VMAT2 inhibitor and preparation method therefor and application thereof
AssigneeLuye Innomind Pharma Shijiazhuang Co., Ltd.
InventorsJingwei Tian, Rui Zhang, Liang Ye, Dawei Yu, Guangying Du, Zongliang Liu, Fangxia Zou, Bo Cui
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Abstract
The present invention relates to a class of compounds that serve as VMAT2 inhibitors, and relates in particular to a compound represented by formula (I), or a stereoisomer or pharmaceutically acceptable salt thereof, and a preparation method therefor, as well as the use thereof in the preparation of a medicament for treating diseases related to VMAT2.
Claims19
A compound represented by formula (I), or a stereoisomer or pharmaceutically acceptable salt thereof,
- wherein
- “- - - ” represents a single bond or a double bond;
- when “- - - ” is a single bond, R is selected from OH, H or
- when “- - - ” is a double bond, R is O;
- R1 is selected from hydrogen, methyl or ethyl;
- R2 is unsubstituted C3-6 cycloalkyl, C3-6 cycloalkyl-C1-6 alkyl, or 3- to 6-membered heterocycloalkyl-C1-3 alkyl, or
- R2 is C3-6 cycloalkyl substituted with 1, 2 or 3 R3, C3-6 cycloalkyl-C1-6alkyl substituted with 1, 2 or 3 R3, or 3- to 6-membered heterocycloalkyl-C1-3 alkyl substituted with 1, 2 or 3 R3, or
- R2 is C2-10 alkyl substituted with 2 or 3 R3;
- and
- R3 is F, Cl, Br, SH or NH2.
A method for preparing a compound of formula (II), comprising the following preparation steps:
- wherein R2 is selected from unsubstituted C3-6cycloalkyl-C1-6alkyl, or, C2-10alkyl substituted with 2 or 3 R3,
- R3 is selected from F, Cl, Br or NH2;
- and
- X is a leaving group.
Dependencies are inferred from the claim text.