发明名称 SUBSTITUTED 4-{ 3-[6-AMINO-9-(3,4-DIHYDROXY-TETRAHYDRO-FURAN-2-YL)-9H-PURIN-2-YL]-PROP-2-YNYL} -PIPERIDINE-1-CARBOXYLIC ACID ESTERS AS A2AR AGONISTS
摘要 Disclosed are 4-{ 3-[6-amino-9-(3,4-dihydroxytetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl} -piperidine-1-carboxylic acid esters as represented by the general formulae I, II and III, wherein R1 and R2 independently are selected from H and C1-3alkyl; Z is selected from cyclopropyl, cyclobutyl, cyclopentyl, tetrahydrofuranyl, azetidin-2-onyl, pyrrolidinyl, and pyrrolidin-2-onyl; Z1 is selected from tetrahydrofuranyl, azetidin-2-onyl, pyrrolidinyl, and pyrrolidin-2-onyl; wherein Z and / or Z1 are optionally substituted with 1 or 2 Z2 substituents; R4 is selected from CH2OR and C(O)NRR; each R independently is selected from H, alkyl, cyclobutyl, and (CH2)acyclopropyl; q is selected from 1, 2, and 3; and wherein the remaining substituents are as defined herein. Also disclosed is a pharmaceutical composition which comprises a compound as defined above, or a stereoisomer and / or pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, for the treatment of inflammation.
申请公布号 NZ586670(A) 申请公布日期 2012.10.26
申请号 NZ20080586670 申请日期 2008.12.20
申请人 FOREST LABORATORIES HOLDINGS LIMITED 发明人 THOMPSON, ROBERT;BEAUGLEHOLE, ANTHONY;SCHMIDTMANN, FRANK;RIEGER, JAYSON
分类号 A61K31/52;A61K31/7052;A61K31/7056;C07H19/16 主分类号 A61K31/52
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