发明名称 NOVEL NAPHTHYRIDINES AND ISOQUINOLINES AND THEIR USE AS CDK8/19 INHIBITORS
摘要 The present invention relates to naphthyridine and isoquinoline compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of CDK8/19, and for the treatment of CDK8/19-related disorders.
申请公布号 US2016016951(A1) 申请公布日期 2016.01.21
申请号 US201514802042 申请日期 2015.07.17
申请人 Merck Patent GmbH ;Cancer Research Technology, Ltd. 发明人 SCHIEMANN Kai;BLAGG Julian;MALLINGER Aurelie;RINK Christian;SEJBERG Jimmy;HONEY Mark
分类号 C07D471/04;C07D401/12;C07D417/14;C07D401/14;C07D413/14;C07D401/10 主分类号 C07D471/04
代理机构 代理人
主权项 1. A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein: A is hydrogen, C1-6 aliphatic, C5-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 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 of which is optionally substituted by R1 and/or R2; or A is halogen; X is CR or N; Y is hydrogen, OR, SR, SO2R, SOR, C(O)R, CO2R, C(O)N(R)2, C(NR)N(R)2, SO2N(R)2, NRC(O)R, NRC(O)N(R)2, NRSO2R, N(R)2; —CN, halogen, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 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 of which is optionally substituted; each R3 is independently —R, halogen, -haloalkyl, -hydroxyalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2; R1 is a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from N, NR, O, S, SO, or SO2, which is optionally substituted by 1-5 of RA; R2 is hydrogen, C1-6 aliphatic, C5-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 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 of which is optionally substituted; or R2 is halogen, -haloalkyl, -hydroxyalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2; or R1 and R2, together with the atoms to which each is attached, forms an optionally substituted 5-6 membered heterocyclic or heteroaryl ring having 1-4 heteroatoms independently selected from N, NR, O, S, SO, or SO2, wherein the ring is not a pyrrole, dihydro-pyrrole, or thiazole; each RA is independently —R, halogen, -haloalkyl, -hydroxyalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2; each R is independently hydrogen, C1-6 aliphatic, C5-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 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 of which is optionally substituted; or two R groups on the same atom are taken together with the atom to which they are attached to form a C5-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 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 of which is optionally substituted; and n is 0, 1, 2, 3, or 4.
地址 Darmstadt DE
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