3-[4-(difluoromethoxy)-3-{[1-(4-fluorobenzoyl)piperidin-4-yl]oxy}phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene | 934806-98-1

• 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: 3-[4-(difluoromethoxy)-3-{[1-(4-fluorobenzoyl)piperidin-4-yl]oxy}phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene
• 英文别名: [4-[2-(Difluoromethoxy)-5-(1,7-dioxa-2-azaspiro[4.4]non-2-en-3-yl)phenoxy]piperidin-1-yl]-(4-fluorophenyl)methanone
• CAS: 934806-98-1
• 化学式: C₂₅H₂₅F₃N₂O₅
• 分子量: 490.479
• InChiKey: RWQGWCZKKARSPD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  35
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  69.6
• 氢给体数：
  0
• 氢受体数：
  9

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。
• Compositions of phosphodiesterase type IV inhibitors
  申请人：Ranbaxy Laboratories Limited

  公开号：EP2111861A1

  公开（公告）日：2009-10-28

  Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV ("PDE-IV"), and atleast one other active ingredients selected from muscarinic receptor antagonists (MRA), β2-agonists, p38 MAP Kinase inhibitors, and corticosteroids and optionally one or more pharmaceutically acceptable excipients and/or other therapeutic agents. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.

  本文提供的药物组合物包含一种或多种IV型磷酸二酯酶抑制剂（"PDE-IV"）、至少一种选自毒蕈碱受体拮抗剂（MRA）、β2-激动剂、p38 MAP激酶抑制剂和皮质类固醇的其他活性成分，以及可选的一种或多种药学上可接受的赋形剂和/或其他治疗剂。此外，还提供了治疗自身免疫性、炎症性或过敏性疾病或紊乱的方法。
• PHARMACEUTICAL COMPOSITIONS OF MUSCARINIC RECEPTOR ANTAGONISTS
  申请人：RANBAXY LABORATORIES, LTD.

  公开号：EP1948164A1

  公开（公告）日：2008-07-30
• COMPOSITIONS OF PHOSPHODIESTERASE TYPE IV INHIBITORS
  申请人：Ray Abhijit

  公开号：US20090054382A1

  公开（公告）日：2009-02-26

  Provided herein are pharmaceutical compositions comprising one or more phosphodiesterase inhibitors of type IV (“PDE-IV”), and at least one other active ingredients selected from muscarinic receptor antagonists (MRA), β2-agonists, p38 MAP Kinase inhibitors, and corticosteroids and optionally one or more pharmaceutically acceptable excipients and/or other therapeutic agents. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.
• [EN] PHARMACEUTICAL COMPOSITIONS OF MUSCARINIC RECEPTOR ANTAGONISTS<br/>[FR] COMPOSITIONS PHARMACEUTIQUES D'ANTAGONISTES DU RECEPTEUR MUSCARINIQUE
  申请人：RANBAXY LAB LTD

  公开号：WO2007045979A1

  公开（公告）日：2007-04-26

  [EN] Provided herein are pharmaceutical compositions comprising one or more muscarinic receptor antagonists ("MRA"), and at least one additional active ingredients selected from one or more ß2-agonists, p38 MAP kinase inhibitors, PDE-IV inhibitors, corticosteroids or a mixture thereof and optionally one or more pharmaceutically acceptable carriers, excipients or diluents. In addition, methods of treating autoimmune, inflammatory or allergic diseases or disorders are provided.
  [FR] L'invention concerne des compositions pharmaceutiques comprenant un ou plusieurs antagonistes du récepteur muscarinique ("MRA") et au moins un principe actif supplémentaire sélectionné parmi un ou plusieurs éléments suivants : des ß2-agonistes, des inhibiteurs de la p38 MAP kinase, des inhibiteurs de PDE-IV, des corticostéroïdes ou un mélange de ceux-ci et éventuellement un ou plusieurs excipients ou diluants acceptables sur le plan pharmaceutique de ceux-ci. De plus, l'invention concerne des méthodes de traitement de maladies ou troubles auto-immuns, inflammatoires ou allergiques.