IP Library Granted Patent US 11,053,216
Granted Patent B2
US 11,053,216 · App. 16/659,775 · Granted Jul 6, 2021

Compounds and methods of use

Inventors: Roopa Rai (San Francisco, CA); Sarvajit Chakravarty (San Francisco, CA); Brahmam Pujala (Noida, IN); Bharat Uttam Shinde (Noida, IN); Anjan Kumar Nayak (Noida, IN); Anil Kumar Agarwal (Noida, IN); Sreekanth A. Ramachandran (Noida, IN); Son Minh Pham (San Francisco, CA)
Assignee: Medivation Technologies LLC
C07D401/12A61K31/444A61K31/4439A61K31/4545A61K31/4709A61K31/506A61K45/06C07D213/72C07D213/73C07D213/82C07D401/14C07D405/14C07D413/14C07D471/04C07D487/04
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Quick Facts
Patent No.
US 11,053,216
App. No.
16/659,775
Granted
Jul 6, 2021
Kind
B2
Abstract

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

Claims (20)

1. A method of providing a first or a second line therapy for treating (a) a breast cancer in an individual diagnosed with the breast cancer or (b) a prostate cancer in an individual diagnosed with the prostate cancer, comprising administering to the individual an effective amount of

4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(1,3-dihydroxypropan-2-yl)nicotinamide or a pharmaceutically acceptable salt thereof, thereby decreasing number of cancer cells, inhibiting cancer cell growth and/or proliferation, or increasing apoptosis of cancer cells.

2. The method of claim 1 , wherein the individual is diagnosed with the breast cancer.

3. The method of claim 2 , wherein the breast cancer is selected from the group consisting of ER negative breast carcinoma, ER positive breast carcinoma, primary breast ductal carcinoma, mammary adenocarcinoma, ER positive mammary ductal carcinoma, ER negative mammary ductal carcinoma, HER2 positive mammary ductal carcinoma, HER2 positive breast cancer, luminal breast cancer, triple negative breast cancer (TNBC), and unclassified breast cancer.

4. The method of claim 3 , wherein the breast cancer is TNBC, and the TNBC is selected from the group consisting of basal-like TNBC, mesenchymal TNBC, mesenchymal stem-like TNBC, immunomodulatory TNBC, and a luminal androgen receptor TNBC.

5. The method of claim 3 , wherein the breast cancer is a luminal breast cancer.

6. The method of claim 1 , wherein the individual is diagnosed with the prostate cancer.

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

8. The method of claim 1 , wherein the treating comprises a reduction of tumor size.

9. The method of claim 1 , wherein the treating comprises a slowing of tumor growth.

10. The method of claim 1 , wherein the treating comprises slowing of metastasis.

11. The method of claim 1 , further comprising administering to the individual a second cancer therapy.

12. The method of claim 11 , wherein the second cancer therapy comprises a therapy selected from the group consisting of surgery, radiation, and chemotherapy.

13. The method of claim 12 , wherein the second cancer therapy is a chemotherapy.

14. The method of claim 13 , wherein the individual is diagnosed with the breast cancer.

15. The method of claim 14 , wherein the breast cancer is a luminal breast cancer.

16. The method of claim 14 , wherein the breast cancer is TNBC.

17. The method of claim 13 , wherein the individual is diagnosed with the prostate cancer.

18. The method of claim 17 , wherein the prostate cancer is prostate adenocarcinoma.

19. The method of claim 1 , wherein the pharmaceutically acceptable salt is a hydrochloride salt.

Assignments (5)
ASSIGNEE ADDRESS CORRECTION Recorded Mar 20, 2023
From: MEDIVATION TECHNOLOGIES LLC
To: MEDIVATION TECHNOLOGIES LLC
Reel/Frame 063117/0642 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2019
From: PHAM, SON MINH
To: MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 051072/0438 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2019
From: CHAKRAVARTY, SARVAJIT; RAI, ROOPA
To: MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 051072/0509 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 21, 2019
From: PUJALA, BRAHMAM; SHINDE, BHARAT UTTAM; NAYAK, ANJAN KUMAR; CHAKLAN, NAVEEN; AGARWAL, ANIL KUMAR; RAMACHANDRAN, SREEKANTH A.
To: MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 051072/0681 →
CHANGE OF NAME Recorded Nov 21, 2019
From: MEDIVATION TECHNOLOGIES, INC.
To: MEDIVATION TECHNOLOGIES LLC
Reel/Frame 051285/0641 →