p-((Aminophenyl)sulfonyl)phenol

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: p-((Aminophenyl)sulfonyl)phenol
• 英文别名: 4-(2-aminophenyl)sulfonylphenol
• 化学式: C₁₂H₁₁NO₃S
• 分子量: 249.29
• InChiKey: YYHDBOAKEXXMPX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  88.8
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT6 RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS DE FLUOROPIPÉRIDINE UTILISÉS EN TANT QU'ANTAGONISTES PURS DU RÉCEPTEUR 5-HT 6
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2019030641A1

  公开（公告）日：2019-02-14

  The present invention relates to fluoropiperidine compounds of formula (I), their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof as 5-HT6 receptor antagonists. In particular the present invention discloses the methods of preparation, pharmaceutical composition, combinations and use of fluoropiperidine compounds, their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof. In formula (I), R1 represents phenyl or pyridyl; wherein the phenyl or pyridyl is optionally substituted with one or more groups selected from halogen, (C1-6)-alkyl or halo(C1-6 )-alkyl; R2 represents hydrogen or (C1-6)-alkyl; R3 represents hydrogen or (C1-6)-alkyl; or R2 and R3 can combine together to form (C3-6)- cycloalkyl; R4 represents hydrogen, (C1-6)-alkyl or halo(C1-6)-alkyl; R5 represents hydrogen, (C1-6)-alkyl, halo(C1-6)-alkyl or -(CH2)0-3- (C3-6)-cycloalkyl. The compounds can be used in the treatment of cognitive disorder mediated by the 5-Hydroxytryptamine 6 receptor, wherein said cognitive disorder is selected from the group consisting of dementia in Alzheimer's disease, dementia in Parkinson's disease, dementia in Huntington's disease, dementia associated with Down syndrome, dementia associated with Tourette's syndrome, dementia associated with post menopause, frontotemporal dementia, Lewy body dementia, Vascular dementia, dementia in HIV, dementia in Creutzfeldt-Jakob disease, substance-induced persisting dementia, dementia in Pick's disease, dementia in schizophrenia, dementia in general medical conditions and senile dementia.

  本发明涉及式(I)的氟哌啶化合物，其立体异构体、同位素形式或药学上可接受的盐作为5-HT6受体拮抗剂。特别是，本发明公开了氟哌啶化合物、其立体异构体、同位素形式或药学上可接受的盐的制备方法、药物组合物、组合及其用途。在式(I)中，R1代表苯基或吡啶基；其中苯基或吡啶基任选地被一个或多个选自卤素、(C1-6)-烷基或卤代(C1-6)-烷基的基团取代；R2代表氢或(C1-6)-烷基；R3代表氢或(C1-6)-烷基；或者R2和R3可以结合在一起形成(C3-6)-环烷基；R4代表氢、(C1-6)-烷基或卤代(C1-6)-烷基；R5代表氢、(C1-6)-烷基、卤代(C1-6)-烷基或-(CH2)0-3-(C3-6)-环烷基。这些化合物可用于治疗由5-羟色胺6受体介导的认知障碍，其中所述认知障碍选自阿尔茨海默病中的痴呆、帕金森病中的痴呆、亨廷顿病中的痴呆、唐氏综合症相关的痴呆、图雷特综合症相关的痴呆、绝经后痴呆、额颞叶痴呆、路易体痴呆、血管性痴呆、HIV中的痴呆、克雅氏病中的痴呆、物质诱发的持续性痴呆、皮克病中的痴呆、精神分裂症中的痴呆、一般医疗条件下的痴呆和老年性痴呆。
• Fluoropiperidine compounds as pure 5-HT 6 receptor antagonists
  申请人：SUVEN LIFE SCIENCES LIMITED

  公开号：US10973831B2

  公开（公告）日：2021-04-13

  The present invention relates to fluoropiperidine compounds of formula (I), their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof as 5-HT6 receptor antagonists. In particular the present invention discloses the methods of preparation, pharmaceutical composition, combinations and use of fluoropiperidine compounds, their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof.

  本发明涉及作为 5-HT6 受体拮抗剂的式 (I) 氟哌啶化合物、其立体异构体、同位素形式或其药学上可接受的盐。特别是本发明公开了氟哌啶化合物、其立体异构体、同位素形式或其药学上可接受的盐的制备方法、药物组合、组合物和用途。
• FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT6 RECEPTOR ANTAGONISTS
  申请人：Suven Life Sciences Limited

  公开号：EP3649124A1

  公开（公告）日：2020-05-13
• FLUOROPIPERIDINE COMPOUNDS AS PURE 5-HT 6 RECEPTOR ANTAGONISTS
  申请人：SUVEN LIFE SCIENCES LIMITED

  公开号：US20200155560A1

  公开（公告）日：2020-05-21

  The present invention relates to fluoropiperidine compounds of formula (I), their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof as 5-HT6 receptor antagonists. In particular the present invention discloses the methods of preparation, pharmaceutical composition, combinations and use of fluoropiperidine compounds, their stereoisomers, isotopic forms or pharmaceutically acceptable salts thereof.