1,3,4-OXADIAZOLE DERIVATIVES AS HISTONE DEACETYLASE 6 INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING THEM Russian patent published in 2023 - IPC C07D413/12 C07D413/14 A61K31/454 A61K31/4427 A61P25/00 A61P31/00 A61P3/00 A61P9/00 

Abstract RU 2810081 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a 1,3,4-oxadiazole derivative represented by the chemical formula I, or to a pharmaceutically acceptable salt thereof, where in the chemical formula I Z1-Z4 each independently represents N, CH or CX, where Z1-Z4 is not may be three or more N's at the same time; L, L1 or L2 are each independently -(C0-C2alkylene)-; R1 represents -CX2H or -CX3; R2 represents C6 aryl, wherein at least one -H of C6 aryl can each be independently substituted with -X, -OH, -(C1-C4alkyl) or -O(C1-C4alkyl); R represents or; Ra-Rd are each independently -H or -(C1-C4alkyl); R´ and R˝ are each independently -H, -(C1-C4alkyl), -(C3-C7cycloalkyl), -(C2-C6heterocycloalkyl) containing one O atom or one S atom in the ring, -(C1-C4alkyl)-(C3-C7cycloalkyl), -(C1-C4alkyl)-(C2-C6heterocycloalkyl), containing one O atom in the ring, -C (=O)-(C1-C4alkyl), -C(=O)-(C3-C7cycloalkyl), -C(=O)-O(C1-C4alkyl) or -S( =O)2 -(C1-C4alkyl), wherein at least one -H of -(C1-C4alkyl) or -C(=O)-(C1-C4alkyl) may be is substituted by -X, -OH, -N(CH3)2 or -O(C1-C4alkyl) and at least one -H in the ring of -(C3-C7cycloalkyl) may be substituted by - X, -OH or -(C1-C4alkyl); m or n are each independently 1, 2 or 3; and X represents either F, Cl, Br or I. The invention also relates to a pharmaceutical composition having inhibitory activity against histone deacetylase 6 (HDAC6), based on the specified derivative of Chemical formula I.

EFFECT: obtaining new compounds and a pharmaceutical composition based on them which may have medical applications to prevent or treat HDAC6-mediated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological or neurodegenerative diseases.

9 cl, 2 tbl, 128 ex

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RU 2 810 081 C1

Authors

Li, Chan Kon

Ko, Mu Sun

Yun, Sok Khen

Kim, Khendzhin Majkl

Dates

2023-12-21Published

2021-04-12Filed