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    • 23. 发明授权
    • Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
    • 5-氨基乙酰丙酸的酯类作为光化学疗法中的光敏剂
    • US07563819B1
    • 2009-07-21
    • US11786878
    • 2007-04-13
    • Jo KlavenessNils Olav NilsenJon Erik BraendenAslak Godal
    • Jo KlavenessNils Olav NilsenJon Erik BraendenAslak Godal
    • A61K31/21A61K31/22C07C229/00
    • C07D213/30A61K31/195A61K41/0061A61K49/0021C07C229/22
    • The invention provides compounds for use in photochemotherapy or diagnosis, said compounds being branched alkyl esters or substituted alkyl esters of 5-aminolevulinic acid, or derivatives or pharmaceutically acceptable salts thereof. In particular, the invention provides compounds of formula (I): R22N—CH2COCH2CH2CO—OR1 (wherein R1 represents an optionally substituted branched alkyl (e.g. C5-30 alkyl) group, or a substituted alkyl group; R2, each of which may be the same or different, represents a hydrogen atom or an optionally substituted alkyl group, preferably a group R1; wherein said substituents are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo, fluoro, —SR3, —NR32 and PR32 groups, and each alkyl group is optionally interrupted by one or more O—, —NR3—, —S— or —PR3— groups; and R3 represents a hydrogen atom or a C1-6 alkyl group) and salts thereof for us in diagnosis and photochemotherapy of disorders of abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
    • 本发明提供用于光化学疗法或诊断的化合物,所述化合物为支链烷基酯或5-氨基乙酰丙酸的取代烷基酯,或其衍生物或药学上可接受的盐。 特别地,本发明提供式(I)的化合物:R 22 N-CH 2 COCH 2 CH 2 CO-OR 1(其中R 1表示任选取代的支链烷基(例如C 5-30烷基)或取代的烷基; R 2,其各自可以是 相同或不同,表示氢原子或任选取代的烷基,优选基团R 1;其中所述取代基选自羟基,烷氧基,酰氧基,烷氧基羰基氧基,氨基,芳基,硝基,氧代,氟,-SR 3,-NR 32和 PR32基团,并且每个烷基任选地被一个或多个O-,-NR 3 - ,-S-或-PR 3 - 基团间隔;并且R 3表示氢原子或C 1-6烷基)及其盐 身体外表面或内表面异常障碍的诊断和光化学治疗,以及用于实施本发明的产品和试剂盒。