CAS: 1079083-63-8; (2R,3R,4R,5S,6S)-2-(Acetoxymethyl)-6-(4-Chloro-3-(4-Hydroxybenzyl)Phenyl)Tetrahydro-2H-Pyran-3,4,5-Triyl Triacetate

上下游产品

acetic anhydride (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one [4-(5-bromo-2-chloro-benzyl)-phenoxy]-tert-butyl-dimethyl-silane (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-hydroxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

📜葡萄糖酸内酯置于n-甲基吗啉,吡啶,三乙基硅烷,4-二甲氨基吡啶,正丁基锂,甲烷磺酸,三氟化硼乙醚,三溴化硼体系中,用 四氢呋喃,正己烷,二氯甲烷,甲苯,乙腈 用作溶剂,化学反应 10.5H,反应生成达格列净杂质23
参考文献:达格列净释放一氧化氮的潜在抗糖尿病和抗血栓形成剂的设计,合成和生物学评价
标题:达格列净释放一氧化氮的潜在抗糖尿病和抗血栓形成剂的设计,合成和生物学评价
摘要:心血管并发症在2型糖尿病(t2Dm)中非常普遍,甚至在t2Dm的早期阶段或强化血糖控制状态下也是如此.因此,迫切需要在t2Dm中干预心血管并发症.本文中,设计了no供体和sglt2抑制剂的新杂种以获得抗高血糖和抗血栓形成的双重作用.如所预期的,优选的杂种2表现出中等的sglt2抑制作用和抗血小板聚集活性,并且在no清除剂的存在下也证实了其由no介导的抗血小板作用.此外,化合物2在小鼠的口服葡萄糖耐量试验中发现了显着的降血糖作用和尿葡萄糖排泄.潜在的多功能复合物(例如化合物2)有望作为干预t2Dm中心血管并发症的潜在候选药物.
Doi:10.1016/j.Bmc.2018.06.017

专利信息

专利号:US-9018249-B2
优先权日:2011-09-13
标题 :SGLT inhibitors
发明人：JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR
权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).

专利号:US-2014228303-A1
优先权日:2011-06-13
标题 :Novel sglt inhibitors
发明人：JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR
权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; NANDA GURMEET KAUR; THUNGATHURTHI SASTRY V R S; SINGH NISHAN; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of Formula I and methods of treating or preventing one or more conditions or diseases that may be regulated or normalized via inhibition of Sodium Glucose Cotransporter-2 (SGLT-2).