Amelioration of cataracts, macular degeneration and other ophthalmic diseases

• US 7,825,134 B2
• Filed: 11/22/2004
• Issued: 11/02/2010
• Est. Priority Date: 05/19/2003
• Status: Expired due to Fees

• Current Assignee: Colby Pharmaceutical Company
• Original Assignee: Othera Holding, Inc.
• Inventors: Matier, William L., Patil, Ghanshyam
• Primary Examiner(s): Wang; Shengjun
• Application Number:
  US10/994,712
• Publication Number:
  US 20050131025A1
• Time in Patent Office: 2,171 Days
• Field of Search: 514/315, 424/400
• US Class Current: 514/315
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears

Abstract

Ophthalmically acceptable compositions used in arresting the development of macular degeneration, retinopathy, glaucoma, eyelid disorders, corneal disease, or uveitis are disclosed. The compositions comprise a pharmaceutically acceptable carrier or diluent and at least one compound having the formula:

wherein R₁, R₂, R₃, R₄, R₅, R₆, and R₇ are as defined herein.

Claims

1. A method of treating macular degeneration, retinopathy, glaucoma, conjunctival diseases, eyelid disorders, corneal disease or uveitis in a patient, the method comprising topically administering to the eye of such patient a composition comprising an ophthalmically acceptable carrier or diluent containing at least one compound having the formula:

2. The method of claim 1 wherein R₁, R₂, R₃, and R₄ are a C₁-C₃ alkyl.

3. The method of claim 2 wherein R₁, R₂, R₃, and R₄ are ethyl groups.

4. The method of claim 2 wherein R₁, R₂, R₃, and R₄ are methyl groups.

5. The method of claim 4 wherein:

each of R₅ is H or methyl,

R₆, is methyl substituted with benzyloxy or C₁-C₆ alkoxy; and

R₇ is methyl.

6. The method of claim 4 wherein:

each of R₅ is H or methyl,

R₆ and R₇ form a cyclopropyl group.

7. The method of claim 4 wherein:

R₅, R₆ and R₇ form a furanyl group.

8. The method of claim 4 wherein:

R₅ is H; and

R₆ and R₇ form a tetrahydrofuranyl group.

9. The method of claim 4 wherein:

R₅ is H; and

R₆ and R₇ form a cyclopropyl ring.

10. The method of claim 1, wherein the administration is via eye drops, eye wash or eye ointment.

11. The method of claim 1 further comprising administering a reducing agent to the patient.

12. The method of claim 11, wherein the reducing agent is coadministered with the composition.

13. The method of claim 11, wherein the reducing agent is administered separately from the composition.

14. The method of claim 11 wherein the reducing agent is a sulfhydryl compound.

15. The method of claim 14 further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β

-mercaptoethylamine, or glutathione to the patient.

16. The method of claim 11 wherein the reducing agent is administered via eye drops, eye wash or ophthalmic ointment.

17. The method of claim 1 wherein said compound is administered to achieve a concentration in the tissues and fluids of about 0.1 μ

M to about 10 mM.

18. The method of claim 1 wherein said compound is administered to achieve a concentration in the tissues and fluids of about 1 μ

M to about 5 mM.

19. The method of claim 1 wherein said compound is administered to achieve a concentration in the tissues and fluids of about 25 μ

M to about 1 mM.

20. The method of claim 1 wherein said compound is administered to achieve a concentration in the tissues and fluids of about 50 μ

M to about 100 μ

M.

21. The method of claim 1 wherein said disease or disorder is blepharitis.

22. The method of claim 1 wherein said disease or disorder is ocular rosacea.

23. The method of claim 1 wherein said disease or disorder is macular degeneration.

24. The method of claim 1 wherein said disease or disorder is retinopathy.

25. The method of claim 1 wherein said disease or disorder is glaucoma.

26. The method of claim 1 wherein said composition further comprises a second compound used to treat said macular degeneration, retinopathy, glaucoma, conjunctival diseases, eyelid disorders, corneal disease or uveitis.

27. The method of claim 26 wherein said second compound is administered simultaneously.

28. The method of claim 26 wherein said second compound is administered sequentially.