FIELD: chemistry.
SUBSTANCE: aminoaryl derivative represented by the chemical formula (1) and exhibiting the activity of a diacylglycerol acyltransferase 2 (DGAT2) inhibitor, a pharmaceutical composition containing it as an active ingredient. The invention relates to an aminoaryl derivative of the general formula (1) or a pharmaceutically acceptable salt or stereoisomer thereof, having inhibitory activity against diacylglycerol acyltransferase 2 (DGAT2). In this formula, each A and D is independently CH or N; each B and E is independently CH, C-halogen, C-halogen-C1-C7 alkyl, or N; R1 is C1-C7 alkyl; R2 is hydrogen or halogen; R3 is -G-J; where G represents C6-C10 aryl, C6-C10 arylene, C6-C10 arylene-C1-C7 alkylene, 5-12-membered heteroaryl or 5-12-membered heteroarylene; J is hydrogen, amino, aminocarbonyl, C1-C7 alkoxy-C1-C7 alkyl, C3-C10 cycloalkyl, C3-C10 cycloalkyloxy, 5-12 membered heterocycloalkyl, C6-C10 aryl, C6-C10 aryloxy, C6-C10 aryl-C1-C7 alkoxy, 5-12-membered heteroaryl, 5-12-membered heteroarylamino, carboxy-C1-C7 alkyl, carboxy-C2-C7 alkenyl, carboxy-C1-C7 alkyl-C6-C10 aryl, carboxy-C1-C7 alkoxy-C6-C10 aryl, carboxy-C1-C7 alkyl - 5-12-membered heterocycloalkyl, carboxy-C2-C7 alkenyl - 5-12-membered heterocycloalkyl, carboxy-C1-C7 alkoxy - 5-12-membered heterocycloalkyl, carboxy-C1-C7 alkylamino-C6-C10 aryl, carboxy-C1-C7 alkyl-C6-C10 aryloxy or carboxy-C1-C7 alkyl - 5-12-membered heteroaryl; where amino, alkyl, alkoxy, cycloalkyl, aryl, heterocycloalkyl, heteroaryl or heteroarylene is optionally substituted with 1-4 substituents selected from halogen, -COOH, C1-C7 alkyl, C1-C7 alkoxy, halogen-C1-C 7 alkyl, C1-C7 alkylsulfonyl and 5-12-membered heteroaryl-C1-C7 alkyl; and heterocycloalkyl, heteroaryl and heteroarylene contain 1-5 heteroatoms selected from N, O and S.
EFFECT: pharmaceutical composition for the treatment of diseases associated with diacylglycerol acyltransferase 2 (DGAT2) containing a compound of formula (1) or a pharmaceutically acceptable salt or stereoisomer as active ingredient together with a pharmaceutically acceptable carrier.
4 cl, 1 tbl, 180 ex
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Authors
Dates
2023-07-12—Published
2020-12-22—Filed