噻苯芦索 | 104383-17-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 中文名称: 噻苯芦索
• 中文别名: 化合物 T28655
• 英文名称: Sabeluzole
• 英文别名: 1-[4-[1,3-benzothiazol-2-yl(methyl)amino]piperidin-1-yl]-3-(4-fluorophenoxy)propan-2-ol
• CAS: 104383-17-7
• 化学式: C₂₂H₂₆FN₃O₂S
• 分子量: 415.5
• InChiKey: IGMKTIJBFUMVIN-UHFFFAOYSA-N

物化性质

• 熔点：
  101.7°
• 沸点：
  577.4±60.0 °C(Predicted)
• 密度：
  1.288±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  29
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  77.1
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  N-methyl-N-(piperidin-4-yl)-1,3-benzothiazol-2-amine 生成 噻苯芦索
  参考文献：
  名称：

  STOKBROEKX, RAYMOND A.;LUYCKX, MARCEL G. M.;JANSSENS, FRANS E.

  摘要：

  DOI：

文献信息

• Central nervous system antiischemic agents
  申请人：Bristol-Myers Squibb Company

  公开号：EP0559569A1

  公开（公告）日：1993-09-08

  A series of phenylalkylaminoalkyl derivatives of Formula I wherein Ar is naphtyl or phenyl;    R¹ is hydrogen, fluoro or R⁴CONH-;    R² is hydrogen or C₁-₆ alkyl;    R₃ is C₁-₆ alkyl;    R⁴ is C₁-₆ alkyl or phenyl- C₁-₆ alkyl;    x is zero or the integers 1 and 2;    m is selected from the integers 1 to 6; and    n is selected from the integers 2 and 3, has been found to provide effective antiischemic protection for CNS tissue, particularly neurons. A method of treatment to protect against CNS ischemia, such as that resulting from trauma or stroke or other ischemic conditions, comprises administration of these novel compounds to an individual in need of such treatment.

  一系列的Formula I的苯基烷基氨基烷基衍生物已被发现能够为中枢神经系统组织，特别是神经元，提供有效的抗缺血保护。一种治疗方法用于保护中枢神经系统缺血，例如由创伤、中风或其他缺血病症引起的缺血情况，包括将这些新化合物用于需要此类治疗的个体。其中Ar为萘基或苯基；R¹为氢、氟或R⁴CONH-；R²为氢或C₁-₆烷基；R₃为C₁-₆烷基；R⁴为C₁-₆烷基或苯基-C₁-₆烷基；x为零或整数1和2；m从整数1到6中选择；n从整数2和3中选择。
• [EN] COMPOUNDS AND THEIR USE AS BACE INHIBITORS<br/>[FR] COMPOSÉS ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE BACE
  申请人：ASTRAZENECA AB

  公开号：WO2016055858A1

  公开（公告）日：2016-04-14

  The present application relates to compounds of formula (I), (la), or (lb) and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing Αβ-related pathologies such as Down's syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia, including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.

  本申请涉及式(I)、(Ia)或(Ib)的化合物及其药物组合物/制剂。本申请进一步涉及治疗或预防与Αβ相关的病理学，如唐氏综合症，β-淀粉样蛋白血管病，如但不限于脑淀粉样蛋白血管病或遗传性脑出血，与认知损害相关的疾病，如但不限于MCI（“轻度认知损害”），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，与疾病如阿尔茨海默病或痴呆症相关的神经退行性疾病，包括混合性血管性和退行性起源的痴呆，早老性痴呆，老年性痴呆和与帕金森病相关的痴呆的方法。
• 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
  申请人：Dunn Robert

  公开号：US20080318941A1

  公开（公告）日：2008-12-25

  The present disclosure provides compounds having affinity for the 5-HT 6 receptor which are of the formula (I): wherein R 1 , R 2 , R 5 , R 6 , B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.

  本公开提供了具有亲和力的化合物，其对5-HT 6 受体具有亲和力，其化学式为（I）： 其中R1、R2、R5、R6、B、D、E、G、Q、x和n如本文所定义。本公开还涉及制备这种化合物的方法、含有这种化合物的组合物以及使用这些化合物的方法。
• HETEROBICYCLIC COMPOUNDS
  申请人：Amgen Inc.

  公开号：US20130225552A1

  公开（公告）日：2013-08-29

  Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.

  Formula (I)的杂环化合物： 或其药用可接受的盐、互变异构体或立体异构体，如规范中所定义，并含有它们的组合物，以及制备这种化合物的方法。本文还提供了通过抑制PDE10来治疗由此可治疗的疾病或疾病的方法，如肥胖症、非胰岛素依赖型糖尿病、精神分裂症、躁郁症、强迫症、亨廷顿病等。
• [EN] SUBSTITUTED N-ARYL BENZAMIDES AND RELATED COMPOUNDS FOR TREATMENT OF AMYLOID DISEASES AND SYNUCLEINOPATHIES<br/>[FR] N-BENZAMIDES D'ARYLE SUBSTITUÉS ET COMPOSÉS LIÉS POUR TRAITEMENT DES MALADIES AMYLOÏDES ET DES SYNUCLÉINOPATHIES
  申请人：PROTEOTECH INC

  公开号：WO2005113489A1

  公开（公告）日：2005-12-01

  Substituted diaryl compounds of the Formulae (I, II, III), where the variables are as defined in the claims, and their pharmaceutically acceptable derivatives, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aß amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided.

  根据权利要求中定义的变量，提供了公式（I，II，III）的取代二芳基化合物及其药学上可接受的衍生物，它们的合成，含有它们的药物组合物，以及它们在治疗淀粉样疾病中的用途，包括阿尔茨海默病中观察到的Aß淀粉样病变，如2型糖尿病中观察到的IAPP淀粉样病变，以及在帕金森病中观察到的α-突触核病变，并提供了用于制造这种治疗药物的方法。