TGR5 modulators and methods of use thereof
The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
1. A method of ameliorating diabesity in a subject comprising administering a compound Ih3e according to the chemical structure:
or a pharmaceutically acceptable salt, glycine or taurine amino acid conjugate thereof.
2. The method of claim 1 , further comprising administering at least one pharmaceutically acceptable excipient.
3. The method of claim 1 , wherein the compound is a glycine amino acid conjugate.
4. The method of claim 1 , wherein the compound is a taurine amino acid conjugate.
5. The method of claim 1 , wherein the compound is compound Ih3e.
6. A kit for ameliorating diabesity or improving insulin sensitivity in a subject, wherein the kit comprises a compound Ih3e according to the chemical structure:
or a pharmaceutically acceptable salt, glycine or taurine amino acid conjugate thereof.
7. A method of improving insulin sensitivity in a subject in need thereof comprising administering a compound Ih3e according to the chemical structure:
or a pharmaceutically acceptable salt, glycine or taurine amino acid conjugate thereof.
8. The method of claim 7 , wherein the compound is a glycine amino acid conjugate.
9. The method of claim 7 , wherein the compound is a taurine amino acid conjugate.
10. The method of claim 7 , wherein the compound is compound Ih3e.
11. The method of claim 7 , further comprising administering at least one pharmaceutically acceptable excipient.