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    HYPEROSMOTIC PREPARATIONS COMPRISING 5-AMINOLEVULINIC ACID OR DERIVATIVE AS PHOTOSENSITIZING AGENT
    1.
    发明申请
    HYPEROSMOTIC PREPARATIONS COMPRISING 5-AMINOLEVULINIC ACID OR DERIVATIVE AS PHOTOSENSITIZING AGENT 审中-公开
    包含5-氨基酸或衍生物作为光敏剂的高效制剂

    公开(公告)号：US20130211215A1

    公开(公告)日：2013-08-15

    申请号：US13806578

    申请日：2011-06-23

    申请人： Inger Ferner Heglund ,  Aslak Godal ,  Jo Klaveness

    发明人： Inger Ferner Heglund ,  Aslak Godal ,  Jo Klaveness

    IPC分类号： A61K41/00 ,  A61B5/00

    CPC分类号： A61K41/0061 ,  A61B5/0071 ,  A61B5/0084 ,  A61K9/0031 ,  A61K47/10 ,  A61K47/26

    摘要： Provided herein are improved methods of photodynamic treatment and diagnosis of cancer and non-cancerous conditions in the gastrointestinal tract, e.g. in the colon, and in particular hyperosmotic enema preparations for use in such methods. The enema preparations comprise a photosensitizer which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative thereof, e.g. a 5-ALA ester, in combination with at least one hyperosmotic agent. The methods and preparations herein described are particularly suitable for use in photodynamic methods of treating and/or diagnosing colorectal cancer.

    摘要翻译： 本文提供了光动力学治疗和诊断胃肠道中的癌症和非癌性病症的改进方法，例如。 在结肠中，特别是用于这些方法的高渗灌肠剂。 灌肠制剂包含5-氨基乙酰丙酸（5-ALA）或其前体或衍生物的光敏剂，例如5-氨基乙酰丙酸。 5-ALA酯，与至少一种高渗剂组合。 本文描述的方法和制剂特别适用于治疗和/或诊断结肠直肠癌的光动力学方法。

    Acid Addition Salts Of-5-Aminolevulinic Acid Or Its Derivatives
    2.
    发明申请
    Acid Addition Salts Of-5-Aminolevulinic Acid Or Its Derivatives 有权
    5-氨基乙酰丙酸或其衍生物的酸加成盐

    公开(公告)号：US20080064752A1

    公开(公告)日：2008-03-13

    申请号：US10594361

    申请日：2005-03-29

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

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

    IPC分类号： A61K31/195 ,  A61P31/00 ,  C07C229/22 ,  G01N21/76

    CPC分类号： A61K41/0061 ,  C07C229/22

    摘要： The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

    摘要翻译： 本发明提供5-氨基乙酰丙酸（5-ALA）或5-ALA衍生物（例如5-ALA酯）与酸的加成盐，所述酸的pKa为约5或更小，优选约3或 较少，条件是酸不是盐酸。 特别优选的盐是衍生自选自磺酸及其衍生物，氢溴酸，硫酸，硝酸和磷酸的酸的酸。 根据本发明的盐特别适用于诊断和光化学治疗身体的外表面或内表面的病症或异常的光敏剂。

    Use of aminolevulinic acid and derivatives thereof
    4.
    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。

    Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
    5.
    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。

    Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
    8.
    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：US07217736B2

    公开(公告)日：2007-05-15

    申请号：US10343209

    申请日：2001-07-25

    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 ,  A61K31/195 ,  C07D221/00 ,  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 use 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 2 2 N-CH 2 COCH 2 其中R 1表示任选取代的支链烷基（例如C 5-30），其中R 1，R 2， 烷基）基团或取代的烷基; R 2各自可以相同或不同，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，烷氧基羰氧基，氨基，芳基，硝基，氧代，氟，-SR 3，-NR 3， 2个和3个以上的2个基团，并且每个烷基任选地被一个或多个O - ，-NR 3 - ，-S-或-PR 3+基; R 3表示氢原子或C 1-6烷基） 和其盐，用于诊断和光化学治疗身体外表面或内表面异常障碍，以及p 用于实施本发明的产品和试剂盒。

    ENEMA PREPARATIONS AND THEIR USE
    10.
    发明申请
    ENEMA PREPARATIONS AND THEIR USE 审中-公开
    ENEMA制剂及其使用

    公开(公告)号：US20110293528A1

    公开(公告)日：2011-12-01

    申请号：US13141919

    申请日：2009-12-23

    申请人： Aslak Godal ,  Jo Klaveness

    发明人： Aslak Godal ,  Jo Klaveness

    IPC分类号： A61K49/06 ,  A61K31/221 ,  A61K49/04 ,  A61P1/00 ,  A61P1/04 ,  A61P31/00 ,  A61K31/197 ,  A61P35/00

    CPC分类号： A61K9/0031 ,  A61K41/0061 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14 ,  A61K47/18 ,  A61K47/20 ,  A61K47/34 ,  A61K47/38

    摘要： This invention relates to improved methods of photodynamic treatment and diagnosis of cancer and non-cancerous conditions, and in particular to improved enema preparations for use in such methods, said enema preparations comprising a photosensitiser which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative thereof, e.g. a 5-ALA ester. Such preparations may further comprise one or more viscosity enhancing agents, mucoadhesive or mucolytic agents, penetration enhancers or chelating agents. The methods and preparations herein described are particularly suitable for use in photodynamic methods of treating and/or diagnosing cancer and non-cancerous conditions in the colon and/or rectum.

    摘要翻译： 本发明涉及光动力学治疗和诊断癌症和非癌症病症的改进方法，特别是涉及用于这些方法的改善的灌肠剂制剂，所述灌肠制剂包含5-氨基乙酰丙酸（5-ALA）的光敏剂或 其前体或衍生物，例如 一种5-ALA酯。 这样的制剂还可以包含一种或多种粘度增强剂，粘膜粘附或粘液溶解剂，渗透增强剂或螯合剂。 本文所述的方法和制剂特别适用于治疗和/或诊断结肠和/或直肠癌和非癌症病症的光动力学方法。