公开(公告)号：US5502051A

公开(公告)日：1996-03-26

申请号：US614459

申请日：1990-11-16

申请人： Peter Scharfenberg ,  Ju/ rgen Liebscher ,  Alexander Knoll ,  Aleksej Uschmajew ,  Andreas Rolfs ,  Dieter Lohman ,  Gottfried Faust ,  Eveline Morgenstern

发明人： Peter Scharfenberg ,  Ju/ rgen Liebscher ,  Alexander Knoll ,  Aleksej Uschmajew ,  Andreas Rolfs ,  Dieter Lohman ,  Gottfried Faust ,  Eveline Morgenstern

IPC分类号： C07D401/04 ,  A61K9/20 ,  A61K9/48 ,  A61K31/40 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5377 ,  A61P25/04 ,  A61P25/08 ,  A61P29/00 ,  C07D207/34 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D207/34

摘要： The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles.Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents.The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations.Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

摘要翻译： 本发明涉及式I的3-氨基吡咯，其主要是新的，用于制备方法和用作药物和制剂，以及含有这些3-氨基吡咯的抗惊厥或镇痛制剂。 二取代和单取代的氨基被要求为3-氨基取代基。 本发明追求的目标是开发大量具有CNS活性的新型3-氨基吡咯，特别是具有抗惊厥或止痛特性的3-氨基吡咯，以及其制备方法和用作药物制剂。 根据本发明，通过使开链前体如氨基丙烯酸衍生物环化或通过改性吡咯来进行合成。