发明名称 Farnesoid X receptor modulators
摘要 The present invention provides a compound of formula (I):; or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
申请公布号 US9611289(B2) 申请公布日期 2017.04.04
申请号 US201414120366 申请日期 2014.05.14
申请人 Intercept Pharmaceuticals, Inc. 发明人 Pellicciari Roberto
分类号 A61K31/56;C07J9/00;C07J41/00;C07J31/00;C07J71/00 主分类号 A61K31/56
代理机构 Cooley LLP 代理人 Cooley LLP ;Elrifi Ivor R.;Erlacher Heidi A.
主权项 1. A compound of formula I:or a pharmaceutically acceptable salt or amino acid conjugate thereof, wherein: R1 is beta-hydroxyl; R2 is hydrogen, hydroxyl, alkyl, or halogen, wherein said alkyl is unsubstituted or substituted with one or more Ra; R3 is hydrogen, hydroxyl, alkyl, or halogen, wherein said alkyl is unsubstituted or substituted with one or more Rb; R4 is alkyl, alkenyl, alkynyl, or halogen, wherein said alkyl is unsubstituted or substituted with one or more Rc; Ra, Rb, and Rc are each independently halogen or hydroxyl; R5 is hydroxyl, OSO3H, OSO3−, O(CO)CH3, OPO3H2, OPO32−, or hydrogen; and R6 is hydroxyl, OSO3H, OSO3−, O(CO)CH3, OPO3H2, OPO32−, or hydrogen; or taken together R5 and R6 with the carbon atom to which they are attached form a carbonyl.
地址 New York NY US