PYRROLOPYRIDINONE DERIVATIVES AS TTX-S BLOCKERS

FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of the following formula (I): [Chem. 1],wherein A is phenyl or 6-membered heteroaryl containing 1 to 2 heteroatoms of N; B is selected from the group consisting of -Calkylene-NR-, -NR- and -(C=O)-; C is selected from the group consisting of -(C=O)- and -NR-; Ris independently selected from the group consisting of: (2) -O-Calkyl wherein alkyl is unsubstituted or substituted by one or more substituents independently selected from R, (3) -O-Ccycloalkyl, where cycloalkyl is unsubstituted, (4) -O-phenyl, wherein phenyl is unsubstituted or is substituted by one or more substituents independently selected from R, (6) -S-phenyl, wherein phenyl is unsubstituted or is substituted by one or more substituents independently selected from R; (7) -NH-Calkyl wherein alkyl is unsubstituted or substituted by one or more substituents independently selected from R, and (9) -O- (5-membered heteroaryl containing 1-2 heteroatoms selected from N), wherein heteroaryl is unsubstituted or substituted by one or more substituents independently selected from R; Rare independently selected from the group consisting of: (1) hydrogen, (2) halogen selected from chlorine, bromine and fluorine, (4) -O-Calkyl, (8) -O-(6-membered heterocyclyl containing 1 N atom), wherein heterocyclyl is unsubstituted or is substituted by one or more substituents independently selected from R, (9) -(C=O)-NRRand (10) -NRR; Rand Rare independently hydrogen or Calkyl; Rare independently selected from the group consisting of: (1) hydrogen and (3) -O-Calkyl; Ris independently hydrogen, Calkyl, Calkoxy, Ccycloalkyl, -NRR, 4-6 membered heterocyclyl containing 1-2 heteroatoms selected from N and O, phenyl, 5-6 membered heteroaryl containing 1-2 heteroatoms selected from N, O and S, phenyl-Calkyl, (5-membered heteroaryl containing 2-3 heteroatoms selected from N) -Calkyl or (6-membered heterocyclyl containing 1-2 heteroatoms selected from N and O) -Calkyl, Rcan form a 5-6-membered ring with R. Values of other radicals are given in the patent claim. Invention also relates to compound of formula (II), compound of formula (III), pharmaceutical composition, condition or disorder treatment method, in which TTX-S channel blockers are involved, use of the compound, method for preparing a pharmaceutical composition, use of the composition.EFFECT: new compounds of formula (I) have been obtained which have blocking activity with respect to potential-dependent sodium