COUMARIN-LIKE CYCLIC COMPOUND AS MEK INHIBITOR AND USE THEREOF Russian patent published in 2021 - IPC C07D491/52 A61K31/436 A61K31/444 A61K31/497 A61K31/5377 A61P35/00 

Abstract RU 2742234 C1

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to a compound represented by formula (I), its pharmaceutically acceptable salt or its tautomer. In formula (I), n is selected from 0, 1 or 2; r is selected from 0, 1, 2 or 3; m is selected from 0 or 1; when m is 0, then is H; ring A is selected from phenyl or 6-member heteroaryl; L is selected from a single bond, -S(=O)-, -S(=O)2-, -C(=O)-, -NH-, -NH-C(=O)-, -NH-C(=O)-O-, -NH-S(=O)2-, -NH-S(=O)-, -NH-C(=O)-NH- and , where -NH-S(=O)2-optionally substituted with 1 R; R 1 is selected from H, NH2, C1–6 alkyl, 4–6-member heterocycloalkyl, C3–6 cycloalkyl and C1–3 heteroalkyl, where each C1–6 alkyl and C1–3 heteroalkyl is optionally 1, 2 R; R2 is selected from H, C1–6 alkyl, C3–6 cycloalkyl and 6-member heterocycloalkyl, where C1–6 alkyl is optionally substituted with 1, 2 or 3 R; R3 is selected from H, F, Cl, Br, I, C 1–3 alkyl; R4 and R5 are independently selected from C1–6 alkyl; R6 and R7 are independently selected from F, Cl, Br, I; R is selected from OH, NH2 and C1–3 heteroalkyl, where NH2 is optionally substituted with 1 R'; R' is selected from C1 C1–3alkyl; each of "hetero" in 6-member heteroaryl, 4–6-member heterocycloalkyl, C1–3heteroalkyl is independently selected from -NH-, N, -O-, -S(=O)2-, -S(=O)2-NH-, - C(=O)-NH-, -C(=O)-; in any of the above cases, the number of heteroatoms and heteroatomic groups is independently selected from 1, 2. Invention also relates to individual compounds, to a pharmaceutical composition and use of the compound.

EFFECT: technical result is obtaining novel compounds of formula (I), having MEK inhibitor properties.

25 cl, 7 tbl, 83 ex

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RU 2 742 234 C1

Authors

Mao, Tsinkhua

Vu, Chende

Khuan, Yun

Gun, Chzhen

Li, Tszyan

Chen, Shukhuej

Dates

2021-02-03Published

2018-06-22Filed