Back to results
US 2017/0304270 A1Published application
Isoxazole derivatives as fxr agonists and methods of use thereof
AssigneeEnanta Pharmaceuticals, Inc.
InventorsYat Sun Or, Brett Granger, Ruichao Shen, Xuechao Xing, Bin Wang, Jun Ma, Jing He, Jiang Long, Yong He, Guoqiang Wang
Life of this patent
Estimating the term…
Abstract
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 as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.
Claims19
A compound represented by Formula I, or a pharmaceutically acceptable salt thereof:
- wherein,
- R1 is hydrogen, halogen, cyano, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C6 cycloalkyl or optionally substituted 3- to 6-membered heterocycloalkyl;
- R2 is an optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, or optionally substituted C3-C8 cycloalkyl;
- is selected from the group consisting of;
- n is 0 or 1;
- is phenyl or a 5- or 6-membered heterocyclic or heteroaryl containing 1, 2 or 3 heteroatoms independently selected from N, O and S, wherein said phenyl, heterocycle or heteroaryl is optionally substituted with one or two substituents independently selected from substituted or unsubstituted —C1-C8 alkyl, halo, and haloalkyl,
- R3 is:
- R4 and R5 are independently selected from the group consisting of:
- 1) Hydrogen;
- 2) Optionally substituted —C1-C8 alkyl;
- 3) Optionally substituted —C2-C8 alkenyl;
- 4) Optionally substituted —C2-C8 alkynyl;
- and
- 5) Optionally substituted —C3-C8 cycloalkyl;
- R6 is selected from the group consisting of:
- 1) Optionally substituted —C1-C8 alkyl;
- 2) Optionally substituted —C2-C8 alkenyl;
- 3) Optionally substituted —C2-C8 alkynyl;
- 4) Optionally substituted —C3-C8 cycloalkyl;
- 5) Optionally substituted aryl;
- 6) Optionally substituted arylalkyl;
- 7) Optionally substituted heterocycloalkyl;
- 8) Optionally substituted heteroaryl;
- 9) Optionally substituted heteroarylalkyl;
- and
- 10) NR7R8;
- wherein, R7 and R8 are each independently selected from hydrogen, optionally substituted —C1-C8 alkyl, optionally substituted —C2-C8 alkenyl, optionally substituted —C2-C8 alkynyl, optionally substituted —C3-C8 cycloalkyl, optionally substituted aryl, optionally substituted alkylaryl, optionally substituted 3- to 8-membered heterocycloalkyl, optionally substituted heteroaryl, optionally substituted alkylheteroaryl, or R7 and R8 are taken together with the nitrogen atom which they are attached to form an optionally substituted heterocyclic ring.
24 more elements
Dependencies are inferred from the claim text.