| abstract |
This invention provides compounds which are agonists and antagonists of the progesterone receptor having general structure (I): wherein R?1 and R2¿ are independently selected from H, COR?A, or NRBCORA¿, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties; or R?1 and R2¿ are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; RB is H, C¿1? to C3 alkyl or substituted C1 to C3 alkyl; R?3¿ is H, OH, NH¿2, COR?C or optionally substituted alkyl, alkenyl, or alkynyl; RC is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R4 is H, halogen, CN, NO¿2?, 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, SO¿2? or NR?6; R6¿ is H or C¿1? 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. |