305790-81-2Relevant articles and documents
Benzimidazolones and analogues
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, (2008/06/13)
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR4; B is a bond between A and C═Q, or the moiety CR5R6; R4, R5, R5are independently selected from H or optionally substituted C1to C6alkyl, C2to C6alkenyl, C2to C6alknyl, C3to C8cycloalkyl, substituted C3to C8cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R4and R5to from a 5 to 7 membered ring; R1is selected from H, OH, NH2, C1to C6alkyl, substituted C1to C6alkyl, C3to C6alkenyl, substituted C1to C6alkenyl, alkynyl, substituted alknyl, —COH, or optionally substituted —CO(C1to C3alkyl), —CO(aryl), —CO(C1to C3alkoxy), or —CO(C1to C3aminoalkyl) groups; R2is selected from H, halogen, CN, NO2, or optionally substituted C1to C6alkyl, C1to C6alkoxy, or C1to C6aminoalkyl groups; R3is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR8, or CR9R10; 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.