1-(5-硫代异喹啉)-3-甲基哌嗪 | 84477-73-6

• 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: 1-(5-硫代异喹啉)-3-甲基哌嗪
• 中文别名: 1-(5-异喹啉磺酰)-3-甲基哌嗪
• 英文名称: 1-(5-Isoquinolinylsulfonyl)-3-methylpiperazine
• 英文别名: 5-(3-methylpiperazin-1-yl)sulfonylisoquinoline
• CAS: 84477-73-6
• 化学式: C₁₄H₁₇N₃O₂S
• 分子量: 291.37
• InChiKey: QGSCXAWTTISKLF-UHFFFAOYSA-N

物化性质

• 沸点：
  495.3±55.0 °C(Predicted)
• 密度：
  1.277±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  20
• 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：
  1
• 氢受体数：
  5

安全信息

• 安全说明：
  S22,S24/25
• 海关编码：
  2935009090

反应信息

• 作为产物：
  描述：

  isoquinoline-5-sulfonyl chloride;sulfuric acid 生成 1-(5-硫代异喹啉)-3-甲基哌嗪
  参考文献：
  名称：

  XIDAKA, XIROESI;SONEH, TAKANORI

  摘要：

  DOI：

文献信息

• Pharmaceutical agent containing Rho kinase inhibitor
  申请人：——

  公开号：US20020032148A1

  公开（公告）日：2002-03-14

  A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.

  提供了一种新型药物代理——Rho激酶抑制剂，特别用于治疗高血压、心绞痛、脑血管收缩抑制剂、哮喘、周围循环障碍的治疗剂、早产预防剂、动脉硬化的治疗剂、抗癌药物、抗炎剂、免疫抑制剂、自身免疫疾病的治疗剂、抗艾滋病药物、避孕药、消化道感染预防剂、骨质疏松症的治疗剂、视网膜病的治疗剂和脑功能改善药物。此外，Rho激酶抑制剂还可作为试剂和诊断工具。
• Isoquinolinesulfonyl derivatives and process for the preparation thereof
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0061673A1

  公开（公告）日：1982-10-06

  A 5-isoquinolinesulfonyl derivative of Formula (I): wherein f is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one; R1 is a hydrogen atom, a C1-10 alkyl group, a C5-6cycloalkyl group or an aryl group; or R2 and R3 each is a hydrogen atom, a C1-10 alkyl group, a C5-6 cycloalkyl group, an aryl group or an aralkyl group; R2 and R3 are C1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the group is a group wherein R4 and Rs each is a hydrogen atom, a C1-10 alkyl group, an aryl group or an aralkyl group and R6 is a hydrogen atom, a C1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a group wherein R, is a C1-8 alkyl group, and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  式(I)的 5-异喹啉磺酰基衍生物： 其中 f 为零或一 m 和 n 均为一至九的整数 m+n 至少为 1 的整数； R1 是氢原子、C1-10 烷基、C5-6 环烷基或芳基；或 R2 和 R3 各为氢原子、C1-10 烷基、C5-6 环烷基、芳基或芳烷基； R2 和 R3 为 C1-6 烯基，直接或通过氧原子连接，与相邻的氮原子形成 5-7 元杂环；或 基团为 其中 R4 和 Rs 分别为氢原子、C1-10 烷基、芳基或芳烷基，R6 为氢原子、C1-10 烷基、芳基、芳烷基、苯甲酰基、肉桂酰基、肉桂酰基、呋喃基或 其中 R 是 C1-8 烷基的基团及其药学上可接受的盐；以及其制备方法。本发明的化合物对血管平滑肌具有松弛作用，可用作血管扩张剂和降压剂。
• CARDIAC PROTECTIVE
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0654266A1

  公开（公告）日：1995-05-24

  A cardiac protective containing an isoquinolinesulfonamide derivative represented by general formula (I) or a salt thereof, suitable for treating myocardial diseases and myocardial cytopathy, wherein R¹ represents H, Cl or OH; A, R², R³, and R⁴ represent each a group selected dependent on R¹; A represents C₂-C₆ alkylene which may be substituted by alkyl, cinnamyl, phenyl or benzyl; R² and R³ represent each independently H, C₁-C₆ alkyl, C₆ or lower cycloalkyl, cinnamyl, phenyl or benzyl, or alternatively R² and R³ may be combined together to represent alkylene which may be alkylated; R⁴ represents H, C₁-C₆ alkyl, phenyl, benzyl, benzoyl, cinnamyl, cinnamoyl, furoyl (a) or (b), or alternatively R⁴ may be combined with R³ to represent a chain which may contain an interposed oxygen atom; R⁵ represents C₁-C₆ alkyl; and R⁶ and R⁷ are each independently selected dependent on R¹ and represent each H or CH₃. or alternatively R⁶ and R⁷ may be combined together to represent C₂-C₄ alkylene.

  一种心脏保护剂，含有通式(I)代表的异喹啉磺酰胺衍生物或其盐，适用于治疗心肌疾病和心肌细胞病变，其中R¹代表H、Cl或OH；A、R²、R³和R⁴各自代表根据R¹选择的基团；A代表C₂-C₆亚烷基，可被烷基、肉桂基、苯基或苄基取代；R² 和 R³ 各自独立地代表 H、C₁-C₆ 烷基、C₆ 或低级环烷基、肉桂基、苯基或苄基，或者 R² 和 R³ 可组合在一起，代表可被烷基化的亚烷基；R⁴ 代表 H、C₁-C₆ 烷基、苯基、苄基、苯甲酰基、肉桂酰基、肉桂酰基、呋喃基 (a) 或 (b)，或者 R⁴ 可与 R³ 结合在一起，代表可包含一个中间氧原子的链；R⁵ 代表 C₁-C₆烷基；以及 R⁶ 和 R⁷ 各自独立地根据 R¹ 进行选择，并各自代表 H 或 CH₃。或者，R⁶ 和 R⁷ 可以组合在一起代表 C₂-C₄ 亚烷基。
• Use of isoquinoline-derivatives for treating and preventing pigmentary disorders
  申请人：Switch Biotech Aktiengesellschaft

  公开号：EP1479386A1

  公开（公告）日：2004-11-24

  The invention relates to the use of isoquinoline-derivatives for treating and/or preventing pigmentary disorders.

  本发明涉及使用异喹啉衍生物治疗和/或预防色素性疾病。
• 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。