N-L-alanyl-D-glutamic acid | 16809-27-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-L-alanyl-D-glutamic acid
• 英文别名: N-L-Alanyl-D-glutaminsaeure；L-Alanyl=>D-glutaminsaeure；L-alanyl-D-glutamic acid；(2R)-2-[[(2S)-2-aminopropanoyl]amino]pentanedioic acid
• CAS: 16809-27-1
• 化学式: C₈H₁₄N₂O₅
• 分子量: 218.21
• InChiKey: VYZAGTDAHUIRQA-CRCLSJGQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.8
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  130
• 氢给体数：
  4
• 氢受体数：
  6

安全信息

• 海关编码：
  2924199090

反应信息

• 作为反应物：
  描述：

  N-L-alanyl-D-glutamic acid 在 N-甲基吗啉 、 N-羟基丁二酰亚胺 、 溶剂黄146 、 N,N'-二环己基碳二亚胺 作用下， 反应 27.5h， 生成 (R)-2-{(S)-2-[(R)-2-((2R,3R,4R,5S,6R)-3-Acetylamino-5-hydroxy-6-hydroxymethyl-2-phenoxy-tetrahydro-pyran-4-yloxy)-propionylamino]-propionylamino}-pentanedioic acid didodecyl ester
  参考文献：
  名称：

  Synthesis of lipophilic diesters of N-acetylmuramoyl-L-alanyl-D-glutamic acid

  摘要：

  DOI：

  10.1007/bf00629840
• 作为产物：
  描述：

  L-Alanyl-D-glutamic acid dibenzyl ester 在 钯 、 溶剂黄146 作用下， 生成 N-L-alanyl-D-glutamic acid
  参考文献：
  名称：

  Optical Rotation of Peptides. VII. α- and γ- Dipeptides of Glutamic Acid and Alanine¹

  摘要：

  DOI：

  10.1021/ja01114a528

文献信息

• [EN] CONJUGATES OF PROTEIN DRUGS AND P/A PEPTIDES<br/>[FR] CONJUGUÉS DE MÉDICAMENTS PROTÉIQUES ET DE PEPTIDES P/A
  申请人：XL PROTEIN GMBH

  公开号：WO2018234455A1

  公开（公告）日：2018-12-27

  The present invention relates to conjugates of a protein drug and two or more P/A peptides, and pharmaceutical compositions comprising them. The conjugates of the invention exhibit an advantageously reduced immunogenicity as compared to the respective unmasked protein drugs as well as a favorable safety and tolerability profile, which render them particularly suitable for therapeutic use. The conjugates further show an enhanced plasma half-life and, thus, a prolonged duration of action as compared to the respective unmasked protein drugs, which allows for a reduction in the dosing frequency and, thus, side-effect burden. The invention also provides processes of preparing such conjugates as well as activated P/A peptides that are useful as synthetic intermediates in the preparation of the conjugates.

  本发明涉及一种蛋白药物和两个或更多P/A肽的共轭物，以及包含它们的制药组合物。本发明的共轭物与相应的未掩蔽蛋白药物相比具有明显降低的免疫原性，以及良好的安全性和耐受性，使它们特别适用于治疗用途。这些共轭物还表现出增强的血浆半衰期和因此延长的作用时间，相比未掩蔽的蛋白药物，这使得减少给药频率和副作用负担成为可能。本发明还提供了制备这种共轭物的方法，以及用作合成中间体的活化P/A肽。
• Glucosaminyl muramyl peptide derivatives
  申请人：Dainippon Pharmaceutical Co., Ltd.

  公开号：EP0094804A1

  公开（公告）日：1983-11-23

  Novel glucosaminyl muramyl peptide derivatives of the formula: wherein X is hydrogen atom or a group of the formula: R1CO-, Y is hydroxy group or a group of the formula: -OR2, or R, is an alkyl or alkenyl group, R2 is a lower alkyl group or a phenylalkyl group, R3 and r4 are the same or different and are each hydrogen atom or an alkyl group, Y' is hydroxy group or a group of the formula: -OR2 or (D) and (L) mean the configuration, provided that when X is hydrogen atom, Y is a group of the formula: or and their pharmaceutically acceptable salts. They have excellent biological activities such as potentiating activity of nonspecific resistance to microbial infections and immunostimulant activity and hence are useful in the prophylaxis and treatment of various microbial infections and the treatment of cancer in mammals.

  式中的新型葡糖胺基 muramyl 肽衍生物： 其中 X 是氢原子或式中的一个基团：R1CO-，Y 是羟基或式中的基团：-OR2、 或 R，是烷基或烯基，R2 是低级烷基或苯基烷基，R3 和 r4 相同或不同且各自是氢原子或烷基，Y' 是羟基或式中的基团：-OR2或 (D)和(L)指构型，条件是当 X 为氢原子时，Y 为式中的基团： 或 及其药学上可接受的盐类。它们具有优异的生物活性，如增强对微生物感染的非特异性抵抗活性和免疫刺激活性，因此可用于预防和治疗各种微生物感染以及治疗哺乳动物的癌症。
• Composition for use in Mycobacteria vaccination
  申请人：Lysando Aktiengesellschaft

  公开号：EP2679232A1

  公开（公告）日：2014-01-01

  The present invention relates to a method for the preparation of a mycobacterial lysate comprising the steps of: a) contacting a sample comprising at least one Mycobacterium species with a composition having the activity of degrading the cell wall of a Mycobacterium species, b) incubating the sample for a distinct period, and c) isolating the mycobacterial lysate resulting from step b) thereby obtaining the mycobacterial lysate. Moreover, the present invention relates to the mycobacterial lysate obtained by the method of the present invention and further to a vaccine composition comprising the mycobacterial lysate, an antibody or antibody fragment generated with the mycobacterial lysate or the vaccine, and a pharmaceutical composition comprising the antibody or antibody fragment.

  本发明涉及一种制备分枝杆菌裂解物的方法，该方法包括以下步骤：a)将包含至少一种分枝杆菌的样品与具有降解分枝杆菌细胞壁活性的组合物接触；b)将样品培养一段时间；以及c)分离步骤b)产生的分枝杆菌裂解物，从而获得分枝杆菌裂解物。此外，本发明还涉及通过本发明方法获得的分枝杆菌裂解物，并进一步涉及包含分枝杆菌裂解物、用分枝杆菌裂解物或疫苗产生的抗体或抗体片段的疫苗组合物，以及包含抗体或抗体片段的药物组合物。
• Composition for use in Mycobacteria therapy
  申请人：Lysando Aktiengesellschaft

  公开号：EP2679677A1

  公开（公告）日：2014-01-01

  The present invention relates to a composition having the activity of degrading the cell wall of a Mycobacterium species. Moreover, the present invention relates in particular to said composition for use as a medicament, a disinfectant, a feed additive, or a food additive as well as the use of said composition in the treatment or prevention of diseases caused by an infection with a Mycobacterium species.

  本发明涉及一种具有降解分枝杆菌细胞壁活性的组合物。此外，本发明尤其涉及所述组合物可用作药物、消毒剂、饲料添加剂或食品添加剂，以及所述组合物可用于治疗或预防由分枝杆菌感染引起的疾病。
• METHOD OF REDUCING CONTAMINATION OF AN OBJECT WITH CLOSTRIDIUM
  申请人：Nomad Bioscience GmbH

  公开号：EP3372091A1

  公开（公告）日：2018-09-12

  The invention provides a method of preventing or reducing contamination of an object such as food or animal feed with Clostridium, comprising contacting said object with a composition comprising at least one endolysin active against said Clostridium.

  本发明提供了一种防止或减少梭状芽孢杆菌污染食品或动物饲料等物体的方法，包括将所述物体与含有至少一种对所述梭状芽孢杆菌有活性的内溶菌素的组合物接触。