US2008241232A1PendingUtilityA1

Use of green porphyrins to treat neovasculature in the eye

73
Individually held — no corporate assignee on recordPriority: Mar 14, 1994Filed: Sep 25, 2007Published: Oct 2, 2008
Est. expiryMar 14, 2014(expired)· nominal 20-yr term from priority
Inventors:Joan W. MillerEvangelos S. Gragoudas
A61K 9/0019A61K 49/0036A61K 31/409A61K 9/1275A61K 41/0071A61K 49/0084A61F 9/008A61K 31/555
73
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Claims

Abstract

Photodynamic therapy of conditions of the eye characterized by unwanted neovasculature, such as age-related macular degeneration, is effective using green porphyrins as photoactive agents, preferably as liposomal compositions.

Claims

exact text as granted — not AI-modified
1 . A method to treat conditions of the eye characterized by unwanted neovasculature, which method comprises:
 administering to a subject in need of such treatment an amount of liposomal formulation of green porphyrin sufficient to permit an effective amount to localize in said neovasculature;   permitting sufficient time to elapse to allow an effective amount of said green porphyrin to localize in said neovasculature; and   irradiating neovasculature with light absorbed by the green porphyrin.   
     
     
         2 . The method of  claim 1  wherein the neovasculature is choroidal neovasculature. 
     
     
         3 . The method of  claim 1  wherein the green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4 . 
     
     
         4 . The method of  claim 1  wherein said green porphyrin is of a formula shown in  FIG. 1  or a mixture thereof
 wherein each of R 1  and R 2  is independently selected from the group consisting of carbalkoxyl (2-6 C), alkyl (1-6 C), arylsulfonyl (6-10 C), cyano and —CONR 5 CO wherein R 5  is aryl (6-10 C) or alkyl (1-6 C);   each R 3  is independently carboxyl, carboxyalkyl (2-6 C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6 C);   R 4  is CH═CH 2  or —CH(OR 4 )CH 3  wherein R 4  is H, or alkyl (1-6 C) optionally substituted with a hydrophilic substituent.   
     
     
         5 . The method of  claim 4  wherein said green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4  or a mixture thereof and wherein each of R 1  and R 2  is independently carbalkoxyl (2-6 C);
 one R 3  is carboxyalkyl (2-6 C) and the other R 3  is the ester of a carboxyalkyl (2-6 C) substituent; and   R 4  is CH═CH 2  or —CH(OH)CH 3 .   
     
     
         6 . The method of  claim 5  wherein said green porphyrin is of the formula shown in  FIG. 1-3  and
 wherein R 1  and R 2  are methoxycarbonyl;   one R 3  is —CH 2 CH 2 COOCH 3  and the other R 3  is CH 2 CH 2 COOH; and   R 4  is CH═CH 2 .   
     
     
         7 . A method to treat unwanted choroidal neovasculature which method comprises
 administering to a subject in need of such in need of such treatment an amount of green porphyrin sufficient to permit an effective amount to localize in said choroidal neovasculature;   permitting sufficient time to elapse to allow an effective amount of said green porphyrin to localize in said choroidal neovasculature; and   irradiating said choroidal neovasculature with light absorbed by the green porphyrin.   
     
     
         8 . The method of  claim 7  wherein said green porphyrin is complexed with low-density lipoprotein. 
     
     
         9 . The method of  claim 7  wherein said green porphyrin is contained in a liposomal preparation. 
     
     
         10 . The method of  claim 7  wherein the green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4 . 
     
     
         11 . The method of  claim 7  wherein said green porphyrin is of a formula shown in  FIG. 1  or a mixture thereof
 wherein each of R 1  and R 2  is independently selected from the group consisting of carbalkoxyl (2-6 C), alkyl (1-6 C), arylsulfonyl (6-10 C), cyano and —CONR 5 CO wherein R 5  is aryl (6-10 C) or alkyl (1-6 C);   each R 3  is independently carboxyl, carboxyalkyl (2-6 C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6 C);   R 4  is CH═CH 2  or —CH(OR 4 ′)CH 3  wherein R 4 ′ is H, or alkyl (1-6 C) optionally substituted with a hydrophilic substituent.   
     
     
         12 . The method of  claim 11  wherein said green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4  or a mixture thereof and wherein each of R 1  and R 2  is independently carbalkoxyl (2-6 C);
 one R 3  is carboxyalkyl (2-6 C) and the other R 3  is the ester of a carboxyalkyl (2-6 C) substituent; and   R 4  is CH═CH 2  or —CH(OH)CH 3 .   
     
     
         13 . The method of  claim 12  wherein said green porphyrin is of the formula shown in.  FIG. 1-3  and
 wherein R 1  and R 2  are methoxycarbonyl;   one R 3  is —CH 2 CH 2 COOCH 3  and the other R 3  is CH 2 CH 2 COOH; and   R 4  is CH═CH 2 .   
     
     
         14 . A method to treat age-related macular degeneration (AMD) which method comprises
 administering to a subject in need of such treatment an amount of green porphyrin sufficient to permit an effective amount to localize in the choroid;   permitting sufficient time to elapse to allow an effective amount of said green porphyrin to localize in said choroid; and   irradiating said choroid with light absorbed by the green porphyrin.   
     
     
         15 . The method of  claim 14  wherein said green porphyrin is complexed with low-density lipoprotein. 
     
     
         16 . The method of  claim 14  wherein said green porphyrin is contained in a liposomal preparation. 
     
     
         17 . The method of  claim 14  wherein the green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4 . 
     
     
         18 . The method of  claim 14  wherein said green porphyrin is of a formula shown in  FIG. 1  or a mixture thereof
 wherein each of R 1  and R 2  is independently selected from the group consisting of carbalkoxyl (2-6 C) alkyl (1-6 C), arylsulfonyl (6-10 C), cyano and —CONR 5 CO wherein R 5  is aryl (6-10 C) or alkyl (1-6 C);   s each R 3  is independently carboxyl, carboxyalkyl (2-6 C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6 C);   R 4  is CH═CH 2  or —CH(OR 4 )CH 3  wherein R 4 ′ is H, or alkyl (1-6 C) optionally substituted with a hydrophilic substituent.   
     
     
         19 . The method of  claim 18  wherein said green porphyrin is of the formula shown in  FIG. 1-3  or  1 - 4  or a mixture thereof and wherein each of R 1  and R 2  is independently carbalkoxyl (2-6 C);
 one R 3  is carboxyalkyl (2-6 C) and the other R 3  is the ester of a carboxyalkyl (2-6 C) substituent; and   R 4  is CH═CH 2  or —CH(OH)CH 3 .   
     
     
         20 . The method of  claim 19  wherein said green porphyrin is of the formula shown in  FIG. 1-3  and wherein R 1  and R 2  are methoxycarbonyl;
 one R 3  is —CH 2 CH 2 COOCH 3  and the other R 3  is CH 2 CH 2 COOH; and   R 4  is CH═CH 2 .

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