发明名称 APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS
摘要 The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
申请公布号 US2016318922(A1) 申请公布日期 2016.11.03
申请号 US201415105372 申请日期 2014.12.15
申请人 GILEAD SCIENCES, INC. 发明人 Notte Gregory
分类号 C07D417/14;A61K31/4545;A61K31/496;A61K31/553;A61K31/435;A61K31/4985;C07D498/04;A61K31/5377;C07D491/107;A61K31/4439;C07D487/04 主分类号 C07D417/14
代理机构 代理人
主权项 1. A compound of Formula (I):wherein: R1 is C1-C6 alkyl, C3-C6 cycloalkyl, or C2-C6 heterocycloalkyl, wherein the alkyl, cycloalkyl, or heterocycloalkyl moiety is optionally substituted with one to four members independently selected from halo, OR11, and NR11R12; R2 is hydrogen or C1-C3 alkyl; R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is C1-C6 alkyl, C3-C6 cycloalkyl, or C2-C6 heterocycloalkyl, wherein the alkyl, cycloalkyl, or heterocycloalkyl moiety is optionally substituted with one to four members independently selected from halo, OR11, and NR11R12; R7 is hydrogen or C1-C3 alkyl; and Ra and Rb combine with the nitrogen atom to which they are attached to form a four to ten member heterocyclic group that is a monocyclic group or a fused or bridged bicyclic, or spirocyclic group optionally containing an oxygen or a nitrogen atom in the heterocyclic group, wherein the heterocyclic group is further optionally substituted with one to four members, at the same atom or different atom, independently selected from C1-C6 alkyl, hydroxyl, cyano, oxo, halo, C1-C6 carbonyl, C1-C6 haloalkyl, C1-C6 alkoxy, C3-C6 cycloalkyl, C2-C6 heterocycloalkyl, C1-C6 acyl, C1-C6 alkyl-R11, OR11, C(O)NR11; wherein R11 and R12 is independently selected from hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;or a pharmaceutically acceptable salt or stereoisomer thereof.
地址 Foster City CA US