CAS: 103878-84-8; Lazabemide

📜5-氯吡啶-2-羧酸置于氯化亚砜,N,N-二甲基甲酰胺体系中,用 二氯甲烷,水 用作溶剂,化学反应 8.0H,反应生成拉扎贝胺
参考文献:Lazabemide衍生物作为单胺氧化酶抑制剂的设计,合成和生物学评估
标题:Lazabemide衍生物作为单胺氧化酶抑制剂的设计,合成和生物学评估
摘要:在研究中,设计,合成和评估了一系列新的lazabemide衍生物作为单胺氧化酶(mao-A或mao-B)的抑制剂.这些化合物以拉沙贝米为先导化合物,并通过对烷基进行化合物的生物等排和修饰,对化学结构进行了修饰.通过对mao的抑制活性来筛选两种抑制剂(对mao-A的抑制和对mao-B的抑制).体外实验表明,化合物3A,3D和3F具有抑制mao-A生物学活性的强度,而化合物3I和3M具有强度抑制mao-B的生物学活性.从体外抑制活性实验的数据可以看出,化合物3D为ic 50 = 3.12+/-0.05μmol/ Ml的mao-A,化合物3M为ic 50 = 5.04+/-0.06μmol/ Ml.通过检测血浆和脑组织中5-Ht,Ne,Da的含量以及mao-A和mao-B的活性,进行体内抑制活性实验以评估化合物3A,3D,3F,3I和3M的抑制活性..体内抑制活性评估结果表明,化合物3A,3D,3F
Doi:10.1016/j.Bmc.2018.08.024

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2006194971-A1
优先权日:2005-02-24
标 题 :Anethole dithiolethione and other dithiolethiones for the treatment of conditions associated with dysfunction of monoamine neruotransmission
发明人：DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T
权利人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T
摘要:The present disclosure relates to dithiolethione derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The present disclosure also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the present disclosure specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) n nwherein the symbols have the meanings given in the specification.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-7354923-B2
优先权日:2001-08-10
标 题 :Piperazine melanocortin-specific compounds
发明人：SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
权利人:PALATIN TECHNOLOGIES INC
摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

专利号:WO-2009094569-A2
优先权日:2008-01-25
标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

专利号:US-2006014773-A1
优先权日:2001-04-19
标题:Mental agility lozenge, edible strip, food or drink
发明人：MCCLEARY EDWARD L
权利人:MCCLEARY EDWARD L
摘要:A mental agility composition is composed of at least one agent which promotes synthesis of ATP and/or creatine phosphate in the body; at least one antioxidant for scavenging free radicals in at least one pathway in the body; at least one agent for normalizing or maintaining membrane function and structure in the body; at least one agent for normalizing or maintaining normal neurotransmitter function in the body; at least one agent for down-regulating cortisol action; and at least one agent for suppressing activation of apoptotic pathways in the body. The composition may further contain one or more of at least one agent for suppressing inflammation in the body; at least one agent for normalizing or maintaining vascular wall function and structure in the body; at least one agent for normalizing or maintaining function of nerve growth factors and/or neurotropic factors in the body; at least one agent for suppressing toxic metal ionic effects; at least one agent for normalizing or maintaining methyl metabolism in the body; at least one agent for normalizing or maintaining metabolism of insulin and glucose in the body; and at least one agent for up-regulating activity of heat shock proteins in the body. The composition is administered in the form of a breath-care strip, mint or lozenge, or a food or beverage product.