1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
US-9789094-B2 · Oct 17, 2017 · US
US10034864B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10034864-B2 |
| Application number | US-201715442876-A |
| Country | US |
| Kind code | B2 |
| Filing date | Feb 27, 2017 |
| Priority date | Jul 8, 2008 |
| Publication date | Jul 31, 2018 |
| Grant date | Jul 31, 2018 |
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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.
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What is claimed is: 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.
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