发明名称 N-SUBSTITUTED PYRAZOLYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF
摘要 The invention provides pyrazolyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
申请公布号 US2016304464(A1) 申请公布日期 2016.10.20
申请号 US201415101126 申请日期 2014.12.10
申请人 LYCERA CORPORATION 发明人 Aicher Thomas D.;Skalitzky Donald J.;Taylor Clarke B.
分类号 C07D231/38;C07D405/04;C07D401/04 主分类号 C07D231/38
代理机构 代理人
主权项 1. A compound represented by Formula I: including all stereoisomers, geometric isomers, and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; wherein: A1 is phenyl substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, C1-C4 haloalkyl, and C1-C6 alkyl; R1 and R2 are independently hydrogen, halogen, C1-C4 haloalkyl, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, or cyano; R3 and R4 are independently hydrogen, halogen, C1-C4 haloalkyl, C1-C6 alkyl, C3-C6 cycloalkyl, or cyano; R5 is one of the following: (a) heterocycloalkyl, heteroaryl, phenyl, —(C1-C6 alkylene)-heterocycloalkyl, —(C1-C6 alkylene)-phenyl, —(C1-C6 alkylene)-heteroaryl, or heterocycloalkanonyl, wherein said heterocycloalkyl, heteroaryl, phenyl, and heterocycloalkanonyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, hydroxyl, C1-C6 alkyl, C1-C4 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 cyanoalkyl, cyano, —CO2H, —CO2R6, —C(O)R6, —C(O)N(R7)(R8), —N(R7)C(O)(R6), —N(R7)CO2(R6), —N(R7)(R8), —O—R6, —S(O)R6, —SO2R6, —SO2N(R7)(R8), —N(R7)SO2(R6), —(C1-C6alkylene)-CO2R7, and —(C1-C6 alkylene)-C(O)N(R7)(R8);(b) C3-C6 cycloalkyl or —(C1-C6 alkylene)-(C3-C6 cycloalkyl), wherein said cycloalkyl is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, hydroxyl, C1-C6 alkyl, C1-C1 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 cyanoalkyl, cyano, —CO2H, —CO2R6, —C(O)R6, —C(O)N(R7)(R8), —N(R7)C(O)(R6), —N(R7)CO2(R6), —N(R7)(R8), —O—R6, —S(O)R6, —SO2R6, —SO2N(R7)(R8), and —N(R7)SO2(R6);(c) C1-C6 alkyl substituted by 1 or 2 substituents independently selected from the group consisting of hydroxyl, C1-C6 alkoxy, cyano, —CO2H, —CO2R6, —C(O)R6, —C(O)N(R7)(R8), —N(R7)C(O)(R6), —N(R7)(R8), —S(O)R6, —SO2R6, —SO2N(R7)(R8), and —N(R7)SO2(R6); or(d) C2-C6 alkenyl; R6 represents independently for each occurrence C1-C6 alkyl, C3-C6 cycloalkyl, aryl, or heteroaryl, each of which is optionally substituted with 1 or 2 substituents independently selected from the group consisting of hydroxyl, cyano, halogen, —CO2H, and aryl; and R7 and R8 each represent independently for each occurrence hydrogen, C1-C6 alkyl, or C3-C6cycloalkyl; or R7 and R8 are taken together with the nitrogen atom to which they are attached to form a 3 to 7 membered heterocyclic ring.
地址 Ann Arbor MI US