4-{[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl}-hexahydro-5H-thieno[3,2-b]pyrrol-5-one | 1076191-65-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 4-{[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl}-hexahydro-5H-thieno[3,2-b]pyrrol-5-one
• 英文别名: 4-[[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl]-3,3a,6,6a-tetrahydro-2H-thieno[3,2-b]pyrrol-5-one
• CAS: 1076191-65-5
• 化学式: C₁₅H₁₄F₃N₃OS
• 分子量: 341.357
• InChiKey: LHHRWUZVJQVXGD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  62.9
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  di-tert-butyl (3-nitro-2-thienyl)malonate 在 palladium 10% on activated carbon 三乙基硅烷 、 氢气 、 sodium cyanoborohydride 、 溶剂黄146 、 三氟乙酸 作用下， 以 乙酸乙酯 、 1,2-二氯乙烷 为溶剂， 20.0~40.0 ℃ 、551.59 kPa 条件下， 反应 29.17h， 生成 4-{[2-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl]methyl}-hexahydro-5H-thieno[3,2-b]pyrrol-5-one
  参考文献：
  名称：

  WO2008/132139

  摘要：

  公开号：

文献信息

• LEVETIRACETAM FOR IMPROVING COGNITIVE FUNCTION
  申请人：The Johns Hopkins University

  公开号：EP3400934A1

  公开（公告）日：2018-11-14

  This invention relates to methods and compositions for treating central nervous system (CNS) disorders with cognitive impairment. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), alone or in combination with valproate, in treating central nervous system (CNS) disorders with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, amyotrphic lateral sclerosis and cancer-therapy-related cognitive impairment.

  本发明涉及治疗伴有认知障碍的中枢神经系统（CNS）疾病的方法和组合物。特别是，本发明涉及突触小泡糖蛋白 2A (SV2A)抑制剂单独或与丙戊酸钠联合用于治疗有需要或有风险的受试者（包括但不限于有年龄相关认知障碍或有年龄相关认知障碍风险的受试者）的伴有认知障碍的中枢神经系统 (CNS) 疾病、轻度认知功能障碍（MCI）、失忆性 MCI（aMCI）、年龄相关记忆障碍（AAMI）、年龄相关认知功能衰退（ARCD）、痴呆、阿尔茨海默病（AD）、前驱 AD、创伤后应激障碍（PTSD）、精神分裂症、肌萎缩侧索硬化症和癌症治疗相关认知功能障碍。
• BRIVARACETAM FOR IMPROVING COGNITIVE FUNCTION
  申请人：The Johns Hopkins University

  公开号：EP3827820A1

  公开（公告）日：2021-06-02

  This invention relates to methods and compositions for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), alone or in combination with valproate, in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism, compulsive behavior, and substance addiction.

  本发明涉及治疗与中枢神经系统（CNS）疾病相关的认知障碍的方法和组合物。特别是，本发明涉及突触小泡糖蛋白 2A (SV2A)抑制剂单独或与丙戊酸钠联合用于治疗与中枢神经系统 (CNS) 疾病相关的认知功能损害，需要治疗或有治疗风险的受试者包括但不限于有年龄相关认知功能损害、轻度认知功能损害 (MCI) 或有此风险的受试者、老年痴呆症、阿尔茨海默病（AD）、前驱 AD、创伤后应激障碍（PTSD）、精神分裂症、双相情感障碍、肌萎缩性脊髓侧索硬化症、癌症治疗相关认知障碍、智力迟钝、帕金森病、自闭症、强迫行为和药物成瘾。
• Methods and compositions for treating schizophrenia
  申请人：The Johns Hopkins University

  公开号：US10154988B2

  公开（公告）日：2018-12-18

  The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs, and prodrugs thereof. The methods and the compositions can be used for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).

  本发明涉及通过使用突触小泡蛋白2A（SV2A）抑制剂和抗精神病药或其药学上可接受的盐、水合物、溶解物、多晶型物和原药的组合来治疗精神分裂症或躁狂症（尤其是狂躁症）的方法和组合物。这些方法和组合物可用于治疗与精神分裂症或双相情感障碍（尤其是躁狂症）相关的一种或多种阳性和/或阴性症状以及认知障碍。
• Methods and compositions for improving cognitive function
  申请人：The Johns Hopkins University

  公开号：US10806717B2

  公开（公告）日：2020-10-20

  This invention relates to methods and compositions for treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of inhibitors of synaptic vesicle glycoprotein 2A (SV2A), alone or in combination with valproate, in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment.

  本发明涉及治疗与中枢神经系统（CNS）疾病相关的认知障碍的方法和组合物。 特别是，本发明涉及突触小泡糖蛋白 2A (SV2A)抑制剂单独或与丙戊酸钠联合用于治疗与中枢神经系统 (CNS) 紊乱相关的认知损伤，需要治疗或有治疗风险的受试者，包括但不限于具有或有年龄相关认知损伤风险的受试者。
• NEW HETEROCYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF CNS DISORDERS
  申请人：UCB Pharma, S.A.

  公开号：EP2152262A2

  公开（公告）日：2010-02-17