CAS: 254740-64-2; 4'-((2-Butyl-4-Oxo-1,3-Diazaspiro[4.4]Non-1-En-3-yl)Methyl)-N-(4,5-Dimethylisoxazol-3-yl)-2'-(Ethoxymethyl)-[1,1'-Biphenyl]-2-Sulfonamide

上下游产品

4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl-N-](4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide 4-bromo-3-methylbenzonirtile 4-bromo-3-(bromomethyl)benzonitrile 4-bromo-3-(ethoxymethyl)benzaldehyde

4-溴-3-(溴甲基)苯甲腈置于盐酸,Sodium Tetrahydroborate,四(三苯基膦)钯,四溴化碳,Sodium Hydride,二异丁基氢化铝,Sodium Carbonate,三苯基膦体系中,用 四氢呋喃,甲醇,乙醇,正己烷,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 33.5H,反应生成4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺
参考文献:双重血管紧张素ii和内皮素a受体拮抗剂:2'-取代的n-3-异恶唑基联苯磺酰胺的合成,具有增强的药效和药代动力学.
标题:双重血管紧张素ii和内皮素a受体拮抗剂:2'-取代的n-3-异恶唑基联苯磺酰胺的合成,具有增强的药效和药代动力学.
摘要:在先前的报告中,我们证明了将at(1)受体拮抗剂(1,厄贝沙坦)中存在的关键结构元素与联苯磺酰胺et(a)受体拮抗剂(2)中的关键结构元素合并在一起,然后进行额外的优化,从而提供了化合物3一种双作用受体拮抗剂(dara),可有效阻断at(1)和et(a)受体.本文描述的是我们致力于改善3的药代动力学以及at(1)和et(a)受体效能的努力.我们的努力集中于修饰3的2'侧链和检查3中的异恶唑基磺酰胺部分这项工作导致了7作为高效第二代dara的发现.与3相比,化合物7还显示出显着改善的药代动力学特性.与单独使用dara 3或at(1)或et(a)受体拮抗剂相比,Dara 7可以更大程度和更长的持续时间降低静脉注射ang Ii或大et-1引起的血压升高.在正常的高血压shr模型中,化合物7以剂量依赖的方式清楚地显示了优于厄贝沙坦(一种at(1)受体拮抗剂)的优越性,表明在单个分子中at(1)和et(a)受体阻滞剂的协同作用.
Doi:10.1021/jm049548X

专利信息

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-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.

专利号:US-10316018-B2
优先权日:2015-08-27
标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
发明人：LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:CN-119775136-A
优先权日:2024-12-30
标 题 :Synthesis method of spasentan intermediate

专利号:CN-119462631-A
优先权日:2024-10-09
标题 :Sebasteine Synthesis method of intermediate