IP Library Granted Patent US 7,825,134
Granted Patent B2
US 7,825,134 · App. 10/994,712 · Granted Nov 2, 2010

Amelioration of cataracts, macular degeneration and other ophthalmic diseases

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Quick Facts
Patent No.
US 7,825,134
App. No.
10/994,712
Granted
Nov 2, 2010
Kind
B2
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 R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined herein.

Claims (45)

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:

where R 1 and R 2 are, independently, H or C 1 to C 3 alkyl;

R 3 and R 4 are, independently C 1 to C 3 alkyl; and

where R 1 and R 2 , taken together, or R 3 and R 4 , taken together, or both may be cycloalkyl;

R 5 is H, OH, or C 1 to C 6 alkyl;

R 6 is or C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl;

R 7 is C 1 to C 6 alkyl, alkenyl, alkynyl, or substituted alkyl or alkenyl

or where R 6 and R 7 , or R 5 , R 6 and R 7 , taken together, form a carbocycle or heterocycle having from 3 to 7 atoms in the ring.

2. The method of claim 1 wherein R 1 , R 2 , R 3 , and R 4 are a C 1 -C 3 alkyl.

3. The method of claim 2 wherein R 1 , R 2 , R 3 , and R 4 are ethyl groups.

4. The method of claim 2 wherein R 1 , R 2 , R 3 , and R 4 are methyl groups.

5. The method of claim 4 wherein:

each of R 5 is H or methyl,

R 6 , is methyl substituted with benzyloxy or C 1 -C 6 alkoxy; and

R 7 is methyl.

6. The method of claim 4 wherein:

each of R 5 is H or methyl,

R 6 and R 7 form a cyclopropyl group.

7. The method of claim 4 wherein:

R 5 , R 6 and R 7 form a furanyl group.

8. The method of claim 4 wherein:

R 5 is H; and

R 6 and R 7 form a tetrahydrofuranyl group.

9. The method of claim 4 wherein:

R 5 is H; and

R 6 and R 7 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 μM 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 μM 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 μM 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 μM to about 100 μM.

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.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 5, 2012
From: OTHERA HOLDING, INC.
To: COLBY PHARMACEUTICAL COMPANY
Reel/Frame 029084/0164 →
RELEASE OF SECURITY INTEREST Recorded Dec 30, 2009
From: OXFORD FINANCE CORPORATION
To: OTHERA HOLDING, INC.
Reel/Frame 023720/0076 →
SECURITY AGREEMENT Recorded Oct 20, 2009
From: OTHERA HOLDING, INC.
To: OXFORD FINANCE CORPORATION
Reel/Frame 023390/0874 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 30, 2006
From: OTHERA PHARMACEUTICALS, INC.
To: OTHERA HOLDING, INC.
Reel/Frame 018189/0968 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2005
From: MATIER, WILLIAM L.; PATIL, GHANSHAYAM
To: OTHERA PHARMACEUTICALS, INC.
Reel/Frame 015773/0438 →