发明名称 PYRIDAZINONE MACROCYCLES AS IRAK INHIBITORS AND USES THEREOF
摘要 The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
申请公布号 US2016229871(A1) 申请公布日期 2016.08.11
申请号 US201615016584 申请日期 2016.02.05
申请人 Merck Patent GmbH 发明人 CHEN Xiaoling;LAN Ruoxi;JORAND-LEBRUN Catherine;YU Henry;GOUTOPOULOS Andreas
分类号 C07D498/22;C07D498/16 主分类号 C07D498/22
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 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; which is optionally substituted; X is absent, —O—, —S—, —SO2—, —SO—, —C(O)—, —CO2—, —C(O)N(R)—, —OC(O)N(R)—, —NRC(O)—, —NRC(O)N(R)—, —NRSO2—, or —N(R)—; or X is (CRR)m—O—, —(CRR)mS—, —(CRR)mSO2—, —(CRR)mSO—, —(CRR)mC(O)—, —(CRR)mCO2—, —(CRR)mC(O)N(R)—, —(CRR)mOC(O)N(R)—, —(CRR)mNRC(O)—, —(CRR)mNRC(O)N(R)—, —(CRR)mNRSO2—, or —(CRR)mN(R)—; Y is an optionally substituted C1-6 aliphatic; Z is absent, a divalent C3-10 aryl, a divalent 3-8 membered saturated or partially unsaturated carbocyclic ring, a divalent 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a divalent 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; or Z is —O—, —S—, —SO2—, —SO—, —C(O)—, —CO2—, —C(O)N(R)—, —OC(O)N(R)—, —NRC(O)—, —NRC(O)N(R)—, —NRSO2—, or —N(R)—; W is CR or N; 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, 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 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 R1 is independently —R, halogen, —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; R2 is —R, halogen, —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; R4 is —R, halogen, —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 m is independently 1 or 2; and n is 0, 1, 2, 3, 4, or 5.
地址 Darmstadt DE