CAS: 486422-57-5; (4-(Pyrrolidin-1-Ylsulfonyl)Phenyl)Boronic Acid

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CAS号98-58-8 对溴苯磺酰氯

📜C16H26Bno4S置于水,Silica Gel体系中,用 四氢呋喃 作为反应溶剂,化学反应生成 4-(磺酰吡咯啉)苯基硼酸
参考文献:Discovery Of Novel Potent And Highly Selective Glycogen Synthase Kinase-3β (Gsk3β) Inhibitors For Alzheimer's Disease: Design,Synthesis,And Characterization Of Pyrazines
标题:Discovery Of Novel Potent And Highly Selective Glycogen Synthase Kinase-3β (Gsk3β) Inhibitors For Alzheimer's Disease: Design,Synthesis,And Characterization Of Pyrazines
摘要:Glycogen Synthase Kinase-3 Beta,Also Called Tau Phosphorylating Kinase,Is A Proline-Directed Serine/threonine Kinase Which Was Originally Identified Due To Its Role In Glycogen Metabolism. Active Forms Of Gsk3 Beta Localize To Pretangle Pathology Including Dystrophic Neuritis And Neurofibrillary Tangles In Alzheimer'S Disease (Ad) Brain. By Using A High Throughput Screening (Hts) Approach To Search For New Chemical Series And Cocrystallization Of Key Analogues To Guide The Optimization And Synthesis Of Our Pyrazine Series,We Have Developed Highly Potent And Selective Inhibitors Showing Cellular Efficacy And Blood-Brain Barrier Penetrance. The Inhibitors Are Suitable For In Vivo Efficacy Testing And May Serve As A New Treatment Strategy For Alzheimer'S Disease.
DOI:10.1021/jm201724M

专利信息

专利号:US-9951062-B2
优先权日:2012-12-14
标 题 :Substituted 1 H-pyrrolo [2, 3-b] pyridine and 1 H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
发明人：VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY; GANIPISETTY VENU BABU; TALLURI SURESHKUMAR; APPALANENI RAJENDRA P
权利人:ARRIEN PHARMACEUTICALS LLC
摘要:Compounds according to Formulas I, IA or IB: n nto pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.