ALG-DEBN-DEBOC | 1330063-52-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: ALG-DEBN-DEBOC
• 英文别名: N-[2-[2-[[6-amino-2-[(3-hydroxy-1-methyl-2-oxopyridine-4-carbonyl)amino]hexyl]-[2-[(3-hydroxy-1-methyl-2-oxopyridine-4-carbonyl)amino]ethyl]amino]ethyl-[2-[(3-hydroxy-1-methyl-2-oxopyridine-4-carbonyl)amino]ethyl]amino]ethyl]-3-hydroxy-1-methyl-2-oxopyridine-4-carboxamide
• CAS: 1330063-52-9
• 化学式: C₄₂H₅₇N₁₁O₁₂
• 分子量: 907.981
• InChiKey: GGWMVWOGNOYJBH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  65
• 可旋转键数：
  23
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  311
• 氢给体数：
  9
• 氢受体数：
  15

反应信息

• 作为反应物：
  描述：

  ALG-DEBN-DEBOC 、 对苯二异硫氰酸酯 以 氯仿 、 水 、 异丙醇 为溶剂， 反应 0.5h， 以26 mg的产率得到ALG-DD-NCS
  参考文献：
  名称：

  Alpha-emitting complexes

  摘要：

  本发明提供了一种组织靶向复合物，包括组织靶向基团、含有八齿羟基吡啶酮配体以及α放射性钍放射性核素离子。该发明还提供了利用这种复合物的治疗方法、其生产和使用方法，以及包含这种复合物的试剂盒和药物组合物。

  公开号：

  US09724436B2
• 作为产物：
  描述：

  ALG-DEBN 在 氨 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 0.83h， 以37 mg的产率得到ALG-DEBN-DEBOC
  参考文献：
  名称：

  Alpha-emitting complexes

  摘要：

  本发明提供了一种组织靶向复合物，包括组织靶向基团、含有八齿羟基吡啶酮配体以及α放射性钍放射性核素离子。该发明还提供了利用这种复合物的治疗方法、其生产和使用方法，以及包含这种复合物的试剂盒和药物组合物。

  公开号：

  US09724436B2

文献信息

• ALPHA-EMITTING COMPLEXES
  申请人：Ramdahl Thomas

  公开号：US20130183235A1

  公开（公告）日：2013-07-18

  The present invention provides a tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand and the ion of an alpha-emitting thorium radionuclide. The invention additionally provides therapeutic methods employing such complexes, methods of their production and use, and kits and pharmaceutical compositions comprising such complexes.

  本发明提供了一种组织靶向复合物，包括一个组织靶向基团、一个含有八齿羟基吡啶酮的配体和一个α放射性钍放射性核素的离子。此外，本发明还提供了使用这种复合物的治疗方法、其生产和使用方法，以及包含这种复合物的试剂盒和药物组合物。
• TARGETED ALPHA-PARTICLE EMITTING COMPLEXES COMPRISING THORIUM RADIONUCLIDE AND HYDROXYPYRIDINONE CONTAINING LIGAND
  申请人：Bayer AS

  公开号：EP2533817B1

  公开（公告）日：2018-03-28
• COMBINATION OF PI3K-INHIBITORS AND TARGETED THORIUM CONJUGATES
  申请人：Bayer AS

  公开号：US20210187134A1

  公开（公告）日：2021-06-24

  The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being a targeted thorium conjugate. Another aspect of the present invention relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of breast and prostate cancer.
• COMBINATION OF AR ANTAGONISTS AND TARGETED THORIUM CONJUGATES
  申请人：Bayer Aktiengesellschaft

  公开号：US20220118123A1

  公开（公告）日：2022-04-21

  The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.
• COMBINATION OF PD-1/PD-L1 INHIBITORS AND TARGETED THORIUM CONJUGATES
  申请人：Bayer Aktiengesellschaft

  公开号：US20220125960A1

  公开（公告）日：2022-04-28

  The present invention relates to combinations of at least two components, component A and component B, component A being a PD-1/PD-L1 inhibitor, and component B being a targeted thorium conjugate. Another aspect of the present invention relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of breast and prostate cancer.