IP Library Granted Patent US 10,034,864
Granted Patent B2
US 10,034,864 · App. 15/442,876 · Granted Jul 31, 2018

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

Inventors: Andrew P. Combs (Kennett Square, PA); Eddy W. Yue (Landenberg, PA); Richard B. Sparks (Wilmington, DE); Wenyu Zhu (Media, PA)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/4245A61K39/0011A61K39/3955C07D271/08C07D413/04C07D413/12
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Quick Facts
Patent No.
US 10,034,864
App. No.
15/442,876
Granted
Jul 31, 2018
Kind
B2
Abstract

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

Claims (20)

1. A method of inhibiting or ameliorating a cancer selected from renal cancer, lung cancer, and head and neck cancer in a patient, comprising administering to said patient a therapeutically effective amount of a compound, which is 4-({2-[(amino sulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, or a pharmaceutically acceptable salt thereof, in combination with an antibody therapeutic.

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

3. The method of claim 2 , wherein the antibody therapeutic is an anti-PD-1 antibody.

4. The method of claim 2 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

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

6. The method of claim 5 , wherein the antibody therapeutic is an anti-PD-1 antibody.

7. The method of claim 5 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

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

9. The method of claim 8 , wherein the antibody therapeutic is an anti-PD-1 antibody.

10. The method of claim 8 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

11. A method of inhibiting or ameliorating a cancer selected from renal cancer, lung cancer, and head and neck cancer in a patient, comprising administering to said patient a therapeutically effective amount of a compound, which is 4-({2-[(amino sulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide in combination with an antibody therapeutic.

12. The method of claim 11 , wherein the cancer is renal cancer.

13. The method of claim 12 , wherein the antibody therapeutic is an anti-PD-1 antibody.

14. The method of claim 12 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

15. The method of claim 11 , wherein the cancer is lung cancer.

16. The method of claim 15 , wherein the antibody therapeutic is an anti-PD-1 antibody.

17. The method of claim 15 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

18. The method of claim 11 , wherein the cancer is head and neck cancer.

19. The method of claim 18 , wherein the antibody therapeutic is an anti-PD-1 antibody.

20. The method of claim 18 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2017
From: COMBS, ANDREW P.; YUE, EDDY W.; SPARKS, RICHARD B.; ZHU, WENYU
To: INCYTE CORPORATION
Reel/Frame 042242/0160 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2017
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 042242/0238 →
Continuity (8)
Continuation 15093420 · Apr 7, 2016
Continuation 14661191 · Mar 18, 2015
Continuation 14322362 · Jul 2, 2014
Continuation 13294711 · Nov 11, 2011
Division 12498782 · Jul 7, 2009
Provisional Application 61150873 · Feb 9, 2009
Provisional Application 61078876 · Jul 8, 2008
Related Publication 20170348289A1 · Dec 7, 2017