发明名称 MINERALOCORTICOID RECEPTOR ANTAGONISTS
摘要 The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.;
申请公布号 US2015182503(A1) 申请公布日期 2015.07.02
申请号 US201314415210 申请日期 2013.07.15
申请人 Merck Sharp & Dohme Corp. 发明人 Cernak Timothy A.;Dykstra Kevin D.;Shen Dong-Ming;Liu Kun;Stamford Andrew;Tan John Qiang
分类号 A61K31/416;C07D231/56 主分类号 A61K31/416
代理机构 代理人
主权项 1. A compound as represented by Formula I: or a pharmaceutically acceptable salt thereof, wherein Each Rx is independently H, halo, or C1-C6 alkyl, said alkyl is optionally substituted with 1 to 3 substituents selected from halo, OR and C1-C6 alkyl; Each R is independently H or C1-C6 alkyl, said alkyl is optionally substituted with 1 to 4 halo substituents; R1 is C1-C6 alkyl, or C(O)NRR6; wherein said alkyl is optionally substituted with one to three CF3, OR, CN, or halo substituents; R2 is C1-C6 alkyl, said alkyl is optionally substituted with one to three OR, CN or halo substituents; R3 is aryl-Xt; R4 is —NR6S(O)2R8, R5 is H, C1-C6 alkyl, CN, or OR; Each R6 is independently H, C1-C6 alkyl, C3-C10 cycloalkyl, heteroaryl or aryl, said alkyl, cycloalkyl, or heteroaryl may be optionally substituted with aryl, heteroaryl or heterocyclyl; Each R8 is independently C1-C6 alkyl, C3-C10 cycloalkyl or aryl, said alkyl, cycloalkyl and aryl are optionally substituted with one to three C3-C10 cycloalkyl or halo substituents; Each X is independently halo, CN, CF3, or SF5; t is 1, 2 or 3; x is 0, 1, 2 or 3.
地址 Rahway NJ US