发明名称 ACC INHIBITORS AND USES THEREOF
摘要 The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
申请公布号 US2016185799(A1) 申请公布日期 2016.06.30
申请号 US201414890344 申请日期 2014.05.08
申请人 NIMBUS APOLLO, INC. 发明人 Greenwood Jeremy Robert;Harriman Geraldine C.;Borg George;Masse Craig E.
分类号 C07D513/04;A01N43/90;C07D495/04 主分类号 C07D513/04
代理机构 代理人
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: W is —C(O)—, —C(S)—, or —S(O)2—; Q is —C(O)—, —C(S)—, —S(O)2—, or N; X is —O—, —S—, —NR—, or N; Y is C or N; Z is C or N; R1 is hydrogen or C1-4 aliphatic, optionally substituted with one or more halogens, —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; R2 is halogen, —R, —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, —SO2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, or —SO2R, —B(OR)2, or Hy, where Hy is selected from 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; wherein R2 is not optionally substituted benzyl; or R1 and R2 are taken together to form an optionally substituted 4-7 membered partially unsaturated carbocyclo-, or heterocyclo-, benzo-, or 5-6 membered heteroarylo-fused ring; 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 a 1-6 membered straight or branched bivalent hydrocarbon chain optionally substituted with R5 and R5′; L2 is a covalent bond or a 1-6 membered straight or branched bivalent hydrocarbon chain optionally substituted with R7 and R7′; R3 is halogen, —CN, —OR, —SR, —N(R)2, —N(R)C(O)R, —C(O)RN(R)2, —C(O)N(R)S(O)2R, —N(R)C(O)N(R)2, —N(R)C(O)OR, —OC(O)N(R)2, —N(R)SO2R, —SO2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —SO2R, —B(OR)2, or an optionally substituted ring selected from phenyl or 5-6 membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R4 is hydrogen or a ring 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, or an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; wherein said ring is optionally substituted with n instances of R8; each of R5 and R5′ is independently —R, —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, —SO2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, or —SO2R; or R5 and R5′ are taken together to form a cyclopropylenyl, cyclobutylenyl, or oxetanyl group; each of R7 and R7′ is independently, —R, —OR6, —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, —SO2N(R)2, —C(O)R, —C(O)OR, —OC(O)R, —S(O)R, —SO2R, or —B(OR)2; or R7 and R7′ are taken together to form a 3-8 membered saturated or partially unsaturated monocyclic carbocyclic ring, or a 4-8 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R6 is —R, —C(O)N(R)2, or —C(O)R; each R8 is independently selected from halogen, —R, —OR, —SR, —N(R)2 or deuterium; and n is 0-5.
地址 Cambridge MA US