2-(二乙基氨基)噻唑-5-甲醛 | 92940-24-4

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 2-(二乙基氨基)噻唑-5-甲醛
• 英文名称: 5-[N,N-bis(ethyl)amino]-1,4-thiazole-2-carboxaldehyde
• 英文别名: 2-diethylamino-5-formylthiazole；2-(diethylamino)-1,3-thiazole-5-carbaldehyde
• CAS: 92940-24-4
• 化学式: C₈H₁₂N₂OS
• mdl: MFCD01568828
• 分子量: 184.262
• InChiKey: KMNXYBHVYDCCNC-UHFFFAOYSA-N

物化性质

• 沸点：
  120°C/0.08mm
• 密度：
  1.190±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  61.4
• 氢给体数：
  0
• 氢受体数：
  4

安全信息

• 危险等级：
  IRRITANT
• 危险品标志：
  Xi
• 海关编码：
  2934100090

反应信息

• 作为反应物：
  描述：

  2-(二乙基氨基)噻唑-5-甲醛 在 正丁基锂 、 potassium tert-butylate 作用下， 生成 2-[[5-[(E)-2-[2-(diethylamino)-1,3-thiazol-5-yl]ethenyl]thiophen-2-yl]methylidene]propanedinitrile
  参考文献：
  名称：

  Synthesis of nonlinear optical chromophores containing electron-excessive and -deficient heterocyclic bridges. The auxiliary donor–acceptor effects

  摘要：

  合成了具有噻唑和噻吩环及夹杂乙烯单元作为π-共轭桥的推拉取代非线性光学染料。讨论了杂环的性质和位置对染料电荷转移跃迁能量的影响。

  DOI：

  10.1039/a708689j
• 作为产物：
  描述：

  2-氯噻唑 、 N,N-二乙基甲酰胺 在 正丁基锂 作用下， 生成 2-(二乙基氨基)噻唑-5-甲醛
  参考文献：
  名称：

  Sawhney, Indu; Wilson, John R. H., Journal of the Chemical Society. Perkin transactions I, 1990, # 2, p. 329 - 331

  摘要：

  DOI：

文献信息

• [EN] USE OF AND SOME NOVEL IMIDAZOPYRIDINES<br/>[FR] NOUVELLES IMIDAZOPYRIDINES ET LEUR UTILISATION
  申请人：ASTRAZENECA AB

  公开号：WO2004016611A1

  公开（公告）日：2004-02-26

  The use of compounds of formula (I) wherein R1, R3, R10, m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial is disclosed. Certain novel compounds of formula (I), together with processes for their preparation, compositions containing them and their use in therapy are also disclosed.

  公开了在制备药物用于治疗或预防抑制激酶Itk活性有益的疾病或症状中，使用式(I)中R1、R3、R10、m和Ar所定义的化合物及其药学上可接受的盐。还公开了式(I)的某些新化合物，以及它们的制备方法、含有它们的组合物和它们在治疗中的用途。
• Alkylidene pyrazolidinedione derivatives
  申请人：——

  公开号：US20040220188A1

  公开（公告）日：2004-11-04

  The present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) for the treatment and/or prevention of diabetes type I and/or II, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity and polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkylidene pyrazolidinedione derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel alkylidene pyrazolidinedione derivatives. (I) R1 and R2 represent independently from each other an unsubstituted or substituted aryl or heteroaryl. 1

  本发明涉及使用式(I)的烷基亚甲基吡唑啉二酮衍生物治疗和/或预防糖尿病I型和/或II型、糖耐量受损、胰岛素抵抗、高血糖、肥胖症和多囊卵巢综合症（PCOS）。特别是，本发明涉及使用式(I)的烷基亚甲基吡唑啉二酮衍生物调节，特别是抑制PTPs的活性，尤其是PTP1B、TC-PTP、SHP和GLEPP-1的活性。本发明还涉及新的烷基亚甲基吡唑啉二酮衍生物。(I)中，R1和R2各自独立地表示未取代或取代的芳基或杂环芳基。
• Use of and some novel imidazopyridines
  申请人：Johansson Henrik

  公开号：US20050261333A1

  公开（公告）日：2005-11-24

  The use of compounds of formula (I) wherein R 1 , R 3 , R 10 , m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or conditions in which inhibition of kinase Itk activity is beneficial is disclosed. Certain novel compounds of formula (I), together with processes for their preparation, compositions containing them and their use in therapy are also disclosed.

  本发明揭示了在制造用于治疗或预防抑制酪氨酸激酶Itk活性对疾病或病况有益的药物时，使用公式（I）中R1、R3、R10、m和Ar定义的化合物及其药学上可接受的盐。本发明还揭示了某些新型公式（I）化合物及其制备方法、含有它们的组合物以及它们在治疗中的应用。
• PYRROL-1-YL BENZOIC ACID DERIVATIVES USEFUL AS MYC INHIBITORS
  申请人：DANA-FARBER CANCER INSTITUTE, INC.

  公开号：US20150291521A1

  公开（公告）日：2015-10-15

  The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The present invention further provides methods of using the compounds described herein for treating Myc-mediated disorders (e.g., cancer and other proliferative diseases). The present invention also provides assays for identifying Myc inhibitors.

  本发明提供了公式(I-A)、(I-B)和(I-C)的化合物，其药学上可接受的盐以及其制药组合物。本发明的化合物可用于抑制Myc（例如c-Myc）的活性。本发明还提供了使用本文所描述的化合物治疗Myc介导的疾病（例如癌症和其他增殖性疾病）的方法。本发明还提供了用于鉴定Myc抑制剂的检测方法。
• Compositions and methods for treating neoplasia, inflammatory disease and other disorders
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US10407441B2

  公开（公告）日：2019-09-10

  The invention features compositions and methods for treating or preventing a neoplasia. More specifically, the invention provides compositions and methods for disrupting the interaction of a BET family polypeptide comprising a bromodomain with chromatin (e.g., disrupting a bromodomain interaction with an acetyl-lysine modification present on a histone N-terminal tail).

  本发明的特点是治疗或预防肿瘤的组合物和方法。 更具体地说，本发明提供了破坏包含溴多聚酶链的 BET 家族多肽与染色质相互作用的组合物和方法（例如，破坏溴多聚酶链与存在于组蛋白 N 端尾上的乙酰-赖氨酸修饰的相互作用）。