Nippon Chemiphar Co., Ltd.

Kyushu University

Toshiyasu Imai

Shogo Sakuma

Kazuhide Inoue

Masatoshi Ushioda

Kunio Kobayashi

Daisuke Saito

Toshihiro Takahashi

Junzo Kamei

Toru Kawasaki

Toru Ogawa

Yoshikazu Watanabe

Masahiko Arai

Atsushi Tendo

Kazuhike Inoue

The present invention pertains to a medicament for preventing or treating cough, including, as an active ingredient, a compound having P2X4 receptor antagonistic action, a tautomer, stereoisomer, or pharmaceutically acceptable salt of the compound, or a hydrate or solvate thereof.

Medicament for treating cough

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 medicine for preventing or treating pain in nociceptive pain, inflammatory pain, or neuropathic pain, the medicine comprising, as an active ingredient, a compound having a P2X4 receptor antagonist action, a tautomer of the compound, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof. The medicine has no effect on driving or machine operation ability, has no effect on car driving ability, does not require any restriction to administration thereof to a patient engaging in operation of a dangerous machine including driving a car, or can be administered to a patient engaging in operation of a dangerous machine including driving a car.

Medicine for diabetic peripheral neuropathy

A medicament for preventive and/or therapeutic treatment of multiple sclerosis, especially a pain accompanying multiple sclerosis such as neuropathic pain, which contains a compound having a P2X4 receptor antagonist activity such as a compound represented by the general formula (IH), or a salt thereof or a hydrate or solvate thereof as an active ingredient.

Medicament for treatment of multiple sclerosis

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: 

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Tokyo, Japan

Toshiyasu Imai