H-9 dihydrochloride

• 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
• 英文名称: H-9 dihydrochloride
• 英文别名: N-(2-aminoethyl)isoquinoline-5-sulfonamide;dihydrochloride
• 化学式: C11H15Cl2N3O2S
• 分子量: 324.2
• InChiKey: HBLCYSFLYMHCBM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -6.82
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  96.3
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  H-9 dihydrochloride 、 S-甲基异硫脲硫酸盐 、 sodium hydroxide 以90%的产率得到
  参考文献：
  名称：

  MORIKAWA, ANRI;SONE, TAKANORI;ASANO, TOSHIO, J. MED. CHEM., 32,(1989) N, C. 42-46

  摘要：

  DOI：
• 作为产物：
  描述：

  异喹啉-5-磺酰氯 、 乙二胺 以71%的产率得到
  参考文献：
  名称：

  MORIKAWA, ANRI;SONE, TAKANORI;ASANO, TOSHIO, J. MED. CHEM., 32,(1989) N, C. 42-46

  摘要：

  DOI：

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。
• METHOD OF PRODUCING PANCREATIC HORMONE-PRODUCING CELLS
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2604685A1

  公开（公告）日：2013-06-19

  The present invention aims to provide a production method of pancreatic hormone-producing cells in a form more mimicking the pancreatogenesis. A method of producing pancreatic hormone-producing cells, comprising subjecting stem cells to the following steps (1) - (6) : (1) a step of cultivating stem cells in a medium containing a Rho kinase inhibitor (2) a step of cultivating the cells obtained in the aforementioned step (1) in a medium containing a GSK3 inhibitor (3) a step of cultivating the cells obtained in the aforementioned step (2) in a medium containing GSK3 inhibitor and an activator of activin receptor-like kinase-4,7 (4) a step of forming a cell mass from the cells obtained in the aforementioned (3), and cultivating the cell mass in a suspension state in a medium (5) a step of cultivating the cells obtained in the aforementioned step (4) in a medium containing a retinoic acid receptor agonist, an inhibitor of AMP-activated protein kinase and/or activin receptor-like kinase-2,3,6, an inhibitor of activin receptor-like kinase-4,5,7 and a cell growth factor (6) a step of cultivating the cells obtained in the aforementioned step (5).

  本发明旨在提供一种生产胰腺激素分泌细胞的方法，其形式更模拟胰腺的生成。 一种生产胰腺激素产生细胞的方法，包括使干细胞经受以下步骤(1)-(6)： (1) 在含有 Rho 激酶抑制剂的培养基中培养干细胞的步骤 (2) 在含有 GSK3 抑制剂的培养基中培养上述步骤(1)中获得的细胞的步骤 (3) 在含有 GSK3 抑制剂和活化素受体样激酶激活剂-4,7 的培养基中培养上述步骤（2）中获得的细胞的步骤 (4) 将上述步骤(3)中获得的细胞形成细胞团，并在培养基中以悬浮状态培养该细胞团的步骤 (5) 在含有维甲酸受体激动剂、AMP 活化蛋白激酶和/或活化因子受体样激酶-2,3,6 的抑制剂、活化因子受体样激酶-4,5,7 的抑制剂和细胞生长因子的培养基中培养上述步骤（4）中获得的细胞的步骤 (6) 培养上述步骤（5）中获得的细胞。
• METHOD FOR PRODUCING CORNEAL ENDOTHELIAL CELL
  申请人：Keio University

  公开号：EP2765188A1

  公开（公告）日：2014-08-13

  The present invention aims to provide a method of efficiently producing corneal endothelial cells, particularly from corneal stroma or iPS cell-derived neural crest stem cells, a method of producing corneal endothelial cells stably in a large amount by inducing more efficient differentiation of stem cells into corneal endothelial cells, and a medicament containing corneal endothelial cells. A method of inducing differentiation of stem cells into corneal endothelial cells, which includes a step of culturing the stem cells in a differentiation induction medium containing a GSK3 inhibitor (preferably a GSK3β inhibitor) and retinoic acid, preferably the differentiation induction medium further containing at least one kind selected from the group consisting of TGFb2, insulin and a ROCK inhibitor, and the like.

  本发明旨在提供一种高效生产角膜内皮细胞的方法，特别是由角膜基质或iPS细胞衍生的神经嵴干细胞生产角膜内皮细胞的方法，一种通过诱导干细胞更有效地分化为角膜内皮细胞而大量稳定生产角膜内皮细胞的方法，以及一种含有角膜内皮细胞的药物。 一种诱导干细胞分化为角膜内皮细胞的方法，它包括在含有GSK3抑制剂（最好是GSK3β抑制剂）和维甲酸的分化诱导培养基中培养干细胞的步骤，最好是分化诱导培养基进一步含有至少一种选自TGFb2、胰岛素和ROCK抑制剂等组成的组的物质。
• METHOD FOR PRODUCING THERAPEUTIC CORNEAL ENDOTHELIAL SUBSTITUTE CELL SPHERE
  申请人：Keio University

  公开号：EP3231863A1

  公开（公告）日：2017-10-18

  The problem of the present invention is to provide a method of efficiently producing therapeutic alternative corneal endothelial cells, particularly, a method capable of stably producing them in a condition suitable for intraocular transplantation (in the anterior chamber) in a large amount. Furthermore, the present invention aims to provide a composition for transplantation, which is preferable for intraocular administration, particularly, into the anterior chamber. A therapeutic alternative corneal endothelial cell sphere can be produced by culturing stem cells in suspension in a differentiation induction medium containing a GSK3 inhibitor, retinoic acid and a ROCK inhibitor. Addition of a viscoelastic substance during intraocular (into the anterior chamber) transplantation of the sphere or cultured corneal endothelial cells dispersed into single cells can increase the number of adherent cells after transplantation.

  本发明的问题是提供一种高效生产治疗性替代角膜内皮细胞的方法，特别是一种能够在适合眼内移植（前房）的条件下大量稳定生产角膜内皮细胞的方法。此外，本发明旨在提供一种用于移植的组合物，该组合物最好用于眼内给药，特别是用于前房。通过在含有 GSK3 抑制剂、维甲酸和 ROCK 抑制剂的分化诱导培养基中培养悬浮干细胞，可生产出治疗性替代角膜内皮细胞球。在眼内（前房）移植球体或分散成单细胞的培养角膜内皮细胞时，加入粘弹性物质可增加移植后附着细胞的数量。
• NAÏVE PLURIPOTENTIAL STEM CELL CULTURING MEDIUM AND PLURIPOTENTIAL STEM CELL CULTURING METHOD
  申请人：KYOWA HAKKO BIO CO., LTD.

  公开号：EP3438248A1

  公开（公告）日：2019-02-06

  An object of the present invention is to provide a medium for culturing naive pluripotent stem cells which is for efficiently proliferating naive pluripotent stem cells while maintaining the undifferentiated state and the pluripotency (pluripotent capability) of the naive pluripotent stem cells. The medium of the invention contains a ROCK inhibitor at a concentration of 5 µM or less

  本发明的目的是提供一种用于培养幼稚多能干细胞的培养基，它能有效地增殖幼稚多能干细胞，同时保持幼稚多能干细胞的未分化状态和多能性（多能能力）。本发明的培养基含有浓度为 5 µM 或更低的 ROCK 抑制剂