(6aS,8E)-3-[[6-[[(6aS,8E)-8-ethylidene-2-methoxy-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxymethyl]-4-[2-[2-[2-[methyl-(2-methyl-2-sulfanylpropyl)amino]ethoxy]ethoxy]ethoxy]pyridin-2-yl]methoxy]-8-ethylidene-2-methoxy-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: (6aS,8E)-3-[[6-[[(6aS,8E)-8-ethylidene-2-methoxy-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxymethyl]-4-[2-[2-[2-[methyl-(2-methyl-2-sulfanylpropyl)amino]ethoxy]ethoxy]ethoxy]pyridin-2-yl]methoxy]-8-ethylidene-2-methoxy-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one
• 化学式: C₄₈H₆₀N₆O₉S
• 分子量: 897.1
• InChiKey: GHAHHZQWBSBRDA-KMFHRKABSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  64
• 可旋转键数：
  20
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  147
• 氢给体数：
  1
• 氢受体数：
  14

文献信息

• ANTI-LAMP1 ANTIBODIES AND ANTIBODY DRUG CONJUGATES, AND USES THEREOF
  申请人：Sanofi

  公开号：EP3400961A1

  公开（公告）日：2018-11-14

  Antibodies are provided which specifically bind human and Macaca fascicularis lysosomal-associated membrane protein 1 (LAMP1) proteins and immunoconjugates comprising said antibodies conjugated or linked to a growth inhibitory agent. Pharmaceutical compositions comprising antibodies or immunoconjugates of the invention and use of the antibodies or immunoconjugates for the treatment of cancer are also provided, as well as LAMP1 antibodies, isolated nucleic acids, vectors and host cells comprising a sequence encoding said antibodies and the use of said antibody as a diagnostic tool. The application further provides for the detection of LAMP1 gene amplification or gain in cancer cells leading to the determination if patients with cancer are likely to respond to anti-LAMP1 therapy. Therefore, it is proposed an in vitro method of selecting patients with cancer which comprises determining, in a biological sample of a patient with cancer which includes cancer cells, if said patient harbors a LAMP1 gene copy number gain; and selecting the patient based on the presence of LAMP1 gene copy number gain. Anti-LAMP1 therapeutic agent for use for treating cancer in a patient harboring LAMP1 gene copy number gain in cancer cells is further provided.

  本发明提供了特异性结合人和猕猴溶酶体相关膜蛋白1（LAMP1）蛋白的抗体，以及由上述抗体与生长抑制剂结合或连接的免疫结合剂。本申请还提供了包含本发明抗体或免疫结合剂的药物组合物和抗体或免疫结合剂治疗癌症的用途，以及 LAMP1 抗体、包含编码所述抗体序列的分离核酸、载体和宿主细胞和所述抗体作为诊断工具的用途。该申请还提供了检测癌细胞中 LAMP1 基因扩增或增殖的方法，从而确定癌症患者是否可能对抗 LAMP1 治疗产生反应。因此，提出了一种选择癌症患者的体外方法，该方法包括在癌症患者的生物样本（包括癌细胞）中确定所述患者是否携带 LAMP1 基因拷贝数增殖；以及根据 LAMP1 基因拷贝数增殖的存在选择患者。进一步提供了用于治疗在癌细胞中携带 LAMP1 基因拷贝数增殖的患者癌症的抗 LAMP1 治疗剂。
• US9809653B2
  申请人：——

  公开号：US9809653B2

  公开（公告）日：2017-11-07
• [EN] ANTI-LAMP1 ANTIBODIES AND ANTIBODY DRUG CONJUGATES, AND USES THEREOF<br/>[FR] ANTICORPS ANTI-LAMP1 ET CONJUGUÉS ANTICORPS MÉDICAMENT, ET UTILISATIONS ASSOCIÉES
  申请人：SANOFI SA

  公开号：WO2014102299A2

  公开（公告）日：2014-07-03

  Antibodies are provided which specifically bind human and Macaca fascicularis lysosomal-associated membrane protein 1 (LAMP1) proteins and immunoconjugates comprising said antibodies conjugated or linked to a growth inhibitory agent. Pharmaceutical compositions comprising antibodies or immunoconjugates of the invention and use of the antibodies or immunoconjugates for the treatment of cancer are also provided, as well as LAMP1 antibodies, isolated nucleic acids, vectors and host cells comprising a sequence encoding said antibodies and the use of said antibody as a diagnostic tool. The application further provides for the detection of LAMP1 gene amplification or gain in cancer cells leading to the determination if patients with cancer are likely to respond to anti-LAMP1 therapy. Therefore, it is proposed an in vitro method of selecting patients with cancer which comprises determining, in a biological sample of a patient with cancer which includes cancer cells, if said patient harbors a LAMP1 gene copy number gain; and selecting the patient based on the presence of LAMP1 gene copy number gain. Anti-LAMP1 therapeutic agent for use for treating cancer in a patient harboring LAMP1 gene copy number gain in cancer cells is further provided.