2,6-dimethyl-piperazine-1-carboxylic acid dimethylamide | 1464016-71-4

• 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: 2,6-dimethyl-piperazine-1-carboxylic acid dimethylamide
• 英文别名: N,N,2,6-tetramethylpiperazine-1-carboxamide
• CAS: 1464016-71-4
• 化学式: C₉H₁₉N₃O
• 分子量: 185.269
• InChiKey: XVVQGSOKJXQUNP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  35.6
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2,6-二甲基哌嗪 、 二甲氨基甲酰氯 在 碳酸氢钠 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以70%的产率得到2,6-dimethyl-piperazine-1-carboxylic acid dimethylamide
  参考文献：
  名称：

  Novel triazine compounds useful as sorbitol dehydrogenase inhibitors

  摘要：

  这项发明涉及到化合物的抑制山梨醇脱氢酶的公式I1，其中R1、R2和R3如规范中所定义。这项发明还涉及含有这些化合物的药物组合物，其抑制山梨醇脱氢酶，并通过向患有糖尿病且因此有发生这些并发症风险的哺乳动物施用这些化合物的方法来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病、糖尿病心肌病和足部溃疡。这项发明还涉及含有本发明公式I的化合物与第二药物剂的组合的药物组合物，包括醛糖还原酶抑制剂、钠氢离子交换（NHE-1）抑制剂、糖原磷酸化酶抑制剂（GPI）、选择性5-羟色胺再摄取抑制剂、3-羟基-3-甲基戊二酸辅酶A还原酶抑制剂、血管紧张素转换酶抑制剂、噻唑烷二酮抗糖尿病药物、血管紧张素II受体拮抗剂、γ-氨基丁酸（GABA）激动剂、磷酸二酯酶5抑制剂、腺苷激动剂和CETP抑制剂，以及使用这些组合组合物的方法。

  公开号：

  US20030004166A1

文献信息

• Triazine compounds useful as sorbitol dehydrogenase inhibitors
  申请人：Mylari Banavara L.

  公开号：US06894047B2

  公开（公告）日：2005-05-17

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of the present invention with a second pharmaceutical agent, including an aldose reductase inhibitor, a sodium hydrogen ion exchange inhibitor, a glycogen phosphorylase inhibitor, a selective serotonin reuptake inhibitor, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, an angiotensin converting enzyme inhibitor, a thiazolidinedione antidiabetic agent, an angiotensin II receptor antagonist, a γ-aminobutyric acid agonist, a phosphodiesterase type 5 inhibitor, an adenosine agonist, and a CETP inhibitor and to methods of using these compositions.

  本发明涉及式I的山梨醇脱氢酶抑制剂，其中R1、R2和R3如规范中所定义。本发明还涉及含有这些化合物的制药组合物以及治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病、糖尿病心肌病和足溃疡的方法。本发明还涉及一种制药组合物，其中包含本发明式I化合物与第二种药物制剂的组合，包括醛固酮还原酶抑制剂、钠氢离子交换抑制剂、糖原磷酸化酶抑制剂、选择性5-羟色胺再摄取抑制剂、3-羟基-3-甲基戊二酰辅酶A还原酶抑制剂、血管紧张素转换酶抑制剂、噻唑烷二酮类抗糖尿病药物、血管紧张素II受体拮抗剂、γ-氨基丁酸激动剂、磷酸二酯酶5抑制剂、腺苷酸激动剂和CETP抑制剂，以及使用这些组合物的方法。
• US6894047B2
  申请人：——

  公开号：US6894047B2

  公开（公告）日：2005-05-17
• Novel triazine compounds useful as sorbitol dehydrogenase inhibitors
  申请人：——

  公开号：US20030004166A1

  公开（公告）日：2003-01-02

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I 1 wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds which inhibit sorbitol dehydrogenase and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers, by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of the present invention with a second pharmaceutical agent, including an aldose reductase inhibitor, a sodium hydrogen ion exchange (NHE-1) inhibitor, a glycogen phosphorylase inhibitor (GPI), a selective serotonin reuptake inhibitor, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, an angiotensin converting enzyme inhibitor, a thiazolidinedione antidiabetic agent, an angiotensin 11 receptor antagonist, a &ggr;-aminobutyric acid (GABA) agonist, a phosphodiesterase type 5 inhibitor, an adenosine agonist, and a CETP inhibitor and to methods of using these combination compositions.

  这项发明涉及到化合物的抑制山梨醇脱氢酶的公式I1，其中R1、R2和R3如规范中所定义。这项发明还涉及含有这些化合物的药物组合物，其抑制山梨醇脱氢酶，并通过向患有糖尿病且因此有发生这些并发症风险的哺乳动物施用这些化合物的方法来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病、糖尿病心肌病和足部溃疡。这项发明还涉及含有本发明公式I的化合物与第二药物剂的组合的药物组合物，包括醛糖还原酶抑制剂、钠氢离子交换（NHE-1）抑制剂、糖原磷酸化酶抑制剂（GPI）、选择性5-羟色胺再摄取抑制剂、3-羟基-3-甲基戊二酸辅酶A还原酶抑制剂、血管紧张素转换酶抑制剂、噻唑烷二酮抗糖尿病药物、血管紧张素II受体拮抗剂、γ-氨基丁酸（GABA）激动剂、磷酸二酯酶5抑制剂、腺苷激动剂和CETP抑制剂，以及使用这些组合组合物的方法。