1-(5-isoquinolinesulfonyl)-6-benzylhomopiperazine | 105628-00-0

• 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: 1-(5-isoquinolinesulfonyl)-6-benzylhomopiperazine
• 英文别名: 5-[(6-benzyl-1,4-diazepan-1-yl)sulfonyl]isoquinoline
• CAS: 105628-00-0
• 化学式: C₂₁H₂₃N₃O₂S
• 分子量: 381.499
• InChiKey: FOHHXQVBNAWSRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  70.7
• 氢给体数：
  1
• 氢受体数：
  5

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。
• 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。
• MEDICINES COMPRISING Rho KINASE INHIBITOR
  申请人：YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

  公开号：EP0956865A1

  公开（公告）日：1999-11-17

  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 Rho 激酶抑制剂作为新型药物制剂，特别是作为高血压的治疗剂、心绞痛的治疗剂、脑血管收缩的抑制剂、哮喘的治疗剂、外周循环障碍的治疗剂、早产的预防剂、动脉硬化的治疗剂、抗癌药物、抗炎药物、免疫抑制剂、自身免疫性疾病的治疗剂、抗艾滋病药物、动脉硬化治疗剂、抗癌药、抗炎药、免疫抑制剂、自身免疫疾病治疗剂、抗艾滋病药、避孕药、消化道感染预防剂、骨质疏松症治疗剂、视网膜病变治疗剂和脑功能改善药。此外，Rho 激酶抑制剂还可用作试剂和诊断剂。
• 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。
• Substituted isoquinolinesulfonyl compounds
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：EP0187371B1

  公开（公告）日：1991-06-19