C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/12 (2006.01) A61K 31/41 (2006.01) A61K 31/435 (2006.01) A61K 31/505 (2006.01) C07D 307/20 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01) C07D 513/04 (2006.01) C07F 7/08 (2006.01)
Patent
CA 2080346
ABSTRACT Compounds of general formula I; Image 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 C1-C6 alkyl, C1-C6 alkoxy, halo, CF3 and CN; Z represents a) a divalent alkanediyl, alkenediyl or alkynediyl group from 2 to 8 carbon atoms which may be a straight or branched-chain having at least 3 carbon atoms in the chain linking W to the oxygen atom, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio and halo: or, b) a Image group wherein n is an integer from 0-3, X is O, S or CH2 and each of R7 and R8 is independently hydrogen or C1-C6 alkyl; or c) a -(CH2)qU(CH2)r- group wherein q is an integer from 0-2, r is an integer from 1-3 and U is a phenylene, furandiyl, tetrahydrofurandiyl, thiophenediyl, tetrahydrothiophenediyl, thiazolediyl or tetrahydrothiazolediyl group; R1 represents a V group wherein V is a Image . group wherein t is an integer from 0-3 and each of R9, R10 and R11 is independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, halo, CN, NO2, SOC1-C6 alkyl, SO2C1-C6 alkyl, SO2(CH2)1-4CH2OH, SO2NH2, CO2H, CO2C1-C6 alkyl, CHO, COC1-C6 alkyl, CH2OH, OH, benzyl, benzoyl, CF3, CONH2, NHCOC1-C6 alkyl, or an NR15R16 group wherein each of R15 and R16 is independently hydrogen or C1-C6 alkyl; and each of R2, R3, R4, R5, and R6 represents independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, halo, C1-C6 alkoxy, C1-C6 alkylthio, C3-C8 cycloalkyl, C4-C8 cycloaLkenyl, CF3, OH, OC(=O)C1-C6 alkyl, a V group, an OV group or an OC(=O)V group; 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 disorders mediated by PAF.
Bowles Stephen Arthur
Davidson Alan Hornsby
Spavold Zoe Marie
Whittaker Mark
British Bio-Technology Limited
Carton John K.
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