Back to results
US 2017/0304271 A1Published application
Isoxazole derivatives as fxr agonists and methods of use thereof
AssigneeEnanta Pharmaceuticals, Inc.
InventorsYat Sun Or, Ruichao Shen, Xuechao Xing, Brett Granger, Bin Wang, Jun Ma, Jing He, Yong He, Jiang Long, 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.
Claims25
A compound represented by Formula I, or a pharmaceutically acceptable salt thereof:
- wherein:
- m is 0, 1, or 2;
- 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 cycloalkyl;
- is optionally substituted aryl or optionally substituted heteroaryl containing 1, 2 or 3 heteroatoms selected from N, O and S;
- R4 is
- R5 and R7 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;
- and
- 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;
- and
- 9) Optionally substituted heteroarylalkyl;
- 10) NR8R9;
- wherein R8 and R9 are each independently selected from hydrogen, substituted or unsubstituted —C1-C8 alkyl, substituted or unsubstituted —C2-C8 alkenyl, substituted or unsubstituted —C2-C8 alkynyl, substituted or unsubstituted —C3-C8 cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, or R8 and R9 are taken together with the nitrogen atom they attached to form a heterocyclic ring.
24 more elements
(canceled)
Dependencies are inferred from the claim text.