abstract |
The invention relates to compounds that are progesterone receptor agonists and have the formulas wherein R 1 and R 2 are independent substituents selected from the group consisting of H, optionally substituted C 1 -C 6 alkyl, alkenyl or alkynyl groups, C 3 C8 cycloalkyl, aryl, substituted aryl or heterocyclic groups or CORA or NRBCORA, or R1 and R2 are fused to form an optionally substituted 3- to 8-membered spirocyclic alkyl or alkenyl ring or a spirocyclic ring containing from one to three heteroatoms selected from the group consisting of is from O, S and N; RA is selected from the group consisting of H, amino or optionally substituted C 1 -C 3 alkyl, aryl, C 1 -C 6 alkoxy or C 1 -C 6 aminoalkyl; RB is H, C1-C3 alkyl or substituted C1-C3 alkyl groups; R3 is H, OH, NH2, COR5 or optionally substituted C1-C6 alkyl, C3-C6 alkenyl or alkynyl groups; RC is H, optionally substituted C1-C3 alkyl, aryl, C1-C3 alkoxy or C1-C3 aminoalkyl; Q 1 is S, NR 7 or CR 8 R 9, R 5 is optionally a tri-substituted benzene ring or an optionally substituted 5- or 6-membered heterocyclic ring having 1, 2 or 3 ring heteroatoms selected from the group consisting of O, S, SO, SO 2 or NR 6 The invention also relates to pharmaceutically acceptable salts of the compounds, to methods of use as contraceptives and to the treatment of progesterone-dependent diseases. |