TGR5 modulators and methods of use thereof
The application relates to compounds of formula A: or a salt, solvate, ester, tautomer, amino acid conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
1. A compound selected from the group consisting of:
Cmpd
No.
Chemical Structure
1
2
3
4
5
6
7
8
9
10
11
12
17
18
19
20
21
22
23
25
26
and
27
or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof.
2. The compound of claim 1 , wherein the compound is selected from the group consisting of:
Cmpd
No.
Chemical Structure
1
2
3
4
5
6
7
8
9
10
and
22
or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof.
3. The compound of claim 1 , wherein the compound is selected from the group consisting of:
Cmpd
No.
Chemical Structure
11
12
17
and
18
or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof.
4. The compound of claim 1 , wherein the compound is selected from the group consisting of:
Cmpd
No.
Chemical Structure
19
20
and
21
or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof.
5. The compound of claim 1 , wherein the compound is selected from the group consisting of:
Cmpd
No.
Chemical Structure
23
25
26
and
27
or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof.
6. A pharmaceutical composition comprising the compound of claim 1 or a pharmaceutically acceptable salt, ester, tautomer, or amino acid conjugate thereof, and at least one pharmaceutically acceptable excipient.