Nippon Chemiphar Co., Ltd.

Kyushu University

Ube Industries, Inc.

J-pharma Co., Ltd.

Dethree Res. Lab. Inc.

Kunio Kobayashi

Shogo Sakuma

Toshiyasu Imai

Kazuhide Inoue

Masatoshi Ushioda

Daisuke Saito

Tomio Yamakawa

Shinichi Yoshida

Atsushi Tendo

Tsuyoshi Endo

Nobutaka Mochiduki

Yoriko Shinohara

Toshihiro Takahashi

Tadashi Kobayashi

Yoshikazu Watanabe

Katsumasa Harada

Shigeyoshi Nishino

Hitoshi Endou

Masahiko Arai

Takashi Kanda

Seiichiro Masui

Masao Yamamoto

Hiroshi Sasaki

Hiroto Tanaka

Masuharu Hirano

Naohiko Anzai

Nobutaka Mochizuki

Hirano Masuharu

The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, Rand Rrepresent hydrogen atom and the like, or Rand Rbind together to form a naphthalene ring and the like together with the benzene ring to which they bind, Rand Rrepresent hydrogen atom and the like, Rrepresents hydrogen atom and the like, Rand Rrepresent 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.

P2X4 receptor antagonist

The present invention relates to a diazepine derivative represented by the following general formula (I) (in the formula, Rand Rrepresent hydrogen atom and the like, or Rand Rbind together to form a naphthalene ring and the like together with the benzene ring to which they bind, Rand Rrepresent hydrogen atom and the like, Rrepresents hydrogen atom and the like, Rand Rrepresent hydrogen atom and the like, X represents C, CH or N, Y represents N, NH or C(&#x2550;O), provided that when X is N, Y is not N or NH, and when X is C or CH, Y is not C(&#x2550;O), Z represents oxygen atom or sulfur atom, A represents benzene ring and the like, B represents NHC(&#x2550;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. 

Compounds represented by the following general formula (I), which has a P2X4 receptor antagonistic activity (in the formula, R, Rand Rrepresent 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(&#x2550;O), provided that when X is C, Y represents N, and when X is N, Y represents C(&#x2550;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). 

Provided are a compound represented by the following Formula (III), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt or solvate thereof used as a therapeutic agent for gout or hyperuricemia. (In the Formula (III), R, R, R, and Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, or a cyano group, Rand Rform a benzene ring or a 5-membered heteroaryl ring containing 1 to 3 heteroatoms, as a ring constituent element, selected from nitrogen atoms, oxygen atoms, and sulfur atoms together with two carbon atoms to which Rand Rare bonded, Rand Rform a benzene ring together with two carbon atoms to which Rand Rare bonded or represent any of the groups represented by Rdescribed above, Wrepresents CRor N, and where, Rrepresents any of the groups represented by R, Xrepresents an oxygen atom or a sulfur atom, Yrepresents an alkylene chain having 1 to 8 carbon atoms, and where, the alkylene chain may be substituted with an alkyl group having 1 to 8 carbon atoms and the alkylene chain may be a linear or branched alkylene chain, the branched alkylene chain may have a 3- to 7-membered ring formed by side chains bonded to carbon atoms which are the same as or different from each other, together with the carbon atoms to which the side chains are bonded and may have a double bond in the middle thereof, and Zrepresents COH). 

URAT1 inhibitor

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, Rand Rrepresent 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(&#x2550;O), provided that when X is C, Y represents N, and when X is N, Y represents C(&#x2550;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). 

The present invention relates to a compound represented by the following general formula (II), wherein, in the formula, Rto Rrepresent hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and the like, Xrepresents C or N, Yrepresents N or C(&#x2550;O), provided that when Xis C, Yrepresents N, and when Xis N, Yrepresents C(&#x2550;O), the double line consisting of the solid line and the broken line represents a single bond or double bond, Arepresents benzene ring, pyridine ring, and the like, Drepresents tetrazole ring, imidazole ring, and the like, Erepresents &#x2014;(CRR)-T-, and Grepresents benzene ring, pyridine ring, and the like, which has a P2X4 receptor antagonistic activity. 

A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2Xreceptor antagonist: 

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The invention relates to compounds of the following formula (I) or their salts: in which Ris a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkoxycarbonyl group having 2-8 carbon atoms, carboxyl, halogen, hydroxyl, nitro, or cyano; Ris cyano, nitro, or the like; Ris hydroxyl or the like; X is oxygen, sulfur, or the like; and Y is oxygen or sulfur, and a xanthine oxidase inhibitor containing the compound.

Substituted 1,3-thiazolo[5,4-d]pyrimidines as xanthine oxidase inhibitors

The invention relates to compounds of the following formula (I) or their salts: in which Rrepresents ORor others, in which Ris an alkyl group having 1-8 carbon atoms which may have a substituent or the like; Ris halogen, nitro, cyano, carboxyl, or the like; Ris hydrogen, halogen, hydroxyl, amino, carboxyl, or the like; X is NR, oxygen, or sulfur, in which Ris hydrogen, or an alkyl group having 1-8 carbon atom which may have a substituent; and each of Y and Z is CRor nitrogen, in which Rhas the same meaning as Rabove, and a xanthine oxidase inhibitor containing the compound as an active ingredient.

Substituted thiazolopyrimidines as xanthine oxidase inhibitors

Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R and R each are hydrogen, C alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X and X are each a free valency, oxygen, S(O) (wherein p is an integer of 0 to 2), C(&boxH;O), C(&boxH;O)NH, NHC(&boxH;O), CH&boxH;CH, or the like; Y is optionally substituted C alkylene; Z is oxygen or sulfur; R and R are each optionally substituted C alkyl; and R is hydrogen or C alkyl, with the proviso that when X is a free valency, X is not O or S(O) , while when X is C(&boxH;O)NH, X is not a free valency.

PPAR delta activators

Preparation of 2-(10,11-dihydro-10-oxodibenzo-[b,f]thiepin-2-yl)

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Saitama, Japan

Kunio Kobayashi