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    Use of aminolevulinic acid and derivatives thereof
    7.
    发明授权
    Use of aminolevulinic acid and derivatives thereof 有权
    氨基乙酰丙酸及其衍生物的应用

    公开(公告)号：US08759396B2

    公开(公告)日：2014-06-24

    申请号：US12523048

    申请日：2008-01-11

    申请人： Hans Christian Wulf ,  Aslak Godal ,  Jo Klaveness

    发明人： Hans Christian Wulf ,  Aslak Godal ,  Jo Klaveness

    IPC分类号： A01N37/12 ,  A61N1/30

    CPC分类号： A61K41/0061 ,  A61K31/221 ,  A61N5/062

    摘要： The invention provides the use of a photosensitizer which is 5-aminolevulinic acid (5-ALA) or a derivative (e.g. an ester) of 5-ALA, or a pharmaceutically acceptable salt thereof, in the manufacture of a composition for use in methods of photodynamic therapy (PDT) on an animal, wherein said PDT comprises: (a) administering to said animal a composition comprising said photosensitizer; and (b) photoactivating said photosensitizer, and wherein side-effects (e.g. pain and/or erythema) of said PDT are prevented or reduced by use of one or more of (i)-(iv): (i) said composition comprises said photosensitizer in a concentration of less than 10% wt (e.g. 0.5 to 8% wt), (ii) said composition is administered for less than 2 hours (e.g. 30 minutes to 90 minutes) prior to said photoactivation, (iii) said photoactivation is carried out with a light source having a fluence rate of less than 50 mW/cm2 (e.g. 5 to 40 mW/cm2), (iv) said photoactivation is carried out with sunlight. Preferably, side-effects of PDT are prevented or reduced by using (iii) or (iv) in combination with (i) and/or (ii).

    摘要翻译： 本发明提供了5-氨基乙酰丙酸（5-ALA）或5-ALA衍生物（例如酯）或其药学上可接受的盐的光敏剂在制备用于 光动力疗法（PDT），其中所述PDT包括：（a）向所述动物施用包含所述光敏剂的组合物; 和（b）光活化所述光敏剂，并且其中通过使用（i） - （iv）中的一种或多种来防止或减少所述PDT的副作用（例如疼痛和/或红斑）：（i）所述组合物包含 浓度小于10％wt（例如0.5至8％wt）的光敏剂，（ii）所述组合物在所述光活化之前施用少于2小时（例如30分钟至90分钟），（iii）所述光活化是 用光通量小于50mW / cm2（例如5〜40mW / cm2）的光源进行，（iv）所述的光活化是在太阳光下进行的。 优选地，通过使用（iii）或（iv）与（i）和/或（ii）组合来防止或减少PDT的副作用。

    5-HT RECEPTOR MODULATING COMPOUNDS
    9.
    发明申请
    5-HT RECEPTOR MODULATING COMPOUNDS 审中-公开
    5-HT受体调节化合物

    公开(公告)号：US20120094989A1

    公开(公告)日：2012-04-19

    申请号：US13262356

    申请日：2010-04-01

    申请人： Jo Klaveness ,  Bjame Brudeli ,  Finn Olav Levy ,  Lise Roman Moltzau ,  Trygve Gulbrandsen

    发明人： Jo Klaveness ,  Bjame Brudeli ,  Finn Olav Levy ,  Lise Roman Moltzau ,  Trygve Gulbrandsen

    IPC分类号： A61K31/5365 ,  C07D211/58 ,  C07D401/10 ,  C07D211/34 ,  A61P13/00 ,  A61K31/454 ,  A61K31/445 ,  A61P9/00 ,  A61P1/00 ,  C07D498/04 ,  A61K31/4468

    CPC分类号： C07D498/04 ,  C07D211/34

    摘要： The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.

    摘要翻译： 本发明涉及具有5-羟色胺受体调节活性的化合物，特别是具有通过刚性连接基保持远离5-HT药效团的酸性部分的化合物，含有这些化合物的组合物和使用它们的治疗方法。 这样的化合物对5-HT受体的亲和力增加并且hERG效应降低。 本发明的某些化合物还表现出血管紧张素II受体调节活性。 要求的是式（I）的化合物：HT-L-A。 HT是含有碱性氮原子的5-HT受体调节部分; A是酸性部分; L是连接体部分。

    Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
    10.
    发明授权
    Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy 失效
    5-氨基乙酰丙酸的酯类作为光化学疗法中的光敏剂

    公开(公告)号：US07563819B1

    公开(公告)日：2009-07-21

    申请号：US11786878

    申请日：2007-04-13

    申请人： Jo Klaveness ,  Nils Olav Nilsen ,  Jon Erik Braenden ,  Aslak Godal

    发明人： Jo Klaveness ,  Nils Olav Nilsen ,  Jon Erik Braenden ,  Aslak Godal

    IPC分类号： A61K31/21 ,  A61K31/22 ,  C07C229/00

    CPC分类号： C07D213/30 ,  A61K31/195 ,  A61K41/0061 ,  A61K49/0021 ,  C07C229/22

    摘要： 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.

    摘要翻译： 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。