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1. 发明公开

EP2550255A1 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 有权转让
标题翻译： BILDGEBUNGSMITTELFÜRDEN NACHWEIS神经病学家LEIDEN
公开(公告)号：EP2550255A1
公开(公告)日：2013-01-30
申请号：EP11711420.7
申请日：2011-03-22
申请人： Siemens Medical Solutions USA, Inc.
发明人： CASHION, Daniel, Kurt , CHEN, Gang , KASI, Dhanalakshmi , KOLB, Hartmuth C. , LIU, Changhui , SINHA, Anjana , SZARDENINGS, Anna, Katrin , WANG, Eric , YU, Chul , ZHANG, Wei , GANGADHARMATH, Umesh, B. , WALSH, Joseph, C.
IPC分类号： C07D235/04 , C07D401/02 , A61K31/4184 , A61K31/4353 , A61P25/00
CPC分类号： C07D235/04 , A61K51/04 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/02 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04
摘要： Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Αβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders. Formula (V) or a pharmaceutically acceptable salt thereof, and stereoisomers thereof, wherein: X
25 -X
28 are each independently CH, CR
11 , or N; X
29 is CH, N, O or S; X
30 is CH, C, or N; X
31-34 are each independently CH, CR
12 , CR
13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy,— (O-CH
2 - CH
2 )
n -, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR
10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R
11 -R
13 is optionally replaced with N, Q, S, triazole, or halo, and, wherein at least one hydrogen is optionally replaced with halo, amine, amino, alkoxy, nitro, alkyl, alkenyL alkynyl, aryloxy, alkylaryl, alkylamino, alkylamine, NRioCOOalkyl, NR
10 COOaryl, NR
10 COalkyl, NR,0 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic saturated heterocycle and unsaturated heterocycle, a leaving group, CN, OH or a radioactive isotope.
摘要翻译：式（I） - （V）的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和β-淀粉样蛋白肽的式（I） - （V）化合物。本发明还涉及A＆bgr的成像方法; 和tau聚集体，其包括引入可检测量的包含放射性标记的式（I） - （V）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。这些方法和组合物使得临床前诊断和监测AD和其他神经障碍的进展。

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