AZAINDOLES AS GLUCOKINASE ACTIVATORS Russian patent published in 2016 - IPC C07D471/04 A61K31/437 A61P3/10 

Abstract RU 2593369 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to compounds of formula (I):

where: R1 is phenyl, unsubstituted or mono-or disubstituted independently halogen, cyano, C1-6 alkyl, alkoxy, -SO2CH3, -CF3, -C(CH3)2OH, -CH(CH3)OH, -C(CH3)(C(CH3)2)OH, -SO2(CH2)2OH, -NH(SO2CH3), -C(O)CH3, -C(CH2CH3)2OH, -N(CH3)2, -SO2CH(CH3)2, -SO2(CH2)2OCH2CH3, -SO2(CH2)2N(CH3)2, pyrasol or -SO2(CH2)2-morpholinium, 6-member heteroaryl containing 1 N heteroatom, unsubstituted or substituted C1-6 alkyl, alkoxy or -SO2CH3, or 2,3-dihydrobenzo[1,4]dioxine-6-yl; R2 is C1-6 alkyl, 5-6-member heterocycloalkyl, containing 1 heteroatom selected from O, N, or C3-6-cycloalkyl, unsubstituted or substituted (=O); R3 is hydrogen, halogen, acyl group, cyano, C1-6 alkyl, unsubstituted or mono-, di- or three-substituted independently hydroxy, alkoxy, halogen, C1-6 alkyl, cyano, (=O) or -N(CH3)2, -OCH3, -OCH2C(O)N(CH3)2, -O(CH2)2OCH3, -O(CH2)2N(CH3)2, -OCH(CH3)2, -OC(CH3)2CH2OH, -OCH2CH2OH, -OC(CH3)2C(O)OCH2CH3, -OC(CH3)2C(O)OH, -CH2OC(O)CH2N(CH3)2, -NHC(O)CH2N(CH3)2 or -SO2-C1-6 alkyl; connection between C1 and C2 is single or double bond; X1 represents hydrogen, hydroxy, alkoxy or is absent, if the relationship between C1 and C2 is a double bond; and X2 represents hydrogen or is absent, if the relationship between C1 and C2 is double bond, as well as their pharmaceutically acceptable salts.

EFFECT: mentioned compounds and containing them pharmaceutical compositions are effective for treating metabolic diseases and disorders, such as, for example, type II diabetes mellitus.

35 cl, 4 tbl, 141 ex

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RU 2 593 369 C2

Authors

Bertel Stiven Dzhozef

Chen Li

Korbett Vendi Li

Fen Lichun

Khejns Nensi-Ellen

Kester Robert Frensis

So Sun-Sau

Tilli Dzhefferson Rajt

Dates

2016-08-10Published

2010-12-13Filed