Compositions and methods for reducing serum glucose and triglyceride levels in diabetic mammals
申请人:——
公开号:US20040147611A1
公开(公告)日:2004-07-29
Diabetic mammals are treated with compounds that are significantly more efficacious as agonists of RXR
&bgr;
retinoid receptors than as agonists of RXR
&agr;
or RXR
&ggr;
retinoid receptors. The treatment reduces serum glucose and triglyceride levels of the mammals without the undesirable side effects of reducing serum thyroxine levels and a transient increase in serum triglyceride levels Compounds suitable for use in the methods of treatments of the present invention are selected by testing and identifying compounds of selective or specific efficacy as agonists of RXR
&bgr;
retinoid receptors in preference over RXR
&agr;
and/or RXR
&ggr;
retinoid receptors. Novel compounds used in the methods of the invention have Formula 1 where the variables are defined as disclosed in the specification.
1
糖尿病哺乳动物使用的化合物,作为RXRβ视黄醇受体的激动剂比作为RXRα或RXRγ视黄醇受体的激动剂更有效。该治疗降低了哺乳动物的血清葡萄糖和甘油三酯水平,而不会出现降低血清甲状腺素水平和短暂增加血清甘油三酯水平的不良副作用。适用于本发明治疗方法的化合物是通过测试和鉴定作为RXRβ视黄醇受体激动剂的选择性或特异性效力的化合物而选择的,而不是选择RXRα和/或RXRγ视黄醇受体。本发明方法中使用的新型化合物具有公式1,其中变量的定义如规范中所披露。