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Last Updated: December 29, 2025

Claims for Patent: 10,654,866


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Summary for Patent: 10,654,866
Title:Selective estrogen receptor degraders
Abstract:Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.
Inventor(s):Jolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall
Assignee: Eli Lilly and Co
Application Number:US16/508,745
Patent Claims: 1. A compound of the formula: wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, 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.

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