NOVEL 3-HYDROXY-5-ARYLISOTHIAZOLE DERIVATIVE Russian patent published in 2015 - IPC C07D275/03 C07D417/12 A61K31/425 A61K31/427 A61K31/4439 A61K31/454 A61K31/506 A61P3/10 

Abstract RU 2567755 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula

,

where n equals 1; p equals 0; j is an integer from 0 to 3; k is an integer from 0 to 2; A is a C6-14aryl group which includes phenyl, 2,3-dihydro-1H-indenyl, 6,7-dihydronaphthyl which is optionally substituted with 1-2 L, or a 6-10-member heterocyclic group which includes piperidinyl, 2,3,-dihydrobenzofuranyl, 3,4-dihydro-2H-chromenyl, which is optionally substituted with 1-5 L; ring B is a benzene ring; X is an oxygen atom or -NR7-; R1 is absent; R2 is a hydrogen atom; R3, R4, R5, R6 and R7 are independently a group randomly selected from a hydrogen atom and a C1-6alkyl group; L is independently a halogen atom, a C1-10alkyl group, which is optionally substituted with 1-5 RI substitutes, C1-10alkoxy group, which is optionally substituted with 1-5 RI substitutes, a phenyl group, which is optionally substituted with 1-5 RII substitutes, a 6-member heterocyclic group selected from pyridyl, pyrimidinyl, piperdinyl and 3,6-dihydro-2H-pyranyl, which is optionally substituted with 1-5 RII substitutes, phenoxy, pyridyloxy, which is optionally substituted with 1-5 RII substitutes, a non-aromatic heterocyclic oxy group selected from piperidinyloxy and oxanyloxy, which is optionally substituted with 1-5 RII substitutes, benzyloxy; Ra is a C1-6alkyl group; RI and RII substitutes are as indicated in claim 1 of the invention; or to pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition containing a compound of formula (I) and to intermediate compounds of formula

for producing compounds of formula (I).

EFFECT: compounds of formula (I), having agonistic action on GPR40.

29 cl, 22 tbl, 144 ex

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RU 2 567 755 C2

Authors

Okano Akikhiro

Kosuga Naoto

Okhkouti Munetaka

Khotta Daido

Makabe Muneesi

Dates

2015-11-10Published

2010-12-24Filed