DIHYDROPYRIDINE ANTI-ALLERGIC AND ANTI-INFLAMMATORY AGENTS

摘要

Compound of the formula:- wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C1-C4 alkyl, C1-C4 alkoxy, aryl(C1-C4 alkoxy), C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluormethyl and cyano; R<1> and R<2> are each independently H or C1-C6 alkyl, or the two groups may be joined together to form with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl)piperazinyl group; or R<2> is H or C1-C4 alkyl and R<1> is CN, C3-C7 cycloalkyl, aryl, heteroaryl, or a C1-C4 alkyl group substituted by one or more substituents selected from C3-C7 cycloalkyl, C1-C4 alkoxycarbonyl, aryl and heteroaryl; R<3> is OH, C1-C6 alkyloxy, aryl(C1-C4 alkoxy), or NR<4>R<5> wherein each of R<4> and R<5> is independently H or C1-C6 alkyl, or the two groups may be joined together to form with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino, morpholino, piperazinyl, or N-(C1-C4 alkyl)-piperazinyl group; Y is an alkylene group of from 2 to 8 carbon atoms which may be straight or branched-chain having at least 2 carbon atoms in the chain linking X to the oxygen atom; X is benzimidazol-1-yl or benzimidazol-2-yl, optionally substituted with one or more substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and CN; and their pharmaceutically acceptable salts are antagonists of PAF and are useful in the treatment of allergic, inflammatory and hypersecretory conditions.