5,6,7,9-Tetrahydro-8-thia-5-aza-benzocycloheptene8,8-dioxide | 1211594-99-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并硫氮卓类
• 英文名称: 5,6,7,9-Tetrahydro-8-thia-5-aza-benzocycloheptene8,8-dioxide
• 英文别名: 1,2,3,5-tetrahydro-4λ6,1-benzothiazepine 4,4-dioxide
• CAS: 1211594-99-8
• 化学式: C₉H₁₁NO₂S
• 分子量: 197.26
• InChiKey: DBTAVLNDPCBSQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  54.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS<br/>[FR] COMPOSÉS ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE BACE1
  申请人：ALLGENESIS BIOTHERAPEUTICS INC

  公开号：WO2016172255A1

  公开（公告）日：2016-10-27

  The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).

  本发明涉及式（I）的化合物或其立体异构体、互变异构体、或其药学上可接受的盐或溶剂，其中X、Y、Z、Q、W、m、u、环（A）、R2、R3、R4、R5和R6如规范和权利要求中所定义。本发明提供了含有式（I）化合物的药物组合物，以及治疗和/或预防唐氏综合征、β-淀粉样血管病、与认知损伤相关的疾病、阿尔茨海默病、记忆丧失、与阿尔茨海默病相关的注意力缺陷症状、神经退行性疾病、早老性痴呆、老年性痴呆和与帕金森病、阿尔茨海默病和/或唐氏综合征相关的痴呆、年龄相关性黄斑变性（AMD）、青光眼、嗅觉功能障碍、创伤性脑损伤、进行性肌肉疾病、2型糖尿病和心血管疾病（中风）的治疗方法。
• Compounds and their use as BACE1 inhibitors
  申请人：ALLGENESIS BIOTHERAPEUTICS, INC.

  公开号：US10870635B2

  公开（公告）日：2020-12-22

  The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, 3-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).

  本发明涉及式(I)化合物或其立体异构体、同分异构体或药学上可接受的盐或溶液，其中X、Y、Z、Q、W、m、u、环(A)、R2、R3、R4、R5和R6如说明书和权利要求书中所定义。本发明提供了一种含有式（I）化合物的药物组合物和一种治疗方法，用于治疗和/或预防唐氏综合征、3-淀粉样血管病、与认知障碍相关的疾病、阿尔茨海默病、记忆力减退、与阿尔茨海默病相关的注意力缺陷症状、神经退行性疾病、老年前期痴呆、老年期痴呆以及与帕金森病、阿尔茨海默病和/或唐氏综合征相关的痴呆、老年黄斑变性（AMD）、青光眼、嗅觉功能损伤、脑外伤、进行性肌肉疾病、II 型糖尿病和心血管疾病（中风）。
• COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS
  申请人：Allgenesis Biotherapeutics Inc.

  公开号：EP3250035A1

  公开（公告）日：2017-12-06
• High-density lipoprotein-cholesterol level elevating agent
  申请人：Nishimoto Tomoyuki

  公开号：US20080058310A1

  公开（公告）日：2008-03-06

  A novel high-density lipoprotein(HDL)-cholesterol level elevating agent containing a compound which has a squalene synthase inhibitory activity.
• Skeletal muscle protecting agent
  申请人：Tozawa Ryuichi

  公开号：US20080113965A1

  公开（公告）日：2008-05-15

  The present invention provides a novel drug which is useful as a skeletal muscle protecting agent comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.