CAS: 110101-66-1; (8S,10S,13S,14S,16R,17S)-17-[2-[4-(2,6-Dipyrrolidin-1-Ylpyrimidin-4-yl)Piperazin-1-Yl]Acetyl]-10,13,16-Trimethyl-6,7,8,12,14,15,16,17-Octahydrocyclopenta[a]Phenanthren-3-One

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    4-(1-哌嗪)-2,6-双-(1-吡咯烷)-嘧啶 4-(1-Piperazinyl)-2,6-Di-1-Pyrrolidinylpyrimidine 111641-17-9

    合成工艺路线路线简述

      📜2,4-Di(1-Pyrrolidinyl)-6-Chloropyrimidine置于吡啶,Potassium Carbonate,Sodium Iodide体系中,用 乙腈 用作溶剂,化学反应 92.0H,反应生成替拉扎特
      参考文献:Novel 21-Aminosteroids That Inhibit Iron-Dependent Lipid Peroxidation And Protect Against Central Nervous System Trauma
      标题:Novel 21-Aminosteroids That Inhibit Iron-Dependent Lipid Peroxidation And Protect Against Central Nervous System Trauma
      摘要:A Novel Class Of 21-Aminosteroids Has Been Developed. Compounds Within This Series Are Potent Inhibitors Of Iron-Dependent Lipid Peroxidation In Rat Brain Homogenates With Ic50'S As Low As 3 Microm. Furthermore,Selected Members Enhance Early Neurological Recovery And Survival In A Mouse Head Injury Model. Significant Improvement In The 1 H Post-Head-Injury Neurological Status (Grip Test Score) By As Much As 168.6% Of The Control Has Been Observed. The Most Efficacious Compound In This Assay (30) Showed An Increase In The 1-Week Survival Of 78.6% As Compared To 27.3% For The Vehicle-Treated Mice In The Head-Injury Model. Based On Its Biological Profile,21-[4-(2,6-Di-1-Pyrrolidinyl-4-Pyrimidinyl)-1-Piperazinyl]-16 Alpha-Methylpregna-1,4,9(11)-Triene-3,20-Dione Monomethanesulfonate (30) Was Selected For Further Evaluation And Is Currently Entering Phase I Clinical Trials For The Treatment Of Head And Spinal Trauma.
      Doi:10.1021/jm00166A010

      海关参考信息

      专利信息


      专利号:US-6355416-B1
      优先权日:1997-02-14
      标 题:Assay for the measurement of DNA synthesis rates
      发明人:ABRAMSON FRED P
      权利人:UNIV GEORGE WASHINGTON
      摘要:Use of nonradioactive tracer technology used to measure DNA synthesis rates. DNA synthesis is determined by administering one or more stable isotope labelled precursors to one or more of DNA molecules and the amount of the stable isotope label in the DNA that is extracted from cells that are of interest is measured.

      专利号:WO-2023016817-A1
      优先权日:2021-08-12
      标 题:Synthesis of delta 9,11 steroids

      专利号:US-2024327451-A1
      优先权日:2021-08-12
      标 题:Synthesis of Delta 9,11 Steroids

      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).

      专利号:EP-4384529-A1
      优先权日:2021-08-12
      标题:Synthesis of delta 9,11 steroids

      专利号:CN-117858886-A
      优先权日:2021-08-12
      标题 :Synthesis of Δ9,11-steroids

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      ✅ COA系统入驻 | 共享模式

      合成参考文献


      参考文献:10.1097/00024382-199608000-00005
      摘要:McKenna R, Laskey RE, Wang Y, Jaeschke H, Mathews WR. Effect of endotoxin-enhanced hepatic reperfusion injury on endothelium-dependent relaxation in rat aorta. Shock. 1996 Aug;6(2):106–11. doi: 10.1097/00024382-199608000-00005.
      参考文献:10.1007/bf00182137
      摘要:Arora P, Lee YS, Origitano TC, Wurster RD. Lazaroids inhibit proliferation of cultured human astrocytoma cells. J Neurooncol. 1996 Aug;29(2):143–8. doi: 10.1007/bf00182137.
      参考文献:10.1203/00006450-199609000-00006
      摘要:Bågenholm R, Andiné P, Hagberg H. Effects of the 21-amino steroid tirilazad mesylate (U-74006F) on brain damage and edema after perinatal hypoxia-ischemia in the rat. Pediatr Res. 1996 Sep;40(3):399–403. doi: 10.1203/00006450-199609000-00006.
      参考文献:10.1089/neu.1996.13.465
      摘要:Mathew P, Bullock R, Teasdale G, McCulloch J. Changes in local microvascular permeability and in the effect of intervention with 21-aminosteroid (Tirilazad) in a new experimental model of focal cortical injury in the rat. J Neurotrauma. 1996 Aug;13(8):465–72. doi: 10.1089/neu.1996.13.465.
      参考文献:10.1097/00003246-199906000-00014
      摘要:Kimura RE, Beno DW. The effect of 21-aminosteroids on endotoxin-induced TNF-alpha release. Crit Care Med. 1999 Jun;27(6):1058–9. doi: 10.1097/00003246-199906000-00014.
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