发明名称 TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
摘要 The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
申请公布号 US2016376283(A1) 申请公布日期 2016.12.29
申请号 US201615194780 申请日期 2016.06.28
申请人 Merck Patent GmbH 发明人 SHERER Brian A.;KARRA Srinivasa;XIAO Yufang
分类号 C07D491/048;C07D519/00 主分类号 C07D491/048
代理机构 代理人
主权项 1. A compound of formula I,or pharmaceutically acceptable derivatives, solvates, salts, hydrates, or stereoisomers thereof, wherein: R1 is hydrogen, optionally substituted C1-6 aliphatic, optionally substituted 3-8 membered saturated or partially unsaturated carbocyclic ring, —OR, or halogen; ring Z is phenyl, pyridine, or pyrimidine; each R2 is independently —R, halogen, —OR, —SR, —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 R3 is independently —R, halogen, —OR, —SR, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2; ring A is phenyl or a 5-6-membered heteroaryl having 1, 2, or 3 nitrogens; R4 is —R, halogen, —OR, —SR, —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 R5 is independently —R, halogen, —OR, —SR, —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, 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, a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or a 6-12 membered spiro, fused, or bridged bicyclic carbocyclic or heterocyclic 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 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; n is 1 or 2; p is 0, 1, or 2; and q is 0, 1, or 2; wherein the following compounds are excluded: 4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-fluoro-N-(2-hydroxy-ethyl)-N-methyl-benzamide; 5-{2-[2-fluoro-4-(piperazine-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yl oxy)-benzonitrile; 5-{2-[2-fluoro-4-(5-oxo-[1,4]diazepane-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile; 5-{2-[2-fluoro-4-(4-hydroxy-piperidine-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile; 5-{2-[2-fluoro-4-(morpholine-4-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile; 4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-N-(2-hydroxy-ethyl)-3-methoxy-N-methyl-benzamide; 5-{2-[4-(4-hydroxy-piperidine-1-carbonyl)-2-methoxy-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile; 4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N,N-dimethyl-benzamide; 4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N—(S)-piperidin-3-yl-benzamide; and 4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N—(R)-piperidin-3-yl-benzamide.
地址 Darmstadt DE