 ,  C07D409/04 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D491/056

CPC分类号： C07D243/10 ,  C07D243/12 ,  C07D243/24 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056

摘要： A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X 4 receptor antagonist: wherein each of R 21 and R 22 is hydrogen, a C 1-8 alkyl group or the like; R 23 is hydrogen, a C 1-8 alkyl group or the like; each of R 24 and R 25 is hydrogen, a C 1-8 alkyl group or the like; R 26 is hydrogen, a C 1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.

摘要翻译： 使用具有下式（III）的二氮杂衍生物或其药理学上可接受的盐作为P2X 4受体拮抗剂：其中R 21和R 22各自为氢，C 1-8烷基等; R 23为氢，C 1-8烷基等; R 24和R 25各自为氢，C 1-8烷基等; R 26是氢，C 1-8烷基，卤素原子，羟基，硝基，氰基，任选具有一个或多个取代基的苯基，或任选具有一个或多个取代基的杂环基等; p为0或1。

公开(公告)号：EP0922704A4

公开(公告)日：2002-01-02

申请号：EP97936857

申请日：1997-08-22

申请人： NIPPON CHEMIPHAR CO ,  UBE INDUSTRIES

发明人： YAMAMOTO MASAO ,  KOBAYASHI KUNIO ,  HARADA KATSUMASA ,  NISHINO SHIGEYOSHI ,  SASAKI HIROSHI

IPC分类号： C07D337/14 ,  C07C205/56 ,  C07C229/40 ,  C07C323/62 ,  C07C229/42 ,  C07C233/11 ,  C07C255/41

CPC分类号： C07D337/14

摘要： A novel process for preparing zaltoprofen[2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid], which, as compared with the conventional processes, has better practicality from an overall viewpoint including availability and handleability of a starting material and profitability, such as the yield. The novel process is characterized by providing 2-(4-amino-3-carboxymethylphenyl)propionic acid or a salt thereof as a starting compound, subjecting the starting compound to, e.g., diazotization reacting the diazotized compound with thiophenol to prepare 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or a salt thereof, and then subjecting this product to a ring-closing reaction. Intermediate compounds useful for the preparation of the above compound are also provided.

公开(公告)号：EP1452528A4

公开(公告)日：2005-11-16

申请号：EP02780099

申请日：2002-11-14

申请人： NIPPON CHEMIPHAR CO

发明人： YOSHIDA SHINICHI ,  TENDO ATSUSHI ,  KOBAYASHI KUNIO ,  MOCHIDUKI NOBUTAKA ,  YAMAKAWA TOMIO ,  SHINOHARA YORIKO

IPC分类号： A61P3/00 ,  A61P13/12 ,  A61P19/06 ,  A61P43/00 ,  C07D235/18 ,  C07D263/56 ,  C07D263/57 ,  C07D277/66 ,  C07D401/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61P9/00

CPC分类号： C07D263/57 ,  C07D235/18 ,  C07D277/66 ,  C07D401/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/30 ,  C07D473/34 ,  C07D473/40 ,  C07D487/04 ,  C07D513/04

摘要： Compounds represented by the general formula (I), and xanthine oxidase inhibitors containing the same as the active ingredient: (I) wherein R1 is OR4 or the like (wherein R4 is optionally substituted C1-8 alkyl or the like); R2 is halogeno, nitro, cyano, carboxyl, or the like; R3 is hydrogen, halogeno, hydroxyl, amino, carboxyl, or the like; X is NR11, oxygen, or sulfur (wherein R11 is hydrogen or optionally substituted C1-8 alkyl); and Y and Z are each CR12 or nitrogen (wherein R12 is the same as defined for R3).

公开(公告)号：EP1310494A4

公开(公告)日：2004-10-20

申请号：EP01955606

申请日：2001-08-09

申请人： NIPPON CHEMIPHAR CO

发明人： SAKUMA SHOGO ,  ENDO TSUYOSHI ,  TENDO ATSUSHI ,  TAKAHASHI TOSHIHIRO ,  YOSHIDA SHINICHI ,  KOBAYASHI KUNIO ,  MOCHIZUKI NOBUTAKA ,  YAMAKAWA TOMIO ,  KANDA TAKASHI ,  MASUI SEIICHIRO

IPC分类号： A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/38 ,  A61P9/00 ,  A61P9/10 ,  A61P19/10 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D233/64 ,  C07D233/70 ,  C07D233/88 ,  C07D233/90 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/38 ,  C07D413/04 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/506 ,  C07D263/34 ,  C07D263/40 ,  C07D263/48 ,  C07D277/26 ,  C07D417/04

CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D277/24

摘要： Compounds of the general formula (|) or salts thereof; and activators of PPARδ (peroxisome proliferator activated receptor δ) containing the compounds or the salts as the active ingredient: (I) wherein R?1 and R2¿ are each hydrogen, C¿1-8? alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X?1 and X2¿ are each a free valency, oxygen, S(O)¿p? (wherein p is an integer of 0 to 2), C(=O), C(=O)NH, NHC(=O), CH=CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R?3 and R4¿ are each optionally substituted C¿1-8? alkyl; and R?8¿ is hydrogen or C¿1-8? alkyl, with the proviso that when X?1¿ is a free valency, X2 is not O or S(O)¿p?, while when X?1¿ is C(=O)NH, X2 is not a free valency.

公开(公告)号：EP1795526A4

公开(公告)日：2010-10-13

申请号：EP05785892

申请日：2005-09-13

申请人： NIPPON CHEMIPHAR CO

发明人： TAKAHASHI TOSHIHIRO ,  ENDO TSUYOSHI ,  USHIODA MASATOSHI ,  KOBAYASHI KUNIO ,  YAMAKAWA TOMIO ,  SHIKA KIICHI ,  KAWASAKI TORU ,  IMAI TOSHIYASU

IPC分类号： C07D211/58 ,  A61K31/4468 ,  A61K31/4525 ,  A61K31/4535 ,  A61P25/02 ,  A61P25/04 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D211/58 ,  C07D405/12 ,  C07D409/12

公开(公告)号：EP1757610A4

公开(公告)日：2009-06-24

申请号：EP05751417

申请日：2005-06-13

申请人： NIPPON CHEMIPHAR CO

发明人： YOSHIDA SHINICHI ,  KOBAYASHI KUNIO ,  MOCHIDUKI NOBUTAKA ,  YAMAKAWA TOMIO ,  KOBAYASHI TADASHI ,  SHINOHARA YORIKO

IPC分类号： C07D498/04 ,  A61K31/519 ,  A61P19/06 ,  A61P43/00 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D498/04

摘要： Disclosed is a compound represented by the following general formula (I) (wherein R1 represents an aryl group having 6-10 carbon atoms or a heteroaryl group which may have, as a substituent, a group selected from an alkyl group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms which is substituted with a halogen atom, an alkoxy group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms which is substituted with an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, a formyl group, a carboxyl group, a halogen atom, a hydroxyl group, a nitro group, a cyano group, an amino group, an aryl group having 6-10 carbon atoms and an aryloxy group having 6-10 carbon atoms; R2 represents a cyano group, a nitro group or the like; R3 represents an hydroxyl group or the like; X represents an oxygen atom, a sulfur atom or the like; and Y represents an oxygen atom or a sulfur atom). Also disclosed is a xanthine oxidase inhibitor containing such a compound.