Carbostyril derivatives and process for preparation thereof

Details Carbostyril derivatives and process for preparation thereof Carbostyril derivatives and process for preparation thereof

C - Chemistry, Metallurgy

07

D

260/266.3, 260/2

C07D 401/12 (2006.01) C07D 215/16 (2006.01) C07D 215/22 (2006.01) C07D 215/227 (2006.01) C07D 215/28 (2006.01)

Patent

CA 1117110

ABSTRACT OF THE DISCLOSURE Novel carbostyril derivatives having anti- histamic action and central nervous controlling action and are useful as an antihistamic agent or a central nervous controlling agent, represented by the general formula, (1) Image wherein R1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group having alkylene group having 1 to 4 carbon atoms; R2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanoyloxy group having 1 to 4 carbon atoms or 3,4,5-trimethoxybenzoyloxy group; R4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted group selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 t? 4 carbon atoms having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, ? and m are respectively an integer of O or 1-6, but the sum of ? and m should not be exceeding 6; the carbon-carbon bond at 3- and 4-positions in the carbostyril skeleton is a single or double bond; the substituted position of the side chain of Image is any one at 4-, 5-, 6-, 7- or 8-position.

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