| 摘要 |
Novel carbostyril derivatives and their salts having antihistaminic effect and central nervous system controlling effect and are useful as antihistaminic agents and central nervous system controlling agents, represented by the general formula (1), <IMAGE> (1) wherein R1 is a hydrogen atom, a lower alkyl group, a phenyl-lower alkyl group, a lower alkenyl group, a lower alkynyl group; A is a group of the formula <IMAGE> or a group of the formula <IMAGE> (wherein R2 is a hydrogen atom or a lower alkyl group); B is a lower alkylene group; l is 1 when A is a group of the formula <IMAGE> or l is 0 or 1 when A is a group of the formula <IMAGE> Z is a group of the formula <IMAGE> (wherein R3 is a substituted-phenyl group having 1 to 3 substituents, on the phenyl ring, selected from the group consisting of a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkoxy-carbonyl group, a carboxyl group, a lower alkylthio group, a lower alkanoyl group, a hydroxyl group, a nitro group, an amino group and a cyano group; or R3 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent, a phenyl-lower alkyl group or a 1,2,3,4-tetrahydronaphthyl group; R4 is a substituted-phenyl group having 1 to 3 substituents, on the phenyl group, selected from the group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; or R4 is a substituted-phenyl group having a lower alkylenedioxy group as the substituent, a phenyl-lower alkyl group, a 1,2,3,4-tetrahydronaphthyl group or a group of the formula <IMAGE> R5 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; or when R5 is a hydrogen atom the carbon-carbon bond between 3- and 4-positions in the piperidine ring is a double bond which is dehydrogenated the hydrogen atoms bonded at 3- and 4-positions of piperidine ring; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond. The carbostyril derivatives of the present invention have antihistaminic effects and central nervous system controlling effects and are useful for antihistaminic agents and central nervous system controlling agents.
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