DIACYLGLYCEROL-ACYLTRANSFERASE 2 INHIBITORS Russian patent published in 2020 - IPC C07D401/14 A61K31/506 A61P3/10 A61P3/06 A61P1/16 A61P9/10 A61P7/02 A61P19/04 A61P1/04 

Abstract RU 2719589 C1

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a novel compound of formula I and a pharmaceutically acceptable salt thereof. In formula (I)

(I)

D1 is CH; and D2 is N or CH; R1 is H or (C1-C2) alkyl, optionally substituted with one or two substitutes, each of which is independently selected from fluorine; R2 denotes H or fluorine; R3 is , or ; R4 is H, cyano or (C1-C4) alkyl optionally substituted with one substitute, each of which is independently selected from -OH and -S(O)2R6; R5 denotes H or -OH; and R6 is (C1-C4) alkyl. Preferred compound is compound

(I')

of formula (I'). Said compound can be obtained in form of a crystalline form I, having powder X-ray powder (PXRD) peaks at CuKα radiation at 2-theta (°) angle of 5.3, 7.7, 15.4, or in the form of crystalline form II, having X-ray powder pattern (PXRD) peaks at radiation of CuKα at angle 2-theta (°) 6.5, 9.3, 13.6.

EFFECT: compounds inhibit the activity of diacylglycerol acyltransferase 2 (DGAT2) and can be used for treating non-alcoholic fatty dystrophy, non-alcoholic steatohepatitis, hyperlipidemia, diabetes and other diseases associated with DGAT2 activity.

14 cl, 4 dwg, 4 tbl, 8 ex

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RU 2 719 589 C1

Authors

Boehm, Markus

Cabral, Shawn

Dowling, Matthew S.

Futatsugi, Kentaro

Huard, Kim

Lee, Esther Cheng Yin

Li, Qifang

Londregan, Allyn T.

Polivkova, Jana

Price, David A.

Dates

2020-04-21Published

2017-08-09Filed