CAS: 4125-93-3; H-Asp-Otbu

该化合物是L-spartic酸的一种酯衍生物,一种在各种生物过程中具有关键作用的氨基酸,该化合物的特点是其叔丁基酯组,与母氨基酸相比,其脂质增加,其脂质与母氨基酸相对应,通常看起来像白色至白色的晶体固体,在有机溶剂中溶解,但在水中表现出有限的溶解性.该异丁基化合物组的存在可影响其再活动性和稳定性,使其在有机合成中有用,并成为制药和农用化学品生产的一个潜在中间体.此外,据了解,L-spartic酸衍生物参与代谢途径和...

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129460-09-9 134098-70-7 34582-32-6

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CAS号129460-09-9 芴甲氧羰基-L- 天冬氨酸-1-叔丁酯 | CAS号94347-11-2 L-天门冬氨酸-4-苄酯叔丁酯盐酸盐

合成工艺路线路线简述

    芴甲氧羰基-L-天冬氨酸-1-叔丁酯置于哌啶体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 0.33H,反应生成 L-天冬氨酸-1-叔丁酯
    参考文献:Conjugates For Cancer Therapy And Diagnosis
    标题:Conjugates For Cancer Therapy And Diagnosis
    摘要:本发明涉及药物与氨基酸或氨基酸衍生物或类似物的结合物,包括该结合物的药物组合物以及使用方法.具体来说,本发明涉及抗增殖药物与天冬氨酸,谷氨酸及其类似物的结合物作为治疗癌症的组合物,以及影像剂载体与氨基酸的结合物用于肿瘤和转移瘤的诊断.

    海关参考信息

    专利信息


    专利号:WO-0050448-A1
    优先权日:1999-02-26
    标 题 :A method for controlling an enzymatic reaction by the alpha and beta domains of metallothionein
    发明人:VALLEE BERT L; MARET WOLFGANG; FISCHER EDMOND H
    权利人:VALLEE BERT L; MARET WOLFGANG; FISCHER EDMOND H
    摘要:The present invention relates to the alpha and beta domains of metallothionein and analogs thereof, their synthesis, and methods for controlling in vitro and industrial enzymatic reactions using them. Purified metal-free and metal-containing alpha and beta domains of metallothionein and analogs thereof are provided as described below. A high yield method of synthesis and purification is also provided for the metal-free and metal containing alpha and beta domains of metallothionein and analogs thereof. Finally, methods for controlling in vitro and industrial enzymatic reactions are provided wherein the enzymatic processes are controlled by transfer or removal of a metal cation, to or from an enzyme metal-inhibitory site using the alpha and beta domains of metallothionein and analogs thereof.

    专利号:US-2008051323-A1
    优先权日:2004-08-21
    标 题 :Chloroquine drug compositions and methods for their synthesis
    发明人:KOSAK KENNETH M
    权利人:KOSAK KENNETH M
    摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. n The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

    专利号:US-2007060499-A1
    优先权日:2005-09-15
    标 题 :Chloroquine combination drugs and methods for their synthesis
    发明人:KOSAK KENNETH M
    权利人:KOSAK KENNETH M
    摘要:This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

    专利号:US-2007166281-A1
    优先权日:2004-08-21
    标题 :Chloroquine coupled antibodies and other proteins with methods for their synthesis
    发明人:KOSAK KENNETH M
    权利人:KOSAK KENNETH M
    摘要:This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing the drug for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and antibody or insulin to their site of action.

    专利号:WO-2024222082-A1
    优先权日:2023-04-28
    标 题 :Amino acid-derived ceramide, synthesis method therefor and use thereof
    发明人:YANG CHAOWEN; YE LIU; LIU LIANGXIAN
    权利人:SHENZHEN DIKEMAN BIOTECHNOLOGY CO LTD
    摘要:An amino acid-derived ceramide, having a structure of general formula I or an isomer of general formula I: (I), wherein M is R 3 or (II), and the R 1 is a residue after condensation of a polypeptide; the R 3 is selected from alanine, threonine, proline, asparagine, glutamine, leucine, tryptophan, serine, valine, methionine, tyrosine, histidine, L-aspartic acid-4-tert-butyl ester, L-aspartic acid-1-tert-butyl ester, glycine, isoleucine, phenylalanine, lysine, arginine, cysteine, L-glutamic acid-5-tert-butyl ester, L-glutamic acid-1-tert-butyl ester, or a residue after condensation of a polypeptide; the polypeptide is formed by condensation of 2-10 amino acids; R 2 is selected from one of the following structures: -C 15 H 29 , -C 15 H 31 , -C 15 H 27 , -CHOHC 14 H 27 , and -CHOHC 14 H 29 . The compound exhibits excellent effects in moisturizing, anti-oxidation, anti-glycation, skin barrier repair, tissue healing, etc.

    专利号:US-12144874-B2
    优先权日:2015-09-09
    标题 :Synthesis and composition of photodynamic therapeutic agents for the targeted treatment of cancer
    发明人:KULARATNE SUMITH A; GAGARE PRAVIN
    权利人:ON TARGET LABORATORIES LLC; ON TARGET LABORATORIES INC
    摘要:The present invention describes new compounds that are useful for image-guided surgery and photodynamic therapy. In particular the compounds may be targeted to the nucleus or the mitochondria after compounds were delivered to diseased tissues such as cancer using a ligand that target receptor that express on the diseased tissue and followed by receptor mediated endocytosis and provide effective activity against cancer cells as well as other disorders. Methods and compositions for use of the same are described.
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    合成参考文献


    参考文献:10.1007/s007750050335
    摘要:Muñoz A, Laib F, Petering DH, Shaw III CF. Characterization of the cadmium complex of peptide 49–61: a putative nucleation center for cadmium-induced folding in rabbit liver metallothionein IIA. JBIC Journal of Biological Inorganic Chemistry. 1999 Aug;4(4):495–507. doi: 10.1007/s007750050335.
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