cis-4-(4-(((1S,2S)-2-(5-Methoxypyridin-2-yl)cyclopropyl)methoxy)-2-methylpyrimidin-5-yl)cyclohexanecarboxylic acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: cis-4-(4-(((1S,2S)-2-(5-Methoxypyridin-2-yl)cyclopropyl)methoxy)-2-methylpyrimidin-5-yl)cyclohexanecarboxylic acid
• 英文别名: 4-[4-[[(1S,2S)-2-(5-methoxypyridin-2-yl)cyclopropyl]methoxy]-2-methylpyrimidin-5-yl]cyclohexane-1-carboxylic acid
• 化学式: C₂₂H₂₇N₃O₄
• 分子量: 397.5
• InChiKey: GZFVCSKUHCRJDJ-IOTAOYMUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  94.4
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] PYRIMIDINE PDE10 INHIBITORS<br/>[FR] INHIBITEURS PYRIMIDINES DE PDE10
  申请人：MERCK SHARP & DOHME

  公开号：WO2014081619A1

  公开（公告）日：2014-05-30

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶化合物，这些化合物用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统障碍的治疗剂。本发明还涉及使用这些化合物来治疗神经和精神障碍，如精神分裂症、精神疾病或亨廷顿病，以及与纹状体功能减退或基底神经节功能障碍相关的疾病。
• CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTICS DELIVERY
  申请人：Cheng Jianjun

  公开号：US20120289480A1

  公开（公告）日：2012-11-15

  The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

  本发明涉及一种新型治疗环糊精含聚合物组合物，设计为小分子治疗药物传递的载体，以及其制药组合物。这些含环糊精聚合物可以提高药物稳定性和溶解度，并在体内使用时减少小分子治疗药物的毒性。此外，通过从各种连接基团和靶向配体中进行选择，聚合物提供了治疗剂的控制释放方法。本发明还涉及使用上述治疗组合物治疗受试者的方法。本发明还涉及进行制药业务的方法，包括制造、许可或分发包含或涉及上述聚合物化合物的试剂盒。
• PYRIMIDINE PDE10 INHIBITORS
  申请人：MCCOMAS Casey C.

  公开号：US20150307489A1

  公开（公告）日：2015-10-29

  The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

  本发明涉及嘧啶化合物，其可作为治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。本发明还涉及使用这些化合物治疗神经和精神障碍，如精神分裂症、精神病或亨廷顿病，以及与纹状体功能低下或基底节功能障碍相关的疾病。
• US9663513B2
  申请人：——

  公开号：US9663513B2

  公开（公告）日：2017-05-30