IP Library › Granted Patent US 12,497,386
Granted Patent B2
US 12,497,386 · App. 18/661,960 · Granted Dec 16, 2025

Estrogen receptor-modulating compounds

Inventor: Chris Miller (San Mateo, CA)
Assignee: RADIUS PHARMACEUTICALS, INC.
C07D403/10A61P35/04C07D209/30C07D333/64C07D409/12C07D487/04C07D495/04
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Quick Facts
Patent No.
US 12,497,386
App. No.
18/661,960
Granted
Dec 16, 2025
Kind
B2
Abstract

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Claims (13)

1 . A compound selected from:

1-(4-(2-((Cyclopropylmethyl)amino)ethyl) benzyl)-2-(4-methoxyphenyl)-3-methyl-1H-indol-5-ol;

1-(4-(2-((Cyclopropylmethyl)amino)ethyl)benzyl)-3-fluoro-2-(o-tolyl)-1H-indol-5-ol; and

2-Fluoro-N-(4-((8-fluoro-7-(o-tolyl)pyrrolo [3,2-e]indazol-6 (3H)yl)methyl) phenethyl)ethan-1-amine.

2 . A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable excipient.

3 . A method of treating a disease, syndrome, illness, or symptom associated with insufficient or overabundant estrogen levels in a mammal in need thereof, comprising administering to said mammal an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

4 . A method of treating a cancer selected from the group consisting of prostate cancer, breast cancer, endometrial cancer, lung cancer, hepatocellular cancer, lymphoma, multiple endocrine neoplasia, vaginal cancer, renal cancer, thyroid cancer, testicular cancer, leukemia, and ovarian cancer in a mammal in need thereof, comprising administering to said mammal an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

5 . The compound according to claim 1 , wherein the compound is

1-(4-(2-((Cyclopropylmethyl)amino)ethyl)benzyl)-2-(4-methoxyphenyl)-3-methyl-1H-indol-5-ol, which is Compound D-03 and has the structure:

6 . The compound according to claim 1 , wherein the compound is

1-(4-(2-((Cyclopropylmethyl)amino)ethyl)benzyl)-3-fluoro-2-(o-tolyl)-1H-indol-5-ol, which is Compound D-39 and has the structure:

7 . The compound according to claim 1 , wherein the compound is

2-Fluoro-N-(4-((8-fluoro-7-(o-tolyl)pyrrolo [3,2-e]indazol-6(3H)yl)methyl) phenethyl) ethan-1-amine, which is Compound D-101 and has the structure:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 7, 2024
From: MILLER, CHRIS
To: RADIUS PHARMACEUTICALS, INC.
Reel/Frame 067653/0467 →
Continuity (4)
Division 17828832 · May 31, 2022
Division 16963794
Provisional Application 62620441 · Jan 22, 2018
Related Publication 20240308986A1 · Sep 19, 2024
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