发明名称 Arylalkene derivatives and use thereof as selective estrogen receptor modulators
摘要 The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.;
申请公布号 US9309211(B2) 申请公布日期 2016.04.12
申请号 US201214369936 申请日期 2012.12.28
申请人 Centaurus Biopharma Co., Ltd. 发明人 Xiao Dengming;Zhu Li;Hu Yuandong;Yu Rong;Hu Wei;Zhao Na;Peng Yong;Luo Hong;Han Yongxin
分类号 C07D307/82;C07D307/79;C07D307/80;C07D307/81;C07D405/06;C07D405/12;C07D405/14;C07D307/76;C07C217/64;C07D213/61;C07D213/64;C07D401/12;C07D333/16;C07D333/28 主分类号 C07D307/82
代理机构 Fox Rothschild LLP 代理人 Fox Rothschild LLP
主权项 1. A compound of formula I: wherein R1 is  wherein the 5-membered ring is optionally and independently substituted with one or more groups selected from the group consisting of halogen, —OH, —SH, alkyl, halogenated alkyl and alkoxy; and R0 is alkyl; wherein R0 is optionally and independently substitued with one or more groups consisting of halogen, —OH, —NH2, and alkoxy; ring A and ring B are each independently selected from aryl and pyridinyl; R2 is selected from halogen, —OH, alkyl, alkoxy, alkysulfanyl, monoalkylamino and dialkylamino, wherein the alkyl, alkoxy, alkylsulfanyl, monoalkylamino and dialkyamino groups are each optionally and independently substituted with —NR4R5, wherein R4 and R5 are each independently hydrogen, alkyl or cycloalkyl, or R4 and R5, together with the nitrogen atom to which they attach, form a hetrocyclyl which is optionally substituted with alkyl; and R3 is selected from the group consisting of halogen, —OH, —NH2, —CN, —SH, —COOH, alkyl, cycloalkyl, alkoxy, alkylsulfanyl, monoalkylamino, and dialkylamino, wherein the alkyl, cycloalkyl, alkoxy, alkylsulfanyl, monoalkylamino, and dialkylamino, are each optionally substituted with —OH or —NR4R5, wherein R4 and R5 are each independently hydrogen, alkyl or cycloalkyl, or R4 and R5, together with the nitrogen atom to which they attach, form a heterocyclyl which is optionally substituted with alkyl; m and n are the number of groups R2 on ring A and the number of groups R3 on ring B, respectively, and m is selected from 1, 2 or 3 and n is selected from 0, 1, 2 or 3, or a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer or prodrug thereof.
地址 Beijing CN