D-谷氨酸二苄基酯 | 47376-46-5

• 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
• 中文名称: D-谷氨酸二苄基酯
• 英文名称: D-glutamic acid dibenzyl ester
• 英文别名: dibenzyl L-glutamate；D-Glutaminsaeure-dibenzylester；Dibenzyl D-glutamate；dibenzyl (2R)-2-aminopentanedioate
• CAS: 47376-46-5
• 化学式: C₁₉H₂₁NO₄
• 分子量: 327.38
• InChiKey: DHQUQYYPAWHGAR-QGZVFWFLSA-N

物化性质

• 沸点：
  453.5±40.0 °C(Predicted)
• 密度：
  1.183±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  24
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  D-谷氨酸二苄基酯 在 palladium on activated charcoal 盐酸 、 氢气 、 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 甲醇 、 二氯甲烷 、 乙酸乙酯 为溶剂， 生成 H-Gly-D-Pro-D-Glu-OH
  参考文献：
  名称：

  Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure–activity relationships

  摘要：

  A series of GPE analogues, including modifications at the Pro and/or Glu residues, was prepared and evaluated for their NMDA binding and neuroprotective effects. Main results suggest that the pyrrolidine ring puckering of the Pro residue plays a key role in the biological responses, while the preference for cis or trans rotamers around the Gly-Pro peptide bond is not important. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.03.015
• 作为产物：
  描述：

  D-谷氨酸 、 苯甲醇 在 盐酸 作用下， 生成 D-谷氨酸二苄基酯
  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] PH 7 INJECTABLE SOLUTION COMPRISING AT LEAST ONE BASAL INSULIN OF WHICH THE PI IS FROM 5.8 TO 8.5 AND A CO-POLYAMINO ACID BEARING CARBOXYLATE CHARGES AND HYDROPHOBIC RADICALS AND A LIMITED AMOUNT OF M-CRESOL<br/>[FR] SOLUTION INJECTABLE DE PH 7 COMPRENANT AU MOINS UNE INSULINE BASALE À PI COMPRIS ENTRE 5,8 ET 8,5 ET UN ACIDE CO-POLYAMINO PORTANT DES CHARGES CARBOXYLATE ET DES RADICAUX HYDROPHOBES ET UNE QUANTITÉ LIMITÉE DE M-CRÉSOL
  申请人：ADOCIA

  公开号：WO2020115333A1

  公开（公告）日：2020-06-11

  The invention relates to physically stable compositions in the form of an injectable aqueous solution, the pH of which is from 6.0 to 8.0, comprising at least: a) a basal insulin whose isoelectric point (pI) is from 5.8 to 8.5, b) m-cresol in a concentration lower than or equal to 30 mM (0 < [m-cresol] ≤ 30 mM), and c) a co-polyamino acid bearing carboxylate charges and at least one Formula X hydrophobic radical.

  这项发明涉及一种物理稳定的组合物，其形式为可注射的水溶液，其pH值为6.0至8.0，包括至少：a) 一种碱性胰岛素，其等电点（pI）为5.8至8.5，b) 间甲酚的浓度低于或等于30毫摩尔（0 < [间甲酚] ≤ 30毫摩尔），以及c) 一种带有羧酸基团和至少一个X式疏水基团的共聚氨基酸。
• ANTIBODY DRUG CONJUGATES (ADCS) AND ANTIBODY PRODRUG CONJUGATES (APDCS) WITH ENZYMATICALLY CLEAVABLE GROUPS
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：US20180169256A1

  公开（公告）日：2018-06-21

  The present invention relates to novel binder-prodrug conjugates (APDCs) where binders are conjugated with inactive precursor compounds of kinesin spindle protein inhibitors, and to antibody-drug conjugates ADCs and to processes for producing these APDCs and ADCs.

  这项发明涉及新型结合物-前药偶联物（APDCs），其中结合物与动力蛋白纺锤体抑制剂的非活性前体化合物偶联，以及抗体药物偶联物ADCs以及制备这些APDCs和ADCs的方法。
• PRODRUGS OF CYTOTOXIC ACTIVE AGENTS HAVING ENZYMATICALLY CLEAVABLE GROUPS
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20190077752A1

  公开（公告）日：2019-03-14

  The invention relates to novel prodrugs or conjugates of the general formula (Ia) in which cytotoxic drugs, for example kinesin spindle protein inhibitors, are masked with legumain-cleavable groups and hence release the drug, and to the use of these prodrugs or conjugates for treatment and/or prevention of diseases, and to the use of these prodrugs or conjugates for production of medicaments for treatment and/or prevention of diseases, especially of hyperproliferative and/or angiogenic disorders, for example cancers.

  该发明涉及通式(Ia)的新型前药或结合物，其中细胞毒性药物，例如动力蛋白抑制剂，被腿蛋白酶可切割基团掩蔽，从而释放药物，并且涉及使用这些前药或结合物用于治疗和/或预防疾病，以及使用这些前药或结合物用于生产用于治疗和/或预防疾病的药物，特别是治疗和/或预防高增殖和/或血管生成异常的疾病，例如癌症。
• [EN] HETEROARYL(HETEROCYCLYL)METHANOL COMPOUNDS USEFUL IN THE TREATMENT OF HYPERGLYCAEMIA<br/>[FR] COMPOSÉS D'HÉTÉROARYL(HÉTÉROCYCLYL)MÉTHANOL UTILES DANS LE TRAITEMENT DE L'HYPERGLYCÉMIE
  申请人：ATROGI AB

  公开号：WO2020188299A1

  公开（公告）日：2020-09-24

  There is herein provided a compound of formula I (I) or a pharmaceutically acceptable salt thereof, wherein the ring comprising Q1 to Q5, R1, m, X1 and ring A have meanings as provided in the description.

  在此提供了一个式I（I）的化合物或其药用可接受的盐，其中包含Q1至Q5、R1、m、X1和环A的含义如描述中所提供。
• [EN] LIGANDS FOR METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] LIGANDS POUR RECEPTEURS METABOTROPES DU GLUTAMATE
  申请人：UNIV GEORGETOWN

  公开号：WO2000064911A1

  公开（公告）日：2000-11-02

  The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

  本发明涉及新型化合物及其配方，这些化合物是代谢型谷氨酸受体或NAALADase酶的配体，例如激动剂或拮抗剂。本发明还涉及使用本发明的化合物或配方调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在需要的主体中。本发明还涉及使用本发明的化合物或配方治疗患有慢性或急性疾病、病症或状况的主体的方法，其中该疾病、病症或状况至少部分由内源性代谢型谷氨酸受体或NAALADase酶的活性异常引起。