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    • 83. 发明授权
    • Cyclic ether acetal PAF antagonists
    • US5637595A
    • 1997-06-10
    • US175411
    • 1993-12-30
    • Mark WhittakerAndrew MillerStephen A. Bowles
    • Mark WhittakerAndrew MillerStephen A. Bowles
    • C07D403/12C07D405/12C07D417/12C07D471/04A61K31/425A61K31/44
    • C07D403/12C07D405/12C07D417/12C07D471/04
    • Compounds of general formula (I), wherein W represents a 5- or 6-membered aromatic heterocyclic ring containing one or more non-quaternised 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 --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; Z represents a) a divalent alkanediyl group from 1 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; or b) a divalent alkenediyl or alkynediyl group from 2 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or subtituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.6 alkyl and halo; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each represents a hydrogen atom, a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.5 together with the carbon atoms to which they are attached can form a five to ten membered monocycycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.5, R.sup.6 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; X represents a bond, an oxygen atom, a sulphur atom, a --NH-- group, a --N(C.sub.1 -C.sub.6 alkyl)-- group, a --(CH.sub.2).sub.n -- group or a --CR.sup.7 R.sup.8 -- group; n represents an integer of 1, 2 or 3; R.sup.7 and R.sup.8 each represents a --C.sub.1 -C.sub.18 alkyl or a --C.sub.2 -C.sub.18 alkenyl group; or R.sup.3 and R.sup.7 together with the carbon atoms to which they are attached can form a five to ten membered monocycloalkyl or bicycloalkyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; or R.sup.3, R.sup.4 and R.sup.7, R.sup.8 and the carbon atoms to which they are attached form a phenyl ring which may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; 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.