公开(公告)号：US20160008494A1

公开(公告)日：2016-01-14

申请号：US14860823

申请日：2015-09-22

Applicant: CLINO LTD.

Inventor： Yukitsuka KUDO ,  Shozo FURUMOTO ,  Nobuyuki OKAMURA

IPC: A61K51/04

CPC classification number: C07D215/12 ,  A61K9/0019 ,  A61K9/08 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07B59/002 ,  C07B2200/05 ,  C07D215/14 ,  C07D215/20 ,  C07D215/233 ,  C07D215/26 ,  C07D215/38 ,  C07D215/40 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D498/04 ,  G01N33/6893 ,  G01N2800/2821

Abstract: An object of the present invention is to provide a probe for imaging a β-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity.According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.

Abstract translation: 本发明的目的是提供一种用于成像结构蛋白的探针，其可用于诊断构象疾病，特别是具有诸如tau蛋白的脑内积累的基本症状的疾病（tau蛋白病），例如 ， 阿尔茨海默氏病。 本发明的另一个目的是提供一种对tau高度特异性并且能够令人满意的感光度的tau成像的化合物，并且还具有高的脑转换，低或未被认可的寻骨性质和低或未被认可的毒性。 根据本发明，通过提供式I化合物（其中A，R 1，R 2，R 3，R 4，R 5，R 6，R a和R b如本说明书中所定义）或其药学上可接受的 盐或其溶剂化物。

公开(公告)号：US20160244411A1

公开(公告)日：2016-08-25

申请号：US15030924

申请日：2014-10-22

Applicant: CLINO LTD.

Inventor： Yukitsuka KUDO ,  Nobuyuki OKAMURA ,  Shozo FURUMOTO

IPC: C07D215/20 ,  A61K51/04 ,  G01N33/68 ,  C07D401/04 ,  C07D405/14 ,  C07B59/00 ,  C07B57/00

CPC classification number: C07D215/20 ,  A61K9/0019 ,  A61K9/08 ,  A61K51/0453 ,  A61K51/0455 ,  C07B57/00 ,  C07B59/002 ,  C07B2200/05 ,  C07B2200/07 ,  C07D401/04 ,  C07D405/14 ,  G01N33/6896 ,  G01N2800/2821

Abstract: An object of the present invention is to provide a compound represented by formula (I) which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or undetected toxicity.

Abstract translation: 本发明的目的是提供一种对tau高度特异性的式（I）表示的化合物，并且可以令人满意的感光度成像tau，并且还具有高脑转移，低或未识别的寻骨性质，低 未检出毒性。