IP Library Granted Patent US 10,450,313
Granted Patent B2
US 10,450,313 · App. 16/025,519 · Granted Oct 22, 2019

Bicyclic heterocycles as FGFR inhibitors

Inventors: Liang Lu (Hockessin, DE); Wenqing Yao (Chadds Ford, PA); Chunhong He (Chadds Ford, PA); Fenglei Zhang (Berwyn, PA)
Assignees: Incyte Holdings Corporation; Incyte Corporation
C07D471/04A61K31/4375A61P35/00
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Quick Facts
Patent No.
US 10,450,313
App. No.
16/025,519
Granted
Oct 22, 2019
Kind
B2
Abstract

The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Claims (16)

1. A method of inhibiting or ameliorating cancer in a patient comprising administering to said patient a therapeutically effective amount of 2′-(2,6-difluoro-3,5-dimethoxyphenyl)-6′-[(2-morpholin-4-ylethyl)amino]-1′,2′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,7]naphthyridin]-3′-one, or a pharmaceutically acceptable salt thereof, wherein said cancer is associated with abnormal expression or activity of FGFR enzymes or FGFR ligands, and wherein said cancer is selected from bladder cancer, breast cancer, endometrial cancer, gastric cancer, lung cancer, esophageal cancer, head and neck cancer, glioblastoma, ovarian cancer, cervical cancer, and kidney cancer.

2. The method of claim 1 , wherein the cancer is bladder cancer.

3. The method of claim 1 , wherein the cancer is breast cancer.

4. The method of claim 1 , wherein the cancer is endometrial cancer.

5. The method of claim 1 , wherein the cancer is gastric cancer.

6. The method of claim 1 , wherein the cancer is lung cancer.

7. The method of claim 6 , wherein the lung cancer is non-small cell lung cancer.

8. The method of claim 6 , wherein the lung cancer is adenocarcinoma.

9. The method of claim 1 , wherein the cancer is esophageal cancer.

10. The method of claim 1 , wherein the cancer is head and neck cancer.

11. The method of claim 1 , wherein the cancer is glioblastoma.

12. The method of claim 1 , wherein the cancer is ovarian cancer.

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

14. The method of claim 1 , wherein the cancer is kidney cancer.

15. The method of claim 6 , wherein the lung cancer is adenocarcinoma, small cell lung cancer, non-small cell lung carcinoma, parvicellular carcinoma, non-parvicellular carcinoma, bronchial carcinoma, bronchial adenoma, or pleuropulmonary blastoma.

16. The method of claim 6 , wherein the lung cancer is small cell lung cancer.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2019
From: SUN, YAPING; LU, LIANG; YAO, WENQING; ZHUO, JINCONG; WU, LIANGXING; XU, MEIZHONG; QIAN, DING-QUAN; HE, CHUNHONG; ZHANG, FENGLEI
To: INCYTE CORPORATION
Reel/Frame 049430/0230 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 11, 2019
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 049430/0302 →
Continuity (4)
Division 15358371 · Nov 22, 2016
Continuation 14256438 · Apr 18, 2014
Provisional Application 61813782 · Apr 19, 2013
Related Publication 20190062327A1 · Feb 28, 2019
Cited By (5)
US 12,428,420 US 12,473,286 US 12,534,463 US 12,552,792 US 12,552,804