IP Library Granted Patent US 10,487,056
Granted Patent B2
US 10,487,056 · App. 16/182,720 · Granted Nov 26, 2019

Small molecule androgen receptor inhibitors and methods of use thereof

Inventors: Milton L. Brown (Brookeville, MD); Shujie Hou (Gaithersburg, MD); Partha Banerjee (Rockville, MD); Karishma Amin (San Francisco, CA)
Assignee: Georgetown University
C07D209/88A61K31/403A61K45/06A61P35/00
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Quick Facts
Patent No.
US 10,487,056
App. No.
16/182,720
Granted
Nov 26, 2019
Kind
B2
Abstract

Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.

Claims (20)

1. A compound selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is

3. The compound of claim 1 , wherein the compound is

4. The compound of claim 1 , wherein the compound is

5. A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

6. A method of treating or preventing cancer in a subject, comprising:

administering to the subject an effective amount of the composition of claim 5 .

7. The method of claim 6 , wherein the cancer is prostate cancer.

8. The method of claim 7 , wherein the prostate cancer is a castration-resistant prostate cancer or a drug-resistant cancer.

9. The method of claim 7 , wherein the prostate cancer is androgen-independent prostate cancer or androgen-dependent prostate cancer.

10. The method of claim 6 , wherein the cancer is breast cancer.

11. The method of claim 6 , wherein the cancer is ovarian cancer.

12. The method of claim 6 , wherein the cancer is peritoneal cancer.

13. The method of claim 6 , wherein the cancer is fallopian tube cancer.

14. The method of claim 6 , further comprising administering a second therapeutic agent to the subject, wherein the second therapeutic agent is a chemotherapeutic agent.

15. A method of inhibiting androgen receptor activity in a cell, comprising:

contacting the cell with an effective amount of the compound of claim 1 .

16. The method of claim 15 , wherein the cell is an androgen-dependent cell or an androgen-independent cell.

17. The method of claim 15 , wherein the contacting is performed in vivo or in vitro.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jan 5, 2024
From: GEORGETOWN UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 066207/0959 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2018
From: BROWN, MILTON L.; HOU, SHUJIE; BANERJEE, PARTHA; AMIN, KARISHMA
To: GEORGETOWN UNIVERSITY
Reel/Frame 047433/0550 →
Continuity (3)
Continuation 15749383
Provisional Application 62201291 · Aug 5, 2015
Related Publication 20190077755A1 · Mar 14, 2019