3-[3-{[(2R)-1-acetylpyrrolidin-2-yl]methoxy}-4-(difluoromethoxy)phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene | 1013656-04-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3-[3-{[(2R)-1-acetylpyrrolidin-2-yl]methoxy}-4-(difluoromethoxy)phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene
• 英文别名: 1-[(2R)-2-[[2-(difluoromethoxy)-5-(1,7-dioxa-2-azaspiro[4.4]non-2-en-3-yl)phenoxy]methyl]pyrrolidin-1-yl]ethanone
• CAS: 1013656-04-6
• 化学式: C₂₀H₂₄F₂N₂O₅
• 分子量: 410.418
• InChiKey: VTIRXKHOOLRNDQ-IWPPFLRJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  69.6
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• INHIBITORS OF PHOSPHODIESTERASE TYPE-IV
  申请人：Rudra Sonali

  公开号：US20110021473A1

  公开（公告）日：2011-01-27

  The present invention relates to catechol derivatives of formula (I), which can be used as inhibitors of phosphodiesterase (PDPI) type 4 or type 7, Compounds disclosed herein can be useful in the treatment of CNS disorders, inflammatory diseases such as, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type 4 or type 7 inhibitors.

  本发明涉及公式（I）的邻苯二酚衍生物，可用作磷酸二酯酶（PDPI）类型4或类型7的抑制剂。本文披露的化合物可用于治疗中枢神经系统疾病、炎症性疾病，如艾滋病、哮喘、关节炎、支气管炎、慢性阻塞性肺病（COPD）、牛皮癣、过敏性鼻炎、休克、特应性皮炎、克罗恩病、成人呼吸窘迫综合征（ARDS）、嗜酸性肉芽肿、过敏性结膜炎、骨关节炎、溃疡性结肠炎和其他炎症性疾病，尤其是在人类身上。提供了用于制备所述化合物的方法，以及含有所述化合物的药物组合物，以及它们作为磷酸二酯酶（PDE）类型4或类型7抑制剂的用途。
• [EN] INHIBITORS OF PHOSPHODIESTERASE TYPE-IV<br/>[FR] INHIBITEURS DE LA PHOSPHODIESTERASE TYPE IV
  申请人：RANBAXY LAB LTD

  公开号：WO2008035315A9

  公开（公告）日：2008-10-23

  [EN] The present invention relates to catechol derivatives of formula I, which can be used as inhibitors of phosphodiesterase (PDPI) type 4 or type 7, Compounds disclosed herein can be useful in the treatment of CNS disorders, inflammatory diseases such as, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type 4 or type 7 inhibitors. (I).
  [FR] La présente invention concerne des dérivés de catéchol pouvant être utilisés en tant qu'inhibiteurs de la phosphodiestérase (PDPI) type 4 ou type 7. Les composés selon l'invention peuvent être utiles dans le traitement des troubles du système nerveux central et de maladies inflammatoires telles que le sida, l'asthme, l'arthrite, la bronchite, la maladie pulmonaire obstructive chronique (MPOC), le psoriasis, la rhinite allergique, le choc, la dermatite atopique, la maladie de Crohn, le syndrome de détresse respiratoire de l'adulte (SDRA), le granulome éosinophile, la conjonctivite allergique, l'arthrose, la colite ulcéreuse et autres maladies inflammatoires, en particulier chez des humains. L'invention concerne également des procédés de préparation de ces composés, ainsi que des compositions pharmaceutiques les contenant et leur utilisation en tant qu'inhibiteurs de la phosphodiestérase (PDE) type 4 ou type 7.