abstract |
17-beta-hydroxysteroid dehydrogenase-II inhibitors having the structural formula (I) wherein the phenyl group labeled A and the group -C(R4)(R6)Y are oriented cis to each other; W represents O or S; R1 represents -H or optionally substituted -(C¿1?-C4)alkyl; n represents 0 or an integer of 1-3; and R?2¿ represents any of a variety of substituents on ring A. R4 generally represents -H but may be a bond terminating at the ortho position of ring A. Y represents fluorine, -OR5, or -SR5 , and R5 represents -H, optionally substituted -(C¿1?-C4)alkyl, optionally substituted -phenyl, optionally substituted -(C1-C4)alkyl-phenyl, or optionally substituted -(C1-C4)acyl. R?6¿ represents any of a variety of groups as defined in the specification and claims, including heteroaryl, arylalkyl, heteroarylalkyl, arylalkenyl, heteroarylalkenyl, alkynyl, arylalkynyl, heteroarylalkynyl, aryl, and indolyl. Pharmaceutically acceptable salts and N-oxides of these materials are also included. Also claimed are pharmaceutical compositions containing these materials and methods of using them. |