1-benzyl 5-(tert-butyl) L-glutamate | 219121-63-8

• 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: 1-benzyl 5-(tert-butyl) L-glutamate
• 英文别名: 1-Benzyl 5-(tert-butyl) D-glutamate；1-O-benzyl 5-O-tert-butyl (2R)-2-aminopentanedioate
• CAS: 219121-63-8
• 化学式: C₁₆H₂₃NO₄
• 分子量: 293.363
• InChiKey: NIMSPPYFNNQHCP-CYBMUJFWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  21
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 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：

  1-benzyl 5-(tert-butyl) L-glutamate 在 palladium 10% on activated carbon 、 氢气 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 、 N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 生成 tert-butyl (S)-4-((2-((9H-fluoren-9-yl-methoxy)carbonyl)amino)acetyl)-(3-(4-(6aR,6bS,7S,8aS,8bS,10R,11aR,12aS,11a,12,12a,12b-dodecahydro-1H-naphtho[2,1:45]indeno[12-d][1,3]dioxol)pentanyl)amino)-5-oxopentanoate
  参考文献：
  名称：

  [EN] ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF
  [FR] ANTICORPS ANTI-VISTA HUMAINS ET UTILISATION ASSOCIÉE

  摘要：

  本发明提供了抗VISTA抗体药物偶联物，可用于针对免疫细胞（例如，髓系细胞）的靶向递送抗炎剂，例如类固醇。本发明还提供了在治疗炎症和/或自身免疫状况以及/或减轻抗炎剂（如类固醇）的毒性中使用抗VISTA抗体药物偶联物的方法。

  公开号：

  WO2021216913A1
• 作为产物：
  描述：

  N-芴甲氧羰基-D-谷氨酸 gamma-叔丁酯 在 4-二甲氨基吡啶 、 二乙胺 、 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 20.0h， 生成 1-benzyl 5-(tert-butyl) L-glutamate
  参考文献：
  名称：

  [EN] CYCLIC TREX1 INHIBITORS
  [FR] INHIBITEURS CYCLIQUES DE TREX1

  摘要：

  本发明提供了一种公式I的化合物，其中X，R1，R2，R3和R4如本文所定义。这些化合物有效地调节TREX1蛋白，并因此可用作治疗或预防受TREX1抑制影响的疾病的药物，例如癌症和病毒感染。

  公开号：

  WO2022075974A1

文献信息

• [EN] ANTIBODY DRUG CONJUGATES COMPRISING STING AGONISTS<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT COMPRENANT DES AGONISTES DE STING
  申请人：MERSANA THERAPEUTICS INC

  公开号：WO2021202984A1

  公开（公告）日：2021-10-07

  The present disclosure provides scaffolds and antibody-drug conjugates (ADCs) comprising a stimulator of interferon genes (STING). The present disclosure also provides uses of the ADCs in treatment, e.g., treatment of cancer.

  本公开提供了包含干扰素基因刺激剂（STING）的支架和抗体药物偶联物（ADCs）。本公开还提供了ADCs在治疗中的用途，例如癌症治疗。
• [EN] FATTY ACID-BIFUNCTIONAL DEGRADER CONJUGATES AND THEIR METHODS OF USE<br/>[FR] CONJUGUÉS DE DÉGRADATION BIFONCTIONNELS À BASE D'ACIDES GRAS ET LEURS PROCÉDÉS D'UTILISATION
  申请人：NOVARTIS AG

  公开号：WO2022189859A1

  公开（公告）日：2022-09-15

  Described herein are fatty acid-bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

  本文描述了脂肪酸双功能降解化合物、它们的各种靶标、它们的制备、含有它们的药物组合物以及它们在治疗由不同靶蛋白介导的疾病、病症和障碍中的应用。
• CYCLIC TREX1 INHIBITORS
  申请人：Venenum Biodesign, LLC

  公开号：US20210015829A1

  公开（公告）日：2021-01-21

  The present invention provides compounds of Formula I: wherein X, R 1 , R 2 , R 3 and R 4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.
• [EN] NOVEL STEROID PAYLOADS, STEROID LINKERS, ADCs CONTAINING AND USE THEREOF<br/>[FR] NOUVELLE CHARGE UTILE DE STÉROÏDE, LIEURS DE STÉROÏDES, CAM LES CONTENANT ET UTILISATION ASSOCIÉE
  申请人：[en]IMMUNEXT, INC.

  公开号：WO2022150637A1

  公开（公告）日：2022-07-14

  The invention provides novel glucocorticosteroids, glucocorticosteroid-linkers and antibody drug conjugates (ADC's) comprising an antibody or antibody fragment which binds to an antigen expressed on immune cells, optionally an antigen expressed on human immune cells. In some instances the ADCs comprise an anti-human VISTA (V-region Immunoglobulin-containing Suppressor of T cell Activation(1)) antibody or anti-VISTA antigen-binding antibody fragment which binds to VISTA expressing cells at physiologic pH having a short serum half-life (≈ 24-72 or 24-48 or 12-24 hours or less in a human VISTA knock-in rodent or ((≈ 1-3.5 days or less in a human or non-human primate). In some instances these ADCs have a rapid onset of action and are potent for prolonged duration as they are very effectively internalized by immune cells in large amounts where they are cleaved releasing large amounts of active steroid payload. The invention also relates to the use of such ADCs and novel steroids for the treatment of autoimmune, allergic and inflammatory conditions. The invention further relates to methods for reducing the adverse side effects and/or enhancing the efficacy of glucocorticoid receptor agonists by using such ADCs to selectively deliver these anti-inflammatory agents to target immune cells, such as monocytes, neutrophils, B cells, T cells, Tregs, eosinophils, NK cells, macrophages, myeloid cells, et al., and particularly myeloid cells, thereby reducing potential toxicity to non-target cells.