发明名称 HETEROARYL COMPOUNDS AND USES THEREOF
摘要 The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
申请公布号 US2016159774(A1) 申请公布日期 2016.06.09
申请号 US201514957761 申请日期 2015.12.03
申请人 Celgene Avilomics Research, Inc. 发明人 Schwartz C. Eric;Surapaneni Sekhar S.;Worm Karin Irmgard
分类号 C07D401/14;C07D403/14;C07D487/08;C07D405/14 主分类号 C07D401/14
代理机构 代理人
主权项 1. A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: Ring A is a saturated 4-8 membered monocyclic or bridged heterocyclic ring having one —N(R1)—, a saturated 7-11 membered spirofused heterocyclic ring having one —N(R1)—, or a saturated 8-10 membered bicyclic heterocyclic ring having one —N(R1)—, wherein Ring A is substituted with 0-3 Rv groups;R1 is -L-Y, wherein:L is an optionally substituted bivalent C2-8 unsaturated, straight or branched, hydrocarbon chain, wherein one, two, or three methylene units of L are optionally and independently replaced by cyclopropylene, —N(R)—, —N(R)C(O)—, —C(O)N(R)—, —N(R)SO2—, —SO2N(R)—, —O—, —C(O)—, —OC(O)—, —C(O)O—, —S—, —SO—, —SO2—, —C(═S)—, —C(═NR)—, —N═N—, or —C(═N2)—; andY is hydrogen, halogen, —CN, C1-6 aliphatic optionally substituted with oxo, halogen, or CN, or a 3-10 membered monocyclic or bicyclic, saturated, partially unsaturated, or aryl ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, and wherein said ring is substituted with 1-4 groups independently selected from -Q-Z, oxo, —NO2, halogen, —CN, and C1-6 aliphatic, wherein: Q is a covalent bond or a bivalent C1-6 saturated or unsaturated, straight or branched, hydrocarbon chain, wherein one or two methylene units of Q are optionally and independently replaced by —N(R)—, —S—, —O—, —C(O)—, —SO—, or —SO2—; andZ is hydrogen or C1-6 aliphatic optionally substituted with oxo, halogen, or CN;Ring B is a saturated 5-7-membered heterocyclo ring having 1-2 nitrogen atoms, wherein Ring B is substituted with 0-5 Rx groups;W is —N(R2)CH2— or —NH—;R2 is selected from hydrogen, C1-6 aliphatic or —C(O)R;R3 and R4 are each independently selected from hydrogen or halogen;each R group is independently hydrogen or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated carbocyclic ring, a 4-7 membered heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;Ry is hydrogen, halogen, —CF3, or C1-4 aliphatic;each Rx is independently oxo, halogen, —OR, —N(R)2, —S(O)xR, —N(R)(CH2)qN(R)2, —N(R)(CH2)qOR, —O(CH2)qOR, —O(CH2)qN(R)2, an optionally substituted C2-6 saturated, straight or branched, hydrocarbon chain wherein one or two methylene units are independently replaced by —O—, —N(R)— or —S(O)x—, or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-7 membered saturated or partially unsaturated carbocyclic ring, a 4-7 membered heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;each Rv is independently selected from halogen or C1-6 aliphatic;q is 1 or 2; andeach x is 0, 1 or 2.
地址 Bedford MA US