Nendratareotide Uzatansine | 1853254-97-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 肽模拟物
• 英文名称: Nendratareotide Uzatansine
• 英文别名: [(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[[(2R)-3-amino-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-oxopropyl]disulfanyl]propanoyl-methylamino]propanoate
• CAS: 1853254-97-3
• 化学式: C₈₃H₁₀₉ClN₁₄O₂₀S₄
• 分子量: 1786.6
• InChiKey: JVPMJFUBODFGNB-UFDFPQQFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  122
• 可旋转键数：
  28
• 环数：
  9.0
• sp3杂化的碳原子比例：
  0.49
• 拓扑面积：
  613
• 氢给体数：
  15
• 氢受体数：
  26

文献信息

• Targeted conjugates and particles and formulations thereof
  申请人：TARVEDA THERAPEUTICS, INC.

  公开号：US10624967B2

  公开（公告）日：2020-04-21

  Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

  现已设计出纳米颗粒和微颗粒及其药物制剂，其中含有通过连接体连接到靶向分子（如体生长抑素受体结合分子）的活性剂（如治疗剂、预防剂或诊断剂）的共轭物。这种纳米颗粒和微颗粒可改善活性剂的时间空间递送和/或生物分布。本文提供了共轭物、颗粒及其制剂的制造方法。还提供了向有需要的受试者施用制剂的方法，例如治疗或预防癌症或传染性疾病。
• SSTR-targeted conjugates and particles and formulations thereof
  申请人：TARVEDA THERAPEUTICS, INC.

  公开号：US11160871B2

  公开（公告）日：2021-11-02

  Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.

  目前已设计出通过连接体将 DM1 等活性剂与体泌素受体结合分子等靶向分子连接的共轭物，以及包含这种共轭物的微粒。这种共轭物和微粒可以改善活性剂的时间空间递送，改善生物分布和在肿瘤中的渗透，和/或降低毒性。本文提供了共轭物、颗粒及其制剂的制造方法。还提供了向有需要的受试者施用制剂的方法，例如治疗或预防癌症。
• TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
  申请人：Tarveda Therapeutics, Inc.

  公开号：US20170095569A1

  公开（公告）日：2017-04-06

  Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.
• SSTR-TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
  申请人：TARVEDA THERAPEUTICS, INC.

  公开号：US20180221499A1

  公开（公告）日：2018-08-09

  Conjugates of an active agent such as DM1 attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker, and particles comprising such conjugates have been designed. Such conjugates and particles can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.
• US9750818B2
  申请人：——

  公开号：US9750818B2

  公开（公告）日：2017-09-05