TGR5 modulators and methods of use thereof

Patent metadata

Field	Value
Publication number	US-9540414-B2
Application number	US-201414449995-A
Country	US
Kind code	B2
Filing date	Aug 1, 2014
Priority date	Jul 30, 2008
Publication date	Jan 10, 2017
Grant date	Jan 10, 2017

Abstract

The invention relates to compounds of Formula A:

or a salt, solvate, or hydrate thereof. The compounds of formula A are TGR5 modulators useful for the treatment of disease.

First claim

What is claimed:

1. A compound of formula A:

or a salt thereof, wherein:
R 1 is hydrogen, hydroxy, substituted or unsubstituted alkyl, or halogen;
R 2 is hydrogen or a-hydroxy;
R 4 is substituted or unsubstituted alkyl, or halogen;
R 5 is hydrogen, unsubstituted alkyl, or aryl;
R 6 is hydrogen, unsubstituted or substituted alkyl, or R 5 and R 6 taken together with the carbons to which they are attached form a ring of size 3, 4, 5, or 6 atoms;
R 7 is hydrogen, substituted or unsubstituted alkyl, or hydroxy;
R 11 is hydroxyl, OSO 3 H, OSO 3 − , OCOCH 3 , OPO 3 H, OPO 3 2− or hydrogen;
R 12 is hydroxyl, OSO 3 H, OSO 3 − , OCOCH 3 , OPO 3 H, OPO 3 2− or hydrogen, or taken together R 11 and R 12 form a carbonyl;
m is 0, 1, or 2;
n is 0 or 1;
o is 0 or 1; and
p is 1; provided that
m+n+o=3 or 4 and
when m+n+o=3, then at least one of R 5 and R 6 is not hydrogen.

2. A pharmaceutical composition comprising a compound according to claim 1 and at least one pharmaceutically acceptable excipient.

Assignees

• Intercept Pharmaceuticals Inc

Inventors

• Pellicciari Roberto

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title