IP Library Granted Patent US 11,173,162
Granted Patent B2
US 11,173,162 · App. 16/816,556 · Granted Nov 16, 2021

Bicyclic heterocycles as FGFR4 inhibitors

Inventors: Alexander Sokolsky (Philadelphia, PA); Liangxing Wu (Wilmington, DE); Wenqing Yao (Chadds Ford, PA)
Assignee: Incyte Corporation
A61K31/541A61K31/4375A61K31/444A61K31/519A61K31/5377A61P35/00C07D471/04
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Quick Facts
Patent No.
US 11,173,162
App. No.
16/816,556
Granted
Nov 16, 2021
Kind
B2
Abstract

The present disclosure relates to bicyclic heterocycles of Formula (I′), and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.

Claims (23)

1. A method for treating cancer in a patient, said method comprising: administering to said patient in need thereof a therapeutically effective amount of a compound selected from:

3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimethyl-1H-pyrazol-4-yl)-1-pyrimidin-4-yl-3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-one, and

4-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimethyl-1H-pyrazol-4-yl)-2-oxo-3,4-dihydropyrido[4,3-d]pyrimidin-1(2H)-yl)benzonitrile,

or a pharmaceutically acceptable salt thereof;

and wherein the cancer is selected from the group consisting of hepatocellular cancer, liver cancer, bladder cancer, multiple myeloma, acute myelogenous leukemia, gastric cancer, lung cancer, breast cancer, pancreatic cancer, cervical cancer endometrial cancer, head and neck cancer, ovarian cancer, esophageal cancer, gall bladder cancer, and glioblastoma.

2. The method of claim 1 , wherein the compound is 3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimethyl-1H-pyrazol-4-yl)-1-pyrimidin-4-yl-3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-one or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the compound is 4-(3-(2,6-difluoro-3,5-dimethoxyphenyl)-7-(1,3-dimethyl-1H-pyrazol-4-yl)-2-oxo-3,4-dihydropyrido[4,3-d]pyrimidin-1(2H)-yl)benzonitrile or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein said cancer is hepatocellular cancer.

5. The method of claim 1 , wherein said cancer is liver cancer.

6. The method of claim 1 , wherein said cancer is bladder cancer.

7. The method of claim 1 , wherein said cancer is multiple myeloma.

8. The method of claim 1 , wherein said cancer is acute myelogenous leukemia.

9. The method of claim 1 , wherein said cancer is gastric cancer.

10. The method of claim 1 , wherein said cancer is lung cancer.

11. The method of claim 1 , wherein said cancer is breast cancer.

12. The method of claim 1 , wherein said cancer is pancreatic cancer.

13. The method of claim 1 , wherein said cancer is cervical cancer.

14. The method of claim 1 , wherein said cancer is endometrial cancer.

15. The method of claim 1 , wherein said cancer is head and neck cancer.

16. The method of claim 1 , wherein said cancer is ovarian cancer.

17. The method of claim 1 , wherein said cancer is esophageal cancer.

18. The method of claim 1 , wherein said cancer is gall bladder cancer.

19. The method of claim 1 , wherein said cancer is glioblastoma.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2021
From: INCYTE CORPORATION
To: INCYTE CORPORATION; INCYTE HOLDINGS CORPORATION
Reel/Frame 058815/0857 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 9, 2020
From: LU, LIANG; SHEN, BO; SOKOLSKY, ALEXANDER; WANG, XIAOZHAO; WU, LIANGXING; YAO, WENQING; YE, YINGDA
To: INCYTE CORPORATION
Reel/Frame 054587/0969 →
Cited By (5)
US 12,428,420 US 12,473,286 US 12,534,463 US 12,552,792 US 12,552,804