2-chloro-4-[2,5-dimethyl-1-(3-trifluoromethoxy-phenyl)-1H-imidazol-4-ylethynyl]-pyridine | 871362-32-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-chloro-4-[2,5-dimethyl-1-(3-trifluoromethoxy-phenyl)-1H-imidazol-4-ylethynyl]-pyridine
• 英文别名: 2-Chloro-4-[2-[2,5-dimethyl-1-[3-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
• CAS: 871362-32-2
• 化学式: C₁₉H₁₃ClF₃N₃O
• 分子量: 391.78
• InChiKey: OMWLMTSXTVGVPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  39.9
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] PYRIDIN-4-YL-ETHYNYL-IMIDAZOLES AND PYRAZOLES AS MGLU5 RECEPTOR ANTAGONISTS<br/>[FR] PYRIDIN-4-YL-ETHYNYL-IMIDAZOLES ET PYRAZOLES, ANTAGONISTES DU RECEPTEUR MGLUR5
  申请人：HOFFMANN LA ROCHE

  公开号：WO2005118568A1

  公开（公告）日：2005-12-15

  The present invention relates to diazole derivatives of the general formula (I) wherein A, E, R1, Wand R3 are as defined in the claims and description, their use for the preparation of medicaments for treating diseases and processes for preparing them.

  本发明涉及一般式(I)的噻唑烯衍生物，其中A、E、R1、W和R3如权利要求和描述中定义的那样，它们用于制备治疗疾病的药物和制备过程。
• METHODS FOR THE TREATMENT OF GERD WITH MGLUR5 ANTAGONISTS
  申请人：Jaeschke Georg

  公开号：US20090054490A1

  公开（公告）日：2009-02-26

  The present invention relates to methods for the treatment, prevention and/or delay of progression of gastro-esophageal reflux disease (GERD) by administering compounds that act as antagonists of metabotropic glutamate type-5 receptors (mGluR5 receptor antagonists), for example compounds of formula (I) wherein A, E, R 1 , R 2 , R 2 and R 4 are as defined in the specification.

  本发明涉及通过给予作为代谢型谷氨酸5型受体拮抗剂（mGluR5受体拮抗剂）的化合物来治疗、预防和/或延缓胃食管反流病（GERD）的进展的方法，例如具有以下结构的化合物（I）其中A、E、R1、R2、R3和R4如规范中定义的那样。
• Diazole derivatives
  申请人：Buettelmann Bernd

  公开号：US20060030559A1

  公开（公告）日：2006-02-09

  The present invention relates to diazole derivatives of the general formula wherein A, E, R 1 , R 2 and R 3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.

  本发明涉及一般式为的二唑类衍生物，其中A，E，R1，R2和R3如申请中所定义，并且含有它们的药物组合物。本发明还涉及使用这种化合物治疗由代谢型谷氨酸受体（mGluR）介导的疾病，例如焦虑，慢性和急性疼痛，保护肝脏损伤，尿失禁，肥胖症，脆性X和自闭症，阿尔茨海默病，癫痫，精神分裂症，缺血，亨廷顿舞蹈症，肌萎缩性侧索硬化（ALS），由艾滋病引起的痴呆症以及帕金森病。
• DIAZOLE DERIVATIVES
  申请人：Buettelmann Bernd

  公开号：US20100048569A1

  公开（公告）日：2010-02-25

  The present invention relates to diazole derivatives of the general formula wherein A, E, R 1 , R 2 and R 3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.

  本发明涉及一般式为的二唑衍生物，其中A、E、R1、R2和R3如申请中所定义，并且包含它们的制药组合物。本发明还涉及使用这种化合物治疗通过代谢型谷氨酸受体（mGluR）介导的疾病，例如焦虑、慢性和急性疼痛、保护肝损伤、尿失禁、肥胖症、脆性X和自闭症、阿尔茨海默病、癫痫、精神分裂症、缺血、亨廷顿舞蹈症、肌萎缩性侧索硬化症（ALS）、由艾滋病引起的痴呆症和帕金森病。
• Pharmaceutical compositions of metabotropic glutamate 5 receptor (MGLU5) antagonists
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2808022A1

  公开（公告）日：2014-12-03

  Pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in matrix tablet. The compositions provide a pH-independent in vitro release profile with NMT 70 % in one hour, NMT 85 % in 4 hour, and NLT 80 % in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment-Resistant Depression (TRD) and Fragile X Syndrome.

  本发明公开了代谢谷氨酸 5 受体（mGlu5）拮抗剂或其药理上可接受的盐的药物组合物。这些组合物在基质片剂中含有治疗活性化合物、非离子聚合物和离子聚合物、粘合剂和填料。该组合物具有与 pH 值无关的体外释放特性，1 小时内的 NMT 释放率为 70%，4 小时内的 NMT 释放率为 85%，8 小时内的 NLT 释放率为 80%。该组合物可用于治疗中枢神经系统疾病，如治疗耐受性抑郁症（TRD）和脆性 X 综合征。