1,3,4-OXADIAZOLE DERIVATIVES AS HISTONE DEACETYLASE 6 INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING THEM Russian patent published in 2022 - IPC C07D413/04 C07D413/14 C07D417/14 A61K31/443 A61K31/4439 A61P25/00 A61P27/02 A61P3/00 A61P31/00 

Abstract RU 2763936 C1

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to 1,3,4-oxadiazole derivatives described by formula I, their optical isomers or their pharmaceutically acceptable salts. In the formula I: X, Y and Z all mean CR3 independently; L means -(C1-C6 alkylene)-, -(C2-C6 alkenylene)-, -(C=O)-(C1-C4 alkylene)-, -(C=O)O-(C1-C4 alkylene)-,-(C=O)NH-(C1-C4 alkylene)-, -O(C=O)-(C1-C4 alkylene)- or an ordinary bond, where at least one H group - (C1-C6 alkylene)-, -(C2-C6 alkenylene)-, -(C=O)-(C1-C4 alkylene)-, -(C=O)O-(C1-C4 alkylene)-, -(C=O)NH-(C1-C4 alkylene)- and -O(C=O)-(C1-C4 alkylene)- can be substituted with phenyl; R1 means hydrogen, -C1-C6 alkyl, -C2-C6 alkenyl, -C3-C8 cycloalkyl, hetero cycloalkyl, benzyl, aryl, heteroaryl or -NR4R5, where at least one H of aryl or heteroaryl can be replaced by a group of -C1-C6 alkyl, -C2-C6 alkenyl, -C1-C6 haloalkyl, -C1-C6 alkoxy group, halogen, nitro group, -CF2H, -CF3 or -S(=O)2-R9; R2 means -CF2H or -CF3; R3 means hydrogen; R4 and R5 all independently mean H or -C1-C6 alkyl; and R9 means H or -C1-C6 alkyl. A pharmaceutical composition and a method for inhibiting histone deacetylase 6 (HDAC6) have also been proposed.

EFFECT: proposed compounds have inhibitory activity with respect to histone deacetylase 6 and are effective for the prevention or treatment of HDAC6-related diseases.

[Formula I ]

9 cl, 2 tbl, 59 ex

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RU 2 763 936 C1

Authors

Lee, Chang Sik

Oh, Jung Taek

Yun, Hokeun

Song, Hyeseung

Kim, Hyunjin Michael

Dates

2022-01-11Published

2019-07-25Filed