US2013131052A1PendingUtilityA1

Amelioration Of The Development Of Cataracts And Other Ophthalmic Diseases

55
Individually held — no corporate assignee on recordPriority: May 17, 2002Filed: Dec 21, 2012Published: May 23, 2013
Est. expiryMay 17, 2022(expired)· nominal 20-yr term from priority
Inventors:William L. MatierGhanshyam Patil
A61P 39/06C07D 401/12C07D 405/12A61K 31/454A61K 38/063A61K 31/445A61P 27/12C07D 413/12A61K 31/198A61P 27/02A61K 31/4525C07D 211/94A61K 31/5377A61K 45/06A61K 31/496A61K 31/4545C07D 417/12A61K 9/0048A61K 31/541
55
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Ophthalmically acceptable compositions used in arresting the development of cataracts or macular degeneration comprising a pharmaceutically acceptable carrier or diluent and a 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.

Claims

exact text as granted — not AI-modified
What is claimed: 
     
         1 . An ophthalmic composition comprising an ophthalmically acceptable carrier or diluent and a compound having an N-hydroxy piperidine portion bound to a solubility modifying portion, the compound having a solubility in water at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient at 25° C. of at least about 5. 
     
     
         2 . The composition of  claim 1  wherein the N-hydroxy piperidine portion is cleaved from the compound under conditions found in the eye. 
     
     
         3 . The composition of  claim 1  wherein the N-hydroxy piperidine portion is cleaved from the compound under conditions found in the lens of the eye. 
     
     
         4 . The composition of  claim 1  wherein the N-hydroxy piperidine portion is cleaved enzymatically. 
     
     
         5 . The composition of  claim 1  wherein the N-hydroxy piperidine portion is 1-oxyl-4-hydroxy-2,2,6,6-tetramethylpiperidyl. 
     
     
         6 . The composition of  claim 1  further comprising a reducing agent. 
     
     
         7 . The composition of  claim 6  wherein the reducing agent is a sulfhydryl compound. 
     
     
         8 . The composition of  claim 1  further comprising mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione. 
     
     
         9 . A method of administering an antioxidant to a mammal comprising contacting the mammal with a composition comprising a pharmaceutically acceptable carrier or diluent and a compound having an N-hydroxy piperidine portion bound to a solubility modifying portion, the compound having a solubility in water at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient at 25° C. of at least about 5. 
     
     
         10 . The method of  claim 9  wherein the composition further comprises a reducing agent. 
     
     
         11 . The method of  claim 9  further comprising coadministering a reducing agent to the patient. 
     
     
         12 . The method of  claim 11  wherein the reducing agent is a sulfhydryl compound. 
     
     
         13 . The method of  claim 9  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         14 . The method of  claim 11  wherein the coadministration is via eye drops or eye wash. 
     
     
         15 . The method of  claim 9  wherein the contact is made via eye drops; eye wash; aerosol; enema or suppositories; oral tablets; liquids and sprays; intravenous, subcutaneous, and intraperitoneal injections; or application to the skin as a patch or ointment. 
     
     
         16 . A method for identifying a pharmaceutical for delivery to the eye of a patient in the form of eye drops comprising selecting a compound having a water solubility at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient of at least about 5 at 25° C., which compound is enzymatically cleavable under conditions obtained in the lens of the eye of a patient to give rise to an N-hydroxy piperidine. 
     
     
         17 . The method of  claim 16  further comprising coadministering a reducing agent to the patient. 
     
     
         18 . The method of  claim 17  wherein the reducing agent is a sulfhydryl compound. 
     
     
         19 . The method of  claim 16  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         20 . A method of administering an antioxidant to a mammal comprising contacting the mammal with a composition comprising a pharmaceutically acceptable carrier or diluent with a 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. 
 
     
     
         21 . The method of  claim 20  wherein said composition is ophthalmically acceptable. 
     
     
         22 . The method of  claim 20  further comprising coadministering a reducing agent to the patient. 
     
     
         23 . The method of  claim 22  wherein the reducing agent is a sulfhydryl compound. 
     
     
         24 . The method of  claim 20  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         25 . The method of  claim 22  wherein the coadministration is via eye drops or eye wash. 
     
     
         26 . The method of  claim 20  wherein the contact is made via eye drops; eye wash; aerosol; enema or suppositories; oral tablets; liquids and sprays; intravenous, subcutaneous, and intraperitoneal injections; or application to the skin as a patch or ointment. 
     
     
         27 . A method of ameliorating the development of a cataract in the eye of a patient comprising administering to the eye of such patient an ophthalmic composition comprising an ophthalmically acceptable carrier or diluent containing a 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 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 atoms. 
 
     
     
         28 . The method of  claim 27  further comprising coadministering a reducing agent to the patient. 
     
     
         29 . The method of  claim 28  wherein the reducing agent is a sulfhydryl compound. 
     
     
         30 . The method of  claim 27  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         31 . The method of  claim 28  wherein the coadministration is via eye drops or eye wash. 
     
     
         32 . A method of ameliorating the development of a cataract in the eye of a patient comprising administering to the eye of such patient an ophthalmic composition comprising an ophthalmically acceptable carrier or diluent and a compound having an N-hydroxy piperidine portion bound to a solubility modifying portion, the compound having a solubility in water at 25° C. of at least about 0.25% by weight and a water-n-octonal partition coefficient at 25° C. of at least about 5. 
     
     
         33 . The method of  claim 32  further comprising coadministering a reducing agent to the patient. 
     
     
         34 . The method of  claim 33  wherein the reducing agent is a sulfhydryl compound. 
     
     
         35 . The method of  claim 32  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         36 . The method of  claim 33  wherein the coadministration is via eye drops or eye wash. 
     
     
         37 . A method of treating macular degeneration in the lens of a patient comprising administering to the eye of such patient an ophthalmologic composition comprising an ophthalmically acceptable carrier or diluent in the form of eye drops containing a 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. 
 
     
     
         38 . The method of  claim 37  further comprising coadministering a reducing agent to the patient. 
     
     
         39 . The method of  claim 38  wherein the reducing agent is a sulfhydryl compound. 
     
     
         40 . The method of  claim 37  further comprising coadministering mercaptopropionyl glycine, N-acetyl cysteine, β-mercaptoethylamine, or glutathione to the patient. 
     
     
         41 . The method of  claim 37  wherein the coadministration is via eye drops or eye wash.

Join the waitlist — get patent alerts

Track US2013131052A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.