N-hydroxy-8-oxooctanamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-hydroxy-8-oxooctanamide
• 化学式: C₈H₁₅NO₃
• 分子量: 173.21
• InChiKey: SCHKJUBSUMJVDP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  12
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• SPECIFICALLY ACTIVATED MICROMOLECULAR TARGET COUPLING BODY IN TUMOR MICROENVIRONMENT AND USE THEREOF
  申请人：Yafei Shanghai Biolog Medicine Science& Technology

  公开号：EP3184540A1

  公开（公告）日：2017-06-28

  Provided are an anticancer compound comprising a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R1 is a normal functional group or a protection group; R2 is Ala, Thr, Val or Ile; R3 is Ala, Val or Asn; R4 is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R4H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.

  本发明提供了一种抗癌化合物及其用途，该化合物包含在肿瘤微环境中特异性激活的可裂解连接体。该抗癌化合物由下式表示，其中，R1为正常官能团或保护基；R2为Ala、Thr、Val或Ile；R3为Ala、Val或Asn；R4为通过羟基或氨基连接的药物基团；药物通式为R4H。该抗癌化合物仅在肿瘤局部被激活，从而避免了传统化疗药物对免疫系统损伤的缺陷，并通过清除肿瘤免疫抑制细胞促进肿瘤免疫。该抗癌化合物或其药物组合物与免疫疗法联合使用，可提高治疗肿瘤的效果，有效抑制肿瘤转移和骨转移。
• Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof
  申请人：Yafei Shanghai Biolog Medicine Science & Technology Co. Ltd.

  公开号：US10682371B2

  公开（公告）日：2020-06-16

  Provided is an anticancer compound including a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R1 is a normal functional group or a protection group; R2 is Ala, Thr, Val or Ile; R3 is Ala, Val or Asn; R4 is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R4H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.

  本发明提供了一种抗癌化合物（包括在肿瘤微环境中特异性激活的可裂解连接体）及其用途。该抗癌化合物由下式表示，其中，R1为正常官能团或保护基；R2为Ala、Thr、Val或Ile；R3为Ala、Val或Asn；R4为通过羟基或氨基连接的药物基团；药物通式为R4H。该抗癌化合物仅在肿瘤局部被激活，从而避免了传统化疗药物对免疫系统损伤的缺陷，并通过清除肿瘤免疫抑制细胞促进肿瘤免疫。该抗癌化合物或其药物组合物与免疫疗法联合使用，可提高治疗肿瘤的效果，有效抑制肿瘤转移和骨转移。
• [EN] SPECIFICALLY ACTIVATED MICROMOLECULAR TARGET COUPLING BODY IN TUMOR MICROENVIRONMENT AND USE THEREOF<br/>[FR] CORPS DE COUPLAGE À CIBLE MICROMOLÉCULAIRE ACTIVÉE DE MANIÈRE SPÉCIFIQUE DANS UN MICRO-ENVIRONNEMENT TUMORAL ET SON UTILISATION<br/>[ZH] 一种肿瘤微环境特异激活的小分子靶向偶联体及其用途
  申请人：YAFEI SHANGHAI BIOLOG MEDICINE SCIENCE & TECHNOLOGY CO LTD

  公开号：WO2016026458A1

  公开（公告）日：2016-02-25

  提供一种含有可在肿瘤微环境中特异激活的可分裂连接基团的抗癌化合物及其用途。所述抗癌化合物如下式所示，其中R 1为常规功能基团或保护基团；R 2为Ala、Thr、Val或Tle；R 3为Ala、Val或Asn；R 4为通过羟基或氨基连接的药物基团，该药物的通式为R 4H。所述抗癌化合物只在肿瘤局部激活，不但避免了传统化疗药物损伤免疫系统的缺陷，而且通过除去肿瘤免疫抑制性细胞来促进抗肿瘤免疫。该抗癌化合物或其药物组合物同免疫治疗联合使用，不仅增加了治愈肿瘤的效果，而且能有效抑制肿瘤转移和骨转移。
• ANTI-KIT ANTIBODIES AND USES THEREOF
  申请人：Celldex Therapeutics, Inc.

  公开号：EP2668210B1

  公开（公告）日：2020-06-17
• SMALL MOLECULE CONJUGATES SPECIFICALLY ACTIVATED IN TUMOR MICROENVIROMENT FOR TARGETING AND USE THEREOF
  申请人：Yafei Shanghai Biolog Medicine Science & Technolog Co., Ltd.

  公开号：US20170266308A1

  公开（公告）日：2017-09-21

  Provided is an anticancer compound including a cleavable linker specifically activated in a tumor microenvironment, and use thereof. The anticancer compound is represented by the following formula, wherein, R 1 is a normal functional group or a protection group; R 2 is Ala, Thr, Val or Ile; R 3 is Ala, Val or Asn; R 4 is a drug group linked via a hydroxyl group or an amino group; and the general formula of the drug is R 4 H. The anticancer compound is only activated at a local portion of a tumor, thus avoiding the defect of immune system damage of a traditional chemotherapeutic drug, and promoting tumor immunization by removing a tumor immunosuppression cell. The anticancer compound or pharmaceutical composition thereof is jointly used with immunotherapy, thus improving the effect of treating the tumor, and effectively inhibiting tumor metastasis and osseous metastasis.