AHR inhibitors and uses thereof
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
1. A compound of formula IV-g:
or a pharmaceutically acceptable salt thereof, wherein:
Hy is a 5-6 membered heteroaryl ring having 1-2 nitrogens;
L 2 is
each R x is independently hydrogen or C 1-4 alkyl;
Ring B is phenyl, or a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
each R 1 is independently hydrogen, deuterium, or optionally substituted C 1-6 aliphatic;
each R is independently hydrogen, deuterium, or optionally substituted C 1-6 aliphatic;
L 1 is a covalent bond; and
each of R 2 and R 3 is independently selected from R, halogen, cyano, nitro, and —OR;
each of m and n is independently 1, 2, 3, 4, or 5; and
p is 0, 1, 2, or 3.
2. The compound according to claim 1 wherein the compound is selected from:
or a pharmaceutically acceptable salt thereof.
3. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.
4. The composition according to claim 3 , further comprising an additional therapeutic agent.
5. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Hy is a 5-membered heteroaryl ring having 1-2 nitrogens.
6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Hy is pyrazolyl, imidazolyl, pyridinyl, or pyrazinyl.
7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is optionally substituted C 1-6 aliphatic.
8. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is unsubstituted C 1-6 aliphatic.
9. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is —CH 3 .
10. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein p is 1.
11. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein
12. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein L 2 is
13. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R x is hydrogen.
14. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein
15. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen.
16. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein L 1 is a covalent bond.
17. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring B is phenyl.
18. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring B is a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur.
19. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Ring B is
20. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 is hydrogen.