COMPOUND WHICH IS PRO-DRUG OF LANOSTEROL, AS WELL AS METHOD FOR PRODUCTION THEREOF AND USE THEREOF Russian patent published in 2020 - IPC C07J9/00 A61K9/08 A61K31/575 A61P27/12 

Abstract RU 2720677 C1

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to compounds of formula (I), (II) or (III), a pharmaceutically acceptable salt or stereoisomer thereof,

where m equals 0 or 1, wherein if m equals 0, fragment is absent; n equals 0; R1 denotes C1 alkyl-O-C(=O)-C2 alkyl-NH-; R2 denotes phenyl-O-; R3 is selected from a group consisting of 6-member aryl and 5–10-member heteroaryl, each of which is optionally substituted with 1 or 2 R, but R3 is not phenyl and ; wherein in R3, when R is NO2, 6-member aryl or 5–10-member heteroaryl is optionally substituted with 1 R; R5 is H; R6 is H; R7 denotes H or phenyl; R8 is H; R9 is H; each of R independently represents F, NO2, OH, CN, CH3, CF3 or CH3C(=O)-O-; Hetero in 5–10-member heteroaryl is independently selected from a group consisting of N and -O-; wherein in any of the above cases, the number of heteroatoms or heteroatom-containing groups independently represents 1, 2 or 3. Compounds presented by a group of specific compounds, a pharmaceutical composition and use are also disclosed.

EFFECT: technical result is obtaining novel organic compounds which are characterized by higher penetrating power than lanosterol, and which are used in preparing a drug preparation for treating cataract.

9 cl, 6 dwg, 9 tbl

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RU 2 720 677 C1

Authors

Liu, Yizhi

Wang, Yandong

Li, Xiaolin

Luo, Zhi

Shen, Liang

Hou, Lijuan

Wen, Xinxin

He, Haiying

Li, Jian

Chen, Shuhui

Dates

2020-05-12Published

2018-01-25Filed