C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/415 (2006.01) A61K 31/435 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07C 311/19 (2006.01) C07C 311/53 (2006.01) C07D 213/74 (2006.01) C07D 235/08 (2006.01) C07D 235/16 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 413/12 (2006.01) C07F 7/18 (2006.01)
Patent
CA 2088761
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, halogen or -OC1-C6 alkyl; each of R1 and R2 independently represents hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, 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, -(COC1-C6 alkyl)phenyl, -(CO2C1-C6 alkyl)phenyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)CO2C1-C6 alkyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl or a group -D wherein D represents a group: Image wherein n is an integer from 0 to 3, and each of R8 and R9 is independently hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C2-C6 alkynyl, halogen, -CN, -CO2H, -CO2C1-C6 alkyl, -CONH2, -CONHC1-C6 alkyl, -CONH(C1-C6 alkyl)2, -CHO, -CH2OH, -CF3, -OC1-C6 alkyl, -SC1-C6 alkyl, -SOC1-C6 alkyl, -SO2C1-C6 alkyl, -NH2 or -NHCOMe; each of R6 and R7 independently represents hydrogen, halogen, -C1-C6 alkyl optionally substituted by one or more halogen atoms, -C2-C6 alkenyl, -C2-C6 alkynyl, -(C1-C6 alkyl)CO2C1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)N(C1-C6 alkyl)2, -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, a side chain of a naturally occurring amino acid, a group -D as defined above or a -(C1-C6 alkyl)OD group wherein D is as defined above; or R6 together with R5 and the atoms to which they are attached form a 5 to 8 membered nitrogen-containing heterocyclic ring; or R6 and R7 together with the carbon atom to which they are attached form a C3-C8 cycloalkyl ring; B represents a) a -ZR10 group wherein Z is -C(=0)-, -C(=O)O-, -C(=S)- or -C(=S)O- and R10 is -C1-C18 alkyl optionally substituted by one or more halogen atoms, -C2-C18 alkenyl, -C2-C18 alkynyl, -(C1-C6 alkyl)OC1-C6 alkyl, -(C1-C6 alkyl)SC1-C6 alkyl, -(C1-C6 alkyl)O(C1-C6 alkyl)OC1-C6 alkyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl, pyridyl, a group -D as defined above or a -(C1-C6 alkyl)OD group wherein D is as defined above; b) a -CONR11R12 group wherein each of R11 and R12 is independently hydrogen, -C1-C18 alkyl optionally substituted by one or more halogen atoms, -C2-C18 alkenyl, -C2-C18 alkynyl, -C3-C8 cycloalkyl, -C4-C8 cycloalkenyl, pyridyl, a group -D as defined above or R11 and R12 together with the nitrogen atom to which they are attached form a 5 to 8 membered nitrogen-containing heterocyclic ring; 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 A.
Miller Andrew
Whittaker Mark
British Bio-Technology Limited
Macera John Stephen
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