N-tert-butyl-4-propoxybenzamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-tert-butyl-4-propoxybenzamide
• 化学式: C₁₄H₂₁NO₂
• mdl: MFCD07129120
• 分子量: 235.32
• InChiKey: MYULXAOTWBHZEV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• Site-specific conjugation of linker drugs to antibodies and resulting ADCS
  申请人：Synthon Biopharmaceuticals B.V.

  公开号：US11136633B2

  公开（公告）日：2021-10-05

  The present invention relates to antibody-drug conjugates (ADCs) wherein a linker drug is site-specifically conjugated to an antibody through an engineered cysteine, and their use as a medicament, notably for the treatment of human solid tumours and haematological malignancies, in particular breast cancer, gastric cancer, colorectal cancer, urothelial cancer, ovarian cancer, uterine cancer, lung cancer, mesothelioma, liver cancer, pancreatic cancer, prostate cancer, and leukaemia.

  本发明涉及抗体-药物共轭物（ADCs），其中连接体药物通过工程半胱氨酸与抗体特异性连接，并涉及其作为药物的用途，特别是用于治疗人类实体瘤和血液恶性肿瘤，尤其是乳腺癌、胃癌、结直肠癌、尿道癌、卵巢癌、子宫癌、肺癌、间皮瘤、肝癌、胰腺癌、前列腺癌和白血病。
• Duocarmycin ADCs showing improved in vivo antitumor activity
  申请人：Byondis B.V.

  公开号：US11382982B2

  公开（公告）日：2022-07-12

  The present invention relates to duocarmycin-containing antibody-drug conjugates (ADCs) for use in the treatment of human solid tumours and haematological malignancies expressing HER2, in particular breast cancer, gastric cancer, bladder cancer, ovarian cancer, lung cancer, prostate cancer, pancreatic cancer, colorectal cancer, head and neck squamous cell cancer or osteosarcoma, and acute lymphoblastic leukaemia. In particular, the present invention relates to duocarmycin-containing ADCs for use in the treatment of human solid tumours with HER2 IHC 2+ or 1+ and HER2 FISH negative tissue status. Advantageously, the present invention relates to duocarmycin-containing ADCs for use in the treatment of triple negative breast cancer (TNBC).

  本发明涉及含杜卡霉素的抗体药物偶联物(ADCs)，用于治疗表达HER2的实体瘤和血液系统恶性肿瘤，尤其是乳腺癌、胃癌、膀胱癌、卵巢癌、肺癌、前列腺癌、胰腺癌、结直肠癌、头颈部鳞状细胞癌或骨肉瘤，以及急性淋巴细胞白血病。特别地，本发明涉及用于治疗HER2免疫组化(IHC)2+或1+且HER2荧光原位杂交(FISH)阴性肿瘤状态的人类实体瘤的含杜卡霉素的ADCs。更有利的是，本发明涉及用于治疗三阴性乳腺癌(TNBC)的含杜卡霉素的ADCs。
• UREA-BASED PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITORS FOR IMAGING AND THERAPY
  申请人：Five Eleven Pharma Inc.

  公开号：US20170189568A1

  公开（公告）日：2017-07-06

  The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [ 68 Ga]GaCl 3 with high yields and excellent radiochemical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.
• DUOCARMYCIN ADCS SHOWING IMPROVED IN VIVO ANTITUMOR ACTIVITY
  申请人：Synthon Biopharmaceuticals B.V.

  公开号：US20190314513A1

  公开（公告）日：2019-10-17

  The present invention relates to duocarmycin-containing antibody-drug conjugates (ADCs) for use in the treatment of human solid tumours and haematological malignancies expressing HER2, in particular breast cancer, gastric cancer, bladder cancer, ovarian cancer, lung cancer, prostate cancer, pancreatic cancer, colorectal cancer, head and neck squamous cell cancer or osteosarcoma, and acute lymphoblastic leukaemia. In particular, the present invention relates to duocarmycin-containing ADCs for use in the treatment of human solid tumours with HER2 IHC 2+ or 1+ and HER2 FISH negative tissue status. Advantageously, the present invention relates to duocarmycin-containing ADCs for use in the treatment of triple negative breast cancer (TNBC).
• ANTI-5T4 ANTIBODIES AND ANTIBODY-DRUG CONJUGATES
  申请人：Byondis B.V.

  公开号：US20210317231A1

  公开（公告）日：2021-10-14

  The present invention relates to antibodies against the human 5T4 oncofoetal antigen and corresponding antibody-drug conjugates that are suitable for testing in clinical trials. The antibodies are cross-reactive for humans and cynomolgus monkeys and exhibit an affinity for human 5T4 antigen which is in the same order of magnitude as their affinity for cynomolgus monkey 5T4 antigen. The invention further relates to the use of the antibodies and corresponding ADCs in the treatment of solid tumours and haematological malignancies.