N-Diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-yl)benzenesulfonamide, dihydrochloride

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 四氢异喹啉
• 英文名称: N-Diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-yl)benzenesulfonamide, dihydrochloride
• 英文别名: N-Diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)benzenesulfonamide, dihydrochloride；N-diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-yl)benzenesulfonamide dihydrochloride；N-diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)benzenesulfonamide dihydrochloride；2-[4-(6,8-dichloro-2-methyl-3,4-dihydro-1H-isoquinolin-4-yl)phenyl]sulfonylguanidine;hydrochloride
• 化学式: C₁₇H₁₈Cl₂N₄O₂S*2ClH
• 分子量: 486.249
• InChiKey: RWPFQKNKCVVSDW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.95
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  110
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)benzenesulfonyl chloride 、 胍 在 盐酸 作用下， 以 四氢呋喃 、 乙醚 、 乙酸乙酯 为溶剂， 反应 29.0h， 生成 N-Diaminomethylene-4-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-yl)benzenesulfonamide, dihydrochloride
  参考文献：
  名称：

  SUBSTITUTED 4-PHENYLTETRAHYDROISOQUINOLINES, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC USE

  摘要：

  本发明涉及取代的4-苯基四氢异喹啉化合物和包含它们的制药组合物，这些化合物是优秀的钠-氢交换酶（NHE）抑制剂，特别是亚型3（NHE-3）的钠-氢交换酶抑制剂。因此，这些化合物在治疗各种肾和呼吸系统疾病方面非常有用，例如急性或慢性肾衰竭，肺部并发症，胆功能障碍，呼吸系统疾病，如打鼾或睡眠呼吸暂停以及心血管/中枢神经系统疾病，例如中风。更具体地说，本发明涉及由公式I定义的取代的4-苯基四氢异喹啉，其中R1-R8在此定义。

  公开号：

  US20080194621A1

文献信息

• METHODS FOR THE IMPROVEMENT OF MEMORY AND NEUROLOGICAL FUNCTION COMPRISING THE ADMINISTRATION OF COMPOSITIONS THAT ACT AS INHIBITORS OF THE SODIUM PROTON (NA+ /H+ ) EXCHANGER, SUBTYPE 5 (NHE-5)
  申请人：KLEEMANN Heinz-Werner

  公开号：US20080234317A1

  公开（公告）日：2008-09-25

  The present invention comprises the use of pharmaceutical compositions that are effective in the inhibition of the Na + /H + exchanger, subtype 5 (NHE-5) as inhibitors of cellular NHE-5 enhance long term potentiation (LTP) and are therefore effective in the treatment of memory impairments, dementing disorders, and for improving memory. Particularly suitable for the treatment of neurodegenerative disorders, memory impairments and dementing disorders, and for improving memory, are the following NHE-5 inhibitors of the formula I Wherein the R1-R8 substituents are further defined herein:

  本发明涉及使用药物组合物作为Na+/H+交换器亚型5（NHE-5）的抑制剂，这些抑制剂可以增强长期增强（LTP）并因此有效治疗记忆障碍、痴呆疾病和改善记忆。特别适用于治疗神经退行性疾病、记忆障碍和痴呆疾病，以及改善记忆的是以下公式I的NHE-5抑制剂，其中R1-R8取代基在此进一步定义：
• SUBSTITUTED 4-PHENYLTETRAHYDROISOQUINOLINES, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THERAPEUTIC USE
  申请人：Lang Hans-Jochen

  公开号：US20080194621A1

  公开（公告）日：2008-08-14

  The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds and pharmaceutical compositions comprising them which are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE-3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines defined by the formula I in which R1-R8 are defined herein.

  本发明涉及取代的4-苯基四氢异喹啉化合物和包含它们的制药组合物，这些化合物是优秀的钠-氢交换酶（NHE）抑制剂，特别是亚型3（NHE-3）的钠-氢交换酶抑制剂。因此，这些化合物在治疗各种肾和呼吸系统疾病方面非常有用，例如急性或慢性肾衰竭，肺部并发症，胆功能障碍，呼吸系统疾病，如打鼾或睡眠呼吸暂停以及心血管/中枢神经系统疾病，例如中风。更具体地说，本发明涉及由公式I定义的取代的4-苯基四氢异喹啉，其中R1-R8在此定义。