2-Methylamino-3-chlor-6-amino-5-(N-guanyl-carbamoyl)-pyrazin | 1140-83-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-Methylamino-3-chlor-6-amino-5-(N-guanyl-carbamoyl)-pyrazin
• 英文别名: 3-amino-6-chloro-5-methylamino-pyrazine-2-carboxylic acid carbamimidoylamide；N-amidino-3-amino-5-methylamino-6-chloro-2-pyrazinecarboxamide；3-amino-N-carbamimidoyl-6-chloro-5-(methylamino)pyrazine-2-carboxamide
• CAS: 1140-83-6
• 化学式: C₇H₁₀ClN₇O
• 分子量: 243.656
• InChiKey: ASAIFKTZEMGZKR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  143
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• N-Pyrazinecarbonyl-N'-substituted-sulfamoyl-guanidine and processes for preparing same
  申请人：Merck & Co., Inc.

  公开号：EP0009054A1

  公开（公告）日：1980-04-02

  The case involves N-pyrazinecarbonyl-N'-substituted- sulfamoylguanidines and processes for making the same. The compounds are depicted in formular I. wherein R' is hydrogen, lower alkyl having from 1 to 5 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, lower alkenyl having from 2 to 3 carbon atoms; R2 is hydrogen, lower alkyl having from 1 to 5 carbon atoms; R1 and R2 can be joined to form, with the nitrogen atom to which they are attached, a heterocyclic ring having 3 to 6 carbon atoms therein; R2 is hydrogen, lower alkyl having from 1 to 5 carbon atoms; R4 is hydrogen, lower alkyl having from 1 to 5 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms; R5 is hydrogen, lower alkyl having from 1 to 5 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms; X is halo; and the pharmaceutically acceptable non-toxic acid addition salts thereof. The compounds are excellent eukalemic agents possessing diuretic and natriuretic properties.

  本案涉及 N-吡嗪羰基-N'-取代-氨基磺酰基胍类化合物及其制造工艺。这些化合物如式 I 所示。 其中 R'是氢 具有 1 至 5 个碳原子的低级烷基、具有 3 至 6 个碳原子的环烷基、具有 2 至 3 个碳原子的低级烯基； R2 是氢 具有 1 至 5 个碳原子的低级烷基； R1 和 R2 可以连接起来，与所连接的氮原子一起形成一个杂环，其中有 3 至 6 个碳原子； R2 是氢、 具有 1 至 5 个碳原子的低级烷基； R4 是氢 R4 是氢、具有 1 至 5 个碳原子的低级烷基、具有 3 至 6 个碳原子的环烷基； R5 是氢 R5 是氢、具有 1 至 5 个碳原子的低级烷基、具有 3 至 6 个碳原子的环烷基； X 是卤素； 及其药学上可接受的无毒酸加成盐。 这些化合物是具有利尿和利钠特性的优良白血病药物。
• AMINO ACID AND PEPTIDE CONJUGATES OF AMILORIDE AND METHODS OF USE THEREOF
  申请人：Gorin Fredric A.

  公开号：US20110195907A1

  公开（公告）日：2011-08-11

  The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the amiloride conjugates of the present invention for treating cancer or a central nervous system disease or disorder or for preventing or reducing ischemia-reperfusion injury. Further, kits are provided for the treatment of a central nervous system disease or disorder or for the prevention or reduction of ischemia-reperfusion injury using the amiloride conjugates of the present invention.
• INHIBITORS OF INTRACELLULAR UROKINASE PLASMINOGEN ACTIVATOR AND METHODS OF USE THEREOF
  申请人：Gorin Fredric A.

  公开号：US20120108494A1

  公开（公告）日：2012-05-03

  The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the compositions for treating cancer and for delivering an amiloride conjugate into cancer cells in a subject in need thereof.
• US4115573A
  申请人：——

  公开号：US4115573A

  公开（公告）日：1978-09-19
• US4140776A
  申请人：——

  公开号：US4140776A

  公开（公告）日：1979-02-20