OXADIAZOLAMINE DERIVATIVES AS HISTONE DEACETYLASE 6 INHIBITOR AND PHARMACEUTICAL COMPOSITION CONTAINING THEM Russian patent published in 2019 - IPC C07D413/04 C07D413/14 C07D271/06 A61K31/4245 A61K31/506 

Abstract RU 2695133 C1

FIELD: medicine; pharmaceuticals.

SUBSTANCE: present invention relates to a compound of an oxadiazolamine derivative of formula I, where R1 is -CF2H or -CF3; L1 and L2 are absent; Z1–Z4, each independently represents N or CRZ {where three or more Z1–Z4 can not simultaneously represent N}, where RZ is -H; R2 is -H; Y1 is -CH2-, -NRc-, where RC is -H, -C(=O)-O(C1-C4alkyl)phenyl; a and b, each independently, is integer of 0, 1, 2, 3 or 4 {where a and b, all can not be 0}; L3 is -(C1-C2alkyl)-, -(C1-C2alkyl)-SO2- or absent; ring B is -phenyl, -heteroaryl (selected from thiophene and pyridine), structure (a), where Z5 and Z6, each independently represents -O-; and R4–R6, each independently represents -H, -F, -Cl, -OH, -O(C1-C4alkyl), -(C1-C4alkyl), -CF3, -OCF3, heterocycloalkyl selected from piperidine and morpholine {where heterocycloalkyl can be unsubstituted or substituted with C1-C4alkyl}, structure (b), where Y2 is -O-, Y3–Y5, each independently represents -CH- or -N-, c–f, each independently, is equal to integer 0, 1, 2 {where c and e, all can not be equal to 0, and d and f, all can not be equal to 0}. Invention also relates to a pharmaceutical composition for preventing or treating histone deacetylase 6 mediated disease containing a therapeutically effective amount of the compound of formula I, and at least one pharmaceutically acceptable carrier.

ring B,

structure (a),

structure (b).

EFFECT: oxadizolamine derivative according to the invention is intended for treating histone deacetylase 6 mediated disease.

10 cl, 3 tbl, 106 ex

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RU 2 695 133 C1

Authors

Kim, Yuntae

Lee, Chang Sik

Oh, Jung Taek

Song, Hyeseung

Choi, Jin

Lee, Jaeyoung

Dates

2019-07-22Published

2016-10-11Filed