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    Methods and agents for preparing 18F-radiolabeled fluorinating agents
    5.
    发明授权
    Methods and agents for preparing 18F-radiolabeled fluorinating agents 有权
    制备18F-放射性标记的氟化剂的方法和试剂

    公开(公告)号：US07744851B2

    公开(公告)日：2010-06-29

    申请号：US11778349

    申请日：2007-07-16

    申请人： Stephen Gregory DiMagno ,  Haoran Sun

    发明人： Stephen Gregory DiMagno ,  Haoran Sun

    IPC分类号： A61K51/04 ,  A61K49/00 ,  A61K101/02

    CPC分类号： A61K51/04

    摘要： The present invention is directed to a method for preparing an anhydrous 18F-radiolabeled fluorinating agent by a nucleophilic reaction of a hydrated 18F-radiolabeled fluoride ion source with an unsaturated carrier compound; treating the 18F-radiolabeled carrier compound to produce a non-aqueous mixture of the 18F-radiolabeled carrier compound in a solvent; and reacting the 18F-radiolabeled carrier compound with a nucleophilic composition in a nucleophilic reaction to produce an anhydrous 18F-radiolabeled fluorinating agent. The present invention is also directed to an anhydrous 18F-radiolabeled fluorinating agent comprising the formula [QnM]x+(18F−)x. Additionally, the present invention is directed to an 18F-radiolabeled fluorinated radiopharmaceutical or an 18F-radiolabeled fluorinated radiotracer prepared by reacting the anhydrous 18F-radiolabeled fluorinating agent with a drug intermediate. The present invention is further directed to methods for treating a disease or imaging a subject using an 18F-radiolabeled fluorinated radiopharmaceutical or an 18F-radiolabeled fluorinated radiotracer.

    摘要翻译： 本发明涉及通过水合18F放射标记的氟离子源与不饱和载体化合物的亲核反应制备无水18F-放射性标记的氟化剂的方法; 处理18F放射性标记的载体化合物以在溶剂中产生18F-放射性标记的载体化合物的非水混合物; 并在亲核反应中使18F-放射性标记载体化合物与亲核组合物反应，生成无水18F-放射性标记的氟化剂。 本发明还涉及包含式[QnM] x +（18F-）x的无水18F-放射性标记氟化剂。 此外，本发明涉及通过使无水18F放射性标记的氟化剂与药物中间体反应制备的18F-放射性标记的氟化放射性药物或18F-放射性标记的氟化放射性示踪剂。 本发明进一步涉及使用18F-放射性标记的氟化放射性药物或18F-放射性标记的氟化放射性示踪剂治疗疾病或使受试者成像的方法。

    Anhydrous fluoride salts and reagents and methods for their production
    6.
    发明授权
    Anhydrous fluoride salts and reagents and methods for their production 有权
    无水氟化物盐及其制备方法

    公开(公告)号：US07592486B2

    公开(公告)日：2009-09-22

    申请号：US11226277

    申请日：2005-09-15

    申请人： Stephen G. DiMagno ,  Haoran Sun

    发明人： Stephen G. DiMagno ,  Haoran Sun

    IPC分类号： C07C211/63

    CPC分类号： C07C211/63 ,  C07B39/00 ,  C07C17/093 ,  C07C17/202 ,  C07C17/208 ,  C07C51/60 ,  C07C19/08 ,  C07C25/18 ,  C07C63/10

    摘要： Anhydrous organic fluoride salts and reagents prepared by a method comprising the nucleophilic substitution of a fluorinated aromatic or fluorinated unsaturated organic compound with a salt having the formula: [QnM]x+Ax− in an inert polar, aprotic solvent; wherein M is an atom capable of supporting a formal positive charge, the n groups Q are independently varied organic moieties, n is an integer such that the [QnM] carries at least one formal positive charge, x is an integer defining the number of formal positive charge(s), +, carried by the [QnM], A− is an anionic nucleophile capable of substituting for F in the fluorinated compound and F represents fluorine or a radioisotope thereof.

    摘要翻译： 通过包括氟化芳族或氟化不饱和有机化合物与具有下式的盐的亲核取代的方法制备的无水有机氟化物盐和试剂：<？in-line-formula description =“In-line Formulas”end =“lead” 在惰性极性非质子溶剂中，α> [QnM] x + Ax- <？in-line-formula description =“In-line Formulas”end =“tail” 其中M是能够支持形式正电荷的原子，n基Q独立地改变有机部分，n是整数，使得[QnM]携带至少一个形式正电荷，x是定义正式电荷数的整数 由[QnM]携带的正电荷+，A-是能够在氟化化合物中取代F的阴离子亲核试剂，F表示氟或其放射性同位素。

    Methods and Agents for Preparing 18F-Radiolabeled Fluorinating Agents
    7.
    发明申请
    Methods and Agents for Preparing 18F-Radiolabeled Fluorinating Agents 有权
    制备18 F放射性标记氟化剂的方法和试剂

    公开(公告)号：US20080019906A1

    公开(公告)日：2008-01-24

    申请号：US11778349

    申请日：2007-07-16

    申请人： Stephen DiMagno ,  Haoran Sun

    发明人： Stephen DiMagno ,  Haoran Sun

    IPC分类号： A61K51/04

    CPC分类号： A61K51/04

    摘要： The present invention is directed to a method for preparing an anhydrous 18F-radiolabeled fluorinating agent by a nucleophilic reaction of a hydrated 18F-radiolabeled fluoride ion source with an unsaturated carrier compound; treating the 18F-radiolabeled carrier compound to produce a non-aqueous mixture of the 18F-radiolabeled carrier compound in a solvent; and reacting the 18F-radiolabeled carrier compound with a nucleophilic composition in a nucleophilic reaction to produce an anhydrous 18F-radiolabeled fluorinating agent. The present invention is also directed to an anhydrous 18F-radiolabeled fluorinating agent comprising the formula [QnM]x+(18F−)x. Additionally, the present invention is directed to an 18F-radiolabeled fluorinated radiopharmaceutical or an 18F-radiolabeled fluorinated radiotracer prepared by reacting the anhydrous 18F-radiolabeled fluorinating agent with a drug intermediate. The present invention is further directed to methods for treating a disease or imaging a subject using an 18F-radiolabeled fluorinated radiopharmaceutical or an 18F-radiolabeled fluorinated radiotracer.

    摘要翻译： 本发明涉及通过水合的18 F放射性标记的氟离子源与不饱和载体的亲核反应制备无水的18 F放射性标记的氟化剂的方法 复合; 处理<！ - SIPO - >放射性标记的载体化合物，以在溶剂中产生非水性混合物的<！ - SIPO < 并在亲核反应中使 F-放射性标记的载体化合物与亲核组合物反应，以产生无水的18 F放射性标记的氟化剂。 本发明还涉及一种无水氟代放射性标记的氟化剂，其包含式[Q N n M M] x +（ - S 18） ）。 另外，本发明涉及一种通过使无水十八烷基二异氰酸酯反应制备的氟代放射性药物或通过氟化放射性标记的氟代放射性药物 F放射性标记的氟化剂与药物中间体。 本发明进一步涉及使用放射性标记的氟化放射性药物或者18 F放射性标记的氟化放射性示踪剂治疗疾病或使受试者成像的方法。

    Anhydrous flouride salts and reagents and methods for their production
    8.
    发明申请
    Anhydrous flouride salts and reagents and methods for their production 有权
    无水氟化物盐及其制备方法

    公开(公告)号：US20060089514A1

    公开(公告)日：2006-04-27

    申请号：US11226277

    申请日：2005-09-15

    申请人： Stephen DiMagno ,  Haoran Sun

    发明人： Stephen DiMagno ,  Haoran Sun

    IPC分类号： C07F9/02 ,  C07C211/63

    CPC分类号： C07C211/63 ,  C07B39/00 ,  C07C17/093 ,  C07C17/202 ,  C07C17/208 ,  C07C51/60 ,  C07C19/08 ,  C07C25/18 ,  C07C63/10

    摘要： Anhydrous organic fluoride salts and reagents prepared by a method comprising the nucleophilic substitution of a fluorinated aromatic or fluorinated unsaturated organic compound with a salt having the formula: [QnM]x+Ax− in an inert polar, aprotic solvent; wherein M is an atom capable of supporting a formal positive charge, the n groups Q are independently varied organic moieties, n is an integer such that the [QnM] carries at least one formal positive charge, x is an integer defining the number of formal positive charge(s), +, carried by the [QnM], A− is an anionic nucleophile capable of substituting for F in the fluorinated compound and F represents fluorine or a radioisotope thereof.

    摘要翻译： 通过包括氟化芳族或氟化不饱和有机化合物与具有下式的盐的亲核取代的方法制备的无水有机氟化物盐和试剂：<？in-line-formula description =“In-line Formulas”end =“lead” ？In In In In x x x x <<<<<<<<<<<<<<<<<<<<<<<