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。

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。

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。

公开(公告)号：US07888526B2

公开(公告)日：2011-02-15

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： C07C229/22 ,  A61K31/195

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。

公开(公告)号：US08692014B2

公开(公告)日：2014-04-08

申请号：US12916326

申请日：2010-10-29

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： C07C229/00 ,  A61K31/195

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。

公开(公告)号：US20110125012A1

公开(公告)日：2011-05-26

申请号：US12916326

申请日：2010-10-29

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： A61B6/00 ,  C12Q1/02 ,  G01N21/64 ,  A61M37/00

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。