CAS: 63001-30-9; Methyl 6-Oxo-1,6-Dihydropyridazine-3-Carboxylate

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933734-91-9 1591827-38-1 74173-58-3

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CAS号89532-94-5 methyl 6-oxo-1,... | CAS号67-56-1 甲醇 | CAS号37972-69-3 6-羟基-3-哒嗪甲酸 | CAS号65202-50-8 6-氯哒嗪-3-甲酸甲酯 | CAS号103854-71-3 1-丁基-6-氧代-1,6-二...

📜Methyl 6-Oxo-1,4,5,6-Tetrahydropyridazine-3-Carboxylate置于吡啶,Manganese(Iv) Oxide体系中,用 甲苯 作为反应溶剂,化学反应 6.0H,以58%的收率获得产物6-氧代-1,6-二氢哒嗪-3-甲酸甲酯
参考文献:脂肪酸酰胺水解酶α-酮杂环抑制剂中心杂环的优化.
标题:脂肪酸酰胺水解酶α-酮杂环抑制剂中心杂环的优化.
摘要:描述了基于恶唑 2 (Ol-135) 的一系列精制 α-酮杂环的合成和评估,其中包含在带有一组关键添加取代基的中心杂环中的系统变化.中心杂环的性质,即使在本文探讨的系统和轻微扰动中,也会显着影响抑制剂活性:1,3,4-恶二唑和 1,2,4-恶二唑 9 > 四唑,异构体 1,2,4-恶二唑 10,1,3,4-噻二唑 > 恶唑,包括 2 > 1,2-二嗪 > 噻唑 > 1,3,4-三唑.在这些趋势中最明显的是观测到在位置 4(恶唑编号,N > O > Ch)引入额外的杂原子会显着增加活性,这可能归因于 Faah 活性位点的不稳定空间相互作用减少.添加的显示明确趋势的杂环取代基可用于增强抑制剂效力,更重要的是增强抑制剂选择性.本文举例说明的这些趋势来自 Faah 活性的增强和对竞争性脱靶酶的结合亲和力的同时破坏.
DOI:10.1021/jm800136B

专利信息

专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人：ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.