This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R 1 , and R 2 are each, independently, hydrogen, alkyl, substituted alkyl; or R 1 and R 2 are taken together form a ring and together contain —CH 2 (CH 2 ) n CH 2 —, —CH 2 CH 2 CMe 2 CH 2 CH 2 —, —O(CH 2 ) p CH 2 —, —O(CH 2 ) q O—, —CH 2 CH 2 OCH 2 CH 2 —, or —CH 2 CH 2 NR 7 CH 2 CH 2 —; n=1-5; p=1-4; q=1-4; R 3 is hydrogen, OH, NH 2 , alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or COR A ; R A is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R 4 is hydrogen, halogen, CN, NH 2 , alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R 5 is hydrogen, alkyl, or substituted alkyl; R 6 is hydrogen, alkyl, substituted alkyl, or COR B ; R B is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R 7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.
1. A method of providing progestational therapy to a mammal having endometriosis or fibroids, wherein said method comprises administering a progestationally effective amount of a compound having the structure of formula 1:
wherein:
T is S;
R 1 and R 2 are each, independently, hydrogen or C 1 to C 6 alkyl; or
R 1 and R 2 are taken together to form —CH 2 (CH 2 ) n CH 2 ;
n=1-5;
R 3 is hydrogen,
R 4 is hydrogen,
R 5 hydrogen,
R 6 is hydrogen or C 1 to C 6 alkyl;
R 7 is hydrogen or alkyl;
or a pharmaceutically acceptable salt thereof, to said mammal.
2. The method according to claim 1 , wherein in formula 1:
R 1 and R 2 are each, independently, hydrogen or CH 1 to CH 6 alkyl.
3. The method according to claim 1 , wherein said progestationally effective amount is 0.02 μg/kg to 750 μg/kg.
4. The method according to claim 1 , wherein said R 1 and R 2 are taken together to form —CH 2 (CH 2 ) n CH 2 — and n is 1.
5. The method according to claim 1 , wherein said R 1 and R 2 are taken together to form —CH 2 (CH 2 ) n CH 2 — and n is 2.
6. The method according to claim 1 , wherein R 1 and R 2 are CH 1 to CH 6 alkyl.