PDE4 INHIBITOR Russian patent published in 2021 - IPC C07D471/04 C07D498/04 A61K31/519 A61P29/00 

Abstract RU 2743126 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof:

where X is selected from O, N(R3), -CH(R3)-; R3 is selected from H, COOH, R4-L1- or selected from a group, consisting of C1-6alkyl, C1-6heteroalkyl, C3-6cycloalkyl and phenyl, each of which is optionally substituted with 1, 2 or 3 R; "hetero" in C1-6heteroalkyl is selected from -O-, -C(=O)O- and -S(=O)2; R4 is selected from a group consisting of phenyl and 5–6-member heteroaryl, each of which is optionally substituted with 1 or 2 R; "hetero" in 5–6-member heteroaryl is selected from -NH-; L 1 is selected from -CH2-; each of R1 and R2 is independently selected from H, F, Cl, Br, I, OH, CN, NH2, R5-L2- or selected from a group consisting of C1-6alkyl, C1-6alkoxy, C2-6alkenyl, 3–6 membered heterocycloalkenyl, C3-6cycloalkyl, phenyl, and 5–6-membered heteroaryl, each of which is optionally substituted with 1, 2 or 3 R; "hetero" in 3–6-member heterocycloalkenyl is selected from -NH- and -C(=O)-; "hetero" in 5–6-member heteroaryl is selected from -NH- and -S-; R5 is selected from a group consisting of phenyl and 5–6-member heteroaryl, each of which is optionally substituted with 1, 2 or 3 R; "hetero" in 5–6-member heteroaryl is selected from -NH-; L2 is selected from -CH2- and O; R6 is selected from C1-3alkyl, which is optionally substituted with 1, 2 or 3 R; R is selected from H, halogen, OH, NH2, CN or is selected from a group consisting of C1-6alkyl and C1-6 heteroalkyl, each of which is optionally substituted with 1, 2 or 3 R'; "hetero" in C1-6heteroalkyl is selected from -O- and -C(=O)O-; R' is selected from F, Me, which is a PDE4 inhibitor, as well as its use in preparing a drug preparation for treating PDE4-related diseases.

EFFECT: disclosed is a PDE4 inhibitor.

30 cl, 11 tbl, 78 ex

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RU 2 743 126 C2

Authors

Luo, Yunfu

Yang, Chundao

Lei, Maoyi

Liu, Ling

Hu, Guoping

Li, Jian

Chen, Shuhui

Dates

2021-02-15Published

2017-08-22Filed