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公开(公告)号:US20100034740A1
公开(公告)日:2010-02-11
申请号:US12518728
申请日:2007-12-27
申请人: Alan Cuthbertson , Magne Solbakken , Hege Karlsen
发明人: Alan Cuthbertson , Magne Solbakken , Hege Karlsen
CPC分类号: A61K51/08 , A61K51/088 , C07B59/001
摘要: The invention relates to conjugates of formula (V) or (VI), their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
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公开(公告)号:US20080213174A1
公开(公告)日:2008-09-04
申请号:US11575158
申请日:2005-09-13
申请人: Matthias Eberhard Glaser , Frank Brady , Sajinder Kaur Luthra , Alan Cuthbertson , Hege Karlsen
发明人: Matthias Eberhard Glaser , Frank Brady , Sajinder Kaur Luthra , Alan Cuthbertson , Hege Karlsen
CPC分类号: A61K51/088
摘要: The invention relates to in vivo imaging agents, specifically radiolabelled insulin derivatives of formula (III); wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—, and is preferably —CO—NH—, —NH— or —O—; Y is H, alkyl or aryl substituents; R* is a radiolabel moiety suitable for detection by SPECT or PET; and methods for preparing the same as well as their use in in vivo imaging methods.
摘要翻译: 本发明涉及体内成像剂,特别是式(III)的放射性标记的胰岛素衍生物; 其中X是-CO-NH-,-NH-,-O-,-NHCONH-或-NHCSNH-,优选为-CO-NH-,-NH-或-O-; Y是H,烷基或芳基取代基; R *是适于通过SPECT或PET检测的放射性标记部分; 及其制备方法以及它们在体内成像方法中的应用。
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公开(公告)号:US20100111865A1
公开(公告)日:2010-05-06
申请号:US12519183
申请日:2007-12-19
申请人: Helge Tolleshaug , Alan Cuthbertson , Hege Karlsen
发明人: Helge Tolleshaug , Alan Cuthbertson , Hege Karlsen
CPC分类号: A61K49/0054 , A61K49/0032 , A61K49/0056
摘要: The present invention provides novel compounds and pharmaceutical compositions containing such compounds, wherein the compounds have affinity for proteoglycans. The compounds comprise an amino acid based core unit linked to positively charged moieties. The compounds further comprise at least one imaging moiety detectable in in vivo imaging making the compounds useful as diagnostic contrast agents for imaging of proteoglycans, such as heparan sulphate proteoglycans.
摘要翻译: 本发明提供含有这些化合物的新化合物和药物组合物,其中化合物对蛋白聚糖具有亲和力。 所述化合物包含与带正电荷部分连接的基于氨基酸的核心单元。 所述化合物还包含在体内成像中可检测的至少一个成像部分,使得该化合物可用作蛋白聚糖成像的诊断造影剂,例如硫酸乙酰肝素蛋白聚糖。
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公开(公告)号:US08197793B2
公开(公告)日:2012-06-12
申请号:US10549082
申请日:2004-03-12
申请人: Alan Cuthbertson , Magne Solbakken , Joseph Maduabuchi Arukwe , Hege Karlsen , Matthias Eberhard Glaser
发明人: Alan Cuthbertson , Magne Solbakken , Joseph Maduabuchi Arukwe , Hege Karlsen , Matthias Eberhard Glaser
IPC分类号: A61K51/00
CPC分类号: C07B59/008 , A61K51/0406 , A61K51/082 , A61K51/088 , C07B39/00 , C07B2200/05 , C07C41/48 , C07C41/56 , C07C45/63 , C07C45/71 , C07C47/55 , C07C47/575 , C07C235/74 , C07C239/20 , C07C243/14 , C07C243/28 , C07C243/38 , C07C271/66 , C07C2601/14 , C07D317/22 , C07K7/06 , C07C43/315 , C07C43/313
摘要: The invention relates to conjugates of formula (V) or (VI): wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
摘要翻译: 本发明涉及式(V)或(VI)的缀合物:其中X是-CO-NH-,-NH-,-O-,-NHCONH-或-NHCSNH-; 它们作为放射性药物的用途,其制备方法以及在这些方法中使用的合成中间体。
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公开(公告)号:US20100068139A1
公开(公告)日:2010-03-18
申请号:US10549082
申请日:2004-03-12
申请人: Alan Cuthbertson , Magne Solbakken , Joseph Maduabuchi Arukwe , Hege Karlsen , Matthias Eberhard Glaser
发明人: Alan Cuthbertson , Magne Solbakken , Joseph Maduabuchi Arukwe , Hege Karlsen , Matthias Eberhard Glaser
IPC分类号: A61K51/08 , C07K1/13 , C07C239/00 , C07C237/02 , C07C243/10 , C07C47/00 , C07C233/01 , C07C49/04 , C07C47/02 , C07K5/08 , C07K2/00
CPC分类号: C07B59/008 , A61K51/0406 , A61K51/082 , A61K51/088 , C07B39/00 , C07B2200/05 , C07C41/48 , C07C41/56 , C07C45/63 , C07C45/71 , C07C47/55 , C07C47/575 , C07C235/74 , C07C239/20 , C07C243/14 , C07C243/28 , C07C243/38 , C07C271/66 , C07C2601/14 , C07D317/22 , C07K7/06 , C07C43/315 , C07C43/313
摘要: The invention relates to conjugates of formula (V) or (VI): wherein X is —CO—NH—, —NH—, —O—, —NHCONH—, or —NHCSNH—; their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
摘要翻译: 本发明涉及式(V)或(VI)的缀合物:其中X是-CO-NH-,-NH-,-O-,-NHCONH-或-NHCSNH-; 它们作为放射性药物的用途,其制备方法以及在这些方法中使用的合成中间体。
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公开(公告)号:US20080274052A1
公开(公告)日:2008-11-06
申请号:US12098537
申请日:2008-04-07
IPC分类号: A61K51/08 , C07C321/04 , C07C233/64 , C07K2/00
CPC分类号: C07B59/008
摘要: The present invention relates to methods and reagents for [18F]-fluorination, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). Thus, a compound of formula 18F-(Linker)-SH, such as a compound of formula (IV), (V), or (VI): may be reacted with an activated peptide as a means for 18F-labelling.
摘要翻译: 本发明涉及[F 18 F] - 氟化,特别是肽的方法和试剂。 所得的18 F标记的化合物可用作放射性药物,特别用于正电子发射断层扫描(PET)。 因此,式(Ⅳ),(Ⅴ)或(Ⅵ)化合物可以将式(ⅩⅥ)F-(接头)-SH的化合物与活化肽作为 用于 18 SUP> F标签的方法。
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公开(公告)号:US07368474B2
公开(公告)日:2008-05-06
申请号:US10508682
申请日:2003-03-20
IPC分类号: A61K51/08 , A61K101/02
CPC分类号: C07B59/008
摘要: The present invention relates to methods and reagents for [18F]-fluorination, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). Thus, a compound of formula 18F-(Linker)-SH, such as a compound of formula (IV), (V), or (VI): 18F—(CH2CH2O)n—(CH2)m—SH (IV) 18F—(CH2)p—SH (V) may be reacted with an activated peptide as a means for 18F-labelling.
摘要翻译: 本发明涉及[F 18 F] - 氟化,特别是肽的方法和试剂。 所得的18 F标记的化合物可用作放射性药物,特别用于正电子发射断层扫描(PET)。 因此,通式(IV)的化合物,如式(IV),(V)或(VI)的化合物: “在线公式”end =“lead”?> 18 SUP> F-(CH 2 2 CH 2 O) β-H(IV)<βin-line-formula description =“In-line Formulas”end =“tail”?> < ?in-line-formula description =“In-line Formulas”end =“lead”?> 18 SUP> F-(CH 2) SUB> -SH(V)<βin-line-formula description =“In-line Formulas”end =“tail”?>可与活化肽反应,作为标记的标记。
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公开(公告)号:US20050142061A1
公开(公告)日:2005-06-30
申请号:US10508682
申请日:2003-03-20
申请人: Alan Cuthbertson , Magne Solbakken , Joseph Arukwe , Hege Karlsen
发明人: Alan Cuthbertson , Magne Solbakken , Joseph Arukwe , Hege Karlsen
CPC分类号: C07B59/008
摘要: The present invention relates to methods and reagents for [18F]-fluorination, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET). Thus, a compound of formula 18F-(Linker)-SH, such as a compound of formula (IV), (V), or (VI): 18F—(CH2CH2O)n—(CH2)m—SH (IV) 18F—(CH2)p—SH (V) may be reacted with an activated peptide as a means for 18F-labelling.
摘要翻译: 本发明涉及[F 18 F] - 氟化,特别是肽的方法和试剂。 所得的18 F标记的化合物可用作放射性药物,特别用于正电子发射断层扫描(PET)。 因此,通式(IV)的化合物,如式(IV),(V)或(VI)的化合物: “在线公式”end =“lead”?> 18 SUP> F-(CH 2 2 CH 2 O) β-H(IV)<βin-line-formula description =“In-line Formulas”end =“tail”?> < ?in-line-formula description =“In-line Formulas”end =“lead”?> 18 SUP> F-(CH 2) SUB> -SH(V)<βin-line-formula description =“In-line Formulas”end =“tail”?>可与活化肽反应,作为标记的标记。
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公开(公告)号:US08273325B2
公开(公告)日:2012-09-25
申请号:US12519183
申请日:2007-12-19
申请人: Helge Tolleshaug , Alan Cuthbertson , Hege Karlsen
发明人: Helge Tolleshaug , Alan Cuthbertson , Hege Karlsen
CPC分类号: A61K49/0054 , A61K49/0032 , A61K49/0056
摘要: The present invention provides novel compounds and pharmaceutical compositions containing such compounds, wherein the compounds have affinity for proteoglycans. The compounds comprise an amino acid based core unit linked to positively charged moieties. The compounds further comprise at least one imaging moiety detectable in in vivo imaging making the compounds useful as diagnostic contrast agents for imaging of proteoglycans, such as heparan sulphate proteoglycans.
摘要翻译: 本发明提供含有这些化合物的新化合物和药物组合物,其中化合物对蛋白聚糖具有亲和力。 所述化合物包含与带正电荷部分连接的基于氨基酸的核心单元。 所述化合物还包含在体内成像中可检测的至少一个成像部分,使得该化合物可用作蛋白聚糖成像的诊断造影剂,例如硫酸乙酰肝素蛋白聚糖。
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公开(公告)号:US08216548B2
公开(公告)日:2012-07-10
申请号:US12518728
申请日:2007-12-27
申请人: Alan Cuthbertson , Magne Solbakken , Hege Karlsen
发明人: Alan Cuthbertson , Magne Solbakken , Hege Karlsen
IPC分类号: A61K51/00
CPC分类号: A61K51/08 , A61K51/088 , C07B59/001
摘要: The invention relates to conjugates of formula (V) or (VI), their use as radiopharmaceuticals, processes for their preparation, and synthetic intermediates used in such processes.
摘要翻译: 本发明涉及式(Ⅴ)或(Ⅵ)的结合物,它们作为放射性药物的用途,其制备方法以及在这些方法中使用的合成中间体。
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