(E)-N-tert-butyl-4-morpholin-4-ylbut-2-enamide

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: (E)-N-tert-butyl-4-morpholin-4-ylbut-2-enamide
• 化学式: C₁₂H₂₂N₂O₂
• 分子量: 226.32
• InChiKey: OIJQXVXWEBUWDA-SNAWJCMRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS<br/>[FR] COMPOSÉS POUR INHIBER LA PROLIFÉRATION CELLULAIRE DANS LES CANCERS INDUITS PAR L'EGFR
  申请人：ARIAD PHARMA INC

  公开号：WO2013169401A1

  公开（公告）日：2013-11-14

  The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.

  这项发明涉及化合物、药物组合物和治疗EGFR驱动的Formula (I)癌症患者的方法，其中变量如本文所定义。
• Substituted heterocyclyl derivatives as CDK inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US10689347B2

  公开（公告）日：2020-06-23

  The present invention provides substituted heterocyclylderivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.

  本发明提供了式(I)的取代杂环二烯丙基衍生物，它们具有治疗作用，特别是作为选择性转录CDK抑制剂，包括CDK7、CDK9、CDK12、CDK13和CDK18，更特别是转录CDK7抑制剂。这些化合物可用于治疗和预防哺乳动物中与选择性转录 CDK 相关的疾病和/或失调。本发明还提供了包含至少一种式（I）的取代杂环烷基衍生物或其药学上可接受的盐或立体异构体的化合物和药物制剂的制备方法。
• Pyrazolo[1,5-A][1,3,5]triazine and pyrazolo[1,5-A]pyrimidine derivatives as CDK inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US11186576B2

  公开（公告）日：2021-11-30

  The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1, R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.

  本发明提供了取代的式(I)吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物，它们具有治疗作用，特别是作为选择性转录 CDK 抑制剂，包括 CDK7、CDK9、CDK12、CDK13 和 CDK18，尤其是转录 CDK7 抑制剂 其中X、环A、环B、L1、L2、R1、R2、R3、R4、R6、m、n和p具有说明书中给出的含义，以及其药学上可接受的盐，可用于治疗和预防哺乳动物中与选择性转录CDK相关的疾病或紊乱。本发明还提供了包含至少一种式（I）的取代吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物或其药学上可接受的盐或其立体异构体的化合物和药物制剂的制备方法。
• Pyrazolo[1,5-A][1,3,5]Triazine and Pyrazolo[1,5-A]Pyrimidine Derivatives as CDK Inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US20180057497A1

  公开（公告）日：2018-03-01

  The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L 1 , L 2 , R 1 , R 2 , R 3 , R 4 , R 6 , m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
• Substituted Heterocyclyl Derivatives as CDK Inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US20180155293A1

  公开（公告）日：2018-06-07

  The present invention provides substituted heterocyclyl derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors. These compounds are useful in the treatment and prevention of diseases and/or disorders associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted heterocyclyl derivatives of formula (I) or a pharmaceutically acceptable salt or a stereoisomer thereof.