发明名称 APELIN RECEPTOR (APJ) AGONISTS AND USES THEREOF
摘要 This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
申请公布号 US2016207889(A1) 申请公布日期 2016.07.21
申请号 US201515023510 申请日期 2015.06.05
申请人 RUNYON Scott P.;MAITRA Rangan;NARAYANAN Sanju;THOMAS James Barnwell;RESEARCH TRIANGLE INSTITUTE 发明人 Runyon Scott P.;Maitra Rangan;Narayanan Sanju;Thomas James Barnwell
分类号 C07D231/14;A61K45/06;A61K31/415;C07D405/12;A61K31/422;A61K31/454;A61K31/4155;A61K31/496;C07D413/12 主分类号 C07D231/14
代理机构 代理人
主权项 1. A compound represented by the Formula I: or a pharmaceutically acceptable salt, a prodrug, or a salt of a prodrug, wherein R1 is represented by the formula: each A is independently C1-8 alkyl, C1-8 alkyl(aryl), C1-8 alkoxy, C1-8 alkoxy aryl, C2-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, —CF3, —(CH2)xNR7R8, —CN, —CONR7R8, —COR7, —CO2(CH2)xNR7R8, —CO2R7, halogen, hydroxyl, —N3, —NHCOR7, —NHSO2C1-8 alkyl, —NHCO2C1-8 alkyl, —NO2, —NR7R8, —O(CH2)xNR7R8, —O(CH2)xCO2R7, —OCOC1-8 alkyl, —OCO(CH2)xNR7R8, —SO(1-3)R7, or —SR7;R7 and R8 are independently alkoxy, aryl, C1-8 alkyl, C1-8 alkyl alcohol, C1-8 alkyl amino, C1-8 alkyl amido, C1-8 alkyl(aryl), C1-8 alkyl (C3-8 cycloalkyl), C1-8 alkyl guanidinyl, C1-8 alkyl heteroaryl, C1-8 alkyl imidazolyl, C1-8 alkyl indolyl, C1-8 alkyl thioether, C1-8 alkyl thiol, C2-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, —(CH2)xCONHR9, —(CH2)xCOR9, —(CH2)xCO2R9, H, or heteroaryl; or R7 and R8 together make a 3-8 member ring which may be substituted with one or more heteroatoms;n is 0, 1, 2, 3, 4 or 5;each x is independently 0-8;R2 is present or absent, and if present, is C1-8 alkyl, C1-8 alkyl (C3-8 cycloalkyl), C3-8 cycloalkyl, or heteroaryl;R3 is present or absent, is absent if R2 is present, and if present is C1-8 alkyl, C1-8 alkyl (C3-8 cycloalkyl), or C3-8 cycloalkyl;R4, R5, and R6 are independently adamantanyl, aryl, C1-8 alkyl, C1-8 alkyl alcohol, C1-8 alkyl amino, C1-8 alkyl amido, C1-8 alkyl(aryl), C1-8 alkyl (C3-8 cycloalkyl), C1-8 alkyl (C3-8 cycloalkyl)-CO2R7, C1-8 alkyl guanidinyl, C1-8 alkyl heteroaryl, C1-8 alkyl imidazolyl, C1-8 alkyl indolyl, C1-8 alkyl thioether, C1-8 alkyl thiol, C2-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkyl-CO2R7, —(CH2)xNR7R8, —(CH2)xOR7, —(CH2)xNHCOR7, —(CH2)xNHCO2R7, —(CH2)xCONR7R8, —(CH2)xCONR7(CH2)yCO2R9, —(CH2)xCONR7(CH2)yCONR7R8, —(CH2)xCONR7(CH2)yR9, —(CH2)xCOR7, —(CH2)xCO2R7, —CHR7COR9, —CHR7CONHCHR8COR9, —CONR7R8, —CONR7(CH2)xCO2R8, —CONR7CHR8CO2R9, —CO2R9, H, or —NHCO2R7; or R4 and R5 together make a 4-8 member ring which may be substituted with one or more heteroatoms or selected from the groups comprising R6;R9 is aryl, C1-8 alkoxy, C1-8 alkyl, C1-8 alkyl(aryl), C3-8 cycloalkyl, H, heteroaryl, or hydroxyl;each y is independently 1-8;and Z is H2 or ═O.
地址 Research Triangle Park NC US
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