CAS: 587871-26-9; 2-Morpholino-6-(Thianthren-1-yl)-4H-Pyran-4-One

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CAS号108847-76-3 1-噻蒽基硼酸 | CAS号119671-47-5 2-氯-6-吗啉代-4H-吡喃-4-酮 | CAS号85839-49-2 4,4-dichloro-1-... | CAS号81189-95-9 4-chloro-4-(2,2...

📜4-Chloro-4-(2,2,2-Trichloroethyl)-Oxetan-2-One置于四(三苯基膦)钯 高氯酸,碳酸氢钠,Potassium Carbonate体系中,用 1,4-二氧六环,二氯甲烷 作为反应溶剂,化学反应 75.33H,反应生成 2-吗啉-4-基-6-噻蒽-1-基吡喃-4-酮
参考文献:Pyranone,Thiopyranone,And Pyridone Inhibitors Of Phosphatidylinositol 3-Kinase Related Kinases. Structure−activity Relationships For Dna-Dependent Protein Kinase Inhibition,And Identification Of The First Potent And Selective Inhibitor Of The Ataxia Telangiectasia Mutated Kinase
标题:Pyranone,Thiopyranone,And Pyridone Inhibitors Of Phosphatidylinositol 3-Kinase Related Kinases. Structure−activity Relationships For Dna-Dependent Protein Kinase Inhibition,And Identification Of The First Potent And Selective Inhibitor Of The Ataxia Telangiectasia Mutated Kinase
摘要:Structure-Activity Relationships Have Been Investigated For Inhibition Of Dna-Dependent Protein Kinase (Dna-Pk) And Atm Kinase By A Series Of Pyran-2-Ones,Pyran-4-Ones,Thiopyran-4-Ones,And Pyridin-4-Ones. A Wide Range Of Ic50 Values Were Observed For Pyranones And Thiopyranones Substituted At The 6-Position,With The 3-And 5-Positions Proving Intolerant To Substitution. Related Pyran-2-Ones,Pyran-4-Ones,And Thiopyran-4-Ones Showed Similar Ic50 Values Against Dna-Pk,Whereas The Pyridin-4-One System Proved,In General,Ineffective At Inhibiting Dna-Pk. Extended Libraries Exploring The 6-Position Of 2-Morpholino-Pyran-4-Ones And 2-Morpholino-Thiopyrano-4-Ones Identified The First Highly Potent And Selective Atm Inhibitor 2-Morpholin-4-Yl-6-Thianthren-1-Yl-Pyran-4-One (151C; Atm; Ic50 = 13 Nm) And Revealed Constrained Sars For Atm Inhibition Compared With Dna-Pk. One Of The Most Potent Dna-Pk Inhibitors Identified,2-(4-Methoxyphenyl)-6-(Morpholin-4-yl)Pyran-4-One (16; Dna-Pk; Ic50 = 220 Nm) Effectively Sensitized Hela Cells To The Topoisomerase Ii Inhibitor Etoposide In Vitro.
DOI:10.1021/jm061121Y

专利信息

专利号:US-8440695-B2
优先权日:2005-11-09
标 题:Use of chloroquine to treat metabolic syndrome
发明人：KASTAN MICHAEL B; SEMENKOVICH CLAY F; SCHNEIDER JOCHEN
权利人:KASTAN MICHAEL B; SEMENKOVICH CLAY F; SCHNEIDER JOCHEN; ST JUDE CHILDRENS RES HOSPITAL; UNIV WASHINGTON
摘要:The present invention provides methods and compositions for modulating certain metabolic processes and for treating a variety of disorders associated with metabolic syndrome, including insulin related disorders, ischemia, oxidative stress, atherosclerosis, hypertension, obesity, abnormal lipid metabolism, and stroke by administering an effective dose of a chloroquine compound. The invention also provides methods and compositions relating to administering an effective dose of a chloroquine compound in combination with at least a second pharmaceutically active ingredient or compound including an antihyperglycemic diabetes treatment, an antihypertensive agent, an antithrombotic agent, and/or an inhibitor of cholesterol synthesis or absorption.