N-methyl-N'-[3-(2-guanidino-4-thiazolyl)-phenyl]-formamidine | 88541-12-2

• 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-N'-[3-(2-guanidino-4-thiazolyl)-phenyl]-formamidine
• 英文别名: N-[3-[2-(diaminomethylideneamino)-1,3-thiazol-4-yl]phenyl]-N'-methylmethanimidamide
• CAS: 88541-12-2
• 化学式: C₁₂H₁₄N₆S
• 分子量: 274.349
• InChiKey: MRTUBNJTWHQTJJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  130
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N-cyano-N'-[3-(2-guanidino-4-thiazolyl)-phenyl]-formamidine 在 甲胺 作用下， 以 水 为溶剂， 生成 N-methyl-N'-[3-(2-guanidino-4-thiazolyl)-phenyl]-formamidine
  参考文献：
  名称：

  Guanidino-heterocyclyl-phenyl-amidines and salts thereof

  摘要：

  具有互变式分子式##STR1##的化合物，其中R、R.sub.1和R.sub.2可以相同也可以不同，分别是氢或1至4个碳原子的烷基；R.sub.3是直链或支链烷基，可由氧、硫或氮等杂原子中断；直链或支链烯基；炔基；氰基；环烷基或环脂肪烷基；双环基团；芳基；或杂环基团；或R.sub.2和R.sub.3与彼此及它们连接的氮原子一起形成杂环基团；R.sub.4是氢、卤素、1至4个碳原子的烷基或1至4个碳原子的烷氧基；Het是含有两个或三个杂原子的取代或未取代杂环；其互变体，以及非毒性、药理学上可接受的酸盐。这些化合物及其盐可用作抗溃疡剂。

  公开号：

  US04548944A1

文献信息

• Guanidino heterocyclicphenylamidines, processes for their preparation and their pharmaceutical use
  申请人：ISTITUTO DE ANGELI S.p.A.

  公开号：EP0089730A2

  公开（公告）日：1983-09-28

  The object of the present invention are new pharmacologically active substituted guanidino heterocyclicphenylami- dines of the following formula in which R, R, and R2 which may be the same or different, each represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R3 represents a linear or branched alkyl group containing optionally heteroatoms such as oxygen, sulfur or nitrogen atom, a linear or branched alkenyl group, an alkynyl group, a cyano group, a cycloalkyl or cycloaliphatic alkyl group, a bicyclic group, an aryl group, a heterocyclic group or R3 and R2 together with the adjacent nitrogen atom represent a heterocyclic group, R4 represents a hydrogen atom, an alkyl or alkoxy group having 1 to 4 carbon atoms or a halogen atom, Het represents a substituted or unsubstituted heterocyclic group containing two or three heteroatoms and tautomers thereof and acid addition salts of the aforesaid compound. Processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also object of this invention. The new compounds are H2- receptor blocking agents which inhibit gastric acid secretion, and are useful antiulcer agents.

  本发明的目的是下式的具有药理活性的新的取代胍基杂环苯胺类化合物 其中 R、R 和 R2 可以相同或不同，各自代表氢原子或具有 1 至 4 个碳原子的烷基，R3 代表含有氧原子、硫原子或氮原子等杂原子的直链或支链烷基、直链或支链烯基、炔基、氰基、环烷基或环脂族烷基、双环基、芳基、杂环基、R3和R2连同邻近的氮原子代表杂环基团，R4代表氢原子、具有1至4个碳原子的烷基或烷氧基或卤素原子，Het代表含有两个或三个杂原子的取代或未取代的杂环基团及其同系物和上述化合物的酸加成盐。制备式（I）化合物以及含有它们的药物组合物的工艺也是本发明的目的。新化合物是 H2- 受体阻断剂，可抑制胃酸分泌，是有用的抗溃疡剂。
• Histamine and CCK2/gastrin receptor blockade in the treatment of acid-peptic disease and cancer
  申请人：Wang C. Timothy

  公开号：US20050042283A1

  公开（公告）日：2005-02-24

  The present invention relates to methods useful for treating or preventing gastrointestinal disorders. More specifically, the invention relates to methods for the treatment and prevention of acid reflux disease (GERD), peptic ulcer disease, dyspepsia, gastritis, and pre-malignant and malignant disease of the stomach.

  本发明涉及治疗或预防胃肠道疾病的方法。更具体地说，本发明涉及治疗和预防胃酸反流病（GERD）、消化性溃疡病、消化不良、胃炎以及胃的恶性和恶性前期疾病的方法。
• Promoting whole body health
  申请人：Doyle Joseph Matthew

  公开号：US20060193790A1

  公开（公告）日：2006-08-31

  The present invention relates to promoting whole body health in humans and animals by using topical oral compositions comprising a safe and effective amount of a host-response modulating agent in admixture with a pharmaceutically acceptable carrier, said compositions being effective in mediating host reaction to the presence of periodontal pathogens in the oral cavity as well as the toxins and endotoxins released by these pathogens and the inflammatory cytokines and mediators prompted by these oral pathogens.

  本发明涉及通过使用局部口服组合物促进人类和动物的全身健康，所述组合物包含安全有效量的宿主反应调节剂，并与药学上可接受的载体混合，所述组合物能有效调节宿主对口腔中存在的牙周病原体以及这些病原体释放的毒素和内毒素以及这些口腔病原体引发的炎症细胞因子和介质的反应。
• ORAL COMPOSITIONS COMPRISING HOST-RESPONSE MODULATING AGENT
  申请人：The Procter & Gamble Company

  公开号：EP1294367A2

  公开（公告）日：2003-03-26
• US4548944A
  申请人：——

  公开号：US4548944A

  公开（公告）日：1985-10-22