Oxolan-2-ylmethyl 4-[[3-[[4-(isoquinolin-5-ylamino)piperidin-1-yl]methyl]phenyl]carbamoyl]benzoate | 1609023-78-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: Oxolan-2-ylmethyl 4-[[3-[[4-(isoquinolin-5-ylamino)piperidin-1-yl]methyl]phenyl]carbamoyl]benzoate
• 英文别名: oxolan-2-ylmethyl 4-[[3-[[4-(isoquinolin-5-ylamino)piperidin-1-yl]methyl]phenyl]carbamoyl]benzoate
• CAS: 1609023-78-0
• 化学式: C₃₄H₃₆N₄O₄
• 分子量: 564.684
• InChiKey: FUWZPFYVWQNJKB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  42
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  92.8
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• [EN] NOVEL ROCK INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE ROCK
  申请人：AMAKEM NV

  公开号：WO2014068035A1

  公开（公告）日：2014-05-08

  The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.

  本发明涉及新型激酶抑制剂，更具体地说是ROCK抑制剂，包括含有此类抑制剂的组合物，尤其是药物，以及此类抑制剂在治疗和预防疾病中的用途。特别是，本发明涉及新型ROCK抑制剂，包括含有此类抑制剂的组合物，尤其是药物，以及此类抑制剂在治疗和预防疾病中的用途。此外，本发明还涉及治疗方法和使用所述化合物在制造药剂中的应用，用于治疗包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病等多种治疗适应症。本发明的化合物表现出软药特性，即它们在进入系统循环后迅速失活。因此，它们允许减少对功能活性ROCK抑制剂的系统性暴露。
• NOVEL ROCK INHIBTORS
  申请人：Amakem NV

  公开号：US20150299173A1

  公开（公告）日：2015-10-22

  The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases. Compounds of the invention display soft drug characteristics, i.e. they are rapidly inactivated upon entry in the systemic circulation. Therefore, they allow for reduced systemic exposure to functionally active ROCK inhibitors.

  本发明涉及新的激酶抑制剂，更具体地涉及ROCK抑制剂，包括此类抑制剂的组合物，特别是制药组合物，以及使用此类抑制剂治疗和预防疾病的用途。具体而言，本发明涉及新的ROCK抑制剂，包括此类抑制剂的组合物，特别是制药组合物，以及使用此类抑制剂治疗和预防疾病的用途。此外，本发明还涉及治疗和使用所述化合物制备药物，用于多种治疗适应症，包括性功能障碍、炎症性疾病、眼科疾病和呼吸系统疾病。本发明的化合物显示出软药特性，即它们在进入系统循环后很快失活。因此，它们允许减少对功能活性ROCK抑制剂的系统曝露。
• NOVEL ROCK INHIBITORS
  申请人：pH Pharma Co., Ltd.

  公开号：EP2914590B1

  公开（公告）日：2016-11-30
• US9394286B2
  申请人：——

  公开号：US9394286B2

  公开（公告）日：2016-07-19