8-amino-1,2,3,4-tetrahydro-1,4,6-trimethylpyrazino[2,3-d]pyridazin-5(6H)-one

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 8-amino-1,2,3,4-tetrahydro-1,4,6-trimethylpyrazino[2,3-d]pyridazin-5(6H)-one
• 英文别名: 8-amino-1,4,6-trimethyl-2,3-dihydropyrazino[2,3-d]pyridazin-5-one
• 化学式: C₉H₁₅N₅O
• 分子量: 209.251
• InChiKey: JFJAARXJCIPMHA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  65.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  6-氨基-4,5-二氯-2-甲基哒嗪-3-酮 、 N,N'-二甲基乙二胺 以 氯仿 、 水 为溶剂， 生成 8-amino-1,2,3,4-tetrahydro-1,4,6-trimethylpyrazino[2,3-d]pyridazin-5(6H)-one
  参考文献：
  名称：

  Chroman derivative and pharmaceutical use thereof

  摘要：

  本发明的化合物及其中医药学上可接受的盐具有选择性和优秀的心脏血管扩张作用，而且具有极其微弱的降压作用。因此，可以在不引起心动过速导致的有害心脏影响的突发性低血压的情况下，选择性地增加冠状动脉血流，并且它们作为心脏血管扩张剂特别有用，尤其是用于预防和治疗心绞痛和心力衰竭等心血管疾病的药物。

  公开号：

  US05719155A1

文献信息

• CHROMAN DERIVATIVE AND MEDICINAL USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：EP0677519A1

  公开（公告）日：1995-10-18

  A chroman derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and a medicinal use thereof, wherein R¹ is cyano, nitro, trihalomethyl, trihalomethoxy or halogen; R² is lower alkoxyalkyl, aryloxyalkyl or dialkoxyalkyl; R³ is lower alkoxyalkyl or aryloxyalkyl; R⁴ is hydroxy, formyloxy or lower alkanoyloxy; X is N-H which may be substituted by lower alkyl, oxygen, sulfur or a single bond; Y is a residue of an aromatic or heterocyclic ring which may be substituted. The compound and pharmaceutically acceptable salt thereof have a prominent selective coronary vasodilator activity while having a minimized hypotensive effect. Therefore, they can selectively increase the coronary blood flow volume without the fear of causing sudden hypotension causative of tachycardia which adversely affects the heart, and hence are useful as a coronary vasodilator, in particular, as a preventive or remedy for cardiovascular disturbance such as angina pectoris or cardiac failure.

  一种由通式(I)代表的色烷衍生物、其药学上可接受的盐及其药用方法，其中 R¹是氰基、硝基、三卤甲基、三卤甲氧基或卤素；R²是低级烷氧基烷基、芳氧基烷基或二烷氧基烷基；R³ 是低级烷氧基烷基或芳氧基烷基；R⁴ 是羟基、甲酰氧基或低级烷酰氧基；X 是可被低级烷基、氧、硫或单键取代的 N-H；Y 是可被取代的芳环或杂环的残基。该化合物及其药学上可接受的盐具有突出的选择性冠状动脉血管扩张活性，同时具有最小的降压作用。因此，它们可以选择性地增加冠状动脉血流量，而不必担心引起突发性低血压导致心动过速，从而对心脏产生不利影响，因此可用作冠状动脉血管扩张剂，特别是作为心绞痛或心力衰竭等心血管疾病的预防或治疗药物。
• Chroman derivative and pharmaceutical use thereof
  申请人：Japan Tobacco Inc.

  公开号：US05719155A1

  公开（公告）日：1998-02-17

  Chroman derivatives of the formula \x9bI! ##STR1## wherein R.sup.1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R.sup.2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R.sup.3 is a lower alkoxyalkyl or an aryloxyalkyl; R.sup.4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action. Accordingly, it is possible to selectively increase the coronary blood flow without causing a sudden hypotention causative of tachycardia which has a detrimental effect on the heart, and they are useful as a coronary vasodilator, in particular, an agent for the prophylaxis and treatment of cardiovascular disorders such as angina pectoris and heart failure.

  本发明的化合物及其中医药学上可接受的盐具有选择性和优秀的心脏血管扩张作用，而且具有极其微弱的降压作用。因此，可以在不引起心动过速导致的有害心脏影响的突发性低血压的情况下，选择性地增加冠状动脉血流，并且它们作为心脏血管扩张剂特别有用，尤其是用于预防和治疗心绞痛和心力衰竭等心血管疾病的药物。