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|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) R.sub.2.sup.2 N--CH.sub.2 COCH.sub.2 --CH.sub.2 CO--OR.sup.1 (wherein R.sup.1 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 R.sup.2 represents a hydrogen atom or a group R.sup.1, and both R.sup.2 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 AS (Oslo, NO)|
|Filing Date:||Dec 21, 1999|
|Claims:||1. A method for the diagnosis or photochemotherapeutic treatment of infections or skin disorders of the body, comprising: i) administering to the sites of investigation or affected surfaces of the body a composition comprising a compound of formula I |
wherein R.sup.1 is alkyl; and each R.sup.2 is independently hydrogen or alkyl; wherein each alkyl of R.sup.1 and R.sup.2 is optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and is optionally interrupted by oxygen atoms; or a salt thereof; and ii) exposing said sites or surfaces to light.
2. The method of claim 1 wherein aryl is phenyl or a monocyclic 5-7 membered heteroaromatic.
3. The method of claim 1 wherein R.sup.1 represents an unsubstituted alkyl group and each R.sup.2 is hydrogen.
4. The method of claim 1 wherein R.sup.1 represents an unsubstituted alkyl group or each R.sup.2 is hydrogen.
5. The method of claim 1 wherein alkyl contains up to 10 carbon atoms.
6. The method of claim 1 wherein the compound is ALA-methyl ester, ALA-ethyl ester, ALA-propyl ester, ALA-hexyl ester, ALA-heptyl ester, or ALA-octyl ester; or a salt thereof.
7. The method of claim 1 wherein the light is in the wavelength region 500-700 nm.
8. The method of claim 1 wherein the skin disorder is psoriasis.
9. The method of claim 1 wherein the infection is a bacterial, viral or fungal infection.
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