(2S,3S,5R,7R,9Z)-2,3,16-trihydroxy-18-methoxy-12-methyl-6,13-dioxatricyclo[13.4.0.05,7]nonadeca-1(15),9,16,18-tetraene-8,14-dione

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 大环内酯类和类似物
• 英文名称: (2S,3S,5R,7R,9Z)-2,3,16-trihydroxy-18-methoxy-12-methyl-6,13-dioxatricyclo[13.4.0.05,7]nonadeca-1(15),9,16,18-tetraene-8,14-dione
• 化学式: C₁₉H₂₂O₈
• 分子量: 378.4
• InChiKey: HDZUUVQEDFZKAX-NGAXKMIMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  27
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  126
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• Histone deacetylase inhibitors for the use in the treatment of drug resistant melanoma
  申请人：STICHTING HET NEDERLANDS KANKER INSTITUUT-ANTONI VAN LEEUWENHOEK ZIEKENHUIS

  公开号：US10864179B2

  公开（公告）日：2020-12-15

  The current invention relates to treatment of drug resistant melanoma with histone deacetylase inhibitors (HDACi). In particular the invention relates to BRAF and NRAS mutated melanoma and that have acquired resistance to MAPK pathway inhibitors, for example due to previous treatment with such MAPK pathway inhibitors. The invention discloses HDACi and/or MAPK pathway inhibitors for use in such treatment and treatment regimens using such inhibitors.

  本发明涉及用组蛋白去乙酰化酶抑制剂（HDACi）治疗耐药黑色素瘤。特别是本发明涉及BRAF和NRAS突变的黑色素瘤，以及对MAPK通路抑制剂产生耐药性的黑色素瘤，例如，由于以前使用过此类MAPK通路抑制剂治疗而产生耐药性的黑色素瘤。本发明公开了用于此类治疗的 HDACi 和/或 MAPK 通路抑制剂以及使用此类抑制剂的治疗方案。
• HISTONE DEACETYLASE INHIBITORS FOR THE USE IN THE TREATMENT OF DRUG RESISTANT MELANOMA
  申请人：Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis

  公开号：EP3355923A1

  公开（公告）日：2018-08-08
• HISTONE DEACETYLASE INHIBITORS FOR USE IN THE TREATMENT OF DRUG RESISTANT MELANOMA
  申请人：Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis

  公开号：EP3355923B1

  公开（公告）日：2022-02-23
• ROCK in Combination with MAPK Pathway
  申请人：STICHTING HET NEDERLANDS KANKER INSTITUUT

  公开号：US20160228451A1

  公开（公告）日：2016-08-11

  The current disclosure relates to pharmaceutical combinations and compositions useful in the treatment of certain types of cancer. The disclosure also relates to method of treatment these certain types of cancer. In particular, the disclosure relates to the combined use of inhibitors of ROCK and proteins of the MAPK/ERK-pathway in the treatment of KRAS-, NRAS- or BRAF-mutated cancer, in particular in NRAS mutated melanoma.
• METHOD FOR TREATING CANCER
  申请人：STICHTING HET NEDERLANDS KANKER INSTITUUT

  公开号：US20170027940A1

  公开（公告）日：2017-02-02

  The current disclosure relates to pharmaceutical combinations and compositions useful in the treatment of certain types of cancer. The disclosure also relates to methods for treatment of these types of cancer. In particular, the disclosure relates to the combined use of of an inhibitor of a protein of the MAPK/ERK pathway and an inhibitor of specific kinases in the treatment of a cancer, in particular melanoma, in a patient. In an important embodiment, the cancer is characterized by the absence or reduced expression of MITF.