| abstract |
Described are compounds of formula (I) and processes for their preparation, pharmaceutical compositions containing them and their use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated. wherein: R1 represents hydrogen, -C1-6alkyl, -C3-6alkenyl, or a group X-W, wherein X represents -C1-3alkylene and W represents -CN, -CO2H, -CONRbRc, -OCI-6alkyl, -CO2CI-6alkyl, phenyl or a 5-or 6-membered aromatic or non-aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, the phenyl or aromatic heterocyclic group being optionally substituted by one or more substituents selected from: -C1-3alkyl, -C1-3alkoxy, -C1-3alkylOH, halogen, -CN, -CF3, -NH2, -CO-H and OH; R2 and R3 is -C1-3alkyl or -CF3 and the other is hydrogen; Rb and Rc independently represent hydrogen or-C1-3alkyl; A represents a group selected from: Z represents one or two optional substituents independently selected from halogen and OH, W represents an optional substituent -C1-3alkyl, elk represents C2-3alkylene or C2-3alkenylene, T represents a heteroatom selected from O, S or N; B represents one or more optional substituents on ring carbon atoms selected from: (i) one or more substituents selected from -CF3, -F, -CO-H, -C1-6alkyl, -C1-6alkylOH, -(C1-3alkyl)NRbRc, -(C0 3alkyl)CONRbRc and -(C0-3alkyl)CO2C1-3alkyl, -CONHC2-3alkylOH, CH2NHC2-3alkylOH, -CH2OC1-3alkyl and -CH2SO2C1-3alkyl ; (ii) a group-Y-R Y represents -C1-3alkylene-, -CO-, -C1-3alkylNH-, -C1-3alkylNHCO-, -C1-3alkylNHSO2-, CH2NHSO2CH2-or a direct link, Re represents phenyl, a 5-or 6-membered cycloalkyl or a 5-or 6-membered heterocycle containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by one or more substituents selected from : -C1-3alkyl, -C1-3alkoxy, -C1-3alkylOH, halogen, -CN, -CF3, -NH2,-CO2H and -OH; or (iii) a second ring Rf, which is fused to the heterocyclic ring, wherein Rf represents phenyl, a 5-or 6-membered cycloalkyl group or a 5-or 6-membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, and the fused bicyclic group is optionally substituted by one or more substituents selected from:-C1 3alkyl, -C1-3alkoxy, -C1-3alkylOH, halogen, -CN, -CF3, -NH2,-CO2H and-OH; and pharmaceutical acceptable derivatives thereof. |