| 摘要 |
This invention provides compounds which are agonists and antagonists of the progesterone receptor having the general structure:wherein:R<1 >and R<2 >are independently selected from H, COR<A>, or NR<B>COR<A>, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties;or R<1 >and R<2 >are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; R<A >is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; R<B >is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R<3 >is H, OH, NH2, COR<C >or optionally substituted alkyl, alkenyl, or alkynyl; R<C >is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R<4 >is H, halogen, CN, NO2, or optionally substituted alkyl alkynyl, alkoxy, amino or aminoalkyl; R<5 >is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR<6>; R<6 >is H or C1 to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, or CR7R8; provided that when G1 is O, G2 is CR7R8, and G1 and G2 cannot both be CR7R8; R7 and R8 are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.
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