OXASPIRO DERIVATIVE, A METHOD FOR PRODUCTION THEREOF AND USE THEREOF IN MEDICINES Russian patent published in 2020 - IPC C07D405/04 C07D405/14 C07D409/14 A61K31/4402 A61K31/4433 A61K31/4436 

Abstract RU 2733373 C2

FIELD: organic chemistry.

SUBSTANCE: present invention relates to a compound of formula (I):

or a tautomer thereof, a mesomer, a racemate, an enantiomer, a diastereomer, or a mixture thereof, or a pharmaceutically acceptable salt thereof. To compound of formula (I) ring A is selected from a group consisting of C3-6 cycloalkyl and 5–6-member heterocyclyl containing one nitrogen atom or one oxygen atom; R is selected from unsubstituted 5–6-member heteroaryl containing one nitrogen atom; each R1 is identical to the other or different from it, and each is independently selected from a group consisting of a hydrogen atom and a halogen atom; each R2 is identical or different from the other and each is independently selected from a group consisting of a hydrogen atom, C1-6 alkyl, C1-6 alkoxy, hydroxyl, oxo, =CH2 and =CH-CN, where each of C1-6 alkyl and C1-6 alkoxy are optionally substituted with one or more groups selected from a group consisting of deuterium, C1-6 alkyl, a halogen atom, cyano, C1-6 alkoxy and C3-6 cycloalkyl; or two R2 together form unsubstituted 5–6 membered heterocyclyl containing two sulfur atoms or two oxygen atoms; p and q each independently represent 0, 1 or 2. Also disclosed is a method of producing a compound of formula (I), a pharmaceutical composition and use of compound (I).

EFFECT: technical result: disclosed is an oxaspiroderivative compound of general formula (I), which can be used as a MOR receptor agonist (μ-opioid receptor).

14 cl, 8 tbl, 31 ex

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RU 2 733 373 C2

Authors

Li Xin

Feng Binqiang

Chen Yang

Liu Tao

He Feng

He Mingxun

Tao Weikang

Sun Piaoyang

Dates

2020-10-01Published

2016-09-30Filed