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US 2019/0241582 A1Published application
Triazole ACC inhibitors and uses thereof
AssigneeGilead Apollo, LLC
InventorsShomir Gjosh, Jeremy Robert Greenwood, Geraldine C. Harriman, Silvana Marcel Leit De Moradei
Life of this patent
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Abstract
The present invention provides triazole compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
Claims2
A compound of formula I:
- or a pharmaceutically acceptable salt or agriculturally acceptable salt thereof, wherein:
- X is —O—, —S—, or —NR—;
- R1 is hydrogen, C1-4 aliphatic optionally substituted with 1-4 halogen, —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)S(O)2R, —S(O)2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, or —S(O)2R;
- each instance of R2, R6, R7, and R8 is independently oxo;
- halogen;
- —CN;
- —OR;
- —Ra, —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)S(O)2R;
- —S(O)2N(R)2;
- —C(O)R;
- —C(O)OR;
- —OC(O)R;
- —S(O)R;
- or —S(O)2R;
- each R is independently hydrogen or Ra;
- each Ra is independently 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;
- a 1-6 membered straight or branched bivalent hydrocarbon chain;
- cyclopropylenyl;
- cyclobutylenyl;
- or oxetanylenyl;
- L2 is a covalent bond or a 1-6 membered straight or branched bivalent hydrocarbon chain;
- wherein L2 is substituted by n instances of R9;
- R3 is —OR, —C(O)OR, —N(R)C(O)OR, —OC(O)N(R)2, —C(O)N(R)OR, —C(O)NH2, —C(O)NHRa, C(O)N(Ra)2, or —C(O)Hy;
- Hy is a 3-8 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;
- wherein Hy is substituted by p instances of R6;
- R4 is selected from a 3-8 membered monocyclic saturated or partially unsaturated carbocyclic ring, a 4-8 membered monocyclic saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, phenyl, an 8-10 membered bicyclic aryl ring, a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, and an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- wherein R4 is substituted by q instances of R7;
- each R5 is independently hydrogen, C1-4 aliphatic, a 3-8 membered monocyclic saturated or partially unsaturated carbocyclic ring, a 4-8 membered monocyclic saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, phenyl, an 8-10 membered bicyclic aryl ring, a 5-6 membered monocyclic heteroaryl 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;
- wherein each R5 is substituted with r instances of R8;
- each R9 is independently oxo or —OR5;
- m is 0, 1, 2, or 3;
- n is 0, 1, or 2;
- p is 0, 1, 2, 3, or 4;
- q is 0, 1, 2, 3, 4, or 5;
- and
- r is 0, 1, 2, 3, or 4.
41 more elements
-26. (canceled)
Dependencies are inferred from the claim text.