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Claims for Patent: 7,247,655

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Claims for Patent: 7,247,655

Title:Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
Abstract:The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N--CH2COCH2--CH2CO--OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
Inventor(s): Gierskcky; Karl E. (Oslo, NO), Moan; Johan (Oslo, NO), Peng; Qian (Oslo, NO), Steen; Harald (Oslo, NO), Warloe; Trond (Oslo, NO), Bjorseth; Alf (Oslo, NO)
Assignee: Photocure ASA (Oslo, NO)
Application Number:10/410,636
Patent Claims: 1. A composition comprising: i) a diagnostically effective amount of hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; and ii) an aqueous solution optionally containing a physiologically acceptable carrier or excipient.

2. The composition of claim 1 wherein the diagnostically effective amount detects bladder cancer.

3. A composition comprising: i) a diagnostically effective amount of hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; and ii) an aqueous base.

4. The composition of claim 3 wherein the aqueous base comprises one or more inert carriers and/or diluents.

5. A composition consisting essentially of: i) a diagnostically effective amount of hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; and ii) a physiologically acceptable carrier.

6. The composition of claim 5 wherein the diagnostically effective amount detects bladder cancer.

7. The composition of claim 6 wherein the physiologically acceptable carrier is water.

8. A composition comprising: i) a diagnostically effective amount of hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; and ii) a physiologically acceptable carrier.

9. The composition of claim 8 wherein the diagnostically effective amount detects bladder cancer.

10. The composition of claim 9 wherein the physiologically acceptable carrier is water.

11. A kit comprising: i) a first container containing hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; and ii) a second container containing a physiologically acceptable carrier.

12. The kit of claim 11 wherein the hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof detects bladder cancer.

13. The kit of claim 12 wherein the physiologically acceptable carrier is water.

14. A method for the diagnosis of abnormalities of a urinary bladder in a patient in need thereof, comprising: i) administering to the urinary bladder a composition comprising hexyl 5-aminolevulinate or a pharmaceutically acceptable salt thereof; ii) exposing said lining of the urinary bladder to photoactivating light in the spectrum 300 800 nm; iii) ascertaining the level of fluorescence; and iv) comparing the level of fluorescence to control levels to locate abnormalities in the bladder.

15. The method of claim 14 wherein the abnormality is bladder cancer.

16. The method of claim 15 wherein the light is in the spectrum 350 500 nm.

17. The method of claim 16 wherein the photoactivating light is applied via an optical fiber inserted through a needle.
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