Nippon Chemiphar Co., Ltd.

Kyushu University

Shogo Sakuma

Toshiyasu Imai

Masatoshi Ushioda

Kazuhide Inoue

Kunio Kobayashi

Seiichiro Masui

Tomio Yamakawa

Takashi Kanda

Daisuke Saito

Toshihiro Takahashi

Atsushi Tendo

Tsuyoshi Endo

Rie Takahashi

Hideki Nakamura

Yoshikazu Watanabe

Masahiko Arai

Shinichi Yoshida

Yutaka Nomura

Nobutaka Mochiduki

Kazuhike Inoue

Nobutaka Mochizuki

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). 

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: 

[object Object]

A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2Xreceptor antagonist: wherein Rrepresents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, Rand Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, Rand Rrepresent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.

Diazepinedione derivative

A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2Xreceptor antagonist: 

P 2&#xd7;4 receptor antagonist

A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR 

Activating agent for peroxisome proliferator activated receptor

A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR&#x3b4;. 

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Saitama, Japan

Shogo Sakuma