3-[4-(difluoromethoxy)-3-(2,3-dihydro-1H-inden-2-yloxy)phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene | 905962-74-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 3-[4-(difluoromethoxy)-3-(2,3-dihydro-1H-inden-2-yloxy)phenyl]-1,7-dioxa-2-azaspiro[4.4]non-2-ene
• CAS: 905962-74-5
• 化学式: C₂₂H₂₁F₂NO₄
• 分子量: 401.41
• InChiKey: HQCWJGOUJLYKBD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  49.3
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• CONDENSED ISOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE TYPE - IV
  申请人：Palle Venkata P.

  公开号：US20090048247A1

  公开（公告）日：2009-02-19

  The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of 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 in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.

  本发明涉及异噁唑啉衍生物，可用作选择性磷酸二酯酶（PDE）IV型抑制剂。特别地，本文所披露的化合物可用于治疗艾滋病、哮喘、关节炎、支气管炎、慢性阻塞性肺疾病（COPD）、银屑病、过敏性鼻炎、休克、特应性皮炎、克罗恩病、成人呼吸窘迫综合症（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的患者，特别是人类。本发明还涉及所披露的化合物的制备方法，以及其作为磷酸二酯酶（PDE）IV型抑制剂的药物组合物及其应用。
• 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。
• CONDENSED ISOXALINE DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE TYPE-IV
  申请人：Ranbaxy Laboratories Limited

  公开号：EP1869054A2

  公开（公告）日：2007-12-26
• COMPOSITIONS OF PHOSPHODIESTERASE TYPE IV INHIBITORS
  申请人：RANBAXY LABORATORIES, LTD.

  公开号：EP1948167A1

  公开（公告）日：2008-07-30
• PHARMACEUTICAL COMPOSITIONS OF MUSCARINIC RECEPTOR ANTAGONISTS
  申请人：RANBAXY LABORATORIES, LTD.

  公开号：EP1948164A1

  公开（公告）日：2008-07-30