发明名称 AUTOTAXIN INHIBITOR COMPOUNDS
摘要 Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
申请公布号 US2016374991(A1) 申请公布日期 2016.12.29
申请号 US201615261659 申请日期 2016.09.09
申请人 PharmAkea, Inc. 发明人 HUTCHINSON John Howard;LONERGAN David
分类号 A61K31/4155;C07D401/14;A61K31/4439;C07D401/04;A61K9/06;A61K9/00;A61K9/08;A61K9/48;A61K9/20;C07D403/04;C07D493/10 主分类号 A61K31/4155
代理机构 代理人
主权项 1. A compound of Formula (III), or a pharmaceutically acceptable salt, or solvate thereof: wherein, R1 is —Cl, —Br, —CN, or C3-C6cycloalkyl; R2 is H, halogen, —CN, —NO2, —OH, —OR9, —SR9, —S(═O)R9, —S(═O)2R9, —S(═O)2N(R10)2, C1-C4alkyl, C1-C4fluoroalkyl, C1-C4deuteroalkyl, or C3-C6cycloalkyl; R3 is H, halogen, —CN, —OH, C1-C4alkyl, C1-C4fluoroalkyl, C1-C4deuteroalkyl, C1-C4alkoxy, or C1-C4fluoroalkoxy; W is CH, CF or N; each RA is H, halogen, —CN, —NO2, —OH, —OR9, —SR9, —S(═O)R9, —S(═O)2R9, —S(═O)2N(R10)2, C1-C6alkyl, or C1-C6fluoroalkyl; L1 is absent, C1-C6alkylene, or C3-C6cycloalkylene; Q is —CO2H, —CO2(C1-C6alkyl), —OH, —CN, —B(OH)2, —C(═O)NHSO2R9, —C(═O)N(R10)2, —SO2NHC(═O)R9, —CN, tetrazolyl, —OP(═O)(OH)2, —P(═O)(OH)2 or carboxylic acid bioisostere; Ring B is a monocyclic heteroaryl; each RB is independently H, halogen, —CN, —NO2, —OH, —OR9, —SR9, —S(═O)R9, —S(═O)2R9, —S(═O)2N(R10)2, C1-C6alkyl, C1-C6fluoroalkyl, C1-C6deuteroalkyl, C1-C6heteroalkyl, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted phenyl, C1-C4alkylene-(substituted or unsubstituted phenyl), substituted unsubstituted monocyclic heteroaryl, C1-C4alkylene-(substituted or unsubstituted monocyclic heteroaryl), a substituted or unsubstituted bicyclic heteroaryl, or C1-C4alkylene-(substituted or unsubstituted bicyclic heteroaryl); n is 0, 1, or 2; R9 is C1-C6alkyl, C1-C6fluoroalkyl, C1-C6deuteroalkyl, C3-C6cycloalkyl, a substituted or unsubstituted phenyl, a substituted or unsubstituted monocyclic heteroaryl, or a substituted or unsubstituted bicyclic heteroaryl; each R10 is independently H, C1-C6alkyl, C1-C6fluoroalkyl, C1-C6deuteroalkyl, C3-C6cycloalkyl, a substituted or unsubstituted phenyl, or a substituted or unsubstituted monocyclic heteroaryl; or two R10 groups attached to the same N atom are taken together with the N atom to which they are attached to form a substituted or unsubstituted heterocycle.
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