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Details for Patent: 8,239,978

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Details for Patent: 8,239,978

Title:Vision through photodynamic therapy of the eye
Abstract: Photodynamic therapy of conditions of the eye, especially those conditions characterized by unwanted neovasculature, such as age-related macular degeneration, results in enhanced visual acuity for treated subjects.
Inventor(s): Strong; H. Andrew (North Vancouver, CA), Levy; Julia G. (Vancouver, CA), Huber; Gustav (Zurich, CH), Fsadni; Mario (Buelach, CH)
Assignee: Novartis Opthalmics AG (Basel, CH)
Filing Date:Sep 10, 2007
Application Number:11/852,965
Claims:1. A method to enhance visual acuity as determined by ability to discern letters of certain sizes in standard eye charts in a human subject, which method comprises: (a) irradiating target ocular tissue in said subject with light absorbed by a photoactive compound that has been administered to said subject and localized to said ocular tissue, and (b) repeating said administering said photoactive compound and irradiating of ocular tissue at least once; whereby visual acuity in said subject is enhanced.

2. The method of claim 1 wherein an eye of said subject contains unwanted neovasculature.

3. The method of claim 2 wherein the neovasculature is choroidal neovasculature.

4. The method of claim 1 wherein the photoactive compound is a green porphyrin, a hematoporphyrin derivative, a chlorin, or a phlorin.

5. The method of claim 4 wherein the photoactive compound is a green porphyrin of the formula ##STR00001## wherein each of R.sup.1 and R.sup.2 is independently selected from the group consisting of carbalkoxyl (2-6C), alkyl (1-6C), arylsulfonyl (6-10C), cyano and --CONR.sup.5CO-- wherein R.sup.5 is aryl (6-10C) or alkyl (1-6C); each R.sup.3 is independently carboxyl, carboxyalkyl (2-6C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6C); R.sup.4 is CH.dbd.CH.sub.2 or --CH(OR.sup.4')CH.sub.3 wherein R.sup.4' is H, or alkyl (1-6C) optionally substituted with a hydrophilic substituent.

6. The method of claim 1 wherein said photoactive compound is contained in a liposomal preparation.

7. The method of claim 1 wherein said subject has been diagnosed with age-related macular degeneration (AMD).

8. The method of claim 1 wherein the subject has been diagnosed with a condition selected from the group consisting of macular degeneration, ocular histoplasmosis syndrome, myopia, and inflammatory diseases.

9. The method of claim 1 wherein said irradiation is administered at an irradiance of about 600 mW/cm.sup.2 to provide a total fluence of 50 J/cm.sup.2-150 J/cm.sup.2 of said light.

10. The method of claim 1, wherein said repeating is performed two weeks following the irradiating of ocular tissue in step (a).

11. A method of detecting an improvement in visual acuity, said method comprising measuring visual acuity as determined by ability to discern letters of certain sizes in standard eye charts of a human subject, which method comprises: (a) irradiating target ocular tissue in said subject with light absorbed by a photoactive compound that has been administered to said subject and localized to said ocular tissue, and (b) repeating said administering said photoactive compound and irradiating of ocular tissue at least once; followed by (c) measuring visual acuity in said subject by determining ability to discern letters of certain sizes in standard eye charts, thereby detecting an improvement in visual acuity.

12. The method of claim 10, which further comprises (c) repeating said administering said photoactive compound and irradiating of ocular tissue at least once six weeks following the irradiating of ocular tissue in step (b).

13. The method of claim 1 wherein said irradiation is administered beginning about 5-30 minutes after said subject has been administered said photoactive compound.

14. The method of claim 4 wherein said green porphyrin is of the formula ##STR00002## wherein each of R.sup.1 and R.sup.2 is independently carbalkoxyl (2-6C); one R.sup.3 is carboxyalkyl (2-6C) and the other R.sup.3 is the ester of a carboxyalkyl (2-6C) substituent; and R.sup.4 is CH.dbd.CH.sub.2 or --CH(OH)CH.sub.3.

15. The method of claim 14 wherein said green porphyrin is of the formula ##STR00003## and wherein R.sup.1 and R.sup.2 are methoxycarbonyl; one R.sup.3 is --CH.sub.2CH.sub.2COOCH.sub.3 and the other R.sup.3 is CH.sub.2CH.sub.2COOH; and R.sup.4 is CH.dbd.CH.sub.2.

16. The method of claim 1 wherein said irradiation is administered beginning about 5 minutes after said subject has been administered said formulation.

17. The method of claim 1, wherein the light is emitted from a laser.

18. The method of claim 1, further comprising measuring visual acuity in the subject.

19. The method of claim 11 wherein the photoactive compound is a green porphyrin, a hematoporphyrin derivative, a chlorin, or a phlorin.

20. The method of claim 19 wherein said photoactive agent is a green porphyrin of the formula ##STR00004## wherein each of R.sup.1 and R.sup.2 is independently selected from the group consisting of carbalkoxyl (2-6C), alkyl (1-6C), arylsulfonyl (6-10C), cyano and --CONR.sup.5CO-- wherein R.sup.5 is aryl (6-10C) or alkyl (1-6C); each R.sup.3 is independently carboxyl, carboxyalkyl (2-6C) or a salt, amide, ester or acyl hydrazone thereof, or is alkyl (1-6C); R.sup.4 is CH.dbd.CH.sub.2 or --CH(OR.sup.4')CH.sub.3 wherein R.sup.4' is H, or alkyl (1-6C) optionally substituted with a hydrophilic substituent.

21. The method of claim 20 wherein said green porphyrin is of the formula ##STR00005## wherein each of R.sup.1 and R.sup.2 is independently carbalkoxyl (2-6C); one R.sup.3 is carboxyalkyl (2-6C) and the other R.sup.3 is the ester of a carboxyalkyl (2-6C) substituent; and R.sup.4 is CH.dbd.CH.sub.2 or --CH(OH)CH.sub.3.

22. The method of claim 21 wherein said green porphyrin is of the formula ##STR00006## and wherein R.sup.1 and R.sup.2 are methoxycarbonyl; one R.sup.3 is --CH.sub.2CH.sub.2COOCH.sub.3 and the other R.sup.3 is CH.sub.2CH.sub.2COOH; and R.sup.4 is CH.dbd.CH.sub.2.

23. The method of claim 11 wherein said photoactive compound is contained in a liposomal preparation.

24. The method of claim 11, wherein the light is emitted from a laser.
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