C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 235/08 (2006.01) A61K 31/415 (2006.01) A61K 31/435 (2006.01) A61K 31/535 (2006.01) A61K 31/695 (2006.01) C07C 311/16 (2006.01) C07D 213/74 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07D 471/04 (2006.01) C07F 7/10 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2088742
Compounds of general formula I; Image wherein: A1 is =N-, =CH- or =CR1-; A2 is =N-, =CH- or =CR2-; provided that, when one of A1 and A2 is a nitrogen atom, the other of A1 and A2 is other than a nitrogen atom; R represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, halogen or -OC1-C6 alkyl; R1 and R2 each independently represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, halogen, -CN, -CO2H, -CO2C1-C6 alkyl, -CONH2, -CHO, -CH2OH, -CF3, -OC1-C6 alkyl, -SC1-C6 alkyl, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -NH2, -NHCOMe or -NO2, or R1 and R2 together with the carbon atoms to which they are attached form a fused phenyl ring; R3 represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, -OC1-C6 alkyl, -SC1-C6 alkyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -CF3, -(C1-C6 alkyl)phenyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl, -(C1-C6 alkyl)C3-C8 cycloalkyl, -(C1-C6 alkyl)C4-C8 cycloalkenyl or thiophenyl; R4 represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, -CO2C1-C6 alkyl, -SC1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)phenyl or thiophenyl; R5 represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, -COC1-C6 alkyl, -CO2C1-C6 alkyl, -(CO2C1-C6 alkyl)phenyl, -(C1-C6 alkyl)CO2C1-C6 alkyl, -(C1-C6 alkyl)phenyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl or phenyl optionally substituted by one or more substituents selected from -C1-C6 alkyl, -OC1-C6 alkyl, halogen, -CF3, -CN; m is an integer from 0 to 3: Z is either a -CR6R7R8 or -CR6=CR7R8 group; wherein each of R6, R7 and R8 independently represents hydrogen, halogen, -C1-C18 alkyl optionally substituted by one or more halogen atoms, -C2-C18 alkenyl, -C2-C18 alkynyl, -(C1-C6 alkyl) OC1-C18 alkyl, -(C1-C6 alkyl) SC1-C18 alkyl, -(C1-C6 alkyl)O(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)S(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)O(C1-C6 alkyl)SC1-C6 alkyl, - (C1-C6 alkyl)S(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)OC2-C6 alkenyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl, -(C1-C6 alkyl)C3-C8 cycloalkyl, -(C1-C6 alkyl)C4-C8 cycloalkenyl, -(C1-C6 alkyl)OC3-C8 cycloalkyl, -(C1-C6 alkyl)OC4-C8 cycloalkenyl, -(C1-C6 alkyl)SC3-C8 cycloalkyl, -(C1-C6 alkyl)SC4-C8 cycloalkenyl, -(C1-C6 alkyl)N(C1-C6 alkyl)2, -(C1-C6 alkyl)morpholino, -(C1-C6 alkyl)OCH2Ph, -CH2OSi(C1-C6 alkyl)3, -CH2OSiPh2C1-C6 alkyl or a group -D wherein D represents a group; Image wherein n is an integer from 0 to 3, and each of R9, R10 and R11 is independently hydrogen, -C1-C6 alkyl, -OC1-C6 alkyl, -SC1-C6 alkyl, -N(C1-C6 alkyl)2, -C2-C6 alkenyl, -C2-C6 alkynyl, -OCH2Ph, halogen, -CN, -CF3, -CO2H, -CO2C1-C6 alkyl, -CONH2, -CONHC1-C6 alkyl, -CONH(C1-C6 alkyl)2, -CHO, -CH2OH, -NH2, -NHCOC1-C6 alkyl, -SOC1-C6 alkyl, or -SO2C1-C6 alkyl; 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.
Miller Andrew
Whittaker Mark
British Bio-Technology Limited
Moffat & Co.
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