BENZIMIDAZOLONES AND ANALOGUES AND THEIR USE AS PROGESTERONE RECEPTOR LIGANDS

摘要

The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having general formula (a): wherein A is O, S, or NR<4>; B is a bond between A and C=Q, or the moiety CR<5>R<6>; R<4>, R<5>, R<6> are independently selected from H or optionally substituted C1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heteorcyclic groups, or cyclic alkyl constructed by fusing R<4> and R<5> to from a 5 to 7 membered ring; R<1> is selected from H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituded C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 toC3 aminoalkyl) groups; R<2> is selected from H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R<3> is selected from a trisubstituted benzene ring; or a 5- or 6- membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR<8>, or CR<9>R<10>; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.