MINERALOCORTICOID RECEPTOR ANTAGONISTS

摘要

The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).;

主权项

1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein X is NH or O; Each R1 is independently halo, C1-C6 alkyl, C3-C10 cycloalkyl, or OR, wherein said alkyl and cycloalkyl are optionally substituted with one to three groups selected from halo, OR, CF3, CF2H, or CN; Each R is independently H, C1-C6 alkyl, CF3, or C3-C10 cycloalkyl, wherein said alkyl and cycloalkyl are optionally substituted with one to three groups selected from halo, OR, CF2H, CF3, or CN; Each R3 is independently halo, OR, C1-C6 alkyl, CF3, C3-C10 cycloalkyl, C(O)OR, (CRc)0-3-heteroaryl, (CRc)0-3-heterocyclyl, NR6S(O)2R7, CN, C(O)NR6R7, or (CRc)0-3-aryl, where said alkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four groups selected from OR, halo, CF2H, CF3, C1-C6 alkyl, or C3-C10 cycloalkyl; R4 is H, C1-C6 alkyl, aryl, C3-C10 cycloalkyl or heterocyclyl, where said alkyl, aryl, cycloalkyl, or heterocyclyl, is optionally substituted with one to four groups selected from halo or OR; R5 is H, CF2H, CF3, C1-C6 alkyl, or C3-C10 cycloalkyl; Each R6 is independently H, CF2H, CF3, C1-C6 alkyl, or C3-C10 cycloalkyl; Each R7 is independently C1-C6 alkyl, (CRd2)t-aryl, C3-C10 cycloalkyl, or (CRd2)t-heteroaryl, where said alkyl, aryl, cycloalkyl, or heteroaryl is optionally substituted with one to four groups selected from OR, halo, or aryl; Each Ra is independently H, C1-C6 alkyl, or C3-C10 cycloalkyl wherein said alkyl, cycloalkyl and aryl are optionally substituted with one to three groups selected from halo, OR, CF2H, CF3, or CN; Each Rb is independently H, C1-C6 alkyl, C3-C10 cycloalkyl, or aryl, wherein said alkyl, cycloalkyl and aryl are optionally substituted with one to three groups selected from halo, OR, CF2H, CF3, or CN; Each Rc is independently H or C1-C6 alkyl; Each Rd is independently H or C1-C6 alkyl; m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4; p is 0, 1, 2 or 3; and t is 0 or 1.