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US 2019/0055218 A1Published application
Ahr inhibitors and uses thereof
AssigneeKyn Therapeutics
InventorsAlfredo C. Castro, Catherine Anne Evans
Life of this patent
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Abstract
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
Claims20
A compound of formula I′:
- or a pharmaceutically acceptable salt thereof, wherein:
- Hy is absent or a 5-6 membered heteroaryl ring having 1-2 nitrogens;
- Ring A is selected from phenyl, pyridyl, pyrimdinyl, quinolinyl, naphthalenyl, benzo[1,3]dioxolyl, indolinyl, quinoxalinyl or chromenonyl;
- L2 is
- each Rx is independently hydrogen or C1-4 alkyl;
- Ring B is absent, a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, phenyl, an 8-10 membered bicyclic aromatic carbocyclic ring;
- a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each R1 is independently selected from R, —C(O)R, —C(O)OR, —SO2R, —C(O)N(R)2, or —SO2RN(R)2;
- each R is independently hydrogen, deuterium, or an optionally substituted group selected from C1-6 aliphatic, a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, phenyl, an 8-10 membered bicyclic aromatic carbocyclic ring;
- a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaromatic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-10 membered bicyclic heteroaromatic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- L1 is a covalent bond or an optionally substituted C1-6 membered straight or branched saturated or unsaturated bivalent hydrocarbon chain wherein one methylene unit of L1 is optionally replaced with -Cy-, —O—, —S—, —NR—, —N═N—, —C(O)—, —C(═NR)—, —C(O)O—, —OC(O)—, —C(O)N(R)—, —N(R)C(O)—, —SO2—, —N(R)SO2—, or —SO2N(R)—;
- and
- Cy- is a 3-8 membered bivalent saturated, partially unsaturated, or aromatic monocyclic ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur.
- each of R2 and R3 is independently selected from R, halogen, cyano, nitro, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)N(R)2, —N(R)C(O)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)SO2R, —SO2RN(R)2, —C(O)R, —C(O)OR, —OC(O)R, —C(O)OR, —S(O)R, or —SO2R, or:
- R2 and Rx are taken together to form an optionally substituted 4-7 membered partially unsaturated ring having 0-2 heteroatoms, in addition to the nitrogen to which Rx is attached, independently selected from nitrogen, oxygen, or sulfur;
- or
- R2 and L1 are taken together to form an optionally substituted 4-7 membered partially unsaturated or aromatic ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of m and n is independently 1, 2, 3, 4, or 5;
- and
- p is 0, 1, 2, or 3,
- wherein said compound is other than:
18 more elements
Dependencies are inferred from the claim text.