(2S,6S)-6-(hydroxymethyl)piperidine-2-carboxylic acid

• 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: (2S,6S)-6-(hydroxymethyl)piperidine-2-carboxylic acid
• 化学式: C₇H₁₃NO₃
• 分子量: 159.18
• InChiKey: OIHIUNWHKBRWJW-WDSKDSINSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.6
• 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

文献信息

• Purine derivative compounds for medical use
  申请人：Manros Therapeutics

  公开号：EP2907514A1

  公开（公告）日：2015-08-19

  The present invention relates to a compound of formula (I): wherein A is N or CH; B is N O, or S; R1 is H, a (C1-C4)alkyl group, a methyl(C1-C6)cycloalkyl group or a (C1-C6)cycloalkyl group; R2 is an aryl, an arylmethyl group or a methylheteroaryl group such as methylpyridine and methylthiophene; R3 is absent when B is O or S, or is H or a (C1-C4)alkyl group when B is N; R4 is a (C1-C5)alkyl group or a (C1-C4)cycloalkyl group, each group bearing a carboxylic acid group, and said (C1-C5)alkyl group or (C1-C4)cycloalkyl being optionally substituted by a hydroxyl group, a halogen group or a methoxy group, and when B is N, R3 and R4 can together form a 5- or 6-membered heterocycle substituted by a carboxylic acid group, and optionally substituted by a halogen atom, a hydroxyl group, a methoxy group or a hydroxymethyl group, or anyone of its pharmaceutically acceptable salt, for use in the treatment of a disease characterized by a reduction in macrophage-mediated bacterial killing. The present invention further relates to a few compounds which are new to the corresponding pharmaceutical composition for the same use.

  本发明涉及一种式 (I) 的化合物： 其中 A 是 N 或 CH；B 是 N O 或 S；R1 是 H、(C1-C4)烷基、甲基(C1-C6)环烷基或(C1-C6)环烷基；R2 是芳基、芳甲基或甲基杂芳基，如甲基吡啶和甲基噻吩；当 B 是 O 或 S 时，R3 不存在，当 B 是 N 时，R3 是 H 或(C1-C4)烷基；R4是(C1-C5)烷基或(C1-C4)环烷基，每个基团都带有一个羧酸基，所述(C1-C5)烷基或(C1-C4)环烷基可选择被羟基、卤素基或甲氧基取代，当 B 为 N 时，R3 和 R4 可共同形成一个被羧酸基取代的 5 或 6 元杂环、和任选被卤原子、羟基、甲氧基或羟甲基取代的杂环，或其任何药学上可接受的盐，用于治疗以巨噬细胞介导的细菌杀伤力降低为特征的疾病。 本发明进一步涉及一些化合物，它们是用于相同用途的相应药物组合物的新化合物。