1-cyclopentyl-6-{5-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]-5-methyl-4,5-dihydroisoxazol-3-yl}-3-ethyl-1H-indazole | 929293-15-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-cyclopentyl-6-{5-[5-(3,4-difluorophenyl)-1,2,4-oxadiazol-3-yl]-5-methyl-4,5-dihydroisoxazol-3-yl}-3-ethyl-1H-indazole
• 英文别名: 3-[3-(1-cyclopentyl-3-ethylindazol-6-yl)-5-methyl-4H-1,2-oxazol-5-yl]-5-(3,4-difluorophenyl)-1,2,4-oxadiazole
• CAS: 929293-15-2
• 化学式: C₂₆H₂₅F₂N₅O₂
• 分子量: 477.514
• InChiKey: JZJZJOMGXDGIRK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  35
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  78.3
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• Substituted Indazoles as Inhibitors of Phosphodiesterase Type-Iv
  申请人：Palle Venkata

  公开号：US20080312285A1

  公开（公告）日：2008-12-18

  The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, 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 IV inhibitors. Formula (Ia)

  本发明涉及结构Ia的异噁唑啉衍生物，可用作磷酸二酯酶（PDE）IV型的选择性抑制剂。本文披露的化合物可用于治疗中枢神经系统疾病、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，尤其是在人类中。提供了所述化合物的制备方法，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）IV型抑制剂的用途。公式（Ia）
• SUBSTITUTED INDAZOLES AS INHIBITORS OF PHOSPHODIESTERASE TYPE-IV
  申请人：Ranbaxy Laboratories Limited

  公开号：EP1928866A1

  公开（公告）日：2008-06-11
• US7781460B2
  申请人：——

  公开号：US7781460B2

  公开（公告）日：2010-08-24
• [EN] SUBSTITUTED INDAZOLES AS INHIBITORS OF PHOSPHODIESTERASE TYPE-IV<br/>[FR] INDAZOLES SUBSTITUES UTILISES EN TANT QU'INHIBITEURS DE PHOSPHODIESTERASE DE TYPE-IV
  申请人：RANBAXY LAB LTD

  公开号：WO2007029077A1

  公开（公告）日：2007-03-15

  [EN] The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, 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 IV inhibitors. Formula (Ia)
  [FR] L'invention concerne des dérivés d'isoxazoline de structure (Ia), pouvant être utilisés en tant qu'inhibiteurs sélectifs de phosphodiestérase (PDE) de type IV. Ls composés de l'invention peuvent être utiles dans le traitement des maladies et troubles suivants : troubles du SNC, SIDA, asthme, arthrite, bronchite, bronchopneumopathie chronique obstructive (BPCO), psoriasis, rhinite allergique, choc, dermatite atopique, maladie de Crohn, syndrome de détresse respiratoire de l'adulte (SDRA), granulome éosinophile des os, conjonctivite allergique, ostéoarthrite, rectocolite hémorragique et autres maladies inflammatoires en particulier chez l'être humain. L'invention concerne également des procédés de préparation desdits composés, ainsi que des compositions pharmaceutiques les contenant, et leur utilisation en tant qu'inhibiteurs de phosphodiestérase (PDE) de type IV.