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参考文献:N-Phenyl-4-Pyrazolo[1,5-B]Pyridazin-3-Ylpyrimidin-2-Amines As Potent And Selective Inhibitors Of Glycogen Synthase Kinase 3 With Good Cellular Efficacy
标题:N-Phenyl-4-Pyrazolo[1,5-B]Pyridazin-3-Ylpyrimidin-2-Amines As Potent And Selective Inhibitors Of Glycogen Synthase Kinase 3 With Good Cellular Efficacy
摘要:Glycogen Synthase Kinase 3 Regulates Glycogen Synthase,The Rate-Determining Enzyme For Glycogen Synthesis. Liver And Muscle Glycogen Synthesis Is Defective In Type 2 Diabetics,Resulting In Elevated Plasma Glucose Levels. Inhibition Of Gsk-3 Could Potentially Be An Effective Method To Control Plasma Glucose Levels In Type 2 Diabetics. Structure-Activity Studies On A N-Phenyl-4-Pyrazolo[1,5-B]Pyridazin-3-Ylpyrimidin-2-Amine Series Have Led To The Identification Of Potent And Selective Compounds With Good Cellular Efficacy. Molecular Modeling Studies Have Given Insights Into The Mode Of Binding Of These Inhibitors. Since The Initial Leads Were Also Potent Inhibitors Of Cdk-2/cdk-4,An Extensive Sar Was Performed At Various Positions Of The Pyrazolo[1,5-B]Pyridazin Core To Afford Potent Gsk-3 Inhibitors That Were Highly Selective Over Cdk-2. In Addition,These Inhibitors Also Exhibited Very Good Cell Efficacy And Functional Response. A Representative Example Was Shown To Have Good Oral Exposure Levels,Extending Their Utility In An In Vivo Setting. These Inhibitors Provide A Viable Lead Series In The Discovery Of New Therapies For The Treatment Of Type 2 Diabetes.
DOI:10.1021/jm040063I

专利信息

专利号:US-7754188-B2
优先权日:2003-06-30
标 题:Radiolabeled cannabinoid-1 receptor modulators
发明人：BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.