1H-Thieno(2,3-C)pyrazole-5-carboxamide, 1-cyclohexyl-N-(6-(4-hydroxy-1-piperidinyl)-3-pyridinyl)-3-methyl- | 873541-45-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 1H-Thieno(2,3-C)pyrazole-5-carboxamide, 1-cyclohexyl-N-(6-(4-hydroxy-1-piperidinyl)-3-pyridinyl)-3-methyl-
• 英文别名: 1-cyclohexyl-N-[6-(4-hydroxypiperidin-1-yl)pyridin-3-yl]-3-methylthieno[2,3-c]pyrazole-5-carboxamide
• CAS: 873541-45-8
• 化学式: C₂₃H₂₉N₅O₂S
• 分子量: 439.6
• InChiKey: NFWMSIMJLJHZPQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  112
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Treatment of Addiction and Impulse-Control Disorders Using PDE7 Inhibitors
  申请人：OMEROS CORPORATION

  公开号：US20130267502A1

  公开（公告）日：2013-10-10

  This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.

  本公开涉及使用磷酸二酯酶7（PDE7）抑制剂，单独或与其他治疗药物联合治疗成瘾和原发性冲动控制障碍。
• Use of PDE7 Inhibitors for the Treatment of Movement Disorders
  申请人：OMEROS CORPORATION

  公开号：US20140179717A1

  公开（公告）日：2014-06-26

  A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.

  一种治疗神经运动障碍病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症，通过给予治疗有效量的PDE7抑制剂。该发明的一个方面是在给予多巴胺激动剂或前体（如左旋多巴）的同时给予PDE7抑制剂。在该发明的另一个方面，PDE7抑制剂可以相对于其他分子靶点（i）已知与帕金森病的病理学有关或（ii）其他治疗帕金森病有效的药物作用的靶点而选择性地作用于PDE7。
• USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS
  申请人：Omeros Corporation

  公开号：US20160015715A1

  公开（公告）日：2016-01-21

  A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.

  本发明涉及一种治疗神经运动障碍病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症，通过给予治疗有效量的PDE7抑制剂。本发明的一个方面提供了与多巴胺激动剂或前体（例如左旋多巴）一起给予PDE7抑制剂的治疗方法。在本发明的另一个方面，PDE7抑制剂可以选择性地作用于PDE7，而相对于其他分子靶点（i）已知与帕金森病的病理学有关或（ii）其他治疗帕金森病的药物作用的靶点。
• Thienopyrazole Derivative Having PDE7 Inhibitory Activity
  申请人：Inoue Hidekazu

  公开号：US20090131413A1

  公开（公告）日：2009-05-21

  To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R 1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R 2 is methyl; R 3 is a hydrogen atom; and R 4 is a group: —CONR 5 R 6 (in which any one of R 5 and R 6 is a hydrogen atom)].

  为了提供选择性抑制PDE 7的噻唑吡啶衍生物，从而增强细胞cAMP水平。因此，该化合物可用于治疗各种疾病，如过敏性疾病、炎症性疾病或免疫性疾病。该化合物是由以下式子(I)表示的噻唑吡啶化合物：[其中，特别地，R1是环己基、环庚基或四氢吡喃基；R2是甲基；R3是氢原子；R4是一个基团：—CONR5R6（其中R5和R6中的任何一个是氢原子）]。
• Thienopyrazole derivatives having PDE7 inhibitory activity
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2433943A1

  公开（公告）日：2012-03-28

  To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: -CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].

  提供选择性抑制 PDE 7 并因此提高细胞 cAMP 水平的噻吩并吡唑衍生物。因此，该化合物可用于治疗各种疾病，如过敏性疾病、炎症性疾病或免疫性疾病。该化合物是由下式（I）代表的噻吩并唑化合物： [其中，R1 特别是环己基、环庚基或四氢吡喃基；R2 是甲基；R3 是氢原子；R4 是基团：-CONR5R6（其中 R5 和 R6 中的任一个是氢原子）]。