CONDENSED CYCLIC DERIVATIVE WITH INHIBITORY ACTIVITY AGAINST MGAT-2 Russian patent published in 2022 - IPC C07D471/04 C07D471/10 C07D491/20 A61K31/438 A61K31/444 A61K31/497 A61K31/501 A61K31/506 A61K31/527 A61P3/04 A61P3/06 A61P3/10 A61P9/10 A61P43/00 

Abstract RU 2770437 C2

FIELD: medicine.

SUBSTANCE: invention relates to a compound represented by the formula (I) or to its pharmaceutically acceptable salt, where the fragment represented by the formula: is ; where X is C(=O); R1 is hydrogen; R2a is represented by the formula: , where ring C is benzene; each R5 is independently halogen or halogenC1-C4alkyloxy, and n is an integer from 1 to 2, R2b is C1-C4alkyl or halogenC1-C4alkyl, or optionally, R2a and R2b are combined together with an adjacent carbon atom to form ring B, ring B is represented by the formula: , where each R6 is independently halogen, halogenC1-C4alkyl, halogenC1-C4alkyloxy, nonaromatic C3-C6carbocyclyl or nonaromatic heterocyclyl, which is a 4-element monocyclic group containing one heteroatom selected from N and optionally substituted with halogen or halogenC1-C4alkyl, each R14a and R14b are independently hydrogen or halogen, and n is an integer from 1 to 2; R3a is hydrogen, R3b is hydrogen; R4a is carboxy or is represented by the formula: ; L3 is a single bond or C1-C4alkylene, R7 is hydrogen, C1-C4alkylsulfonyl, nonaromatic heterocyclyl, which is a 4-element monocyclic group containing one heteroatom selected from S and optionally substituted with oxo, or nonaromatic C3-C6carbocyclylsulfonyl optionally substituted with C1-C4alkyl, or is represented by the formula: -S(=O)(=N-H)-RS1, R4b is C1-C4alkyl optionally substituted with a substituent of the α group, phenyl optionally substituted with a substituent of the β group, or aromatic heterocyclyl, which is a 5-6-element ring containing one or two identical or different heteroatoms selected from O and N, and optionally substituted by a substituent of the β group, RS1 is C1-C4alkyl, a substituent of the α group is halogen, halogenC1-C4alkyloxy and non-aromatic C3-C6carbocyclyl, and a substituent of the β group is halogen, cyano, C1-C4alkyl, halogenC1-C4alkyl and C1-C4alkyloxy. The invention also relates to a pharmaceutical composition with inhibitory activity against MGAT2, based on the specified compounds of the formula (I).

EFFECT: production of new compounds and a pharmaceutical composition based on them, which can be used in medicine for the treatment or prevention of obesity, metabolic syndrome, hyperlipidemia, hypertriglyceridemia, hyper-VLDL-triglyceridemia, hyperlipoacidemia, diabetes mellitus or arteriosclerosis.

15 cl, 10 tbl, 14 ex

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RU 2 770 437 C2

Authors

Nodu, Kouhei

Tateno, Yusuke

Masuda, Kengo

Nishiura, Yuji

Sasaki, Yoshikazu

Dates

2022-04-18Published

2018-07-13Filed