公开(公告)号：EP1858505A2

公开(公告)日：2007-11-28

申请号：EP05825898.9

申请日：2005-12-22

申请人： University of Basel ,  University of Bern ,  Swiss Tropical Institute

发明人： SIMMEN, Urs ,  SIGEL, Erwin ,  BRUN, Reto ,  SEQUIN, Urs ,  SENN, Martin

IPC分类号： A61K31/22 ,  A61K36/25 ,  A61P25/22

CPC分类号： A61K31/22 ,  A61K36/25

摘要： The present invention relates to certain linear polyacetylene containing compounds which are indicated as having a positive allosteric modulating activity on the GABAA receptor. More specifically the invention relates to linear polyacetylene containing compounds having a β-subunit selective, positive allosteric modulating activity on the GABAA receptor and substantially lacking a binding capability at the benzodiazepine binding site, their use as agents for the treatment of diseases of the central nervous system (CNS) in mammals, such as humans, and in particular in the treatment of CNS diseases, such as anxiety and epilepsy.

摘要翻译： 本发明涉及某些含有线性聚乙炔的化合物，其被表明对GABAA受体具有正变构调节活性。 更具体地说，本发明涉及含有线型聚乙炔的化合物，该化合物对GABAA受体具有β亚单位选择性，正变构调节活性并基本上不具有对苯二氮卓结合位点的结合能力，它们作为治疗中枢神经系统疾病的药物 系统（CNS）在哺乳动物如人类中的应用，特别是用于治疗CNS疾病，如焦虑和癫痫。