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公开(公告)号：US09809585B2
公开(公告)日：2017-11-07
申请号：US14890922
申请日：2014-11-07
发明人： Mengchao Cui , Chunping Lin , Boli Liu , Yuzhi Guo , Zhiyong Zhang
IPC分类号： C07D417/04 , C07D413/04 , C07D263/57 , C07D277/66 , A61K51/04 , A61K49/10
CPC分类号： C07D417/04 , A61K49/10 , A61K51/0453 , A61K51/0455 , C07D263/57 , C07D277/66 , C07D413/04
摘要： A fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ plaques and containing a chiral side chain substituent, has a general formula (I) as follows: wherein X is N; Y is S or O; Z is N or CH; R1 is a 5 or 6-substituent and is F is 19F or 18F; R2 is NHCH3 or N(CH3)2. The compound of the present invention has high affinity to Aβ plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.
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2.发明申请公开(公告)号：US20170037008A1
公开(公告)日：2017-02-09
申请号：US15101385
申请日：2014-11-06
发明人： Zhiyong Zhang , Mengchao Cui , Chunping Lin , Boli Liu , Yuzhi Guo
IPC分类号： C07D213/64 , C07C201/12 , C07C43/205 , C07C319/20 , C07C217/86 , C07C213/02 , C07C323/20 , C07C205/37 , C07C41/18
CPC分类号： C07D213/64 , A61K51/04 , A61K51/0406 , C07B2200/05 , C07C41/18 , C07C43/2055 , C07C43/225 , C07C43/23 , C07C201/12 , C07C205/37 , C07C211/53 , C07C213/02 , C07C217/86 , C07C319/20 , C07C323/20 , C07D213/65 , C07F7/2208
摘要： Parts of compounds, after being labeled by radionuclide, of the phenyl benzyl ether derivative, are used as Aβ plaque imaging agent. The structural formula of the phenyl benzyl ether derivative is shown by formula (I). The present invention develops a kind of brand new phenyl benzyl ether derivative which has high affinity with Aβ plaques in brains of AD patients. The chemical structure of the phenyl benzyl ether derivative is different from that of compounds disclosed in the prior art and the phenyl benzyl ether derivative belongs to a brand new compound for diagnosing and treating AD. The obtained Aβ plaque imaging agent has the advantages that the in-vivo stability is good, the fat solubility is low, the removal speed for the brain is fast, the problem of removing the radionuclide in vivo does not exist, and the application prospect and the market value are great.
摘要翻译： 本发明涉及苯基苄基醚衍生物及其制备方法和用途，一部分化合物在放射性核素标记后作为Aβ斑块显像剂，苯基苄基醚衍生物用于制备 用于诊断和治疗阿尔茨海默病（AD）的药物。 苯基苄基醚衍生物具有式（I）所示的结构式; 本发明开发了一种对AD患者大脑中的Aβ斑块具有高亲和力的全新苯基苄基醚衍生物，其化学结构与现有技术公开的化合物的化学结构不同，属于 用于诊断和治疗阿尔茨海默病的全新化合物; 得到的Aβ噬菌斑显像剂体内稳定性好，脂质溶解度低，使得脑部消除速度快，体内不含放射性核素的去除问题，具有广阔的应用前景， 市场价值。
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3.发明申请Fluorinated 2-arylbenzo heterocyclic compound with high affinity to A beta 946; plaques and containing chiral side chain substituent, and preparation method and usage thereof 审中-公开对Aβ946具有高亲和力的氟化2-芳基苯并杂环化合物; 斑块和含有手性侧链取代基及其制备方法和用途公开(公告)号：US20160207910A1
公开(公告)日：2016-07-21
申请号：US14890922
申请日：2014-11-07
发明人： Mengchao Cui , Chunping Lin , Boli Liu , Yuzhi Guo , Zhiyong Zhang
IPC分类号： C07D417/04 , A61K51/04 , C07D413/04 , C07D277/66 , C07D263/57
CPC分类号： C07D417/04 , A61K49/10 , A61K51/0453 , A61K51/0455 , C07D263/57 , C07D277/66 , C07D413/04
摘要： A fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ plaques and containing a chiral side chain substituent, has a general formula (I) as follows: wherein X is N; Y is S or O; Z is N or CH; R1 is a 5 or 6-substituent and is F is 19F or 18F; R2 is NHCH3 or N(CH3)2. The compound of the present invention has high affinity to Aβ plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.
摘要翻译： 对A＆Bgr具有高亲和力的氟化2-芳基苯并杂环化合物; 含有手征侧链取代基，具有如下通式（I）：其中X为N; Y为S或O; Z是N或CH; R1是5或6取代基，F是19F或18F; R2是NHCH3或N（CH3）2。 本发明化合物对A＆Bgr具有高亲和力; 斑块，可用于制备适当的放射性核素标记探针，用于早期诊断AD。
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