CAS: 486424-20-8; 3-Amino-6-(4-((4-Methylpiperazin-1-yl)Sulfonyl)Phenyl)-N-(Pyridin-3-yl)Pyrazine-2-Carboxamide

上下游产品

methyl 3-amino-6-bromopyrazine-2-carboxylate pyridin-3-ylamine 1-((4-bromophenyl)sulfonyl)-4-methylpiperazine 4-[(4-methylpiperazin-1-yl)sulfonyl]phenylboronic acid

1-(4-溴苯基磺酰基)-4-甲基哌嗪置于正丁基锂,1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,水,Silica Gel,Sodium Carbonate体系中,用 四氢呋喃,乙醇,水,甲苯 作为反应溶剂,化学反应 18.5H,反应生成 3-氨基-6-[4-(4-甲基哌嗪-1-基)磺酰基苯基]-N-吡啶-3-基吡嗪-2-羧酰胺
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:WO-2008080986-A1
优先权日:2006-12-28
标 题 :Furan derivatives, method of synthesis and uses thereof
发明人：MARTINEZ GIL ANA; MEDINA PADILLA MIGUEL; FALL DIOP YAGAMARE; GOMEZ PACIOS GENEROSA; PEREZ VAZQUEZ MANUEL; MARTIN APARICIO ESTER; FUERTES HUERTA ANA; DEL MONTE MILLAN MARIA; NAVARRO RICO MARIA LUISA; PEREZ PUERTO MARIA JOSE
权利人:NEUROPHARMA SA; MARTINEZ GIL ANA; MEDINA PADILLA MIGUEL; FALL DIOP YAGAMARE; GOMEZ PACIOS GENEROSA; PEREZ VAZQUEZ MANUEL; MARTIN APARICIO ESTER; FUERTES HUERTA ANA; DEL MONTE MILLAN MARIA; NAVARRO RICO MARIA LUISA; PEREZ PUERTO MARIA JOSE
摘要:The present invention relates to furan derivatives of formula (I), their method of synthesis and uses thereof. Concretely, the compounds disclosed have proved to be inhibitors of glycogen synthase kinase 3β, GSK-3 β, which is known to be involved in different disease and conditions, such as Alzheimer's disease or non-insulin dependent diabetes mellitus. The present invention also relates to pharmaceutical compositions comprising the same. Further, the present invention is directed to the use of the compounds in the manufacture of a medicament for the treatment and/or prevention of a GSK-3 mediated disease or condition.

专利号:EP-1939191-A1
优先权日:2006-12-28
标题 :Furan derivatives, method of synthesis and uses thereof

专利号:WO-2008080988-A2
优先权日:2006-12-28
标题:Cyclopentanone derivatives, method of synthesis and uses thereof

专利号:EP-1939192-A1
优先权日:2006-12-28
标 题:Cyclopentanone derivatives, method of synthesis and uses thereof