申请人:ELI LILLY AND COMPANY
公开号:EP0677517A1
公开(公告)日:1995-10-18
This invention provides novel benzylidene rhodanines of the formula
wherein
nis 0, 1, 2, 3, or 4;
qis 0, 1, 2, 3, or 4;
Ais -O, -NH-, or -S(O)m-;
where m is 0, 1, or 2;
R¹is hydrogen, C₁-C₆ alkyl, di(C₁-C₆ alkyl)amino-, amino, (C₁-C₆ alkyl)amino-, cyano(C₁-C₆ alkyl)-, or carboxy(C₁-C₆ alkylidenyl)-;
Ris phenyl, oxazolyl, benzophenonyl, or naphthyl optionally substituted with one or more substituents, which are useful as agents in treating or preventing conditions associated with β-amyloid peptide. This invention further provides methods of treating or preventing Alzheimer's Disease which comprises administering to a mammal in need thereof an effective amount of one or more of the benzylidene rhodanines of the present invention. This invention also provides methods for reducing blood glucose concentrations which comprises administering to a mammal in need thereof an effective amount of one or more of the benzylidene rhodanines of the present invention.
本发明提供了式如下的新型亚苄基罗丹宁
式中
n为0、1、2、3或4;
q为0、1、2、3或4;
A是-O、-NH-或-S(O)m-;
其中 m 为 0、1 或 2;
R¹是氢、C₁-C₆烷基、二(C₁-C₆烷基)氨基、氨基、(C₁-C₆烷基)氨基、氰基(C₁-C₆烷基)-或羧基(C₁-C₆亚烷基)-;
里氏苯基、恶唑基、二苯甲酮基或任选被一个或多个取代基取代的萘基,可用作治疗或预防与 β 淀粉样肽相关的疾病的药物。本发明进一步提供了治疗或预防阿尔茨海默病的方法,其中包括向有需要的哺乳动物施用有效量的一种或多种本发明的亚苄基罗丹宁。本发明还提供了降低血糖浓度的方法,其中包括向有需要的哺乳动物施用有效量的一种或多种本发明的亚苄基罗丹宁。