1-(4-(4-bromo-3,5-dimethoxyphenyl)oxazol-2-yl)-2-methoxy-2-(4-(pyrrolidin-1-yl)phenyl)ethanone | 1333471-31-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-(4-(4-bromo-3,5-dimethoxyphenyl)oxazol-2-yl)-2-methoxy-2-(4-(pyrrolidin-1-yl)phenyl)ethanone
• 英文别名: 1-[4-(4-Bromo-3,5-dimethoxyphenyl)-1,3-oxazol-2-yl]-2-methoxy-2-(4-pyrrolidin-1-ylphenyl)ethanone
• CAS: 1333471-31-0
• 化学式: C₂₄H₂₅BrN₂O₅
• 分子量: 501.377
• InChiKey: BPBNOCQFEYNCKE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  32
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  74
• 氢给体数：
  0
• 氢受体数：
  7

文献信息

• PDE10 INHIBITORS AND RELATED COMPOSITIONS AND METHODS
  申请人：Cutshall Neil S.

  公开号：US20110224202A1

  公开（公告）日：2011-09-15

  Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

  揭示了抑制PDE10的化合物，对治疗多种疾病有用，包括（但不限于）精神病、焦虑、运动障碍和/或神经系统疾病，如帕金森病、亨廷顿病、阿尔茨海默病、脑炎、恐惧症、癫痫、失语症、贝尔氏面瘫、脑瘫、睡眠障碍、疼痛、抽动综合征、精神分裂症、妄想症、药物诱发的精神病、恐慌和强迫症。还提供了这些化合物的药用盐、立体异构体、溶剂合物和前药。还揭示了含有化合物与药用载体组合的组合物，以及与使用有关的方法，用于在需要的温血动物中抑制PDE10。
• PDE10 inhibitors and related compositions and methods
  申请人：Omeros Corporation

  公开号：US10106516B2

  公开（公告）日：2018-10-23

  Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

  已公开的抑制 PDE10 的化合物可用于治疗多种疾病，包括（但不限于）精神病、焦虑症、运动障碍和/或神经系统疾病，如帕金森病、亨廷顿病、阿尔茨海默病、脑炎、恐惧症、癫痫、失语症、贝尔麻痹、脑瘫、睡眠障碍、疼痛、抽动秽语症、阿尔茨海默病、脑炎、恐惧症、癫痫、失语症、贝尔氏麻痹、大脑性麻痹、睡眠障碍、疼痛、抽动秽语综合征、精神分裂症、妄想症、药物性精神病以及恐慌症和强迫症。还提供了这些化合物的药学上可接受的盐、立体异构体、溶解物和原药。还公开了含有与药学上可接受的载体结合的化合物的组合物，以及有关使用其在需要的温血动物中抑制 PDE10 的方法。
• US8343970B2
  申请人：——

  公开号：US8343970B2

  公开（公告）日：2013-01-01
• US9102643B2
  申请人：——

  公开号：US9102643B2

  公开（公告）日：2015-08-11
• US9434707B2
  申请人：——

  公开号：US9434707B2

  公开（公告）日：2016-09-06