N-methyl-5-phenylthiazol-2-amine | 1344198-25-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-methyl-5-phenylthiazol-2-amine
• 英文别名: N-methyl-5-phenyl-1,3-thiazol-2-amine
• CAS: 1344198-25-9
• 化学式: C₁₀H₁₀N₂S
• mdl: MFCD17258258
• 分子量: 190.269
• InChiKey: LPNMADQKOPLFBG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  53.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  甲胺 、 2-溴-5-苯基噻唑 以 乙醇 为溶剂， 反应 16.0h， 以100%的产率得到N-methyl-5-phenylthiazol-2-amine
  参考文献：
  名称：

  [EN] NOVEL COMPOUNDS
  [FR] NOUVEAUX COMPOSÉS

  摘要：

  本发明涉及式（I）的新化合物和制造去泛素化酶（DUBs）抑制剂的方法。具体而言，本发明涉及抑制泛素C-末端水解酶30或泛素特异性肽酶30（USP30）。本发明还涉及在治疗涉及线粒体功能障碍和治疗癌症方面使用DUB抑制剂。

  公开号：

  WO2017141036A1

文献信息

• [EN] Novel Compounds<br/>[FR] NOUVEAUX COMPOSÉS
  申请人：MISSION THERAPEUTICS LTD

  公开号：WO2017103614A1

  公开（公告）日：2017-06-22

  The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C- terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.

  本发明涉及新型化合物和制备去泛素酶（DUBs）抑制剂的方法。具体而言，本发明涉及抑制泛素C-末端水解酶30或泛素特异性肽酶30（USP30）。本发明进一步涉及在治疗涉及线粒体功能障碍和癌症的疾病中使用DUB抑制剂。本发明的化合物包括具有以下式（I）的化合物：（I）或其药用可接受盐，其中R1a、R1b、R1c、R1d、R1e、R1f、R1g、R2、X、L和A如本文所定义。
• Compounds
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US10640498B2

  公开（公告）日：2020-05-05

  The present invention relates to novel compounds of formula (I) and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and in the treatment of cancer.

  本发明涉及式（I）的新型化合物和去泛素化酶（DUB）抑制剂的制造方法。特别是，本发明涉及泛素 C 端水解酶 30 或泛素特异性肽酶 30（USP30）的抑制。本发明进一步涉及 DUB 抑制剂在涉及线粒体功能障碍的疾病治疗和癌症治疗中的应用。
• Cyanopyrrolidines as dub inhibitors for the treatment of cancer
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US10669234B2

  公开（公告）日：2020-06-02

  The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein.

  本发明涉及新型化合物和去泛素化酶（DUB）抑制剂的制造方法。特别是，本发明涉及对泛素 C 端水解酶 L1（UCHL1）和泛素 C 端水解酶 30 或泛素特异性肽酶 30（USP30）的抑制。本发明进一步涉及 DUB 抑制剂在治疗癌症和涉及线粒体功能障碍的疾病中的用途。本发明的化合物包括具有式(I)的化合物或其药学上可接受的盐，其中R1、R2、R3、R4、R5、R6、R7、R8和R9如本文所定义。
• Cyanopyrrolidine derivatives with activity as inhibitors of USP30
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US11014912B2

  公开（公告）日：2021-05-25

  The present invention relates to substituted-cyanopyrrolidines of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction. (I)

  本发明涉及式(I)的取代-氰基吡咯烷，其具有作为去泛素化酶，特别是泛素C-末端水解酶30或泛素特异性肽酶30（USP30）的抑制剂的活性，可用于各种治疗领域，包括癌症和涉及线粒体功能障碍的疾病。(I)
• Cyano-substituted heterocycles with activity as inhibitors of USP30
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US11370784B2

  公开（公告）日：2022-06-28

  The present invention relates to cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction.

  本发明涉及式（I）的氰基取代的杂环化合物，其具有作为去泛素化酶（特别是泛素 C 端水解酶 30 或泛素特异性肽酶 30 (USP30)）抑制剂的活性，可用于各种治疗领域，包括癌症和涉及线粒体功能障碍的疾病。