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    • 10. 发明专利
    • 1-OXA-2,9-DIPHENYL-SPIRO(4,4)NONANE DERIVATIVES AS PAF ANTAGONISTS
    • AU1412192A
    • 1992-10-06
    • AU1412192
    • 1992-03-04
    • BRITISH BIO-TECHNOLOGY LIMITED
    • ALAN HORNSBY DAVIDSONMARK WHITTAKERZOE MARIE SPAVOLD
    • C07D307/94C07D405/06
    • Compounds of general formula I; wherein: each of R , R , and R independently represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C1-C6 alkyl, -SC1-C6 alkyl, halo, -CN, -NO2, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -SO2NH2, -COC1-C6 alkyl, -CHO, -COOC1-C6 alkyl, -CH2OH, benzyl, benzoyl, -CF3, -CONH2, -NHCOC1-C6 alkyl; each of R and R independently represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -OC1-C6 alkyl, -SC1-C6 alkyl, halo, -CN, -NO2, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -SO2NH2, -COOH, -COC1-C6 alkyl, -CHO, -COOC1-C6 alkyl, -CH2OH, -OH, benzyl, benzoyl, -CF3, -CONH2, -NHCOC1-C6 alkyl or a -OC(=O)R group wherein R represents -C1-C6 alkyl, -C2-C6 alkenyl, -OC1-C6 alkyl, -SC1-C6 alkyl, -COC1-C6 alkyl, -COOC1-C6 alkyl, benzyl, benzoyl, -CF3, -CN or a V group wherein V represents a) a group wherein t is an integer from 0 to 3 and each of R , R and R is independently hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -OC1-C6 alkyl, -SC1-C6 alkyl, halo, -CN, -NO2, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -SO2NH2, -COOH, -COC1-C6 alkyl, -CHO, -COOC1-C6 alkyl, -CH2OH, -OH, benzyl, benzoyl, -CF3, -CONH2, -NHCOC1-C6 alkyl; b) a group -(CH2)s-Y wherein s is an integer from 0 to 5 and Y represents a 5- or 6-membered aromatic heterocyclic ring containing one or more sp2 nitrogen atoms in its ring, which heterocyclic ring may be optionally fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, wherein at least one of the said heterocyclic rings may also contain an oxygen or sulphur atom, and wherein any of the rings may be optionally substituted with one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halo, -CF3 and -CN; or R together with R forms a =O, =N-OH, =NHR or =CHR group, wherein R is as defined above; each of R and R independently represents hydrogen, -C1-C6 alkyl, -COC1-C6 alkyl, benzyl, a group V as defined above or a -COV group wherein V is as defined above; or R together with R form a =CR R group wherein each of R and R independently represent a hydrogen atom, a C1-C18 alkyl, a -C2-C6 alkenyl, pyrrole or a group V as defined above; and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or conditions mediated by PAF.