CAS: 721-50-6; 2-(Propylamino)-N-(O-Tolyl)Propanamide

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propylamine N-(2-methylphenyl)-2-chloropropanamide 2-chloropropionyl chloride o-toluidineo-toluidineL(+)-α-Propylamino-2-methyl-propioanilid D(-)-α-Propylamino-2-methyl-propioanilid 42H70O35*C13H20N2°C42H70O35*C13H20N2O pril°Caine hydr°Chloride

2,5-Dimethyl-1-Propyl-3-O-Tolyl-Imidazolidin-4-One; Hydrochloride 以 Phosphate Buffer,Acetate Buffer 作为反应溶剂,化学反应生成 丙胺卡因
参考文献:由丙胺卡因与甲醛和乙醛反应制得的4-咪唑啉酮前药类型的降解动力学.
标题:由丙胺卡因与甲醛和乙醛反应制得的4-咪唑啉酮前药类型的降解动力学.
摘要:通过将丙胺卡因(i)与甲醛和乙醛反应制得的4-咪唑啉酮前体类型的分解动力学已分别在ph范围为1-7.4的水溶液中于60和37摄氏度下进行了研究.在ph <5时,衍生自甲醛(II)的衍生物水解反应生成i的过程遵循明显的一级动力学.在较高的ph下,分解反应进行到平衡,并且该反应可以通过一阶和二阶可逆动力学来描述.ii相对于ph的水解的表观一级速率常数的对数图,导致了许多n-Mannich碱水解的s型ph速率分布特征.计算出化合物ii在ph 7.4(60oc)下6.9H的半衰期.与ii相比,衍生自乙醛(iii)的4-咪唑啉酮在水性缓冲溶液中显示出增强的不稳定性.在37oc下进行分解,监测完整(iii)浓度的降低.在酸性ph下,反应显示出严格的一级动力学,Iii的消失伴随着i的形成.在ph 7.4下,尽管观测到少量的iii是在ph 7.4下由含有等摩尔浓度的乙醛和丙胺卡因(10(-4)m)的溶液形成.如果
DOI:10.1016/s0928-0987(03)00198-2

专利信息

专利号:US-10022366-B2
优先权日:2013-04-23
标 题:Extending and maintaining micropore viability of microneedle treated skin with lipid biosynthesis inhibitors for sustained drug delivery
发明人：STINCHCOMB AUDRA L; GHOSH PRIYANKA
权利人:STINCHCOMB AUDRA L; GHOSH PRIYANKA; UNIV MARYLAND; UNIV KENTUCKY RES FOUND
摘要:Microneedles and their use as a physical skin permeation enhancement technique facilitate drug delivery across the skin in therapeutically relevant concentrations. Micropores created in the skin by MNs reseal because of normal healing processes of the skin, thus limiting the duration of the drug delivery window. Pore lifetime enhancement strategies can increase effectiveness of MNs as a drug delivery mechanism by prolonging the delivery window. Fluvastatin (FLU) was used to enhance pore lifetime by inhibiting the synthesis of cholesterol, a major component of the stratum corneum lipids. The skin recovered within a 30-45-min time period following the removal of occlusion, and there was no significant irritation observed due to the treatment compared to the control sites. Thus, it can be concluded that localized skin treatment with FLU can be used to extend micropore lifetime and deliver drugs for up to 7 days across MN-treated skin.

专利号:US-2023047214-A1
优先权日:2020-02-03
标题:Methods for microwave synthesis of degradable polymers for drug delivery
发明人：MURATOGLU ORHUN K; ORAL EBRU; GRINDY SCOTT
权利人:MASSACHUSETTS GEN HOSPITAL
摘要:Provided herein are methods of making degradable, additive-blended polymeric materials using microwave radiation and catalysts. The methods can include incorporation of therapeutic materials into the polymeric materials. There also are provided polymeric materials made by the methods and medical devices comprising the polymeric materials made by the methods.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-9023813-B2
优先权日:2011-04-13
标题:Synthesis and use of glycoside derivatives of propofol
发明人：SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN
权利人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN; NUTEK PHARMA LTD
摘要:The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.

专利号:US-2012295866-A1
优先权日:2011-04-13
标题:Synthesis And Use Of Glycoside Pro-Drug Analogs
发明人：SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN
权利人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN; NUTEK PHARMA LTD
摘要:The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug analogs. This invention relates to a method for the production of a broad group of glycosylated drugs, including but not limited to propofol, acetaminophen, and camptothecin carbohydrate derivatives.

专利号:US-2015352230-A1
优先权日:2013-01-11
标 题:Synthesis and isolation of dendrimer based imaging systems
发明人：MULLEN DOUGLAS GURNETT; BAKER JR JAMES R; BANASZAK HOLL MARK M; HUANG BAOHUA; DOUGHERTY CASEY; BALL JACK
权利人:UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis and isolation of antibodies conjugated with modular dendrimer nanoparticles. In particular, the present invention is directed to antibodies conjugated with novel modular dendrimer nanoparticles having precise numbers of imaging agents, methods of synthesizing the same, compositions comprising such antibodies conjugated with such modular dendrimer nanoparticles, as well as systems and methods utilizing the conjugates (e.g., in imaging settings) (e.g., in diagnostic and/or therapeutic settings) (e.g., for the delivery of therapeutics, imaging, and/or targeting agents).