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Last Updated: December 23, 2024

Claims for Patent: 8,168,614


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Summary for Patent: 8,168,614
Title:Boron-containing small molecules as anti-inflammatory agents
Abstract: Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.
Inventor(s): Baker; Stephen J. (Mountain View, CA), Sanders; Virginia (San Francisco, CA), Akama; Tsutomu (Sunnyvale, CA), Bellinger-Kawahara; Carolyn (Redwood City, CA), Freund; Yvonne (Los Altos, CA), Maples; Kirk R. (San Jose, CA), Plattner; Jacob J. (Berkeley, CA), Zhang; Yong-Kang (San Jose, CA), Zhou; Huchen (Shanghai, CN), Hernandez; Vincent S. (Watsonville, CA)
Assignee: Anacor Pharmaceuticals, Inc. (Palo Alto, CA)
Application Number:11/676,120
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,168,614
Patent Claims: 1. A method of treating an inflammatory-related disease in a human or an animal, said method comprising administering to the human or the animal a therapeutically effective amount of a compound which is selected from the group consisting of ##STR00126## ##STR00127## ##STR00128## or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, further comprising administering said compound as part of a pharmaceutical formulation, said formulation further comprising a pharmaceutically acceptable excipient.

3. The method of claim 1, wherein said compound is present in a form which is a member selected from a hydrate with water, a solvate with an alcohol, an adduct with an amino compound, and an adduct with an acid.

4. The method of claim 1, wherein said compound has a structure which is selected from the group consisting of ##STR00129##

5. The method of claim 1, wherein the compound is in an amount sufficient to treat the inflammatory-related disease by inhibiting pro-inflammatory cytokine expression or by stimulating anti-inflammatory cytokine expression, but the amount is less than sufficient to substantially inhibit cyclin dependent kinases.

6. The method of claim 5, wherein the compound has a structure which is selected from the group consisting of ##STR00130##

7. The method of claim 1, wherein the disease is a member selected from arthritis, rheumatoid arthritis, an inflammatory bowel disease, psoriasis, multiple sclerosis, a neurodegenerative disorder, congestive heart failure, stroke, aortic valve stenosis, kidney failure, lupus, pancreatitis, allergy, fibrosis, anemia, atherosclerosis, a metabolic disease, a bone disease, a cardiovascular disease, a chemotherapy/radiation related complication, diabetes type I, diabetes type II, a liver disease, a gastrointestinal disorder, an ophthalmological disease, allergic conjunctivitis, diabetic retinopathy, Sjogren's syndrome, uveitis, a pulmonary disorder, a renal disease, dermatitis, HIV-related cachexia, cerebral malaria, ankylosing spondylitis, leprosy, anemia and fibromyalgia.

8. The method of claim 7, wherein the compound has a structure which is selected from the group consisting of ##STR00131##

9. The method of claim 7, wherein the neurodegenerative disorder is a member selected from Alzheimer's disease and Parkinson disease, the inflammatory bowel disease is a member selected from Crohn's disease or ulcerative colitis; the gastrointestinal complication is diarrhea; the liver disease is a member selected from an autoimmune hepatitis, hepatitis C, primary biliary cirrhosis, primary sclerosing cholangitis and fulminant liver failure; the gastrointestinal disorder is a member selected from celiac disease and non-specific colitis; the pulmonary disorder is a member selected from allergic rhinitis, asthma, chronic obstructive pulmonary disease, chronic granulomatous inflammation, cystic fibrosis, and sarcoidosis; the cardiovascular disease is a member selected from atheroscleotic cardiac disease, congestive heart failure and restenosis; and the renal disease is a member selected from glomerulonephritis and vasculitis.

10. The method of claim 9, wherein the compound has a structure which is selected from the group consisting of ##STR00132##

11. The method of claim 1, wherein the compound is administered at a concentration sufficient to inhibit a cytokine which is a member selected from IL-1.alpha., .beta., IL-2, IL-3, IL-6, IL-7, IL-9, IL-12, IL-17, IL-18, IL-23, TNF-.alpha., LT, LIF, Oncostatin, and IFNc1.alpha., .beta., .gamma..

12. The method of claim 11, wherein the compound has a structure which is selected from the group consisting of ##STR00133##

13. The method of claim 1, where the compound is administered at a concentration sufficient to stimulate expression of a cytokine which is a member selected from IL-4, IL-10, IL-11, W-13 and TGF-.beta..

14. The method of claim 13, wherein the compound has a structure which is selected from the group consisting of ##STR00134##

15. A method of treating an inflammatory-related disease associated with cytokine expression levels, which comprises administering to a human or an animal in need of such treatment a compound which is selected from the group consisting of ##STR00135## ##STR00136## ##STR00137## or a pharmaceutically acceptable salt thereof.

16. The method of claim 15, wherein the compound has a structure which is selected from the group consisting of ##STR00138##

17. The method of claim 1, wherein the animal is a human being.

18. A method for inhibiting the production of an inflammatory cytokinc protein by cells capable of producing said inflammatory cytokine protein, said method comprising: combining said cells with a therapeutic amount of, a compound which is selected from the group consisting of ##STR00139## ##STR00140## ##STR00141## or a pharmaceutically acceptable salt thereof, wherein production of said inflammatory cytokine by said cells is inhibited.

19. The method of claim 18, wherein the compound has a structure which is selected from the group consisting of ##STR00142##

20. The method of claim 18, wherein said therapeutic amount is sufficient to inhibit the production of said inflammatory cytokine protein between about 50% and about 99%.

21. A method for inhibiting an inflammatory response in a human or an animal, said method comprising: contacting said human or animal with a therapeutic amount of a compound which is selected from the group consisting of ##STR00143## ##STR00144## ##STR00145## or a pharmaceutically acceptable salt thereof, wherein said inflammatory response is inhibited.

22. The method of claim 21, wherein the compound has a structure which is selected from the group consisting of ##STR00146##

23. The method of claim 1, wherein the disease is a member selected from Crohn's disease, ulcerative colitis, arthritis, rheumatoid arthritis, psoriasis, Alzheimer's disease, Parkinson disease, atopic dermatitis, and actinic keratosis.

24. The method of claim 23, wherein the compound has a structure selected from the group consisting of ##STR00147##

25. A method of treating an inflammatory-related disease in a human or an animal, said method comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00148## or a pharmaceutically acceptable salt thereof.

26. A method of treating an inflammatory-related disease in a human or an animal, said method comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00149## or a pharmaceutically acceptable salt thereof.

27. A method of treating psoriasis, comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00150## or a pharmaceutically acceptable salt thereof.

28. A method of treating psoriasis, comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00151## or a pharmaceutically acceptable salt thereof.

29. A method of treating atopic dermatitis, comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00152## or a pharmaceutically acceptable salt thereof.

30. A method of treating atopic dermatitis, comprising administering to the human or the animal a therapeutically effective amount of a compound having the following structure ##STR00153## or a pharmaceutically acceptable salt thereof.

31. The method of claim 25, wherein the inflammatory-related disease is dermatitis or eczema.

32. The method of claim 25, wherein the inflammatory-related disease is contact dermatitis.

33. The method of claim 25, wherein the inflammatory-related disease is rheumatoid arthritis or psoriatic arthritis.

34. The method of claim 26, wherein the inflammatory-related disease is dermatitis or eczema.

35. The method of claim 26, wherein the inflammatory-related disease is contact dermatitis.

36. The method of claim 26, wherein the inflammatory-related disease is rheumatoid arthritis or psoriatic arthritis.

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