Glycine, glycylglycyl-L-phenylalanyl- | 200427-88-9

• 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: Glycine, glycylglycyl-L-phenylalanyl-
• 英文别名: 2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]acetic acid
• CAS: 200427-88-9
• 化学式: C₁₅H₂₀N₄O₅
• 分子量: 336.34
• InChiKey: HXUVTXPOZRFMOY-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.7
• 重原子数：
  24
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  151
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• [EN] ANTIFOLATE LINKER-DRUGS AND ANTIBODY-DRUG CONJUGATES<br/>[FR] MÉDICAMENTS LIEURS D'ANTIFOLATE ET CONJUGUÉS ANTICORPS-MÉDICAMENT
  申请人：BYONDIS BV

  公开号：WO2022008419A1

  公开（公告）日：2022-01-13

  The present invention relates to novel antifolate linker-drugs, conjugates comprising such antifolate linker-drugs, and the use thereof in the treatment of diseases, such as cancer, autoimmune and infectious diseases, optionally in combination with other therapeutic agents.

  本发明涉及新型抗叶酸连接剂药物，包括这种抗叶酸连接剂的共轭物，并将其用于治疗疾病，如癌症、自身免疫和传染病，可选择性地与其他治疗剂联合使用。
• Camptothecin derivatives
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP0757049A1

  公开（公告）日：1997-02-05

  A camptothecin derivative comprising a compound of the formula [I]: wherein R1 is a substituted or unsubstituted lower alkyl group, X1 is a group of the formula: -NHR2 (R2 is a hydrogen atom or a lower alkyl group) or a group of -OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.

  一种喜树碱衍生物，由式[I]化合物组成： 其中 R1 是取代或未取代的低级烷基，X1 是式中的基团：-NHR2（R2为氢原子或低级烷基）或-OH基团，Alk为直链或支链亚烷基，其链中可选择有一个氧原子，通过氨基酸或肽与具有羧基的多糖结合，或其药学上可接受的盐。与传统抗癌剂不同，上述喜树碱衍生物显示出更强的抗肿瘤活性，但副作用很小，因此，这些化合物作为药物非常有用。
• DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF
  申请人：DAIICHI PHARMACEUTICAL CO., LTD.

  公开号：EP1298145A1

  公开（公告）日：2003-04-02

  A DDS compound in which amino group at 1-position of (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]pyrano[3',4':6,7]-indolizino[1,2-b]quinoline-10,13(9H,15H)-dione as a drug compound is bound to a carboxyl group of a carboxymethyldextran polyalcohol with a spacer containing one amino acid or two to eight amino acids linked by peptide bond(s); characterized in that an introduced amount of residue of the drug compound is in a range of from 3.2% to 8.4% by weight; a weight-average molecular weight of the carboxymethyldextran polyalcohol is in a range of from 240,000 to 480,000; and degree of carboxymethylation is in a range of from 0.14 to 0.47; and a method for preparing said DDS compound, which comprises the steps of, for example, adding an aqueous solution containing sodium periodate to an aqueous solution containing dextran at a temperature of 4°C ± 2°C to oxidize the dextran, and then adding the resulting reaction mixture to an aqueous solution containing sodium borohydride at a temperature not higher than 15°C to obtain a dextran polyalcohol.

  一种 DDS 化合物，其中 (1S,9S)-1-氨基-9-乙基-5-氟-2,3-二氢-9-羟基-4-甲基-1H,12H-苯并[de]吡喃并[3',4'：6,7]-吲哚利嗪并[1,2-b]喹啉-10,13(9H,15H)-二酮作为药物化合物与羧甲基二葡聚糖多元醇的羧基结合，羧甲基二葡聚糖多元醇含有通过肽键连接的一个氨基酸或二至八个氨基酸的间隔物；其特征在于，药物化合物的引入残留量范围为3.2% 至 8.4% (按重量计)；羧甲基二葡聚糖多元醇的重量-平均分子量在 240,000 至 480,000 之间；羧甲基化程度在 0.14 至 0.47 之间；以及制备所述羧甲基二葡聚糖多元醇的方法。47；以及制备所述DDS化合物的方法，该方法包括以下步骤，例如，在4℃±2℃的温度下，将含有高碘酸钠的水溶液加入到含有葡聚糖的水溶液中，使葡聚糖氧化，然后在不高于15℃的温度下，将得到的反应混合物加入到含有硼氢化钠的水溶液中，得到葡聚糖多元醇。
• (ANTI-HER2 ANTIBODY)-DRUG CONJUGATE
  申请人：Daiichi Sankyo Co., Ltd.

  公开号：EP3130608A1

  公开（公告）日：2017-02-15

  As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L1-L2-LP-NH-(CH2)n1-La-Lb-Lc or -L1-L2-LP-wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the terminal Lc or LP with the nitrogen atom of the amino group at position 1 as the connecting position.

  作为一种抗肿瘤效果和安全性极佳且治疗效果极佳的抗肿瘤药物，本发明提供了一种抗体-药物共轭物，其中下式表示的抗肿瘤化合物通过具有下式表示的结构的连接体与抗 HER2 抗体共轭：L1-L2-LP-NH-(CH2)n1-La-Lb-Lc或-L1-L2-LP-其中，抗 HER2 抗体与末端 L1 连接，抗肿瘤化合物与末端 Lc 或 LP 连接，连接位置为 1 位氨基的氮原子。
• NOVEL CYCLIC DINUCLEOTIDE DERIVATIVE AND ANTIBODY-DRUG CONJUGATE THEREOF
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3848054A1

  公开（公告）日：2021-07-14

  Desired is development of novel CDN derivatives having STING agonist activity; and a therapeutic agents and/or therapeutic methods using the novel CDN derivatives for diseases associated with STING agonist activity. Further desired is development of a therapeutic agents and/or therapeutic methods capable of delivering the novel CDN derivatives specifically to targeted cells and organs for diseases associated with STING agonist activity. The present invention provides novel CDN derivatives having potent STING agonist activity, and antibody-CDN derivative conjugates including the novel CDN derivatives.

  希望开发出具有 STING 激动剂活性的新型 CDN 衍生物；以及使用新型 CDN 衍生物治疗与 STING 激动剂活性相关疾病的治疗剂和/或治疗方法。还希望开发一种治疗剂和/或治疗方法，能够将新型 CDN 衍生物特异性地输送到靶细胞和器官，以治疗与 STING 激动剂活性相关的疾病。本发明提供了具有强效 STING 激动剂活性的新型 CDN 衍生物，以及包括新型 CDN 衍生物的抗体-CDN 衍生物共轭物。