(3S,5S)-5-methylpiperidin-3-ol | 1101987-19-2

• 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: (3S,5S)-5-methylpiperidin-3-ol
• CAS: 1101987-19-2
• 化学式: C₆H₁₃NO
• 分子量: 115.175
• InChiKey: QDPYHRSTDJTFRG-WDSKDSINSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  8
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (3S,5S)-5-methylpiperidin-3-ol 在 戴斯-马丁氧化剂 、 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 生成 N-Boc-3-methyl-5-piperidone
  参考文献：
  名称：

  Core modification of substituted piperidines as Novel inhibitors of HDM2–p53 protein–protein interaction

  摘要：

  The discovery of 3,3-disubstituted piperidine 1 as novel p53-HDM2 inhibitors prompted us to implement subsequent SAR follow up directed towards piperidine core modifications. Conformational restrictions and further functionalization of the piperidine core were investigated as a strategy to gain additional interactions with HDM2. Substitutions at positions 4, 5 and 6 of the piperidine ring were explored. Although some substitutions were tolerated, no significant improvement in potency was observed compared to 1. Incorporation of an allyl side chain at position 2 provided a drastic improvement in binding potency. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.02.055
• 作为产物：
  描述：

  ((2R,4S)-1-benzyl-4-methylpyrrolidin-2-yl)methanol 在 palladium 10% on activated carbon 、 氢气 、 三氟乙酸酐 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 20.75h， 生成 (3S,5S)-5-methylpiperidin-3-ol
  参考文献：
  名称：

  Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

  摘要：

  DOI：

  10.1021/acs.jmedchem.1c02175

文献信息

• NOVEL HETEROCYCLYL COMPOUNDS
  申请人：Aebi Johannes

  公开号：US20110092698A1

  公开（公告）日：2011-04-21

  The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 7 , R 8 , R 9 , and R 10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.

  这项发明涉及式(I)的新颖双环化合物，其中n、m、p、A、L、R1、R2、R3、R4、R5、R6、R7、R7、R8、R9和R10如描述和索赔中所定义，并且其生理上可接受的盐。这些化合物是CCR2受体、CCR5受体和/或CCR3受体的拮抗剂，例如可用于预防和/或治疗炎症性疾病，特别是外周动脉闭塞疾病或动脉粥样硬化形成。
• [EN] DIAZEPAM DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTORS<br/>[FR] DÉRIVÉS DU DIAZÉPAM EN TANT QUE MODULATEURS DES RÉCEPTEURS DES CHIMIOKINES
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011048032A1

  公开（公告）日：2011-04-28

  The invention is concerned with novel bicyclic compounds of Formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9 and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.

  这项发明涉及公式（I）的新颖双环化合物，其中n、m、p、A、L、R1、R2、R3、R4、R5、R6、R7、R7、R8、R9和R10的定义如描述和索赔中所述，以及其生理上可接受的盐。这些化合物是CCR2受体、CCR5受体和/或CCR3受体的拮抗剂，可用作药物。
• Heterocyclyl compounds
  申请人：Aebi Johannes

  公开号：US08445674B2

  公开（公告）日：2013-05-21

  The invention is concerned with novel bicyclic compounds of formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, and R10 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor may be used, for example, in the prevention and/or treatment of inflammatory diseases, particularly peripheral arterial occlusive diseases or atherothrombosis.

  该发明涉及公式（I）的新型双环化合物，其中n、m、p、A、L、R1、R2、R3、R4、R5、R6、R7、R8、R9和R10如说明书和权利要求中所定义，并且它们的生理上可接受的盐。这些化合物是CCR2受体、CCR5受体和/或CCR3受体的拮抗剂，例如可用于预防和/或治疗炎症性疾病，特别是外周动脉闭塞病或动脉粥样硬化。
• [EN] 3-(1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND MEDICAL USES THEREOF<br/>[FR] DÉRIVÉS DE 3-(1-OXOISOINDOLIN-2-YL)PIPÉRIDINE-2,6-DIONE ET LEURS UTILISATIONS MÉDICALES
  申请人：NOVARTIS AG

  公开号：WO2022254362A1

  公开（公告）日：2022-12-08

  The application relates to compounds of formula (I), pharmaceutical compositions comprising them and their use in reducing Widely Interspaced Zinc Finger Motifs (WIZ) expression levels, or inducing fetal hemoglobin (HbF) expression, and in the treatment of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta- thalassemia.

  该申请涉及式(I)的化合物、包含它们的制药组合物以及它们在降低广泛间隔锌指结构基序（WIZ）表达水平、诱导胎儿血红蛋白（HbF）表达和治疗遗传性血液疾病（如血红蛋白病，如镰状细胞贫血和β-地中海贫血）方面的用途。
• NOVEL HETEROCYCLYL COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISEASE
  申请人：F. Hoffmann-La Roche AG

  公开号：EP2307387A1

  公开（公告）日：2011-04-13