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US 11,691,963 B2Granted
6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
AssigneeAjax Therapeutics, Inc.
InventorsCraig E. Masse, Jeremy R. Greenwood, Sayan Mondal, Jiayi Xu, Phani Ghanakota, Fiona Michelle McRobb, Nicholas Boyles
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Abstract
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Claims30
A compound of Formula I-1:
- or a pharmaceutically acceptable salt thereof, wherein:
- W is CRw or N;
- X is CRx or N;
- Y is CRy or N;
- Z is —O— or —NRz;
- Rw, Rx, and Ry are each independently hydrogen, halogen, —OR3, —N(R3)2, —SR3, optionally substituted C1-6 aliphatic, or —CN;
- Rz is hydrogen or optionally substituted C1-6 aliphatic;
- R1 is —N(R)2, —N(R)C(O)R′, —C(O)N(R)2, or —N(R)C(O)N(R)2;
- R2 is optionally substituted C1-6 aliphatic;
- R3 is hydrogen or optionally substituted C1-6 aliphatic;
- Ring A is optionally substituted 5- to 6-membered monocyclic heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, optionally substituted 8- to 10-membered bicyclic heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic carbocyclyl, optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic heterocyclyl having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or optionally substituted 7- to 10-membered saturated or partially unsaturated bicyclic heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- L is a covalent bond or a bivalent C1-3 straight or branched hydrocarbon chain;
- Ra is hydrogen, halogen, optionally substituted C1-6 aliphatic, optionally substituted phenyl, optionally substituted 5- to 6-membered monocyclic heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic carbocyclyl, optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic heterocyclyl having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or optionally substituted 7- to 10-membered saturated or partially unsaturated bicyclic heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- each R is independently hydrogen, optionally substituted C1-6 aliphatic, optionally substituted 3- to 7-membered saturated or partially unsaturated carbocyclyl, or optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic heterocyclyl having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or two R when attached to the same nitrogen atom are taken together form an optionally substituted 3- to 7-membered saturated or partially unsaturated monocyclic heterocyclyl having 0-2 additional heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- and
- each R′ is independently optionally substituted C1-6 aliphatic or optionally substituted 3- to 7-membered saturated or partially unsaturated carbocyclyl.
13 more elements
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.