Carbostyril derivatives, process for producing thereof and...

Details Carbostyril derivatives, process for producing thereof and... Carbostyril derivatives, process for producing thereof and...

C - Chemistry, Metallurgy

07

D

260/266.3, 260/2

C07D 401/06 (2006.01) C07D 215/22 (2006.01) C07D 215/227 (2006.01)

Patent

CA 1155119

ABSTRACT OF THE DISCLOSURE Novel crbostyril 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 or Image (wherein R2 is a hydrogen atom or a lower alkyl group): B is a lower alkylene group; ? is 1 when A is a group of the formula Image , or ? is 0 or 1 when A is a group of the formula Image or Image ; Z is a group of the formula Image or Image (wherein R3 is a substituted- phenyl group having 1 to 3 substituents, on the phenyl ring, selectd 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-tetrahydro- naphthyl 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 carbo- styril 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.

371904

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