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Last Updated: August 13, 2020

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Claims for Patent: 6,794,379

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Summary for Patent: 6,794,379
Title: CXCR3 antagonists
Abstract:Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.
Inventor(s): Medina; Julio C. (San Carlos, CA), Johnson; Michael G. (San Francisco, CA), Li; An-Rong (So. San Francisco, CA)
Assignee: Tularik Inc. (South San Francisco, CA)
Application Number:10/164,690
Patent Claims:1. A compound having the formula: ##STR205## or a pharmaceutically acceptable salt, isomer or prodrug thereof.

2. The compound of claim 1 or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1.

4. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier or diluent.

5. A method of treating an inflammatory or immune condition or disease in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1.

6. The method of claim 5, wherein said compound is administered topically.

7. The method of claim 5, wherein said compound modulates CXCR3.

8. The method of claim 5, wherein said inflammatory or immune condition or disease is selected from the group consisting of neurodegenerative diseases, multiple sclerosis, systemic lupus erythematosus, rheumatoid arthritis, atherosclerosis, encephalitis, meningitis, hepatitis, nephritis, sepsis, sarcoidosis, psoriasis, eczema, uticaria, type I diabetes, asthma, conjunctivitis, otitis, allergic rhinitis, chronic obstructive pulmonary disease, sinusitis, dermatitis, inflammatory bowel disease, Behcet's syndrome, gout, viral infections, bacterial infections, organ transplant conditions and skin transplant conditions.

9. The method of claim 8 wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease.

10. The method of claim 5, wherein said compound is administered in combination with a second therapeutic agent, wherein said second therapeutic agent is useful for treating neurodegenerative diseases, multiple sclerosis, systemic lupus erythematosus, rheumatoid arthritis, atherosclerosis, encephalitis, meningitis, hepatitis, nephritis, sepsis, sarcoidosis, psoriasis, eczema, uticaria, type I diabetes, asthma, conjunctivitis, otitis, allergic rhinitis, chronic obstructive pulmonary disease, sinusitis, dermatitis, inflammatory bowel disease, Behcet's syndrome, gout, viral infections, bacterial infections, organ transplant conditions or skin transplant conditions.

11. The method of claim 10 wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease.

12. A method of treating a CXCR3-mediated condition or disease in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1.

13. A method in accordance with claim 12, wherein said CXCR3-mediated condition is selected from the group consisting of neurodegenerative diseases, multiple sclerosis, systemic lupus erythematosus, rheumatoid arthritis, atherosclerosis, encephalitis, meningitis, hepatitis, nephritis, sepsis, sarcoidosis, psoriasis, eczema, uticaria, type I diabetes, asthma, conjunctivitis, otitis, allergic rhinitis, chronic obstructive pulmonary disease, sinusitis, dermatitis, inflammatory bowel disease, Behcet's syndrome, gout, viral infections, bacterial infections, organ transplant conditions and skin transplant conditions.

14. The method of claim 13 wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease.

15. The method of claim 12, wherein said compound modulates CXCR3.

16. The method of claim 12, wherein said compound is administered in combination with a second therapeutic agent, wherein said second therapeutic agent is useful for treating neurodegenerative diseases, multiple sclerosis, systemic lupus erythematosus, rheumatoid arthritis, atherosclerosis, encephalitis, meningitis, hepatitis, nephritis, sepsis, sarcoidosis, psoriasis, eczema, uticaria, type I diabetes, asthma, conjunctivitis, otitis, allergic rhinitis, chronic obstructive pulmonary disease, sinusitis, dermatitis, inflammatory bowel disease, Behcet's syndrome, gout, viral infections, bacterial infections, organ transplant conditions or skin transplant conditions.

17. The method of claim 16 wherein said inflammatory bowel disease is ulcerative colitis or Crohn's disease.

18. The method of claim 16, wherein said organ transplant condition is a bone marrow transplant condition or a solid organ transplant condition.

19. The method of claim 18, wherein said solid organ transplant condition is a kidney transplant condition, a liver transplant condition, a lung transplant condition, a heart transplant condition or a pancreas transplant condition.

20. A method in accordance with claim 12, wherein said CXCR3-mediated condition is psoriasis.

21. A method in accordance with claim 12, wherein said CXCR3-mediated condition is inflammatory bowel disease.

22. A method in accordance with claim 12, wherein said CXCR3-mediated condition is selected from the group consisting of multiple sclerosis, rheumatoid arthritis and organ transplant conditions.

23. A method in accordance with claim 12, wherein said compound is used in conjunction with another therapeutic agent selected from the group consisting of Remicade.RTM., Enbrel.RTM., a COX-2 inhibitor, a glucocoiticoid, an immunosuppressant, methotrexate, prednisolone, azathioprine, cyclophosphamide, tacrolimus, mycophenolate, hydroxychloroquine, sulfasalazine, cyclosponne A, D-penicillaniine, a gold compound, an antilymphocyte or antithymocyte globulin, betaseron, avonex and copaxone.

24.A method in accordance with claim 12, wherein said CXCR3-mediated condition is an organ transplant condition and said compound is used alone or in combination with a second therapeutic agent selected from the group consisting of cyclosporine A, FK-506, rapamycin, mycophenolate, prednisolone, azathioprine, cyclophosphamide and an antilymphocyte globulin.

25. A method in accordance with claim 12, wherein said CXCR3-mediated condition is rheumatoid arthritis and said compound is used alone or in combination with a second therapeutic agent selected from the group consisting of methotrexate, sulfasalazine, hydroxychloroquine, cyclosporine A, D-penicillamine, Remicade.RTM., Enbrel.RTM., auranofin and aurothioglucose.

26. A method in accordance with claim 12, wherein said CXCR3-mcdiated condition is multiple sclerosis and said compound is used alone or in combination with a second therapeutic agent selected from the group consisting of betaseron, avonex, azathioprine, copaxone, prednisolone and cyclophosphamide.

27. A method in accordance with claim 11, wherein said subject is a human.

28. A method for the modulation of CXCR3 function in a cell, comprising contacting said cell with the compound of claim 1.

29. A method for the modulation of CXCR3 function, comprising contacting a CXCR3 protein with the compound of claim 1.

30. A method of treating asthma in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

31. A method of treating rheumatoid arthritis in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

32. A method of treating psoriasis in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

33. A method of treating inflammatory bowel disease in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

34. A method of treating multiple sclerosis in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

35. A method of treating organ transplant conditions in a subject, said method comprising administering to a subject in need of such treatment a therapeutically effective amount of the compound of claim 1 or a salt thereof.

36. The pharmaceutical composition of claim 4 in a form suitable for topical use.

37. The pharmaceutical composition of claim 4 in a form of a sterile aqueous or oleagenous solution or suspension suitable for parenteral injection.

38. The pharmaceutical composition of claim 4 in a form suitable for oral use.

39. The method of claim 5, wherein said compound is administered parenterally.

40. The method of claim 5, wherein said compound is administered orally.

Details for Patent 6,794,379

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Bayer Healthcare Pharms BETASERON interferon beta-1b VIAL; SUBCUTANEOUS 103471 001 1993-07-23   Start Trial Tularik Inc. (South San Francisco, CA) 2021-06-06 RX Orphan search
Biogen AVONEX interferon beta-1a VIAL 103628 001 1996-05-17   Start Trial Tularik Inc. (South San Francisco, CA) 2021-06-06 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

International Patent Family for US Patent 6,794,379

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