发明名称 ERK inhibitors and uses thereof
摘要 Compounds, compositions thereof, and methods for inhibiting one or both ERK1 and ERK2 kinases are provided.
申请公布号 US9561228(B2) 申请公布日期 2017.02.07
申请号 US201414768190 申请日期 2014.02.07
申请人 Celgene Avilomics Research, Inc. 发明人 Haq Nadia;Niu Deqiang;Petter Russell C.;Qiao Lixin;Singh Juswinder;Zhu Zhendong
分类号 A61K31/505;A61K31/506;C07D239/48;C07D401/12;C07D401/14;C07F9/6558;C07D495/04;C07D403/12;C07D405/12;A61K31/5377;A61K31/541;A61K31/675 主分类号 A61K31/505
代理机构 Choate, Hall & Stewart—LLP 代理人 Choate, Hall & Stewart—LLP ;Buteau Kristen C.;Nihan Danielle M.
主权项 1. A compound of formula II-a: or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from: each R2 is independently hydrogen, an optionally substituted C1-6 aliphatic, halogen, or —OR; Ring B is an optionally substituted group selected from a 3-7 membered saturated or partially unsaturated carbocyclic ring, a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 4-7 membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 7-12 membered bicyclic saturated, partially unsaturated or aryl ring, a 7-12 membered bicyclic saturated or partially unsaturated heterocyclic ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered bicyclic heteroaryl ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each R3 is independently selected from —R, —Cy, halogen, —OR, —SR, —CN, —NO2, —SO2NR, —SO2R, —SOR, —C(O)R, —C(O)OR, —OC(O)R, —OC(O)N(R)2, —C(O)N(R)2, —C(O)N(R)—OR—C(O)C(O)R, —P(O)(R)2, —NRC(O)OR, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2; or two R3 groups on the same carbon atom together form —C(O)—, —C(S)—, or —C(N—R)—; each R is independently hydrogen or an optionally substituted group selected from C1-6 aliphatic, phenyl, a 3-8 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; or two R groups on the same nitrogen are taken together with the nitrogen atom to which they are attached to form a 4-7 membered heterocyclic ring having 0-2 additional heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 4-7 membered heteroaryl ring having 0-4 additional heteroatoms independently selected from nitrogen, oxygen, or sulfur; Cy is an optionally substituted 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an optionally substituted 4-7 membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; and m and p are each independently 0-4.
地址 Cambridge MA US