1-(5-(3,4-difluoro-2-(2-(1,3,5-trimethyl-1H-pyrazol-4-yl)ethoxy)phenyl)-1-methyl-1H-indazol-3-yl)-N,N-dimethylmethanamine | 2059148-82-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(5-(3,4-difluoro-2-(2-(1,3,5-trimethyl-1H-pyrazol-4-yl)ethoxy)phenyl)-1-methyl-1H-indazol-3-yl)-N,N-dimethylmethanamine
• 英文别名: Imp-1088；1-[5-[3,4-difluoro-2-[2-(1,3,5-trimethylpyrazol-4-yl)ethoxy]phenyl]-1-methylindazol-3-yl]-N,N-dimethylmethanamine
• CAS: 2059148-82-0
• 化学式: C₂₅H₂₉F₂N₅O
• 分子量: 453.535
• InChiKey: SOXNKJCQBRQUMS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  48.1
• 氢给体数：
  0
• 氢受体数：
  6

安全信息

• 危险性防范说明：
  P501,P270,P264,P280,P302+P352,P337+P313,P305+P351+P338,P362+P364,P332+P313,P301+P312+P330
• 危险性描述：
  H302,H315,H319

文献信息

• Compounds and their use as inhibitors of N-myristoyl transferase
  申请人：Imperial College Innovations Limited

  公开号：US10759804B2

  公开（公告）日：2020-09-01

  This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).

  本发明提供了式(I)化合物及其盐类，它们具有作为N-肉豆蔻酰转移酶(NMT)抑制剂的活性。本发明还涉及此类化合物作为药物的用途，特别是在治疗抑制 N-肉豆蔻酰基转移酶可提供治疗或预防效果的疾病或紊乱中的用途，包括原生动物感染（如疟疾和利什曼病）、病毒感染（如人类鼻病毒和 HIV）和过度增殖性紊乱（如 B 细胞淋巴瘤）。
• COMPOUNDS AND THEIR USE AS INHIBITORS OF N-MYRISTOYL TRANSFERASE
  申请人：Imperial College Innovations Limited

  公开号：EP3313833B1

  公开（公告）日：2021-01-06
• Compounds And Their Use As Inhibitors Of N-Myristoyl Transferase
  申请人：Imperial College Innovations Limited

  公开号：US20200339586A1

  公开（公告）日：2020-10-29

  This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).
• CANCER TREATMENTS
  申请人：IMPERIAL COLLEGE INNOVATIONS LIMITED

  公开号：US20220071960A1

  公开（公告）日：2022-03-10

  The present invention relates to the use of compounds which display activity as inhibitors of the human N-myristoyl transferases (NMT) in the treatment of MYC addicted cancers, such as, for example, cancers comprising MYC overexpression. The present invention also relates to the use of compounds which display activity as inhibitors of NMT, in combination with one or more other therapeutic agents, in the treatment of MYC addicted cancers and/or MYC dysregulated cancers.
• Novel compounds and their use in therapy
  申请人：Imperial College Innovations Limited

  公开号：US20220411431A1

  公开（公告）日：2022-12-29

  This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).