.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 8,889,656

« Back to Dashboard

Details for Patent: 8,889,656

Title:Boron-containing small molecules
Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
Inventor(s): Baker; Stephen J. (Mountain View, CA), Akama; Tsutomu (Sunnyvale, CA), Bellinger-Kawahara; Carolyn (West Linn, OH), Hernandez; Vincent S. (Watsonville, CA), Hold; Karin M. (Belmont, CA), Leyden; James J. (Malvern, PA), Maples; Kirk R. (San Jose, CA), Plattner; Jacob J. (Orinda, CA), Sanders; Virginia (San Francisco, CA), Zhang; Yong-Kang (San Jose, CA)
Assignee: Anacor Pharmaceuticals, Inc. (Palo Alto, CA)
Filing Date:Apr 30, 2013
Application Number:13/874,329
Claims:1. A pharmaceutical composition, comprising: (a) 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof; (b) a pharmaceutically acceptable excipient for use in an animal suffering from an infection by a microorganism.

2. The pharmaceutical composition of claim 1, wherein said pharmaceutical composition is for topical administration.

3. The pharmaceutical composition of claim 1, wherein said excipient is a pharmaceutically acceptable topical carrier.

4. The pharmaceutical composition of claim 1, wherein said formulation is a member selected from a lacquer, lotion, cream, gel, ointment, and spray.

5. The pharmaceutical composition of claim 1, wherein said composition is a lacquer.

6. The pharmaceutical composition of claim 1, wherein said composition is a gel.

7. The pharmaceutical composition of claim 1, wherein said composition further comprises one or more members selected from an emulsifier, emollient, antioxidant, preservative, chelating agent, neutralizing agent, viscosity increasing agent, penetration enhancer, anti-inflammatory agent, vitamin, anti-aging agent, sunscreen, and acne-treating agent.

8. The pharmaceutical composition of claim 1, wherein said composition further comprises a member selected from the group consisting of a thickener, a gel phase carrier, nail penetration enhancer, and a viscosity increasing agent.

9. The pharmaceutical composition of claim 1, wherein said composition comprises a chelating agent.

10. The pharmaceutical composition of claim 9, wherein said chelating agent is selected from the group selected from citric acid, ethylene diamine tetraacetic acid (EDTA), ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA) and 8-Amino-2-[(2-amino-5-methylphenoxy)methyl]-6-methoxyquinoline-N,N,N',N'-- tetraacetic acid, tetrapotassium salt (QUIN-2).

11. The pharmaceutical composition of claim 9, wherein said chelating agent is ethylene diamine tetraacetic acid.

12. The pharmaceutical composition of claim 9, wherein said chelating agent is present in an amount of between 0.005% to 2% by weight.

13. The pharmaceutical composition of claim 1, wherein said composition comprises alcohol.

14. The pharmaceutical composition of claim 1, wherein said composition comprises alcohol and water.

15. The pharmaceutical composition of claim 1, wherein said composition comprises one or more members selected from ethanol and propylene glycol.

16. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole is present in said composition in a concentration from about 0.5% to about 15% w/v.

17. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole is present in said composition in a concentration from about 0.1% to about 12.5% w/v.

18. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole is present in said composition in a concentration from about 1% to about 5% w/v.

19. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole is present in said composition in a concentration from about 2% to about 8% w/v.

20. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro- 1-hydroxy-2,1-benzoxaborole is present in said composition in a concentration from about 4% to about 9% w/v.

21. The pharmaceutical composition of claim 1, wherein said 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole 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.

22. The pharmaceutical composition of claim 1, wherein a site of said topical administration is skin or nail or hair or skin surrounding the nail or skin surrounding the hair.

23. The pharmaceutical composition of claim 1, wherein the microorganism is a fungus or a yeast.

24. The pharmaceutical composition of claim 23, wherein said fungus or yeast is a member selected from Candida species, Trichophyton species, Microsporium species, Aspergillus species, Cryptococcus species, Blastomyces species, Cocciodiodes species, Histoplasma species, Paracoccidiodes species, Phycomycetes species, Malassezia species, Fusarium species, Epidermophyton species, Scytalidium species, Scopulariopsis species, Alternaria species, Penicillium species, Phialophora species, Rhizopus species, Scedosporium species and Zygomycetes species.

25. The pharmaceutical composition of claim 23, wherein said fungus or yeast is a member selected from Aspergilus fumigatus, Blastomyces dermatitidis, Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans, Candida parapsilosis, Candida tropicalis, Cocciodiodes immitis, Epidermophyton floccosum, Fusarium solani, Histoplasma capsulatum, Malassezia furfur, Malassezia pachydermatis, Malassezia sympodialis, Microsporum audouinii, Microsporum canis, Microsporum gypseurn, Paracoccidiodes brasiliensis, Trichophyton mentagrophytes, Trichophyton rubrum and Trichophyton tonsurans.

26. The pharmaceutical composition of claim 23, wherein said fungus or yeast is a member selected from Trichophyton concentricum, Trichophyton violaceum, Trichophyton schoenleinii, Trichophyton verrucosum, Trichophyton soudanense, Microsporum gypseum, Microsporum equinum, Candida guilliermondii, Malassezia globosa, Malassezia obtuse, Malassezia restricta, Malassezia slooffiae and Aspergillus flavus.

27. The pharmaceutical composition of claim 23, wherein said fungus or yeast is a dermatophyte.

28. The pharmaceutical composition of claim 23, wherein said fungus or yeast is a member selected from Tinea unguium, Trichophyton rubrum and Trichophyton mentagrophytes.

29. The pharmaceutical composition of claim 1, wherein the infection is a cutaneous infection.

30. The pharmaceutical composition of claim 1, wherein the infection is a member selected from an ungual, periungual and subungual infection.

31. The pharmaceutical composition of claim 1, wherein the infection is onychomycosis.

32. The pharmaceutical composition of claim 1, wherein the animal is a human.

33. The pharmaceutical composition of claim 1, wherein said composition is in a cosmetically effective amount.

34. The pharmaceutical composition of claim 1, wherein said composition is in a therapeutically effective amount.

35. A method of treating an infection in an animal, said method comprising administering to the animal a therapeutically effective amount of 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof, sufficient to treat said infection.

36. The method of claim 35, wherein said infection is a member selected from a systemic infection, a cutaneous infection, and an ungual or periungual infection.

37. The method of claim 35, wherein said infection is a member selected from chloronychia, paronychia, erysipeloid, gonorrhea, swimming-pool granuloma, leprosy, acute bacterial perionyxis, sporotrichosis, syphilis, tuberculosis verrucosa cutis, tularemia, Mycotic keratitis, Extension oculomycosis, Endogenous oculomycosis, Lobomycosis, Mycetoma, Piedra, Pityriasis versicolor, Tinea corporis, Tinea cruris, Tinea pedis, Tinea barbae, Tinea capitis, Tinea nigra, Otomycosis, Tinea favosa, Chromomycosis, and Tinea imbricata.

38. The method of claim 35, wherein said infection is onychomycosis.

39. The method of claim 35, wherein said onychomycosis is tinea unguium.

40. The method of claim 35, wherein said animal is a member selected from a cattle, goat, pig, sheep, horse, cow, bull, dog, guinea pig, gerbil, rabbit, cat, chicken, and turkey.

41. The method of claim 35, wherein said animal is a human.

42. The method of claim 35, wherein, the administering is at a site which is a member selected from the skin, nail, hair, hoof and claw.

43. The method of claim 42, wherein said skin is the skin surrounding the nail, hair, hoof or claw.

44. The method of claim 35, wherein said infection is a fungal infection.

45. A method of treating onychomycosis in a human, said method comprising administering to the human a therapeutically effective amount of 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof, sufficient to treat said onychomycosis.

46. A method of inhibiting the growth of a fungus in a human, said method comprising administering to the human a therapeutically effective amount of 1,3-dihydro-5-chloro-1-hydroxy-2,1-benzoxaborole, or a pharmaceutically acceptable salt thereof.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc