USRE47929EActiveUtility
Amide-substituted heterocyclic compounds useful as modulators of IL-12, IL-23 and/or IFNα responses
Est. expiryNov 8, 2032(~6.3 yrs left)· nominal 20-yr term from priority
Inventors:Ryan M. MoslinDavid S. WeinsteinStephen T. WrobleskiJohn S. TokarskiShuqun LinSteven H. SpergelYanlei Zhang
A61P 43/00A61P 29/00A61P 13/12C07D 403/12C07D 413/12C07D 401/14C07D 401/12C07B 59/002C07B 2200/05C07D 417/14A61P 7/00A61P 17/06C07D 417/12A61P 19/02C07D 403/14A61P 1/04C07D 413/14C07D 237/24A61P 37/06A61P 1/00A61P 37/02A61P 37/00
94
PatentIndex Score
19
Cited by
75
References
39
Claims
Abstract
Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1. A compound which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
2. A compound according to claim 1 which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
3. A compound according to claim 2 which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
4. A compound according to claim 2 which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
5. A compound according to claim 2 which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
6. A compound according to claim 3 which is
or a stereoisomer or pharmaceutically-acceptable salt thereof.
7. A pharmaceutical composition comprising one or more compounds according to claim 1 and a pharmaceutically acceptable carrier or diluent.
8. A pharmaceutical composition comprising a compound according to claim 6 and a pharmaceutically acceptable carrier or diluent.
9. A method of treating a disease, comprising administering to a patient in need of such treatment a therapeutically-effective amount of a compound according to claim 6 wherein the disease is systemic lupus erythematosus.
10. A compound having the structure
11. A pharmaceutically acceptable salt of a compound having the structure
12. The pharmaceutically acceptable salt according to claim 11, which is a monohydrochloride salt.
13. A pharmaceutical composition comprising the compound according to claim 10 and a pharmaceutically acceptable carrier or diluent.
14. A pharmaceutical composition comprising the pharmaceutically acceptable salt according to claim 11 and a pharmaceutically acceptable carrier or diluent.
15. A pharmaceutical composition comprising the pharmaceutically acceptable salt according to claim 12 and a pharmaceutically acceptable carrier or diluent.
16. A method of treating systemic lupus erythematosus in a patient, comprising administering to the patient the compound according to claim 10.
17. A method of treating systemic lupus erythematosus in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
18. A method of treating systemic lupus erythematosus in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
19. A method of treating psoriasis in a patient, comprising administering to the patient the compound according to claim 10.
20. A method of treating psoriasis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
21. A method of treating psoriasis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
22. A method of treating psoriatic arthritis in a patient, comprising administering to the patient the compound according to claim 10.
23. A method of treating psoriatic arthritis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
24. A method of treating psoriatic arthritis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
25. A method of treating lupus nephritis in a patient, comprising administering to the patient the compound according to claim 10.
26. A method of treating lupus nephritis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
27. A method of treating lupus nephritis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
28. A method of treating Sjögren's syndrome in a patient, comprising administering to the patient the compound according to claim 10.
29. A method of treating Sjögren's syndrome in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
30. A method of treating Sjögren's syndrome in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
31. A method of treating inflammatory bowel disease in a patient, comprising administering to the patient the compound according to claim 10.
32. A method of treating inflammatory bowel disease in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
33. A method of treating inflammatory bowel disease in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
34. A method of treating Crohn's disease in a patient, comprising administering to the patient the compound according to claim 10.
35. A method of treating Crohn's disease in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
36. A method of treating Crohn's disease in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.
37. A method of treating ankylosing spondylitis in a patient, comprising administering to the patient the compound according to claim 10.
38. A method of treating ankylosing spondylitis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 11.
39. A method of treating ankylosing spondylitis in a patient, comprising administering to the patient the pharmaceutically acceptable salt according to claim 12.Cited by (0)
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References (0)
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