发明名称 FARNESOID X RECEPTOR MODULATORS
摘要 The present application provides a compound of formula I:;;or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1-R10, m, n, p, and are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.
申请公布号 US2017101434(A1) 申请公布日期 2017.04.13
申请号 US201615288390 申请日期 2016.10.07
申请人 Intercept Pharmaceuticals, Inc. 发明人 Pellicciari Roberto;Gioiello Antimo
分类号 C07J43/00;C07J31/00;C07J9/00 主分类号 C07J43/00
代理机构 代理人
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein: R1 is OH, alkoxy, halogen, or oxo;R2 and R3 are each independently H, OH, halogen, or alkyl optionally substituted with one or more halogen or OH, or R2 and R3 taken together with the carbon atom to which they are attached form a carbonyl;R4 is H, halogen, alkyl optionally substituted with one or more halogen or OH, alkenyl, or alkynyl;R5 and R6 are each independently H, OH, OSO3H, OCOCH3, OPO3H2, or halogen, or R5 and R6 taken together with the carbon atom to which they are attached form a carbonyl;R7 is OH, OSO3H, SO3H, OSO2NH2, SO2NH2, OPO3H2, PO3H2, CO2H, C(O)NHOH, tetrazolyl, oxadiazolyl, thiadiazolyl, 5 -oxo-1,2,4-oxadiazolyl, 5-oxo-1,2,4-thiadiazolyl, oxazolidine-dionyl, thiazolidine-dionyl, 3-hydroxyisoxazolyl, 3-hydroxyisothiazolyl, or 2,4-difluoro-3-hydroxyphenyl;R8, R9, and R10 are each independently H, OH, halogen, or alkyl optionally substituted with one or more halogen or OH, or R8 and R9 taken together with the carbon atoms to which they are attached form a 3- to 6-membered carbocyclic or heterocyclic ring comprising 1 or 2 heteroatoms selected from N, O, and S, or R9 and R10 taken together with the carbon atoms to which they are attached form a 3- to 6-membered carbocyclic or heterocyclic ring comprising 1 or 2 heteroatoms selected from N, O, and S;m is 0, 1, or 2;n is 0 or 1;p is 0 or 1; and is a single or double bond, provided that when each is a single bond, the sum of m, n, and p is 2, R1 is OH, and R8, R9, and R10 are each H, then R7 is not CO2H.
地址 New York NY US