Selective estrogen receptor degraders
Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R 1 or R 2 is independently selected from Cl, F, —CF 3 , or —CH 3 , and the other is hydrogen, and methods for their use are provided.
1. A compound of the formula:
wherein either R 1 or R 2 is independently selected from Cl, F, —CF 3 , or —CH 3 , and the other is hydrogen,
or a pharmaceutically acceptable salt thereof.
2. The compound according to claim 1 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
3. The compound according to claim 1 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
4. The compound according to claim 1 , wherein the pharmaceutically acceptable salt is a benzenesulfonic acid salt.
5. The compound according to claim 1 , wherein the pharmaceutically acceptable salt is a 4-methylbenzenesulfonic acid salt.
6. The compound according to claim 2 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
7. The compound according to claim 6 , wherein the pharmaceutically acceptable salt is a benzenesulfonic acid salt.
8. The compound according to claim 6 , wherein the pharmaceutically acceptable salt is a 4-methylbenzenesulfonic acid salt.
9. The compound according to claim 6 , wherein the compound is
10. The compound according to claim 3 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
11. The compound according to claim 10 , wherein the pharmaceutically acceptable salt is a benzenesulfonic acid salt.
12. The compound according to claim 10 , wherein the pharmaceutically acceptable salt is a 4-methylbenzenesulfonic acid salt.
13. The compound according to claim 10 , wherein the compound is
14. A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt thereof according to claim 1 in combination with a pharmaceutically acceptable excipient, carrier, or diluent.
15. The pharmaceutical composition according to claim 14 , comprising one or more other therapeutic agents.
16. A method of treating breast cancer, ovarian cancer, endometrial cancer, prostate cancer, uterine cancer, gastric cancer, or lung cancer, comprising administering to a patient in need of such treatment an effective amount of a compound or a pharmaceutically acceptable salt thereof according to claim 1 .
17. The method according to claim 16 , wherein the breast cancer is ER-positive breast cancer.
18. The method according to claim 16 , wherein the gastric cancer is ER-positive gastric cancer.
19. The method according to claim 16 , wherein the lung cancer is ER-positive lung cancer.