1,4-Bis[4-(3,4,5-trimethoxyphenyl)butyl]-1,4-diazepane;dihydrochloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1,4-Bis[4-(3,4,5-trimethoxyphenyl)butyl]-1,4-diazepane;dihydrochloride
• 化学式: C31H50Cl2N2O6
• 分子量: 617.6
• InChiKey: KWTZMDXTAJVKJN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.94
• 重原子数：
  41
• 可旋转键数：
  16
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  61.9
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• NEW DIAMINE COMPOUND AND BRAIN PROTECTING AGENT CONTAINING THE SAME
  申请人：KOWA COMPANY LTD.

  公开号：EP0541798A1

  公开（公告）日：1993-05-19

  The present invention provides a diamine compound of formula (I) or an acid addition salt thereof: wherein R1, R2, R3, R4, R5 and R6 are the same or different from each other and represent individually a hydrogen atom, halogen atom, hydroxyl group, lower alkyl group, lower alkoxy group, lower acyloxy group, lower alkoxycarbonyloxy group, lower alkylsulfonyloxy group or am amino group, among which the lower alkyl group and lower alkoxy group may be substituted by a halogen atom or a phenyl group; R7 and R8 are the same or different from each other and represent individually a lower alkyl group or the two bind to each other to represent an alkylene group having 1 to 4 carbon atoms; A and A' are the same or different from each other and represent individually a single bond, -O-, -NH-, -NHCO→, -CONH→, -NHCOO→, NHCONH-, -SO₂NH→ or -COS→ (here, the symbol '→' denotes a bond to Y or Y'), Y and Y' are the same or different from each other and represent a lower alkylene group or lower alkenylene group; and cerebral protective drugs containing such compound. The diamine compounds (I) or its acid addition salts have an excellent cerebral protective action, are very safe, and exhibit a strong action when even orally administered, and therefore, medicines containing such compounds are effective for treating disorders caused by cerebral hemorrhage, cerebral infarction, subarachnoid hemorrhage, transient ischemic attack, cerebrovascular disorders and the like, or preventing progress of such disorders.

  本发明提供了一种式 (I) 的二胺化合物或其酸加成盐： 其中 R1、R2、R3、R4、R5 和 R6 彼此相同或不同，分别代表氢原子、卤素原子、羟基、低级烷基、低级烷氧基、低级酰氧基、低级烷氧基羰氧基、低级烷基磺酰氧基或氨基，其中低级烷基和低级烷氧基可被卤素原子或苯基取代；R7 和 R8 彼此相同或不同，单独代表一个低级烷基，或两者相互结合代表一个具有 1 至 4 个碳原子的亚烷基；A和A'相同或不同，分别代表单键、-O-、-NH-、-NHCO→、-CONH→、-NHCOO→、NHCONH-、-SO₂NH→或-COS→（此处符号'→'表示与Y或Y'的键），Y和Y'相同或不同，分别代表低级亚烷基或低级亚烯基；以及含有此类化合物的脑保护药物。 二胺化合物(I)或其酸加成盐具有很好的脑保护作用，非常安全，即使口服也能表现出很强的作用，因此，含有此类化合物的药物可有效治疗由脑出血、脑梗塞、蛛网膜下腔出血、短暂性脑缺血发作、脑血管疾病等引起的疾病，或预防此类疾病的进展。
• Therapeutic agent for myocardial ischemic damages or reperfusion injuries
  申请人：KOWA COMPANY, LTD.

  公开号：EP0710482A2

  公开（公告）日：1996-05-08

  A therapeutic agent for myocardial ischemic damages or reperfusion injuries which contains, as an active ingredient, a compound of the following formula (1), an acid addition salt thereof, or a hydrate thereof: wherein R¹ to R⁶ are lower alkoxy groups and A and A' are lower alkylene groups; a method for treating those disorders which uses the above compound; and use of the compound in the manufacture of such a therapeutic agent. The therapeutic agent has an excellent action of recovering lowered heart functions caused by myocardial ischemia-reflow, and have low toxicity.

  一种治疗心肌缺血损伤或再灌注损伤的药物，其活性成分包含下式（1）的化合物、其酸加成盐或其水合物： 其中 R¹ 至 R⁶ 为低级烷氧基，A 和 A' 为低级亚烷基；一种使用上述化合物治疗这些疾病的方法；以及该化合物在制造这种治疗剂中的用途。该治疗剂对恢复因心肌缺血再流引起的心功能减退有很好的作用，而且毒性低。
• PREVENTIVE OR REMEDY FOR KIDNEY DISEASES
  申请人：KOWA CO. LTD.

  公开号：EP0786254A1

  公开（公告）日：1997-07-30

  A preventive or remedy for kidney diseases comprising as the active ingredient a compound represented by general formula (1), its acid-addition salt or hydrates thereof, wherein R1, R2, R3, R4, R5 and R6 are the same or different and each represents lower alkoxy; and A and A' are the same or different and each represents lower alkylene. The compound has an excellent effect of preventing and treating acute kidney failure, a potent effect of inhibiting ischemia-reflow disorders in the kidney ad a low toxicity, which makes it useful in the prevention or treatment of kidney diseases.

  一种预防或治疗肾脏疾病的药物，其活性成分包括通式(1)代表的化合物、其酸加成盐或其水合物，其中R1、R2、R3、R4、R5和R6相同或不同，且各自代表低级烷氧基；A和A'相同或不同，且各自代表低级亚烷基。该化合物对预防和治疗急性肾衰竭有很好的效果，对抑制肾脏缺血再流障碍有很强的作用，且毒性低，因此可用于预防或治疗肾脏疾病。
• JPH032144A
  申请人：——

  公开号：JPH032144A

  公开（公告）日：1991-01-08
• US5389630A
  申请人：——

  公开号：US5389630A

  公开（公告）日：1995-02-14