3- SULFONYLAMINO- PYRROLIDINE- 2- ONE DERIVATIVES AS INHIBITORS OF FACTOR XA

摘要

The invention relates to compounds of formula (I): wherein: R<1> represents a group selected from: formula (II), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, alk represents alkylene or alkenylene, T represents S, O or NH; R<2> represents hydrogen, -C1-6alkyl, -C1-3alkylCONR<a>R<b>, -C1-3alkylCO2C1-4alkyl, -CO2C1-4alkyl or -C1-3alkylCO2H; R<a> and R<b> independently represent hydrogen, -C1-6alkyl, or together with the N atom to which they are bonded form a 5-, 6- or 7- membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S, optionally substituted by C1-4alkyl, and optionally the S heteroatom is substituted by O, i.e. represents S(O)n; n represents 0-2; X represents phenyl or a 5- or 6- membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from: halogen, -C1-4alkyl, -C2-4alkenyl, -CN, -CF3, -NR<a>R<b>, -C0-4alkylOR<e>, -C(O)R<f> and -C(O)NR<a>R<b>; Re represents hydrogen or -C1-6alkyl; R<f> represents -C1-6alkyl; Y represents a group -C(R<x>)(R<z>)C0-2alkylNR<c>R<d>; Rx represents C1-4alkyl optionally substituted by halogen (e.g. CF3, -CH2CF3); R<z> represents hydrogen or C1-4alkyl optionally substituted by halogen (e.g. CF3, -CH2CF3); R<c> and R<d> independently represent hydrogen, -C1-6alkyl, -C1-4alkylOH, or together with the N atom to which they are bonded form a 4-, 5-, 6- or 7- membered non-aromatic heterocyclic ring, the 5-, 6- or 7- membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S, optionally substituted by C1-4alkyl; and/or pharmaceutically acceptable derivative 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.