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1.发明申请Fluorination Process of Anilide Derivatives and Benzothiazole Fluorinate Derivatives as in VIVO Imaging Agents 有权苯乙烯衍生物和苯并噻唑氟化物衍生物的氟化方法如VIVO成像剂公开(公告)号：US20100234611A1
公开(公告)日：2010-09-16
申请号：US12063470
申请日：2006-08-11
申请人： Anthony Eamon Storey , Clare Louise Jones , Denis Raymond Christophe Bouvet , Nicolas Lasbistes , Steven Michael Fairway , Lorenzo Williams , Alexander Mark Gibson , Robert James Nairne , Farhad Karimi , Bengt Langstrom
发明人： Anthony Eamon Storey , Clare Louise Jones , Denis Raymond Christophe Bouvet , Nicolas Lasbistes , Steven Michael Fairway , Lorenzo Williams , Alexander Mark Gibson , Robert James Nairne , Farhad Karimi , Bengt Langstrom
IPC分类号： C07D277/66 , G21C1/01
CPC分类号： A61K51/0453 , B01J19/24 , B01J2219/24 , C07D277/66 , Y02P20/55
摘要： The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.
摘要翻译： 本发明涉及制备式（I）化合物的方法：R1选自C 1-6烷基，C 2-6烯基和C 2-6炔基; 其包括：（i）与氟化物，适当的[18 F]氟化物反应，相应的式（II）化合物：其中R 2选自氢，C 1-10烷基，C 1-10卤代烷基，C 6-14芳基，C 6-14芳烷基， （CH 2 CH 2 O）q -CH 3，其中q是1至10的整数; R1如式（I）化合物所定义; R3是离去基团。 还要求具有式（II）的某些新型前体和含有这些前体的放射性药物试剂盒。
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2.发明授权Fluorination process of anilide derivatives and benzothiazole fluorinate derivatives as in vivo imaging agents 有权苯胺衍生物和苯并噻唑氟化物衍生物作为体内显像剂的氟化方法公开(公告)号：US08410312B2
公开(公告)日：2013-04-02
申请号：US12063470
申请日：2006-08-11
申请人： Anthony Eamon Storey , Clare Louise Jones , Denis Raymond Christophe Bouvet , Nicolas Lasbistes , Steven Michael Fairway , Lorenzo Williams , Alexander Mark Gibson , Robert James Nairne , Farhad Karimi , Bengt Langstrom
发明人： Anthony Eamon Storey , Clare Louise Jones , Denis Raymond Christophe Bouvet , Nicolas Lasbistes , Steven Michael Fairway , Lorenzo Williams , Alexander Mark Gibson , Robert James Nairne , Farhad Karimi , Bengt Langstrom
IPC分类号： C07C211/46
CPC分类号： A61K51/0453 , B01J19/24 , B01J2219/24 , C07D277/66 , Y02P20/55
摘要： The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.
摘要翻译： 本发明涉及制备式（I）化合物的方法：R1选自C 1-6烷基，C 2-6烯基和C 2-6炔基; 其包括：（i）与氟化物，适当的[18 F]氟化物反应，相应的式（II）化合物：其中R 2选自氢，C 1-10烷基，C 1-10卤代烷基，C 6-14芳基，C 6-14芳烷基， （CH 2 CH 2 O）q -CH 3，其中q是1至10的整数; R1如式（I）化合物所定义; R3是离去基团。 还要求具有式（II）的某些新型前体和含有这些前体的放射性药物试剂盒。
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公开(公告)号：US20140135531A1
公开(公告)日：2014-05-15
申请号：US14131442
申请日：2012-07-20
申请人： Radha Achhanath , Srinath Balaji , Asfal Mohammed Kadavilpparampu Mohamed , Sondre Nilsen , Steven Michael Fairway
发明人： Radha Achhanath , Srinath Balaji , Asfal Mohammed Kadavilpparampu Mohamed , Sondre Nilsen , Steven Michael Fairway
IPC分类号： C07C45/78
CPC分类号： C07C45/78 , C07C41/44 , C07C43/174 , C07C45/42 , C07C49/757 , C07C319/20 , C07C2601/04 , C07C49/753 , C07C323/65
摘要： The present invention relates to a method of obtaining radiopharmaceutical precursors, and in particular precursors to protected amino acid derivatives, which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures, such as positron emission tomography (PET).
摘要翻译： 本发明涉及一种获得放射性药物前体的方法，特别是被保护的氨基酸衍生物的前体，其用作用于生物体内成像方法如正电子发射断层摄影（PET）的放射性标记氨基酸的前体。
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4.发明申请PREPARATION OF A 1-AMINO-3-HYDROXY-CYCLOBUTAINE-1-CARBOXYLIC ACID DERIVATIVE 有权1-氨基-3-羟基 - 环孢菌素-1-羧酸衍生物的制备公开(公告)号：US20130345468A1
公开(公告)日：2013-12-26
申请号：US14002184
申请日：2012-03-07
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , A61K51/0406 , C07C269/06 , C07C2601/04 , Y02P20/55 , C07C271/24
摘要： The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F]FACBC) PET agent, ensuring that the reaction efficiently goes to completion.
摘要翻译： 本发明涉及一种制备放射性药物前体的方法，特别是用作生产用于体内成像方法如正电子发射断层摄影（PET）的放射性标记氨基酸的前体的保护的氨基酸衍生物。 特别地，本发明涉及制备[18 F] -1-氨基-3-氟环丁烷羧酸（[18 F] FACBC）PET试剂的前体的方法，确保反应有效地完成。
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5.发明授权Preparation of a 1-amino-3-hydroxy-cyclobutane-1-carboxylic acid derivative 有权1-氨基-3-羟基 - 环丁烷-1-羧酸衍生物的制备公开(公告)号：US09242924B2
公开(公告)日：2016-01-26
申请号：US14002184
申请日：2012-03-07
IPC分类号： C07C227/16 , C07C269/06 , A61K51/04
CPC分类号： C07C227/16 , A61K51/0406 , C07C269/06 , C07C2601/04 , Y02P20/55 , C07C271/24
摘要： The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET agent, ensuring that the reaction efficiently goes to completion.
摘要翻译： 本发明涉及一种制备放射性药物前体的方法，特别是用作生产用于体内成像方法如正电子发射断层摄影（PET）的放射性标记氨基酸的前体的保护的氨基酸衍生物。 特别地，本发明涉及制备[18 F] -1-氨基-3-氟环丁烷羧酸（[18 F] FACBC）PET试剂的前体的方法，确保反应有效地完成。
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公开(公告)号：US08946483B2
公开(公告)日：2015-02-03
申请号：US14131442
申请日：2012-07-20
申请人： Radha Achhanath , Srinath Balaji , Asfal Mohammed Kadavilpparampu Mohamed , Sondre Nilsen , Steven Michael Fairway
发明人： Radha Achhanath , Srinath Balaji , Asfal Mohammed Kadavilpparampu Mohamed , Sondre Nilsen , Steven Michael Fairway
IPC分类号： C07C43/20 , C07C45/00 , C07C41/00 , C07C45/78 , C07C41/44 , C07C43/174 , C07C45/42 , C07C49/757 , C07C319/20
CPC分类号： C07C45/78 , C07C41/44 , C07C43/174 , C07C45/42 , C07C49/757 , C07C319/20 , C07C2601/04 , C07C49/753 , C07C323/65
摘要： The present invention relates to a method of obtaining radiopharmaceutical precursors, and in particular precursors to protected amino acid derivatives, which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures, such as positron emission tomography (PET).
摘要翻译： 本发明涉及一种获得放射性药物前体的方法，特别是被保护的氨基酸衍生物的前体，其用作用于生物体内成像方法如正电子发射断层摄影（PET）的放射性标记氨基酸的前体。
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