2-Piperazinyl-4-methylamino-5-methylthieno(2,3-d)pyrimidine | 87479-20-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 2-Piperazinyl-4-methylamino-5-methylthieno(2,3-d)pyrimidine
• 英文别名: N,5-dimethyl-2-piperazin-1-ylthieno[2,3-d]pyrimidin-4-amine
• CAS: 87479-20-7
• 化学式: C₁₂H₁₇N₅S
• 分子量: 263.36
• InChiKey: JIZGLWMXPOCVEF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  81.3
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Thienopyrimidine derivatives, their preparation and their medical use
  申请人：SANKYO COMPANY LIMITED

  公开号：EP0082023A2

  公开（公告）日：1983-06-22

  Compounds of formula (I): [wherein R1 represents a variety of aliphatic diamino or triami- no groups, a 6- or 7- membered heterocyclic ring containing two nitrogens, one of which is optionally substituted or a tetrahydro-1,4-thiazin-4-yl group; R2 represents an optionally mono- or di- alkyl-substituted amino group, a mono- or di-(2-hydroxyethyl)-substituted amino group or an optionally mono- or di- alkyl-substituted aminoethylamino group; and R3 and R4 each represents hydrogen or C1-C4 alkyl or together represent tri- to penta- methylene] and salts thereof may be prepared by reacting an equivalent compound, but in which the groups R1 and R2 are replaced by leaving groups, with compounds R'H (in which free amino groups are optionally protected) and R2H. Various of the compounds have one or more of the following activities: hypoglycaemic activity; the ability to inhibit aggregation of blood platelets; hypotensive activity; or diuretic activity. They can be used in the treatment or prophylaxis of thrombosis, hyperglycaemia, hypertension or oedema and may be formulated as compositions with conventional pharmaceutical carriers or diluents.

  式(I)化合物： [其中 R1 代表各种脂肪族二氨基或三氨基、含有两个硝基（其中一个被任选取代）的 6-或 7-成员杂环或四氢-1,4-噻嗪-4-基；R2 代表任选的单-或二-烷基取代的氨基、单-或二-（2-羟乙基）取代的氨基或任选的单-或二-烷基取代的氨基乙氨基；R3和R4各自代表氢或C1-C4烷基，或共同代表三亚甲基至五亚甲基]及其盐类可通过将等效化合物（但其中基团R1和R2被离去基团取代）与化合物R'H（其中游离氨基可任选被保护）和R2H反应制备。这些化合物具有以下一种或多种活性：降血糖活性；抑制血小板聚集的能力；降血压活性；或利尿活性。它们可用于治疗或预防血栓形成、高血糖、高血压或水肿，并可与常规药物载体或稀释剂配制成组合物。