CAS: 5011-34-7; 1-[(2,3,4-Trimethoxyphenyl)Methyl]Piperazine

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CAS号53531-01-4 曲美他嗪N-羧酸乙酯 | CAS号2103-57-3 2,3,4-三甲氧基苯甲醛

Tert-Butyl 4-(2,3,4-Trimethoxybenzyl)Piperazine-1-Carboxylate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,反应生成 曲美他嗪
参考文献:发现新型芹菜素-哌嗪杂合体作为有效的选择性聚(adp-核糖)聚合酶-1(parp-1)抑制剂用于治疗癌症
标题:发现新型芹菜素-哌嗪杂合体作为有效的选择性聚(adp-核糖)聚合酶-1(parp-1)抑制剂用于治疗癌症
摘要:聚(adp-核糖)聚合酶-1 (Parp-1) 是发现化学增敏剂和抗癌药物的潜在靶标.据报道,Amentoflavone (Amf) 是一种选择性 Parp-1 抑制剂.在这里,Amf的结构修饰和修剪分别产生了一系列amf衍生物 (9A-h) 和芹菜素-哌嗪/哌啶杂化物 (14A-p,15A-p,17A-h和19A-f).在这些化合物中,15L表现出有效的parp-1抑制作用(ic 50 = 14.7 Nm),并且对parp-1的选择性高于对parp-2的选择性(61.2倍).分子动力学模拟和细胞热位移测定表明15L直接与parp-1结构结合.在体外和体内研究中,15L对 A549 细胞显示出有效的化疗增敏作用,并通过 Parp-1 抑制对 Sk-Ov-3 细胞具有选择性细胞毒作用. 15L.2Hcl还表现出非常好的 Adme 特性,药代动力学参数和理想的安全裕度.
DOI:10.1021/acs.Jmedchem.1C00735

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-6472190-B1
优先权日:2000-03-16
标 题:Biocatalytic synthesis of galloid organics
发明人：FROST JOHN W
权利人:UNIV MICHIGAN STATE
摘要:The present invention provides a bioengineered synthesis scheme for the production of gallic acid from a carbon source. Methods of producing gallic acid from a carbon source based on the synthesis scheme are also provided. The gallic acid produces from these methods can be further converted to pyrogallol. Methods for the biosynthesis of pyrogallol from gallic acid are also provided.

专利号:US-12110275-B2
优先权日:2020-06-30
标题 :Methods of synthesizing 2-[4-[(2,3,4-trimethoxyphenyl)methyl] piperazin-1-yl]ethyl pyridine-3-carboxylate
发明人：BUCKLEY NEIL; BELMONT DAN; HAUSER BRYAN; KIM MYOUNG GOO; KANNAN KUMAR
权利人:IMBRIA PHARMACEUTICALS INC
摘要:The invention provides methods of chemical synthesis of the pharmacological agent 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethyl pyridine-3-carboxylate, also called CV-8972. The methods entail formation of a free base form of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin-1-yl]ethanol, also called CV-8814, as intermediate without producing a salt form of CV-8814.

专利号:US-6084097-A
优先权日:1997-10-20
标题:Methods for preparing 1-[4-arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl] propanes
发明人：SINHA NEELIMA; JAIN SANJAY; SAXENA ANIL KUMAR; ANAND NITYA; SAXENA RAM MOHAN; DUBEY MANGAL PRASAD; RAY MADHUR; PATNAIK GYANENDRA KUMAR
权利人:COUNCIL SCIENT IND RES
摘要:The invention relates to a process for the synthesis of 1-[4-Arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes used as potential therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders, having general formula 1 ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; a process of preparing said compounds and a method of treating hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders.

专利号:US-10814013-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications

专利号:WO-2022005928-A1
优先权日:2020-06-30
标 题:Crystal forms of 2-[4-[(2,3,4-trimethoxyphenyl)methyl]piperazin -1-yl]ethyl pyridine-3-carboxylate and methods of synthesis
发明人：BUCKLEY NEIL; BELMONT DAN; BETHUNE SARAH; DIAZ KRISTA; HAUSER BRYAN; KIM MYOUNG; KANNAN KUMAR
权利人:IMBRIA PHARMACEUTICALS INC
摘要:The invention provides polymorphs of a compound of Formula (X). The invention also provided pharmaceutical compositions containing polymorphs of the compound and methods treating conditions in a subject by providing polymorphs of the compound.