公开(公告)号：EP1751553B1

公开(公告)日：2008-10-08

申请号：EP05759896.3

申请日：2005-05-24

申请人： Ludwig-Maximilians-Universität München ,  Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

发明人： BERTSCH, Uwe ,  GIESE, Armin ,  KRETZSCHMAR, Hans ,  TAVAN, Paul ,  HIRSCHBERGER, Thomas ,  BIESCHKE, Jan ,  WEBER, Petra ,  WINKLHOFER, Konstanze, F. ,  TATZELT, Jörg ,  HARTL, F., Ulrich ,  WÜNSCH, Gerda ,  HÖGEN, Tobias, Johannes

IPC分类号： G01N33/68 ,  A61K31/155 ,  C07C281/18 ,  C07C243/24 ,  A61K31/16

CPC分类号： G01N33/6896 ,  A61K31/155 ,  G01N2500/02 ,  G01N2500/10

摘要： The present invention relates to a method of identifying a compound for inhibiting aggregation of proteins involved in diseases linked to protein aggregation and/or neurodegenerative diseases, comprising the steps of: (a) bringing into contact a labeled monomeric protein and a differently labeled aggregate of said protein in the (1) presence and (2) absence of a candidate inhibitor of aggregation, (b) determining the amount of co-localized labels, representing the extent of binding of the monomeric proteins to the aggregates of said protein; and (c) comparing the result obtained in the presence and absence of said compound, wherein a decrease of co-localized labels in the presence of said compound is indicative of the compound's ability to inhibit aggregation of said protein. Moreover, the present invention relates to a pharmaceutical composition containing said inhibitor of aggregation as well as to a kit.

公开(公告)号：EP2307381A2

公开(公告)日：2011-04-13

申请号：EP09772072.6

申请日：2009-06-09

申请人： Ludwig-Maximilians-Universität München ,  Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

发明人： GIESE, Armin ,  BERTSCH, Uwe ,  KRETZSCHMAR, Hans ,  HABECK, Mathias ,  HIRSCHBERGER, Thomas ,  TAVAN, Paul ,  GRIESINGER, Christian ,  LEONOV, Andrei ,  RYAZANOV, Sergey ,  WEBER, Petra ,  GEISSEN, Markus ,  GROSCHUP, Martin, H. ,  WAGNER, Jens

IPC分类号： C07D231/06 ,  C07D231/12 ,  C07D233/22 ,  C07D261/08 ,  C07D271/06

CPC分类号： C07D231/12 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/4245 ,  C07D207/333 ,  C07D231/06 ,  C07D233/64 ,  C07D261/08 ,  C07D271/06 ,  C07D405/04 ,  C07D413/04 ,  G01N33/6896 ,  G01N2800/2828

摘要： The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed.

摘要翻译： 本发明涉及由式（E）表示的化合物。 因此，本发明涉及用于治疗或预防与蛋白聚集和/或神经变性疾病的疾病使用由式（E）表示的化合物。 更过地，本发明涉及药物和诊断组合物包括本发明的化合物以及一种试剂盒。 进一步地，本发明涉及聚集蛋白的成像沉积物的方法。 因此，一种制备本发明的可检测标记的化合物的试剂盒是游离缺失盘。

公开(公告)号：EP1751553A2

公开(公告)日：2007-02-14

申请号：EP05759896.3

申请日：2005-05-24

申请人： Ludwig-Maximilians-Universität München ,  Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

发明人： BERTSCH, Uwe ,  GIESE, Armin ,  KRETZSCHMAR, Hans ,  TAVAN, Paul ,  HIRSCHBERGER, Thomas ,  BIESCHKE, Jan ,  WEBER, Petra ,  WINKLHOFER, Konstanze, F. ,  TATZELT, Jörg ,  HARTL, F., Ulrich ,  WÜNSCH, Gerda ,  HÖGEN, Tobias, Johannes

IPC分类号： G01N33/68 ,  A61K31/155 ,  C07C281/18 ,  C07C243/24 ,  A61K31/16

CPC分类号： G01N33/6896 ,  A61K31/155 ,  G01N2500/02 ,  G01N2500/10

摘要： The present invention relates to a method of identifying a compound for inhibiting aggregation of proteins involved in diseases linked to protein aggregation and/or neurodegenerative diseases, comprising the steps of: (a) bringing into contact a labeled monomeric protein and a differently labeled aggregate of said protein in the (1) presence and (2) absence of a candidate inhibitor of aggregation, (b) determining the amount of co-localized labels, representing the extent of binding of the monomeric proteins to the aggregates of said protein; and (c) comparing the result obtained in the presence and absence of said compound, wherein a decrease of co-localized labels in the presence of said compound is indicative of the compound's ability to inhibit aggregation of said protein. Moreover, the present invention relates to a pharmaceutical composition containing said inhibitor of aggregation as well as to a kit.