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US 10,149,835 B2Granted
Isoxazole derivatives as FXR agonists and methods of use thereof
AssigneeElmore Patent Law Group, P.C.
InventorsYat Sun Or, Xuechao Xing, Ruichao Shen, Bin Wang, Brett Granger, Jun Ma, Jing He, Jiang Long, Yong He, Guoqiang Wang
Life of this patent
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Abstract
The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR and methods for their preparation and use.
Claims18
A compound represented by Formula I or a pharmaceutically acceptable salt thereof:
- wherein:
- R1 is an optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, or optionally substituted —C3-C8 cycloalkyl;
- R2 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;
- A is optionally substituted aryl or optionally substituted heteroaryl;
- 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;
- R7 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 —C3-C8 cycloalkenyl;
- 6) Optionally substituted aryl;
- 7) Optionally substituted arylalkyl;
- 8) Optionally substituted 3- to 8-membered heterocycloalkyl;
- 9) Optionally substituted heteroaryl;
- 10) Optionally substituted heteroarylalkyl;
- and
- 11) NR8R9;
- wherein R5 and R9 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 arylalkyl, optionally substituted 3- to 8-membered heterocycloalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, alternatively, R8 and R9 are taken together with the nitrogen atom to which they are attached to form an optionally substituted heterocyclic ring.
23 more elements
Dependencies are inferred from the claim text.