2-methylamino-1-phenyl-propanediol-(1.3) | 100132-16-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-methylamino-1-phenyl-propanediol-(1.3)
• 英文别名: 2-Methylamino-1-phenyl-propandiol-(1.3)；2-(Methylamino)-1-phenylpropane-1,3-diol
• CAS: 100132-16-9
• 化学式: C₁₀H₁₅NO₂
• 分子量: 181.235
• InChiKey: SOKBWEQHPUIPMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  52.5
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Rapamycin peptides conjugates: synthesis and uses thereof
  申请人：Sharma K. Sanjay

  公开号：US20070129394A1

  公开（公告）日：2007-06-07

  The present invention relates to new rapamycin derivatives for the inhibition of cell proliferation. The compounds can advantageously target two proteins in dividing cells and interfere with cell cycle. There is thus provided derivatives of rapamycin in which the 42 position of rapamycin is linked to an amino acid or a peptide through a carbamate ester linkage. These rapamycin derivatives can be synthesized by reacting 42-O-(4-Nitrophenoxycarbonyl) rapamycin and an amino acid or a free amino peptide under basic conditions. These rapamycin derivatives can be used to inhibit the cell cycle and are therefore useful for treating cell proliferation disorders.

  本发明涉及新的雷帕霉素衍生物，用于抑制细胞增殖。这些化合物可以有利地靶向分裂细胞中的两种蛋白质并干扰细胞周期。因此提供了雷帕霉素衍生物，其中雷帕霉素的42位通过氨基酸或肽的氨基甲酸酯键连接。这些雷帕霉素衍生物可以通过在碱性条件下反应42-O-(4-硝基苯氧羰基)雷帕霉素和氨基酸或自由氨基肽来合成。这些雷帕霉素衍生物可以用于抑制细胞周期，因此对于治疗细胞增殖性疾病非常有用。
• 8-ARM POLYETHYLENE GLYCOL DERIVATIVE, MANUFACTURING METHOD AND MODIFIED BIO-RELATED SUBSTANCE THEREBY
  申请人：Xiamen Sinopeg Biotech Co., Ltd.

  公开号：EP3315531A1

  公开（公告）日：2018-05-02

  Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups Ec form a highly symmetric octavalent central structure CORE0 together, Lc connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n1-n8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k ≥ 1), and said PEG chain and F can be directly connected (g = 0) or connected with a divalent linking group L0 connected with a terminal branched group G (g = 1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.

  本发明公开了一种 8 臂聚乙二醇（PEG）衍生物（式 1）、其制造方法和改性生物相关物质，其中一个四价基团 U 和四个三价基团 Ec 共同形成一个高度对称的八价中心结构 CORE0，Lc 将八价中心连接到八个 PEG 臂上，这些 PEG 臂具有多元性或单元性，其聚合度为 n1-n8。一条 PEG 链的末端与至少一个官能团 F（k ≥ 1）相连，所述 PEG 链和 F 可以直接相连（g = 0），也可以通过二价连接基 L0 与中间的末端支化基 G（g = 1）相连。后者提供了更多的反应位点，可以结合更多的药物分子，从而提高药物负载能力。衍生物的近中心对称结构可以在大规模生产过程中更精确地控制分子量，从而有利于获得分子量分布更窄的产品。由此改性的生物相关物质具有更均匀、更可控的性能。
• US7659244B2
  申请人：——

  公开号：US7659244B2

  公开（公告）日：2010-02-09