Platelet activating factor antagonists

Details Platelet activating factor antagonists Platelet activating factor antagonists

C - Chemistry, Metallurgy

07

D

167/211, 260/271

C07D 401/00 (2006.01) A61K 31/395 (2006.01) C07D 401/10 (2006.01) C07D 401/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07D 513/04 (2006.01)

Patent

CA 1340785

Platelet activating factor antagonists of formula (I): (see formula I) 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, fluoro(C1-C4)alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring; R1 and R2 are each independently H or C1-C6 alkyl, or R1 and R2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C1-C4 alkyl)piperazinyl or N-(C2-C4 alkanoyl)-piperazinyl group; or R2 is H or C1-C4 alkyl and R1 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 or heteroaryl; Z is selected from C1-C6 alkoxy, aryl(C1-C4)alkoxy, hydroxy, and -NR4R5 wherein each of R4 and R5 is independently H or C1-C6 alkyl, or R4 and R5 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl or N-(C1-C4 alkyl)piperazinyl group; Y is 1,4 phenylene or pyridine-2,5-diyl, and X is a 5 or 6 membered aromatic heterocyclic group containing one or more nitrogen atoms in its ring; which ring may be fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, at least one of said heterocyclic rings optionally also containing an oxygen or sulphur atom, and being optionally substituted with one or more substituents selected from C1-C4 alkyl, C1-C4 alkoxy, halo, CF3 and CN; and their pharmaceutically acceptable salts.

578630

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