3,6-dimethoxy-5,5-dimethyl-2-propan-2-yl-2H-pyrazine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 甲亚胺酸及其衍生物
• 英文名称: 3,6-dimethoxy-5,5-dimethyl-2-propan-2-yl-2H-pyrazine
• 化学式: C₁₁H₂₀N₂O₂
• 分子量: 212.29
• InChiKey: MAZVAPTXLQRRNV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  43.2
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Stapled and stitched polypeptides and uses thereof
  申请人：President and Fellows of Harvard College

  公开号：US11332496B2

  公开（公告）日：2022-05-17

  The present invention provides stapled polypeptides of the Formulae (I) and (VI): and salts thereof; wherein the groups ; R1a, R1b, R1c, R2a, R3a, R2b, R3b, R4a, R4b, RA, RZ, L1a, L1b, L2, L3, XAA, v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.

  本发明提供了式 (I) 和 (VI) 的钉状多肽： 及其盐；其中基团；R1a、R1b、R1c、R2a、R3a、R2b、R3b、R4a、R4b、RA、RZ、L1a、L1b、L2、L3、XAA、v、w、p、m、s、n、t 和 q 如本文所定义。本发明进一步提供了从非钉书钉多肽前体制备本发明钉书钉多肽的方法。本发明进一步提供了包含式（I）或（VI）的钉状多肽的药物组合物，以及使用钉状多肽的方法。本发明还提供了闭环偏析后对钉状多肽的修饰。
• STAPLED AND STITCHED POLYPEPTIDES AND USES THEREOF
  申请人：President and Fellows of Harvard College

  公开号：US20190202862A1

  公开（公告）日：2019-07-04

  The present invention provides stapled polypeptides of the Formulae (I) and (VI): and salts thereof; wherein the groups ; R 1a , R 1b , R 1c , R 2a , R 3a , R 2b , R 3b , R 4a , R 4b , R A , R Z , L 1a , L 1b , L 2 , L 3 , X AA , v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.