H-7二盐酸盐

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: H-7二盐酸盐
• 中文别名: 1-(5-异喹啉基磺酰基)-2-甲基哌嗪二盐酸盐；H-7双盐酸盐
• 英文名称: hydron;5-(2-methylpiperazin-1-yl)sulfonylisoquinoline;dichloride
• 化学式: C14H19Cl2N3O2S
• 分子量: 364.3
• InChiKey: OARGPFMFRLLKPF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.06
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  70.7
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Dopamine analog amide
  申请人：——

  公开号：US20010056116A1

  公开（公告）日：2001-12-27

  The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

  该发明涉及使用脂肪酸载体和神经活性药物形成前药。该前药在胃和血液流动环境中稳定，并可通过口服递送。该前药容易穿过血脑屏障。一旦进入中枢神经系统，前药被水解成脂肪酸载体和药物以释放药物。在首选实施方式中，载体是4,7,10,13,16,19二十二碳六烯酸，药物是多巴胺。两者都是中枢神经系统的正常成分。药物和载体之间的共价键通常是酰胺键，这种键可以在胃的条件下存活。因此，前药可以被摄入，并且不会在胃中完全水解成载体分子和药物分子。
• Prevention of glycoprotein enveloped virus infectivity by pyridyloxazole-2-ones
  申请人：MERRELL DOW PHARMACEUTICALS INC.

  公开号：EP0428103A2

  公开（公告）日：1991-05-22

  This invention relates to pyridinyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

  本发明涉及吡啶并噁唑-2-酮，由于它们能够作为蛋白激酶 C 抑制剂而成为有用的抗包膜病毒制剂。据披露，这些衍生物可有效治疗包膜病毒感染，包括艾滋病病毒感染，因此可用于治疗艾滋病和 ARC。
• Use of a modulator of protein phosphorylation in the treatment of amyloidosis associated with Alzheimer's disease
  申请人：THE ROCKEFELLER UNIVERSITY

  公开号：EP0457295A2

  公开（公告）日：1991-11-21

  Disclosed is the use of at lease one kinase modulator or phosphatase modulator being capable of increasing or decreasing the rate of proteolytic processing of proteins found in intracellular neurofibrillary tangles and extracellular amyloid plaques for the preparation of a pharmaceutical composition for the treatment of amyloidosis associated with Alzheimer's disease, wherein said pharmaceutical composition contains said modulator in an amount effectively regulating phosphorylation of said proteins.

  公开了至少一种激酶调节剂或磷酸酶调节剂的用途，它们能够提高或降低细胞内神经纤维缠结和细胞外淀粉样斑块中蛋白质的蛋白水解处理速度，用于制备治疗与阿尔茨海默病相关的淀粉样变性的药物组合物，其中所述药物组合物含有所述调节剂，其用量可有效调节所述蛋白质的磷酸化。
• Protein phosphatase inhibitors for use in therapy
  申请人：NATIONAL UNIVERSITY OF SINGAPORE

  公开号：EP0551200A1

  公开（公告）日：1993-07-14

  Protein phosphatase inhibitors such as okadaic acid, a phosphatase inhibitor dervied from a marine black sponge, and calyculin A are able to mimic tumor necrosis factor or interleukin-1. These phosphatase inhibitors may therefore be used to treat conditions which are treatable by tumor necrosis factor or interleukin-1 such as an advanced cancer or a leukaemia.

  蛋白磷酸酶抑制剂，如 okadaic 酸（一种从海洋黑海绵中提取的磷酸酶抑制剂）和钙霉素 A 能够模拟肿瘤坏死因子或白细胞介素-1。因此，这些磷酸酶抑制剂可用于治疗肿瘤坏死因子或白介素-1 可治疗的疾病，如晚期癌症或白血病。
• GUT FLORA-DERIVED EXTRACELLULAR VESICLES, AND METHOD FOR SEARCHING FOR A DISEASE MODEL, VACCINE, AND CANDIDATE DRUG AND FOR DIAGNOSIS USING SAME
  申请人：Aeon Medix Inc.

  公开号：EP2494865A2

  公开（公告）日：2012-09-05

  The present invention relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present invention relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present invention, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.

  本发明涉及一种包括源自肠道菌群的细胞外囊泡的组合物，以及使用该组合物的动物疾病模型。此外，本发明还涉及一种使用肠道菌群衍生的胞外囊泡来有效寻找候选药物的方法，该候选药物可预防或治疗因肠道菌群衍生的胞外囊泡而发生的疾病；本发明还涉及一种疫苗，该疫苗可有效预防或治疗由肠道菌群引起的感染或因肠道菌群衍生的胞外囊泡而发生的疾病。此外，还可以开发诊断技术，利用本发明的肠道菌群源性细胞外囊泡发现因肠道菌群源性细胞外囊泡引起的疾病的病因。