| abstract |
The invention relates to compounds of formula (I), wherein: R1 represents hydrogen or -C¿1-3?alkylCONR?aRb¿; One of R?2 and R3¿ represents -C¿1-3?alkyl and the other represents hydrogen; R?4¿ represents hydrogen, -C¿1-4?alkyl, -C3-4alkenyl, -C2-4alkylOH, -C2-4alkylOC1-4alkyl, -C1-4alkylCN or -C0-4alkylC3-6cycloalkyl; R?5¿ represents -C¿2-4?alkylOH, -C1-4alkyl, -C2-4alkylOC1-4alkyl, -C1-4alkylCN, -C1-4alkylCONR?cRd¿, -C¿2-4?alkylNR?aRb¿, -C¿2-4?alkylNHCOC1-3alkyl, -C2-4alkylNHCONR?aRb¿, -C2-4alkylNHSO¿2R?e, -C¿2-4?alkylSO2NR?aRb¿, -C¿2-4?alkylNHCO2C1-4alkyl, -C2-4alkylNHC(NH2)=NR?f¿, or a group X-Y; X represents -C¿1-4?alkylene- optionally substitued by -OH, or a direct link, with the proviso that when X is substituted by -OH, X represents C2-4alkylene and the -OH group is not alpha with respect to the amide N atom to which the group X is attached; Y represents -C3-6cycloalkyl, phenyl, or an aromatic or non-aromatic 5-, 6- or 7-membered heterocyclic group containing at least one heteroatom selected from O, N or S and optionally substituted at C and/or N atoms by -C1-3alkyl, C1-3alkoxy, C1-3alkylOH, halogen, -CN, -CF3, -NH2, -CO2H and -OH; R?a and Rb¿ independently represent hydrogen or -C¿1-4?alkyl; R?c and Rd¿ independently represent hydrogen or -C¿1-4?alkyl or together with the N atom to which they are attached form a non-aromatic 5-, 6- or 7- membered heterocyclic group optionally substituted by a heteroatom selected from O, N or S; R?e¿ represents -C¿1-4?alkyl or -CF3; R?f¿ represents NO¿2? or CN; R?6¿ represents a group selected from: (i), (ii), (iii), (iv), (v), Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents a heteroatom selected from S or N; and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated. |