CAS: 1093403-33-8; 4-Methyl-N-(2-(3-(Morpholinomethyl)Imidazo[2,1-B]Thiazol-6-yl)Phenyl)-2-(Pyridin-3-yl)Thiazole-5-Carboxamide

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4-methyl-2-pyridin-3-yl-thiazol-5-carboxylic acid chloride 2-(3-morpholin-4-ylmethyl-imidazo[2,1-b]thiazol-6-yl)-phenylamine 3-chloromethyl-6-(2-nitro-phenyl)-imidazo[2,1-b]thiazole (6-(2-nitrophenyl)imidazo[2,1-b]thiazol-3-yl)methanol

合成工艺路线路线简述

    📜3-羟基甲基-6-(2-硝基苯基)咪唑并[2,1-B]噻唑置于palladium On Activated Charcoal,氢气,三乙胺,Sodium Iodide体系中,化学反应生成玻玛西林
    参考文献:The Identification Of The Sirt1 Activator Srt2104 As A Clinical Candidate
    标题:The Identification Of The Sirt1 Activator Srt2104 As A Clinical Candidate
    摘要:我们发现 Srt2104 (4) 是首个直接合成的 Sirt1 激活剂临床候选药物.该化合物是通过优化之前描述的咪唑并[1,2-B]噻唑支架而得到的.Srt2104 是基于生化活性和药代动力学特征的综合考虑而被选为候选开发药物的.Srt2104 的体内特性优于具有类似活化特征的类似物.整体临床前研究结果表明,该化合物具有在临床环境中提供治疗益处的潜力.
    Doi:10.2174/15701808113100990021

    海关参考信息

    专利信息


    专利号:US-9376461-B2
    优先权日:2011-06-06
    标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof
    发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B
    权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC
    摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.

    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2015218202-A1
    优先权日:2011-06-06
    标 题:Non-enzymatic synthesis of o-acetyl-adp-ribose and analogues thereof

    专利号:WO-2012170494-A1
    优先权日:2011-06-06
    标题 :Non-enzymatic synthesis of o-acetyl-adp-ribose and analogues thereof

    专利号:US-2018230127-A1
    优先权日:2015-08-13
    标题 :Bicyclic-Fused Heteroaryl Or Aryl Compounds
    发明人:ANDERSON DAVID RANDOLPH; CURRAN KEVIN JOSEPH; GAVRIN LORI KRIM; GOLDBERG JOEL ADAM; LEE ARTHUR; LOWE MICHAEL DENNIS; PATNY AKSHAY; PIERCE BETSY SUSAN; SAIAH EDDINE; TRZUPEK JOHN DAVID
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds of Formula (Ia) are disclosed which are inhibitors of Interleukin-1 receptor associated kinase (IRAK4). Methods of treatment, methods of synthesis, and intermediates are also disclosed as defined in the specification.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Baksi A, Kraydashenko O, Zalevkaya A, Stets R, Elliott P, Haddad J, Hoffmann E, Vlasuk GP, Jacobson EW. A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes. Br J Clin Pharmacol. 2014 Jul;78(1):69-77. doi: 10.1111/bcp.12327.
    2: van der Meer AJ, Scicluna BP, Moerland PD, Lin J, Jacobson EW, Vlasuk GP, van der Poll T. The Selective Sirtuin 1 Activator SRT2104 Reduces Endotoxin-Induced Cytokine Release and Coagulation Activation in Humans. Crit Care Med. 2015 Jun;43(6):e199-202. doi: 10.1097/CCM.0000000000000949. doi: 10.1097/MIB.0000000000000597.
    4: Venkatasubramanian S, Noh RM, Daga S, Langrish JP, Joshi NV, Mills NL, Hoffmann E, Jacobson EW, Vlasuk GP, Waterhouse BR, Lang NN, Newby DE. Cardiovascular effects of a novel SIRT1 activator, SRT2104, in otherwise healthy cigarette smokers. J Am Heart Assoc. 2013 Jun 14;2(3):e000042. doi: 10.1161/JAHA.113.000042.

    合成参考文献


    摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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