3-(2,4-Difluorophenyl)-5-methyl-1,2,4-oxadiazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-(2,4-Difluorophenyl)-5-methyl-1,2,4-oxadiazole
• 化学式: C₉H₆F₂N₂O
• 分子量: 196.15
• InChiKey: FAYAHABVIUYVAZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  38.9
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Phosphodiesterase Inhibitors
  申请人：Palle P. Venkata

  公开号：US20070259874A1

  公开（公告）日：2007-11-08

  The present invention relates to isoxazoline derivatives and their analogues, which can be used as phosphodiesterase (PDE) type IV selective inhibitors. 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, especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and their use as PDE type IV selective inhibitors, are provided.

  本发明涉及异噁唑啉衍生物及其类似物，可用作磷酸二酯酶（PDE）IV型选择性抑制剂。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，尤其是在人类中。本文提供了所披露的化合物的制备方法、含有所披露的化合物的药物组合物以及它们作为PDE IV型选择性抑制剂的用途。
• Heteroaryl allosteric modulators of nicotinic acetylcholine receptors
  申请人：Merck Sharp & Dohme Corp.

  公开号：US11198687B2

  公开（公告）日：2021-12-14

  The present disclosure relates to compounds of formula I that are useful as modulators of 7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation (I).

  本公开涉及可用作 7 nAChR 调节剂的式 I 化合物、包含此类化合物的组合物，以及使用此类化合物预防、治疗或改善疾病，特别是中枢神经系统疾病，如阿尔茨海默病、帕金森病和精神分裂症中的认知障碍，以及 L-DOPA 诱导的运动障碍和炎症 (I)。
• HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
  申请人：Merck Sharp & Dohme LLC

  公开号：EP3684357B1

  公开（公告）日：2022-12-28