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公开(公告)号：US08277777B2
公开(公告)日：2012-10-02
申请号：US12308715
申请日：2007-06-21
申请人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Anthony Eamon Storey , Denis Raymond Christophe Bouvet
发明人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Anthony Eamon Storey , Denis Raymond Christophe Bouvet
IPC分类号： A61K51/00 , A61M36/14 , C07D491/02
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.
摘要翻译： 具有与淀粉样蛋白亲和性的化合物，显示出与正常组织的足够快速的清除，并且由下式（1）表示的毒性如诱变性被抑制：或其盐，其中R1是选自 氢，羟基，羧基，硫酸根基，氨基，硝基，氰基，具有1-4个碳原子的烷基取代基或具有1-4个碳原子的烷氧基取代基; R2是放射性卤素取代基; 并且m为0〜2的整数，还提供了含有上述式所示化合物或其盐的阿尔茨海默病的低毒性诊断剂。
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公开(公告)号：US20100092387A1
公开(公告)日：2010-04-15
申请号：US12308715
申请日：2007-06-21
申请人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Storey Anthony Eamon , Denis Raymond Christophe Bouvet
发明人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Storey Anthony Eamon , Denis Raymond Christophe Bouvet
IPC分类号： A61K51/04 , C07D471/04
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.
摘要翻译： 具有与淀粉样蛋白亲和性的化合物，显示出与正常组织的足够快速的清除，并且由下式（1）表示的毒性如诱变性被抑制：或其盐，其中R1是选自 氢，羟基，羧基，硫酸根基，氨基，硝基，氰基，具有1-4个碳原子的烷基取代基或具有1-4个碳原子的烷氧基取代基; R2是放射性卤素取代基; 并且m为0〜2的整数，还提供了含有上述式所示化合物或其盐的阿尔茨海默病的低毒性诊断剂。
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公开(公告)号：US20090252680A1
公开(公告)日：2009-10-08
申请号：US12312596
申请日：2007-10-30
IPC分类号： A61K51/04 , C07D471/04 , A61K101/02
CPC分类号： C07B59/002 , A61K51/0455 , C07D471/04
摘要： A compound represented by the following formula or a salt thereof: wherein each of A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a group selected from the group consisting of hydrogen, hydroxyl group, carboxyl group, sulfuric acid group, amino group, nitro group, cyano group, non-radioactive halogen substituents, alkyl substituents with 1-4 carbon atoms and alkoxy substituents with 1-4 carbon atoms; and R2 is a radioactive halogen substituent, provided at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4, is effective as an image diagnosis probe targeting amyloid and as well as a diagnostic agent for Alzheimer's disease including the compound represented by the above formula or a salt thereof.
摘要翻译： 由下式表示的化合物或其盐：其中A1，A2，A3和A4各自独立地表示碳或氮; R1是选自氢，羟基，羧基，硫酸基，氨基，硝基，氰基，非放射性卤素取代基，具有1-4个碳原子的烷基取代基和具有1个 -4个碳原子; 并且R2是放射性卤素取代基，只要A1，A2，A3和A4中的至少一个代表碳，并且R1与由A1，A2，A3或A4表示的碳结合，作为靶向淀粉样蛋白的图像诊断探针是有效的， 以及阿尔茨海默氏病的诊断剂，包括由上式表示的化合物或其盐。
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公开(公告)号：US08399672B2
公开(公告)日：2013-03-19
申请号：US12739624
申请日：2008-10-24
IPC分类号： C07D491/02 , C07D498/02
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1, R2 and R3 independently represent a group selected from the group consisting of a hydrogen, hydroxyl group, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, excluding the case where two or more of the substituents R1, R2 and R3 are hydrogen, R4 is a group selected from the group consisting of a hydrogen, hydroxyl group, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, and m is an integer of 1 to 4, provided that at least one of R1, R2, R3 and R4 represents a radioactive halogen substituent, and a reagent comprising the same.
摘要翻译： 提供了有效作为靶向用于图像诊断的淀粉样蛋白的探针的化合物和包含用于检测沉积在生物组织上的淀粉样蛋白的化合物的试剂。 提供由下式（1）表示的化合物：其中R 1，R 2和R 3独立地表示选自氢，羟基，具有1至4个碳原子的烷基取代基的烷基取代基，烷基链与 1至4个碳原子和卤素取代基，不包括两个或多个取代基R 1，R 2和R 3为氢的情况，R 4为选自氢，羟基，具有烷基链的烷氧基取代基 至4个碳原子和卤素取代基，m为1至4的整数，条件是R 1，R 2，R 3和R 4中的至少一个表示放射性卤素取代基，和包含该取代基的试剂。
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公开(公告)号：US20100069640A1
公开(公告)日：2010-03-18
申请号：US12312867
申请日：2007-10-30
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound represented by the following formula or a salt thereof: wherein each of A1, A2, A3 and A4 independently represents a carbon or nitrogen, R1 is a radioactive halogen substituent, R2 is a group selected from the group consisting of hydrogen, a hydroxyl group, a methoxy group, a carboxyl group, an amino group, an N-methylamino group, an N,N-dimethylamino group and a cyano group, and p is an integer of 0 to 2, provided at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4, is effective as an image diagnosis probe targeting amyloid and a diagnostic agent for Alzheimer's disease.
摘要翻译： 由下式表示的化合物或其盐：其中A1，A2，A3和A4各自独立地表示碳或氮，R1是放射性卤素取代基，R2是选自氢，羟基 基团，甲氧基，羧基，氨基，N-甲基氨基，N，N-二甲基氨基和氰基，p为0〜2的整数，提供A1，A2 ，A3和A4表示碳，R1与由A1，A2，A3或A4表示的碳结合，作为靶向淀粉样蛋白的图像诊断探针和阿尔茨海默氏病的诊断剂是有效的。
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公开(公告)号：US20100249418A1
公开(公告)日：2010-09-30
申请号：US12739348
申请日：2008-10-24
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1 is a group selected from the group consisting of a halogen substituent, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and hydroxyl group, R2 is a group selected from the group consisting of a cyano substituent, alkyl substituent with 1 to 4 carbon atoms and halogen substituent, R3 is a group selected from the group consisting of a hydroxyl group, halogen substituent and substituent represented by the following formula: (wherein R4 is a hydrogen, halogen substituent or hydroxyl group, and m is an integer of 1 to 4), provided that at least one of R1, R2, R3 and R4 represents a radioactive halogen, and a reagent comprising the same.
摘要翻译： 提供了有效作为靶向用于图像诊断的淀粉样蛋白的探针的化合物和包含用于检测沉积在生物组织上的淀粉样蛋白的化合物的试剂。 提供由下式（1）表示的化合物：其中R 1是选自卤素取代基，具有1至4个碳原子的烷基取代基，具有1至4个碳原子的烷基链的烷氧基取代基和羟基的基团 基团，R 2为选自氰基取代基，具有1〜4个碳原子的烷基取代基和卤素取代基的基团，R 3为选自羟基，卤素取代基和下述基团的取代基的基团 式（R 4为氢，卤素取代基或羟基，m为1〜4的整数），条件是R 1，R 2，R 3和R 4中的至少一个表示放射性卤素，和含有该卤素的试剂 。
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公开(公告)号：US20100249407A1
公开(公告)日：2010-09-30
申请号：US12226561
申请日：2007-04-26
IPC分类号： C07F7/22 , C07D471/04 , C07D487/04 , C07D487/00
CPC分类号： C07D487/04 , A61K51/0455 , A61K51/0459 , C07D471/04 , C07F7/2208
摘要： The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, andR3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R3 binds to a carbon represented by A1, A2, A3 or A4.
摘要翻译： 本发明涉及对淀粉样蛋白具有亲和性的化合物，与正常组织相比具有足够快速的清除作用，并且其毒性如致突变性被抑制，并且还涉及含有该化合物的阿尔茨海默病的低毒性诊断剂。 该化合物由下式（1）表示或其盐：其中A1，A2，A3和A4独立地表示碳或氮，R3表示下式所示的基团：其中R1是放射性卤素取代基 ; m为0〜4的整数。 并且n为0或1的整数，条件是A1，A2，A3和A4中的至少一个表示碳，R3与由A1，A2，A3或A4表示的碳结合。
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![Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid](/abs-image/US/2012/11/06/US08303935B2/abs.jpg.150x150.jpg)
8.发明授权Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid 失效具有对淀粉样蛋白亲和力的烷氧基取代的咪唑并[1,2-a]吡啶公开(公告)号：US08303935B2
公开(公告)日：2012-11-06
申请号：US12227487
申请日：2007-05-15
CPC分类号： C07D487/04 , A61K51/0455 , A61K51/0459 , C07D471/04 , C07F7/2208
摘要： The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.
摘要翻译： 本发明提供了与淀粉样蛋白亲和性的化合物，与正常组织显示足够快的清除，并且被抑制在毒性如突变性。 提供由下式（1）表示的化合物或其盐：其中A1，A2，A3和A4独立地表示碳或氮; R1是卤素取代基; R2是卤素取代基; 并且m为0〜2的整数，只要R1和R2中的至少一个为放射性卤素取代基，则A1，A2，A3，A4中的至少一个为碳，R1与由A1表示的碳结合， A2，A3或A4，以及含有上述式表示的化合物或其盐的低毒诊断剂。
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9.发明申请USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME 审中-公开使用具有AMYLOID的亲和性的新化合物及其生产方法公开(公告)号：US20100267952A1
公开(公告)日：2010-10-21
申请号：US12740627
申请日：2008-10-28
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , A61K51/0455 , A61K51/0459 , C07D471/04
摘要： The invention provides a reagent for detecting amyloid in a biological tissue which can be detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 and A4.
摘要翻译： 本发明提供一种用于检测生物组织中的淀粉样蛋白的试剂，其可以使用与淀粉样蛋白亲和性并且被抑制在毒性如致突变性的化合物，以高灵敏度体外和体内检测淀粉样蛋白。 用于检测沉积在生物组织中的淀粉样蛋白的试剂包含由下式（1）表示的化合物或其盐：其中A1，A2，A3和A4独立地表示碳或氮; R1是卤素取代基; R2是卤素取代基; 并且m为0〜2的整数，只要R1和R2中的至少一个为放射性卤素取代基，则A1，A2，A3，A4中的至少一个为碳，R1与由A1表示的碳结合， A2，A3和A4。
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公开(公告)号：US20090252679A1
公开(公告)日：2009-10-08
申请号：US12227487
申请日：2007-05-15
IPC分类号： A61K51/04 , C07D471/04 , A61K101/02
CPC分类号： C07D487/04 , A61K51/0455 , A61K51/0459 , C07D471/04 , C07F7/2208
摘要： The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.
摘要翻译： 本发明提供了与淀粉样蛋白亲和性的化合物，与正常组织显示足够快的清除，并且被抑制在毒性如突变性。 提供由下式（1）表示的化合物或其盐：其中A1，A2，A3和A4独立地表示碳或氮; R1是卤素取代基; R2是卤素取代基; 并且m为0〜2的整数，只要R1和R2中的至少一个为放射性卤素取代基，则A1，A2，A3，A4中的至少一个为碳，R1与由A1表示的碳结合， A2，A3或A4，以及含有上述式表示的化合物或其盐的低毒诊断剂。
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