| abstract |
FIELD: organic chemistry, medicine, pharmacy. n SUBSTANCE: invention relates to novel pyrrolidine-2-ones of the formula (I): , wherein R 1 means group chosen from the following formulae: n n n n n n n n n n n n wherein each of them comprises optionally additional nitrogen (N) atom as a heteroatom; Z means optional substitute halogen atom, -CH 2 NH 2 , -NR a R b or -CN; Z' means optional substitute halogen atom, -CH 2 NH 2 or -CN; alk means alkylene or alkenylene; T means sulfur atom (S), oxygen atom (O); R 2 means hydrogen atom (H), -(C 1 -C 3 )-alkyl-CONR a R b , -(C 1 -C 3 )-alkyl-CO 2 -(C 1 -C 4 )-alkyl, -(C 1 -C 3 )-alkylmorpholino-group, -CO 2 -(C 1 -C 4 )-alkyl or -(C 1 -C 3 )-alkyl-CO 2 H; X means phenyl or 5- or 6-membered aromatic or nonaromatic heterocyclic group comprising one or two heteroatoms chosen from O, N or S wherein each of them is substituted optionally with 0-2 groups chosen from halogen atom, -CN, -(C 1 -C 4 )-alkyl, -(C 2 -C 4 )-alkenyl, -CF 3 , -NR a R b , -NO 2 , -N-(C 1 -C 4 )-alkyl-(CHO), -NHCO-(C 1 -C 4 )-alkyl, -NHSO 2 R c , -(C 0 -C 4 )-alkyl-OR d , -C(O)R c , -C(O)NR a R b , -S(O) n R c and -S(O) 2 NR a R b ; Y means: (i) a substitute chosen from H, halogen atom, -CN, -(C 1 -C 4 )-alkyl, -(C 2 -C 4 )-alkenyl, -CF 3 , -NR a R b , -NO 2 , -N-(C 1 -C 4 )-alkyl-(CHO), -NHCO-(C 1 -C 4 )-alkyl, -NHSO 2 R c , -(C 0 -C 4 )-alkyl-OR d , -C(O)R c , -C(O)NR a R b , -S(O) n R c and -S(O) 2 NR a R b , or (ii) phenyl or 5- or 6-membered aromatic or nonaromatic heterocyclic group comprising one or two heteroatoms, chosen from O, N or S and wherein each of them is substituted optionally with 0-2 groups chosen from halogen atom, -CN, -(C 1 -C 4 )-alkyl, -(CH 2 ) n NR a R b , -(CH 2 ) n N + R a R b CH 2 CONH 2 , -(C 0 -C 4 )-alkyl-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 at N atom in cycle, -CHO, -NO 2 and -N-(R a )(SO 2 R c ) wherein R a and R b mean independently H, -(C 1 -C 6 )-alkyl; R c means -(C 1 -C 6 )-alkyl; R d means H, -(C 1 -C 6 )-alkyl; n means 0-2, and to their pharmaceutically acceptable salts or solvates. Compounds inhibit Xa factor that allows their using as components of pharmaceutical composition. n EFFECT: valuable medicinal properties of compounds and pharmaceutical composition. n 10 cl, 144 ex |