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US 9,789,094 B2Granted
1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
AssigneesIncyte Holdings Corporation, Incyte Corporation
InventorsAndrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
Life of this patent
Estimating the term…
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.
Claims23
A method of suppressing immunosuppression;
- or inhibiting or ameliorating a disease in a patient, wherein the disease is selected from breast cancer, ovarian cancer, lung cancer, head and neck cancer, pancreatic cancer, renal cancer, melanoma, HIV infection, HCV infection, depression, Alzheimer's disease, Huntington's disease, trauma, age-related cataracts, organ transplant rejection, asthma, rheumatoid arthritis, multiple sclerosis, allergic inflammation, inflammatory bowel disease, psoriasis, and systemic lupus erythematosus, said method comprising administering to the patient in need thereof a therapeutically effective amount of a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, in combination with an anti-cancer vaccine, wherein:
- R1 is NH2 or CH3;
- R2 is Cl, Br, CF3, CH3, or CN;
- R3 is H or F;
- and
- n is 1 or 2.
4 more elements
A method of suppressing immunosuppression;
- or inhibiting or ameliorating a disease in a patient, wherein the disease is selected from breast cancer, ovarian cancer, lung cancer, head and neck cancer, pancreatic cancer, renal cancer, melanoma, HIV infection, HCV infection, depression, Alzheimer's disease, Huntington's disease, trauma, age-related cataracts, organ transplant rejection, asthma, rheumatoid arthritis, multiple sclerosis, allergic inflammation, inflammatory bowel disease, psoriasis, and systemic lupus erythematosus, said method comprising administering to the patient in need thereof a therapeutically effective amount of a compound of Formula F28:
- or a pharmaceutically acceptable salt thereof, in combination with an anti-cancer vaccine, wherein:
- R4 is F, Cl, Br, or I;
- and
- n is 1 or 2.
2 more elements
A method of suppressing immunosuppression;
- or inhibiting or ameliorating a disease in a patient, wherein the disease is selected from breast cancer, ovarian cancer, lung cancer, head and neck cancer, pancreatic cancer, renal cancer, melanoma, HIV infection, HCV infection, depression, Alzheimer's disease, Huntington's disease, trauma, age-related cataracts, organ transplant rejection, asthma, rheumatoid arthritis, multiple sclerosis, allergic inflammation, inflammatory bowel disease, psoriasis, and systemic lupus erythematosus, said method comprising administering to the patient in need thereof a therapeutically effective amount of 4-({2-[(aminosulfonyl)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 anti-cancer vaccine.
Dependencies are inferred from the claim text.