公开(公告)号：US20070142467A1

公开(公告)日：2007-06-21

申请号：US11256583

申请日：2005-10-21

申请人： Christopher Esslinger ,  Richard Bridges ,  Michael Kavanaugh

发明人： Christopher Esslinger ,  Richard Bridges ,  Michael Kavanaugh

IPC分类号： A61K31/277 ,  A61K31/198 ,  C07C255/28 ,  C07C229/38

CPC分类号： C07C229/36

摘要： The present invention provides an L-aspartate derivative compound represented by the following structure wherein Ar represents an aromatic group; L represents a linking moiety; R represents hydrogen, alkyl, aryl, or heteroaryl; and indicates that the stereochemistry at the 3-position can be R or S. The compounds of the invention are useful for selectively inhibiting EAAT3 and for enhancing synaptic transmission. Additionally, the inventive compounds can be used to treat a patient suffering from Alzheimers disease or a neuropathy or a neurodegenerative disease in which L-glutamate transporter activity is involved in the onset of the disease.

摘要翻译： 本发明提供由以下结构表示的L-天冬氨酸衍生物化合物，其中Ar表示芳族基团; L表示连接部分; R代表氢，烷基，芳基或杂芳基; “img id =”custom-character-00001“he =”1.78mm“wi =”4.91mm“file =”US20070142467A1-20070621-P00001.TIF“alt =”custom character“img-content =”character“img- format =“tif”/>表示3位的立体化学可以是R或S.本发明的化合物可用于选择性抑制EAAT3和增强突触传递。 此外，本发明的化合物可用于治疗患有阿尔茨海默病或神经病变或神经变性疾病的患者，其中L-谷氨酸转运蛋白活性参与疾病发作。