TETRAHYDROCARBOLINE DERIVATIVE Russian patent published in 2016 - IPC C07D471/04 C07D471/14 A61K31/437 A61K31/4375 A61K31/4545 A61K31/497 A61P11/00 A61P13/00 A61P13/08 A61P17/00 A61P19/02 A61P21/00 A61P29/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: claimed invention relates to field of organic chemistry, namely to novel heterocyclic compounds of general formula (I) and to its pharmaceutically acceptable salt or its solvate, where R¹ represents halogen atom, C1-4 alkyl group, C1-4 alkoxygroup, C1-4 halogenalkyl group, cyanogroup, carbamoyl group, R² represents hydrogen atom, R³ represents C1-4 alkyl group, R⁴ represents hydrogen atom or C1-4 alkyl group, ring A represents (i) C3-6 monocyclic carbon ring, including phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cyclohexene, (iii) 5-6-membered monocyclic heterocyclic ring, containing one-two heteroatoms, selected from oxygen atom, nitrogen atom and sulphur atom, including thiophene, furan, isoxazole, imidazole, pyrazole, thiazole, pyridine or (iv) 9-membered bicycic heterocyclic ring, including indole, X represents nitrogen atom or carbon atom, T represents bond or linear C1-4 alkylene group, C2-4 alkenylene group or C2-4 alkinylene group, optionally substituted with two R⁵ (where R⁵ represents C1-4 alkyl group or aminogroup), U represents (i) methylene group, (ii)oxygen atom, (iii) -NR⁶- (where R⁶ represents hydrogen atom or methyl group) or (iv) 3-6-membered monocycle, including cyclobutane, cyclopentane, cyclohexane, phenyl, thiophene, pyrrolidine, pyrazole, imidazole, triazole, oxazole, piperazine, piperidine, tetrahydropyridine C7-8 bridge carbon ting, including bicyclooctane, bicycloheptane and imidazolidine, optionally substituted with one-three R⁷ (where R⁷ represents halogen atom, C1-4 alkyl group; hydroxygroup, C1-4 alkoxygroup or benzyloxy group), Y represents (i) bond or (ii) linear C1-3 alkylene group, optionally substituted with one or two R⁸ (where R⁸ represents methyl group), W represents bond or linear C1-3 alkylene group; Z represents methylene group, oxygen atom or sulphur atom, q represents integer number 1, r represents integer number from 0 to 5, and t represents integer number from 0 to 2, on condition that groups, represented by set R¹, R², R³, R⁵, R⁷ and R⁸, can be similar or different, respectively, and two R³ or R⁵, bound with one and the same carbon atom, can be taken together with carbon atom with formation of C3cycloalkyl, respectively. Invention also relates to pharmaceutical composition, pharmaceutical preparation and ENPP2 inhibitor, based on formula (I) compound.

EFFECT: novel compounds, possessing inhibiting activity with respect to ENPP2, have been obtained.

29 cl, 2 dwg, 3 tbl, 937 ex