5-methylthieno[2,3-d]pyrimidine-4-amine | 13145-89-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: 5-methylthieno[2,3-d]pyrimidine-4-amine
• 英文别名: 4-Amino-5-methyl-thieno<2.3-d>pyrimidin；5-methyl-thieno[2,3-d]pyrimidin-4-ylamine；5-methylthieno[2,3-d]pyrimidin-4-amine
• CAS: 13145-89-6
• 化学式: C₇H₇N₃S
• 分子量: 165.219
• InChiKey: UNYNHNRSEFPIOV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  80
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-methylthieno[2,3-d]pyrimidine-4-amine 以 二苯醚 为溶剂， 生成 3-carbethoxy-4-oxo-9-methylthieno[3,2-e]pyrimido[1,2-c]pyrimidine
  参考文献：
  名称：

  Gould-Jacob Type of Reaction in the Synthesis of Thieno[3,2-e]pyrimido[1,2-c]pyrimidines: A Comparison of Classical Heating vs Solvent-Free Microwave Irradiation

  摘要：

  DOI：

  10.3987/com-99-8545
• 作为产物：
  描述：

  2-氨基-4-甲基噻吩-3-甲腈 、 原甲酸三乙酯 生成 5-methylthieno[2,3-d]pyrimidine-4-amine
  参考文献：
  名称：

  Heterocyclic synthesis from o-aminonitriles. XXIX. A new synthesis of 5-substituted pyrimidines

  摘要：

  DOI：

  10.1021/jo01283a003

文献信息

• 6,6-Bicyclic ring substituted sulfur containing heterobicyclic protein kinase inhibitors
  申请人：Ji Qun-Sheng

  公开号：US20070032512A1

  公开（公告）日：2007-02-08

  Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

  该式化合物及其药用可接受盐，其中X1、X2、X3和Q1的定义如本文所述，可抑制IGF-1R酶，并用于治疗和/或预防增生性疾病，如癌症、炎症、牛皮癣、过敏/哮喘、免疫系统疾病和病症以及中枢神经系统疾病和病症。
• AMINOPYRIMIDINE INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
  申请人：Borchardt Allen J.

  公开号：US20100063047A1

  公开（公告）日：2010-03-11

  The present invention relates to compounds and methods which may be useful as inhibitors of H 1 R and/or H 4 R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.

  本发明涉及化合物和方法，可能作为H1R和/或H4R的抑制剂用于治疗或预防炎症性、自身免疫性、过敏性和眼部疾病。
• CHEMICAL COMPOUNDS
  申请人：Axten Jeffrey Michael

  公开号：US20120077828A1

  公开（公告）日：2012-03-29

  The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R 1 , R 2 , and R 3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  本发明涉及取代的吲哚啉衍生物。具体而言，本发明涉及按式I所示的化合物：其中R1、R2和R3在此定义。本发明的化合物是PERK的抑制剂，可用于治疗癌症、眼部疾病和与激活的未折叠蛋白质应答途径相关的疾病，如阿尔茨海默病、中风、1型糖尿病帕金森病、亨廷顿病、肌萎缩性侧索硬化、心肌梗死、心血管疾病、动脉硬化和心律失常，更具体地，乳腺癌、结肠癌、胰腺癌和肺癌。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和治疗相关疾病的方法。
• PYRAZOLOPYRIMIDINE COMPOUNDS USEFUL AS RET INHIBITORS
  申请人：Cancer Research Technology Limited

  公开号：EP4105219A1

  公开（公告）日：2022-12-21

  The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X1, X2, X3, X4, R2, and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.

  本发明涉及作为 RET（转染过程中重排）激酶酶活性抑制剂的式 I 化合物： 其中HET、键a、b、c和d、X1、X2、X3、X4、R2和R3各自如本文所定义。本发明还涉及这些化合物的制备工艺、包含这些化合物的药物组合物，以及它们在治疗增殖性疾病（如癌症）和其他涉及 RET 激酶活性的疾病或病症中的用途。
• Ashok; Satish Goud; Shravani, Indian Journal of Heterocyclic Chemistry, 2010, vol. 20, # 2, p. 101 - 104
  作者：Ashok、Satish Goud、Shravani、Rajaiah、Sarasija、Bhaskar

  DOI：——

  日期：——