Prodrugs of GABA analogs, compositions and uses thereof
申请人:Gallop A. Mark
公开号:US20060229361A1
公开(公告)日:2006-10-12
The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
aggregation induced by adenosine diphosphate or collagen. Ring-expanded homologous derivatives and an acyclic analogue of 12 were also synthesized and tested for the biological activities. The azetidin-2-one skeleton bearing a 2-oxoalkylidene moiety at the 3 position was found to be essential for the platelet aggregation inhibitory activities of these compounds.
[Problem] To provide a compound which is useful as a GK activator.
[Means for Resolution] As a result of an extensive study on thiazole derivatives, the present inventors have found that a compound having an oxamoyl group, a glycol group or the like on a thiazole ring and a compound having an acetamide group substituted by a bicyclic heteroaryl group such as a quinolyl have a good GK activation effect, and thereby have accomplished the present invention.
Since the compounds of the present invention have a good GK activation effect, these are useful as therapeutic agents for diabetes, particularly type II diabetes.