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US 8,410,083 B2Granted
23-substituted bile acids as TGR5 modulators and methods of use thereof
AssigneeIntercept Pharmaceuticals, Inc.
InventorRoberto Pellicciari
Life of this patent
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Abstract
The invention relates to compounds of Formula A: (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.
Claims19
A compound according to formula A:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is hydroxy, substituted or unsubstituted alkyl, or halogen;
- R2 is α-hydroxy;
- R3 is hydrogen, hydroxy, NH(CH2)mSO3H, or NH(CH2)nCO2H;
- R4 is substituted or unsubstituted alkyl, or halogen;
- R5 is unsubstituted or substituted alkyl, or aryl;
- R6 is hydrogen, unsubstituted or substituted alkyl, or R5 and R6 taken together with the carbons to which they are attached form a ring of size 4, 5, or 6 atoms;
- R7 is hydrogen, substituted or unsubstituted alkyl, or hydroxy;
- R8 is hydrogen or substituted or unsubstituted alkyl;
- R9 is hydrogen, substituted or unsubstituted alkyl or taken together R8 and R9 form a carbonyl;
- R10 is R3 or SO3H;
- m is an integer 0, 1, 2, 3, 4, or 5;
- and
- n is an integer 0, 1, 2, 3, 4, or 5.
11 more elements
A method of ameliorating obesity, or insulin sensitivity in a subject in need thereof by administering a compound according to formula A:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is hydrogen, hydroxy, substituted or unsubstituted alkyl, or halogen;
- R2 is α-hydroxy;
- R3 is hydrogen, hydroxy, NH(CH2)mSO3H, or NH(CH2)nCO2H;
- R4 is hydrogen, substituted or unsubstituted alkyl, or halogen;
- R5 is unsubstituted or substituted alkyl, or aryl;
- R6 is hydrogen, unsubstituted or substituted alkyl, or R5 and R6 taken together with the carbons to which they are attached form a ring of size 4, 5, or 6 atoms;
- R7 is hydrogen, substituted or unsubstituted alkyl, or hydroxy;
- R8 is hydrogen or substituted or unsubstituted alkyl;
- R9 is hydrogen, substituted or unsubstituted alkyl or taken together R8 and R9 form a carbonyl;
- and
- R10 is R3or SO3H;
- m is an integer 0, 1, 2, 3, 4, or 5;
- and
- n is an integer 0, 1, 2, 3, 4, or 5.
12 more elements
Dependencies are inferred from the claim text.