3,4-dihydroxy-5-hydroxymethylpiperidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3,4-dihydroxy-5-hydroxymethylpiperidine
• 英文别名: 5-hydroxymethyl-3,4-piperidinediol；5-(Hydroxymethyl)piperidine-3,4-diol
• 化学式: C₆H₁₃NO₃
• 分子量: 147.174
• InChiKey: QPYJXFZUIJOGNX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.5
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  72.7
• 氢给体数：
  4
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  tert-butyl 3-((1R,2S,5R)-2-isopropyl-5-methyl-1-cyclohexyloxy)acetoxymethyl-4,5-epoxypiperidine-1-carboxylate 、 氢氧化钾 在 silica gel 、 异丙醇 作用下， 反应 3.0h， 以to give 5-hydroxymethyl-3,4-piperidinediol as an oil (Yield: 56 mg, 65%)的产率得到3,4-dihydroxy-5-hydroxymethylpiperidine
  参考文献：
  名称：

  Heterocyclic compounds

  摘要：

  提供了新型哌啶化合物，这些化合物可用于治疗和/或预防糖尿病，特别是非胰岛素依赖性糖尿病（NIDDM或2型糖尿病），包括夜间或餐后治疗以及治疗或预防长期并发症，如视网膜病变、神经病变、肾病、微血管和宏血管病变；治疗高血糖、高胆固醇血症、高血压、高胰岛素血症、高脂血症、动脉粥样硬化或心肌缺血。

  公开号：

  US06046214A1

文献信息

• Use of glycogen phosphorylase inhibitors for treatment of cardiovascular diseases
  申请人：——

  公开号：US20040082641A1

  公开（公告）日：2004-04-29

  The present invention provides methods of treatment and prevention of early cardiac and early cardiovascular diseases, for instance of ischemic origin, such as left ventricular hypertrophy, coronary artery disease, essential hypertension, acute hypertensive emergency, cardiomyopathy, heart insufficiency, exercise tolerance, chronic heart failure, arrhythmia, cardiac dysrhythmia, syncopy, arteriosclerosis, mild chronic heart failure, angina pectoris, cardiac bypass reocclusion, intermittent claudication (arteriosclerosis oblitterens), diastolic dysfunction and systolic dysfunction, as well as improving the success of heart transplantations, through administration of glycogen phosphorylase inhibitor compounds.

  本发明提供了治疗和预防早期心脏和早期心血管疾病的方法，例如缺血性疾病，如左心室肥大，冠状动脉疾病，高血压，急性高血压紧急情况，心肌病，心力衰竭，运动耐受性，慢性心力衰竭，心律失常，心脏心律失常，晕厥，动脉硬化，轻度慢性心力衰竭，心绞痛，心脏旁路再闭塞，间歇性跛行（闭塞性动脉硬化），舒张功能和收缩功能障碍，以及通过给予糖原磷酸化酶抑制剂化合物来提高心脏移植的成功率。
• [EN] PIPERIDINES AND PYRROLIDINES<br/>[FR] PIPERIDINES ET PYRROLIDINES
  申请人：NOVO NORDISK A/S

  公开号：WO1995024391A1

  公开（公告）日：1995-09-14

  (EN) Compounds (I) and (II), the use of these compounds as medicament, the use of these medicaments in the treatment of diabetes and pharmaceutical compositions containing these compounds.(FR) Composés (I) et (II), leur utilisation comme médicaments, utilisation de ces médicaments pour le traitement du diabète et compositions pharmaceutiques renfermant ces composés.

  (EN) 化合物（I）和（II），这些化合物作为药物的使用，这些药物在糖尿病治疗中的使用以及含有这些化合物的制药组合物。 (FR) 化合物（I）和（II），这些化合物作为药物的使用，这些药物在糖尿病治疗中的使用以及含有这些化合物的制药组合物。
• METHOD FOR THE TREATMENT OF NEUROLOGICAL DISORDERS BY ENHANCING THE ACTIVITY OF BETA-GLUCOCEREBROSIDASE
  申请人：Wustman Alan Brandon

  公开号：US20080009516A1

  公开（公告）日：2008-01-10

  Provided is a method of increasing the stability of wild-type β-glucocerebrosidase. Also provided are methods of treating and/or preventing an individual having a neurological disease in which increased expression or activity of β-glucocerebrosidase in the central nervous system would be beneficial. This method comprises administering an effective amount of a pharmacologic chaperone for β-glucocerebrosidase, with the proviso that the individual does not have a mutation in the gene encoding β-glucocerebrosidase. Further provided are β-glucocerebrosidase inhibitors which have been identified as specific pharmacologic chaperones and which have been shown to increase activity of β-glucocerebrosidase in vivo in the central nervous system.

  提供了一种增加野生型β-葡萄糖苷酶稳定性的方法。同时，提供了一种治疗和/或预防神经系统疾病的方法，其中在中枢神经系统中增加β-葡萄糖苷酶的表达或活性将有益。该方法包括给予β-葡萄糖苷酶的药理伴侣的有效剂量，但前提是该个体没有β-葡萄糖苷酶编码基因的突变。进一步提供了β-葡萄糖苷酶抑制剂，这些抑制剂已被确定为特定的药理伴侣，并已被证明在中枢神经系统内增加β-葡萄糖苷酶的活性。
• Method for the Treatment of Neurological Disorders by Enhancing the Activity of Beta-Glucocerebrosidase
  申请人：Amicus Therapeutics, Inc.

  公开号：US20150025109A1

  公开（公告）日：2015-01-22

  Provided is a method of increasing the stability of wild-type β-glucocerebrosidase. Also provided are methods of treating and/or preventing an individual having a neurological disease in which increased expression or activity of β-glucocerebrosidase in the central nervous system would be beneficial. This method comprises administering an effective amount of a pharmacologic chaperone for β-glucocerebrosidase, with the proviso that the individual does not have a mutation in the gene encoding β-glucocerebrosidase. Further provided are β-glucocerebrosidase inhibitors which have been identified as specific pharmacologic chaperones and which have been shown to increase activity of β-glucocerebrosidase in vivo in the central nervous system.

  提供了一种增加野生型β-葡萄糖苷酶稳定性的方法。还提供了治疗和/或预防神经系统疾病的方法，其中在中枢神经系统中增加β-葡萄糖苷酶的表达或活性将有益。该方法包括给予β-葡萄糖苷酶药理伴侣的有效剂量，前提是个体没有β-葡萄糖苷酶编码基因的突变。此外，还提供了已被确定为特定药理伴侣并已被证明能够在中枢神经系统中增加β-葡萄糖苷酶活性的β-葡萄糖苷酶抑制剂。
• 2-ACYLAMINOPROPANOL COMPOUND AND MEDICINAL COMPOSITION
  申请人：SEIKAGAKU CORPORATION

  公开号：EP0765865A1

  公开（公告）日：1997-04-02

  This invention relates to a 2-acylaminopropanol compound represented by the formula (I): (wherein R1 represents a phenyl group which may be substituted by 1 to 3 same or different substituents selected from alkyl, alkoxy, hydroxyl, hydroxyalkyl and nitro, R2 represents the following formula (II), (III), (IV), (V) or (VI), (wherein R3, R4, R5, R6, R7, R8, R9, m and p are those defined in the specification) R11 represents a hydrogen atom or a hydroxyl group, and n represents an integer of 3 to 15) or a pharmaceutically acceptable salt thereof.

  本发明涉及一种由式（I）代表的 2-酰基氨基丙醇化合物： (其中 R1 代表可被 1 至 3 个相同或不同的选自烷基、烷氧基、羟基、羟烷基和硝基的取代基取代的苯基，R2 代表下式（II）、（III）、（IV）、（V）或（VI）、 (其中 R3、R4、R5、R6、R7、R8、R9、m 和 p 是本说明书中定义的）。 R11 代表氢原子或羟基，n 代表 3 至 15 的整数) 或其药学上可接受的盐。