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US 2020/0157076 A1Published application
Acly inhibitors and uses thereof
AssigneeNimbus Artemis, Inc.
InventorsSilvana Marcel Leit de Moradei, Kevin Kreutter, H. James Harwood, Eric Therrien
Life of this patent
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Abstract
The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.
Claims20
A compound of formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- Ring A is a mono-, bi-, or tricyclic ring selected from
- Ring B is a ring selected from phenyl or 5-6 membered heteroaryl having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- Ring C is a ring selected from phenyl or 5-6 membered heteroaryl having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- Ring D is a fused ring selected from benzo or 5-6 membered heteroaro-having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- X1 is a bivalent moiety selected from —CH2—, —CH(R1)—, —C(R1)2—, —C(O)—,
- or —O—;
- each R1 is independently independently hydrogen, —R3, halogen, —CN, —NO2, —OR, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —OPh, —C(R)2Ph, —C(R)2OR, —C(R)2C(O)OR, —C(R)2C(O)NR2, —CH2C(R)2C(O)OR, —CH2C(R)2C(O)NR2, —CH2OPh, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)S(O)2R, or —N(R)S(O)2NR2;
- or two instances of R1 are optionally taken together to form an oxo;
- or R1 at N forms an N-oxide;
- each R is independently hydrogen, or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 4-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or:
- two R groups on the same nitrogen are optionally taken together with their intervening atoms to form a 4-7 membered saturated, partially unsaturated, or heteroaryl ring having 0-3 heteroatoms, in addition to the nitrogen, independently selected from nitrogen, oxygen, and sulfur;
- each R2 is independently hydrogen, —R3, halogen, —CN, —NO2, —OR, —OC(R)2Ph, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —C(R)2OR, —C(R)2C(O)OR, —C(R)2C(O)NR2, —CH2C(R)2C(O)OR, —CH2C(R)2C(O)NR2, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)S(O)2R, or —N(R)S(O)2NR2;
- or two instances of R2 are optionally taken together to form an oxo;
- each R3 is independently an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated carbocyclic ring, a 4-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
- each n is 0, 1, 2, 3, or 4;
- and
- each m is 0, 1, 2, 3, or 4.
15 more elements
Dependencies are inferred from the claim text.