发明名称 BILE ACID ANALOGS AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF
摘要 The present invention provides compounds of Formula I:;;pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
申请公布号 US2016229886(A1) 申请公布日期 2016.08.11
申请号 US201615041811 申请日期 2016.02.11
申请人 ENANTA PHARMACEUTICALS, INC. 发明人 Shen Ruichao;Or Yat Sun;Wang Guoqiang
分类号 C07J41/00;C07J43/00 主分类号 C07J41/00
代理机构 代理人
主权项 1. A compound represented by Formula I or pharmaceutically acceptable salt, solvate, hydrate, ester or prodrug thereof:wherein: R1 is selected from the group consisting of: 1) Hydrogen;2) Substituted or unsubstituted —C1-C8 alkyl;3) Substituted or unsubstituted —C2-C8 alkenyl;4) Substituted or unsubstituted —C2-C8 alkynyl;5) Substituted or unsubstituted —C3-C8 cycloalkyl;6) Substituted or unsubstituted aryl;7) Substituted or unsubstituted arylalkyl;8) Substituted or unsubstituted heterocycloalkyl;9) Substituted or unsubstituted heteroaryl; and10) Substituted or unsubstituted heteroarylalkyl; Ra, Rb, and Rc are each independently selected from R1; or Ra and Rb, or Ra and Rc, or Rb and Rc are taken together with the two nitrogen atoms to which they are attached and the intervening carbon atom to form a heterocyclic, heteroaryl or heterocycloalkenyl ring; R2 is selected from the group consisting of: 1) Hydrogen;2) Halogen;3) Substituted or unsubstituted —C1-C8 alkyl;4) Substituted or unsubstituted —C2-C8 alkenyl;5) Substituted or unsubstituted —C2-C8 alkynyl;6) Substituted or unsubstituted arylalkyl; and7) Substituted or unsubstituted aryl; m is 0, 1, 2 or 3; R3 is hydrogen, hydroxyl, —OSO3H, —OSO3−, —OAc, —OPO3H2 or —OPO32−; R4 is hydrogen, halogen, CN, N3, hydroxyl, —OSO3H, —OSO3−, —OAc, —OPO3H2, —OPO32−, —SR2 or —NHR2, wherein, R2 is as defined previously; or R3 and R4 are taken together with the carbons to which they are attached to form —CH═CH—, a cycloalkyl ring or a heterocycloalkyl ring; R5 and R6 are each independently selected from hydrogen or hydroxyl protecting group; and R7 is selected from the group consisting of: 1) Hydrogen;2) Halogen;3) Substituted or unsubstituted —C1-C8 alkyl;4) Substituted or unsubstituted —C2-C8 alkenyl;5) Substituted or unsubstituted —C2-C8 alkynyl; and6) Substituted or unsubstituted —C3-C8 cycloalkyl.
地址 WATERTOWN MA US