| abstract |
"Pyrolidine-2-Onas as Factor XA Inhibitors". The invention relates to the compounds of formula (I): wherein: R3 represents a group selected from: each of which optionally contains an additional N-heteroatom, Z represents an optional substituent halogen, -CH-2-NH-2 -, -NR4 a ^ R4b4 or -CN, Z <39> represents an optional halogen substituent, -CH-2-NH-2 ~, or -CN, alkyl represents alkylene or alkenylene, T represents S, O or NH; R 2 R 2 represents hydrogen, C 1-3 alkyl-CONR a a R 2 b 4 -C 1-3 alkyl-C 2 2- C 1-4 alkyl-C 1-1 alkyl 3-morpholino, -CO-2-C 1-4 alkyl or -C-1-3 alkyl-CO 2 H; X represents phenyl or a 5- or 6-membered aromatic or non-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, -CN, - C 1-4 alkyl, -C 2-4 alkenyl, -CF -3, -NR 4 a ^ R 4 b ^, NO ~ 2 ~, N (C 1-4 alkyl) ( CHO), -NHCO C 1-4 alkyl-NHSOR 4 C 4, C 0-4 alkyl OR 4 d 4 -C (O) R 4 c 4 -C (O) NR 4 a ^ R ^ b ^, -S (O) ~ n ~ R ~ c ~, and -S (O) ~ 2 ~ NR ^ a ^ R ^ b ^; Y represents (i) a substituent selected from hydrogen, halogen, -CN, C 1-4 alkyl, -C 2-4 alkenyl CF 3, -NR 4 a ^ R 4 b 4, - NO ~ 2 ~, -N (C 1-4 alkyl) (CHO), -NHCO C 1-4 alkyl, NHSO ~ 2 ~ R 4 c 4, C 0-4 alkyl OR 4 d ^, C (O) R ^ c ^, -C (O) NR ^ a ^ R ^ b ^ S (O) ~ n ~ R ^ c ^, or -S (O) ~ 2 ~ NR ^ a ^ R ^ b or (ii) phenyl or a 5- or 6-membered aromatic or non-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, -CN, -C 1-4 alkyl, -CF ~ 3 ~, (CH ~ 2 ~) ~ n ~ NR ^ a ^ R ^ b ^, (CH ~ 2 ~) ~ n ~ N ^ + ^ R ^ a ^ R ^ b ^ CH ~ 2 ~ CONH ~ 2 ~, alkyl C ~ 0-4 ~ OR ^ d ^ -C (O) R ^ c ^, ^ - C (O) NR ^ a ^ R ^ b , -S (O) ~ n ~ R ^ c ^, - S (O) ~ 2 ~ NR ^ a ^ R ^ b ^, = O, oxide to a ring N, CHO, -NO ~ 2 ~, and - N (R 3 a 4) (SO 2 R 2 c); R 2a 2 and R 4 b 4 independently represent hydrogen, C 1-6 alkyl, or together with the N atom to which they are attached form a 5-, 6- or 7-membered heterocyclic ring optionally containing an additional selected heteroatom. of 0, N or S, optionally substituted by C 1-4 alkyl, and optionally heteroatom S is substituted by O that is S (O) - n -; R2 represents C1-6 alkyl; R2 represents hydrogen or C1-6 alkyl; n represents 0-2; and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of the compounds of formula (I), pharmaceutical compositions containing the compounds of formula (I) and the use of the compounds of formula (I) in medicine, specifically in the amelioration of a clinical condition for which they are present. a Factor Xa inhibitor is indicated. |