PYRROLOPYRIDINONE DERIVATIVES AS TTX-S BLOCKERS Russian patent published in 2018 - IPC C07D471/04 A61K31/437 A61P25/00 

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 -C_1-6 alkylene-NR²-, -NR²- and -(C=O)-; C is selected from the group consisting of -(C=O)- and -NR²-; R¹ is independently selected from the group consisting of: (2) -O_n-C_1-6 alkyl wherein alkyl is unsubstituted or substituted by one or more substituents independently selected from R¹¹, (3) -O_n-C_3-7 cycloalkyl, where cycloalkyl is unsubstituted, (4) -O_n-phenyl, wherein phenyl is unsubstituted or is substituted by one or more substituents independently selected from R¹¹, (6) -S-phenyl, wherein phenyl is unsubstituted or is substituted by one or more substituents independently selected from R¹¹; (7) -NH-C_1-6 alkyl wherein alkyl is unsubstituted or substituted by one or more substituents independently selected from R¹¹, and (9) -O_n- (5-membered heteroaryl containing 1-2 heteroatoms selected from N), wherein heteroaryl is unsubstituted or substituted by one or more substituents independently selected from R¹¹; R² are independently selected from the group consisting of: (1) hydrogen, (2) halogen selected from chlorine, bromine and fluorine, (4) -O_n-C_1-6 alkyl, (8) -O_n-(6-membered heterocyclyl containing 1 N atom), wherein heterocyclyl is unsubstituted or is substituted by one or more substituents independently selected from R⁷, (9) -(C=O)-NR⁸R⁹ and (10) -NR⁸R⁹; R³ and R⁴ are independently hydrogen or C_1-6 alkyl; R⁵ are independently selected from the group consisting of: (1) hydrogen and (3) -O_n-C_1-6 alkyl; R⁶ is independently hydrogen, C_1-6 alkyl, C_1-6 alkoxy, C_3-7 cycloalkyl, -NR⁸R⁹, 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-C_1-6 alkyl, (5-membered heteroaryl containing 2-3 heteroatoms selected from N) -C_1-6alkyl or (6-membered heterocyclyl containing 1-2 heteroatoms selected from N and O) -C_1-6 alkyl, R⁶ can form a 5-6-membered ring with R². 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 channels as TTX-S channels and which can be used in the treatment or prevention of disorders and diseases in which potential-dependent sodium channels are involved.

15 cl, 4 tbl, 520 ex