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    • 8. 发明授权
    • Esters of 5-aminolevulinic acid and their use as photosensitizing compounds in photochemotherapy
    • US06992107B1
    • 2006-01-31
    • US09655570
    • 2000-09-06
    • Karl E. GierskckyJohan MoanQian PengHarald SteenTrond WarloeAlf Bjorseth
    • Karl E. GierskckyJohan MoanQian PengHarald SteenTrond WarloeAlf Bjorseth
    • A61K31/22A61K31/21C07C229/00B65D71/00
    • C07C229/22A61K41/0061A61K49/0021A61K49/0052
    • The present invention provides a compound of formula I; R22N—CH2COCH2—CH2CO—OR1  (I) wherein R1 represents (a) an optionally substituted branched C6-30 alkyl group, comprising a straight chain C4-29 alkyl group, branched by substitution with one or more C1-6 alkyl groups, wherein said site of substitution is at C2 or a higher C atom, (b) a non-heteroaromatic aryl substituted alkyl group, wherein said aryl group is substituted, or (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group, wherein in (a) and (b) said substituents are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo or fluoro groups, and said alkyl group is optionally interrupted or terminated by one or more —O—, NR3—, —S— or PR3— groups; R2, each of which may be the same or different, represents a hydrogen atom or a group R1, wherein R1 represents (a) an optionally substituted branched C5-30 alkyl group, comprising a straight chain C4-29 alkyl group, branched by substitution with one or more C1-6 alkyl groups, wherein said site of substitution is at C2 or a higher C atom, (b) a non-heteroaromatic aryl substituted alkyl group, wherein said aryl group is substituted, or (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group, wherein in (a) and (b) said substituents are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo or fluoro groups, and said alkyl group is optionally interrupted or terminated by one or more —O—, NR3—, —S— or PR3— groups; and R3 represents a hydrogen or C1-6 alkyl group, and salts thereof for use in photochemotherapy or diagnosis. Pharmaceutical compositions comprising said compound, methods of diagnosis or photochemotherapy using said compound and related compounds and compositions, and products and kits comprising said compounds are also provided.