公开(公告)号：US10059704B2

公开(公告)日：2018-08-28

申请号：US14112864

申请日：2012-04-20

申请人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

发明人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

IPC分类号： C07D451/04 ,  A61K51/04 ,  C07D453/02 ,  C07D455/02

CPC分类号： C07D451/04 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D453/02 ,  C07D455/02 ,  G01N2333/70571 ,  G01N2800/28 ,  G01N2800/2821

摘要： A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN′ groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

公开(公告)号：US06180083B2

公开(公告)日：2001-01-30

申请号：US09180281

申请日：1998-11-10

申请人： Laurent Mauclaire ,  Patrick Emond ,  Denis Guilloteau ,  Jean-Claude Besnard ,  Yves Frangin

发明人： Laurent Mauclaire ,  Patrick Emond ,  Denis Guilloteau ,  Jean-Claude Besnard ,  Yves Frangin

IPC分类号： A61K5100

CPC分类号： C07D451/02 ,  A61K51/0448 ,  A61K2123/00

摘要： The present invention relates to tropane derivatives having particular use for the in vivo detection of dopamine transporters. These derivatives meet the formula in which R1 is I or Sn (R3)3, R2 is for example the methyl group, and X and Y are various substituents. The derivatives with X═CH3 and Y═H show strong specificity for the dopamine transporter compared with the serotonin transporter (74% inhibition when the transporter is previously saturated with GBR 12909).

摘要翻译： 本发明涉及特异性用于体内检测多巴胺转运蛋白的托烷衍生物。这些衍生物涉及R1为I或Sn（R3）3，R2为例如甲基的化合物，X和Y为各种取代基 具有X = CH 3和Y = H的衍生物与血清素转运蛋白相比显示出对多巴胺转运蛋白的强特异性（当转运蛋白先前用GBR12909饱和时，其抑制为74％）。

公开(公告)号：US20140030191A1

公开(公告)日：2014-01-30

申请号：US14112864

申请日：2012-04-20

申请人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

发明人： Sylvain Routier ,  Franck Suzenet ,  Frederic Pin ,  Sylvie Chalon ,  Johnny Vercouillie ,  Denis Guilloteau

IPC分类号： C07D451/04 ,  C07D453/02 ,  A61K51/04

CPC分类号： C07D451/04 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D453/02 ,  C07D455/02 ,  G01N2333/70571 ,  G01N2800/28 ,  G01N2800/2821

摘要： A compound having the following general formula (I): wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN′ groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

摘要翻译： 具有以下通式（I）的化合物：其中：X是氮原子，Y是碳原子; 或X为碳原子，Y为氮原子; Ar基团是芳基或杂芳基; 并且RN和RN'基团与它们所结合的碳原子一起形成单环或双环氮杂环烷基。 还描述了其药学上可接受的盐，其水合物或多晶型结构以及其外消旋物，非对映异构体或其对映异构体。