2-(4-hydroxypiperidin-4-yl)acetic acid | 328401-29-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-(4-hydroxypiperidin-4-yl)acetic acid
• CAS: 328401-29-2
• 化学式: C₇H₁₃NO₃
• 分子量: 159.185
• InChiKey: LOVXIGLSLONCIB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(4-hydroxypiperidin-4-yl)acetic acid 在 哌啶 、 sodium carbonate 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 水 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 23.17h， 生成 tert-butyl ((1-(5-((2-chloro-3-(2-(4-hydroxypiperidin-4-yl)acetamido)phenyl)thio)pyrazin-2-yl)-4-methylpiperidin-4-yl)methyl)carbamate
  参考文献：
  名称：

  [EN] COMPOUND HAVING SHP2 PROTEIN DEGRADING ACTIVITY, AND MEDICAL USES THEREOF
  [FR] COMPOSÉ AYANT UNE ACTIVITÉ DE DÉGRADATION DE LA PROTÉINE SHP2 ET SES UTILISATIONS MÉDICALES
  [KO] SHP2 단백질 분해활성을 갖는 화합물 및 이들의 의약 용도

  摘要：

  본 개시는 SHP2를 분해하는 측면에서 우수한 활성을 갖는 특정 화학구조의 화합물 또는 이의 약학적으로 허용 가능한 염을 제공한다. 본 개시는 또한 이러한 화합물 또는 이의 약학적으로 허용 가능한 염을 포함하는 조성물을 제공한다. 본 개시는 또한 본 개시에 따른 화합물, 이의 염 및 이들을 포함하는 조성물의 SHP2 관련 질환(예를 들어, 암)의 치료 또는 예방용 의약 용도를 제공한다. 본 개시는 또한 본 개시에 따른 화합물, 이의 염 또는 이들을 포함하는 조성물의 유효한 양을 치료가 필요한 개체에게 투여하는 것을 포함하는 SHP2 관련 질환(예를 들어, 암)의 치료 또는 예방 방법을 제공한다.

  公开号：

  WO2023018155A1

文献信息

• [EN] PYRAZOLO [1, 5-A] PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS<br/>[FR] DÉRIVÉS PYRAZOLO[1, 5-A]PYRIMIDINE EN TANT QU'INHIBITEURS DE MTOR
  申请人：SCHERING CORP

  公开号：WO2010118207A1

  公开（公告）日：2010-10-14

  The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.

  本发明提供了使用吡唑并[1,5-a]嘧啶化合物抑制 mTOR 的方法，以及利用这些化合物治疗、预防、抑制或改善与 mTOR 相关的一种或多种疾病的方法。
• 4-hydroxypiperidine derivatives having antiarrhythmic activity
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：US20020188006A1

  公开（公告）日：2002-12-12

  The present invention relates to a compound represented by the following formula (I) or a salt thereof, or a pharmaceutical composition containing the compound as an effective ingredient: 1 (wherein A represents, for example, phenyl group substituted with R 1 and R 2 or unsubstituted thienyl group; R 1 and R 2 each independently represent, for example, hydrogen atom, halogen atom or lower alkoxycarbonyl group; R 3 represents, for example, hydrogen atom; R 4 represents, For example, lower alkyl group; R 5 represents, for example, lower alkoxy group; R 6 represents, for example, hydrogen atom; R 7 and R 8 each represent, for example, hydrogen atom, respectively; X represents, for example, a single bond; Y represents, for example, methylene group or benzylidene group substituted with R 1 ; and Z represents, for example, methylene group.) The compounds according to the present invention that do not suppress the transient sodium current of the cardiac muscle and do not manifest proarrhythimic activity is useful as a therapeutic agent for preventing and/or treating arrhythimia and for preventing sudden death.

  本发明涉及以下式(I)所表示的化合物或其盐，或含有该化合物作为有效成分的药物组合物：1（其中A代表例如被R1和R2取代的苯基或未被取代的噻吩基；R1和R2各自独立地代表例如氢原子、卤素原子或低碳酸酯基；R3代表例如氢原子；R4代表例如低烷基基团；R5代表例如低烷氧基团；R6代表例如氢原子；R7和R8各自代表例如氢原子；X代表例如单键；Y代表例如被R1取代的亚甲基基团或苄亚甲基基团；以及Z代表例如亚甲基基团。）本发明的化合物不抑制心肌瞬时钠电流，也不表现出致心律失常活性，因此可用作预防和/或治疗心律不齐和预防猝死的治疗剂。
• Benzoxazepine compounds, their production and use
  申请人：Yukimasa Hidefumi

  公开号：US20070117787A1

  公开（公告）日：2007-05-24

  This invention provides new benzoxazepine compounds represented by the formula: [wherein R stands for a lower alkyl group optionally substituted with a hydroxyl group, X stands for an optionally substituted carbamoyl group or an optionally substituted heterocyclic group having a deprotonatable hydrogen atom, R 1 stands for a lower alkyl group and W stands for a halogen atom] having activities of lowering cholesterol-level and lowering triglyceride-level, and being useful for prophylaxis and therapy of hyperlipidemia.

  本发明提供了一种新的苯并噁唑化合物，其表示为以下式子：[其中R代表可选地取代羟基的低碳基，X代表可选地取代的氨基甲酰基或具有可去质子氢原子的可选地取代的杂环基，R1代表低碳基，W代表卤素原子]，具有降低胆固醇水平和降低甘油三酯水平的活性，适用于预防和治疗高脂血症。
• [EN] THERAPEUTICS FOR THE DEGRADATION OF MUTANT BRAF<br/>[FR] AGENTS THÉRAPEUTIQUES POUR LA DÉGRADATION DE BRAF MUTANTE
  申请人：C4 THERAPEUTICS INC

  公开号：WO2022261250A1

  公开（公告）日：2022-12-15

  The present invention provides compounds or their pharmaceutically acceptable salts and their pharmaceutical compositions that can be administered to a host such as a human in need thereof for the treatment of a disorder, such as cancer, mediated by mutant BRAF. The compounds efficiently degrade Class I, II and III mutant BRAF proteins.

  本发明提供了化合物或其药学上可接受的盐类及其药物组合物，这些化合物或其药学上可接受的盐类及其药物组合物可施用给需要的宿主（如人类），用于治疗由突变 BRAF 介导的疾病（如癌症）。这些化合物能有效降解 I、II 和 III 类突变 BRAF 蛋白。
• 4-HYDROXYPIPERIDINE DERIVATIVES HAVING ANTIARRHYTHMIC EFFECT
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP1182192A1

  公开（公告）日：2002-02-27

  The present invention relates to a compound represented by the following formula (I) or a salt thereof, or a pharmaceutical composition containing the compound as an effective ingredient: (wherein A represents, for example, phenyl group substituted with R1 and R2 or unsubstituted thienyl group; R1 and R2 each independently represent, for example, hydrogen atom, halogen atom or lower alkoxycarbonyl group; R3 represents, for example, hydrogen atom; R4 represents, for example, lower alkyl group; R5 represents, for example, lower alkoxy group; R6 represents, for example, hydrogen atom; R7 and R8 each represent, for example, hydrogen atom, respectively; X represents, for example, a single bond; Y represents, for example, methylene group or benzylidene group substituted with R1; and Z represents, for example, methylene group.) The compounds according to the present invention that do not suppress the transient sodium current of the cardiac muscle and do not manifest proarrhythimic activity is useful as a therapeutic agent for preventing and/or treating arrhythimia and for preventing sudden death.

  本发明涉及下式(I)代表的化合物或其盐，或含有该化合物作为有效成分的药物组合物： (其中 A 代表例如被 R1 和 R2 取代的苯基或未取代的噻吩基；R1 和 R2 各自独立地代表例如氢原子、卤素原子或低级烷氧羰基；R3 代表例如氢原子；R4 代表例如低级烷基；R5 代表例如低级烷氧基； R6 代表例如氢原子； R7 和 R8 分别代表例如氢原子； X 代表例如单键； Y 代表例如亚甲基或被 R1 取代的亚苄基；以及 Z 代表例如亚甲基。)根据本发明的化合物不抑制心肌的瞬态钠电流，不表现出促心律失常活性，可作为预防和/或治疗心律失常和预防猝死的治疗剂。