BIARYL DERIVATIVES AS AGONISTS GPR120 Russian patent published in 2018 - IPC C07D213/30 A61K31/4412 A61P3/00 A61P29/00 

Abstract RU 2641003 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to diaryl derivatives of the formula 1 , or their pharmaceutically acceptable salts or isomers of formula 1, wherein A and B are independently phenyl or pyridine provided that when B is phenyl, -G-COOR7 is substituted in the para-position of phenyl and, when B is pyridine, -G-COOR7 is substituted in position 3 of pyridine, any of R1-D and R2-E may be absent, D and E are independently carbon, nitrogen, oxygen or sulfur, or represent a direct bond, and any of R1 and R2 may be absent, or R1 is a halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted by C3-C10-alkylsilanyloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted by C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl, R2 is hydrogen, halogen, C1-C6-alkyl, optionally substituted with halogen, C3-C10-cycloalkyl, C1-C6-alkoxy, C1-C6-alkylamino, C3-C10-heterocycloalkyl or C1-C6-alkyl-C3-C10-heterocycloalkyl, C3-C10-cycloalkyl, optionally substituted with C3-C10-alkylsilaniloxy or hydroxy, C2-C6-alkenyl, C2-C6-alkynyl, C3-C10-heterocycloalkyl, optionally substituted with C1-C6-alkylamino or halogen, C1-C6-alkyl-C3-C10-heterocycloalkyl, phenyl, C3-C9-heteroaryl or C1-C6-alkyl-C5-C6-heteroaryl and, when D and E represent nitrogen or carbon, R1 and R2 may represent two or three groups, which may be the same or different, isolated from C1-C6-alkyl or phenyl, G is -J-(CR5C6)p, where J is oxygen or sulfur, R5 and R6 independently represent hydrogen, C1-C6-alkyl or C3-C10-cycloalkyl and R5 and R6, substituted in the one and the same or different carbon atoms, may be bound producing C3-C10-cycloalkyl, R1 and R4 independently from each other may be absent depending on m and n value or independently represent hydrogen, halogen or C1-C6-alkyl, or C1-C6-alkoxy, R7 is hydrogen or C1-C6-alkyl, m and n independently represent an integral number from 0 to 5 and p is an integral number from 2 to 6, where heterocycloalkyl and heteroaryl contain at least one heteroatom, isolated from N, O, and S, to the pharmaceutical composition, containing them, and method of its production.

EFFECT: stimulates the formation of GLP-1 in the gastrointestinal tract and improves insulin resistance in the liver or muscles, effective prevention or treatment of diabetes, complications of diabetes, obesity, non-alcoholic fatty hepatosis, steatohepatitis, osteoporosis or inflammation.

6 cl, 1 tbl, 279 ex

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RU 2 641 003 C2

Authors

Kim Yang Kvan

Park Sang Yun

Dzoo Khiun Voo

Choi Eun Sil

Dates

2018-01-15Published

2014-06-26Filed