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US 2016/0096862 A1Published application
TGR5 Modulators and Methods of Use Thereof
AssigneeIntercept Pharmaceuticals, Inc.
InventorRoberto Pellicciari
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Abstract
The invention relates to compounds of Formula A: or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including obesity, insulin sensitivity, inflammation, cholestasis, and bile desaturation.
Claims16
A method of preparing a compound of Formula I
- or a pharmaceutically acceptable salt thereof, wherein:
- R1, R2, and R3 are hydroxy,
- R4 is hydrogen or lower alkyl,
- R5 is methyl, and
- R6 is hydrogen;
- the method comprising the steps of:
- protecting the hydroxy groups of Compound 1 with 3,4-dihydro-2H-pyran to form Compound 2:
- alkylating the C-23 carbon of Compound 2 with methyl iodide followed by treatment with methanolic HCl to form Compound 3:
- and hydrolyzing the ester of Compound 3 with NaOH to form the compound of Formula I.
6 more elements
Dependencies are inferred from the claim text.