发明名称 TETRAHYDROCARBOLINE DERIVATIVE
摘要 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 Rrepresents halogen atom, C1-4 alkyl group, C1-4 alkoxygroup, C1-4 halogenalkyl group, cyanogroup, carbamoyl group, Rrepresents hydrogen atom, Rrepresents C1-4 alkyl group, Rrepresents 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 R(where Rrepresents C1-4 alkyl group or aminogroup), U represents (i) methylene group, (ii)oxygen atom, (iii) -NR- (where Rrepresents 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 R(where Rrepresents 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 R(where Rrepresents 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 R, R, R, R, Rand R, can be similar or different, respectively, and two Ror R, 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
申请公布号 RU2572818(C2) 申请公布日期 2016.01.20
申请号 RU20130104866 申请日期 2011.07.05
申请人 ONO FARMAS'JUTIKAL KO., LTD. 发明人 OKHATA AKIRA;NAKATANI SINGO;SUGIJAMA TETSUJA;MORIMOTO TAKASI
分类号 C07D471/04;A61K31/437;A61K31/4375;A61K31/4545;A61K31/497;A61P11/00;A61P13/00;A61P13/08;A61P17/00;A61P19/02;A61P21/00;A61P29/00;A61P35/00;C07D471/14 主分类号 C07D471/04
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