N-acetyl-γ-aminobutyric acid N'-methylamide | 154656-89-0

• 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: N-acetyl-γ-aminobutyric acid N'-methylamide
• 英文别名: 4-Acetamido-N-methylbutanamide
• CAS: 154656-89-0
• 化学式: C₇H₁₄N₂O₂
• mdl: MFCD24388774
• 分子量: 158.2
• InChiKey: KCCKCJGGGZMKTM-UHFFFAOYSA-N

物化性质

• 沸点：
  438.6±28.0 °C(Predicted)
• 密度：
  1.014±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.714
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  tert-butyl (4-(methylamino)-4-oxobutyl)carbamate 在 盐酸 、 三乙胺 作用下， 以 1,4-二氧六环 为溶剂， 反应 20.0h， 生成 N-acetyl-γ-aminobutyric acid N'-methylamide
  参考文献：
  名称：

  Dado; Gellman, Journal of the American Chemical Society, 1994, vol. 116, # 3, p. 1054 - 1062

  摘要：

  DOI：

文献信息

• [EN] LINKERS FOR IMPROVING THE STABILITY OF BIOCONJUGATES AND THE SELECTIVITY OF PAYLOAD RELEASE<br/>[FR] LIEURS PERMETTANT D'AMÉLIORER LA STABILITÉ DE BIOCONJUGUÉS ET LA SÉLECTIVITÉ DE LIBÉRATION DE CHARGE UTILE
  申请人：EQIP LLC

  公开号：WO2022165335A1

  公开（公告）日：2022-08-04

  Disclosed herein are linker architectures for conjugates that do not rely on the SAR of the cleavable trigger or the large steric bulk of a closely positioned antibody to alter payload release. These linkers are expected to reduce off-target payload release facilitated by extracellular cathepsins, and may also be applicable to conjugates of antibody fragments that lack the steric protection from a full antibody. In addition, the linkers disclosed herein are expected to provide more selective intracellular payload release. Thus, these linkers can function synergistically with the targeting vector to confer differential payload release rates in vivo that improve the selectivity of intracellular payload release and reduce off target toxicity.

  本文揭示了一种连接体架构，用于结合物，不依赖于可切割触发器的SAR或临近抗体的大立体体积来改变荷载释放。预计这些连接剂将减少由细胞外半胱天蛋白酶促进的非靶向荷载释放，并且也适用于缺乏完整抗体的抗体片段的结合物。此外，本文揭示的连接剂预计提供更有选择性的细胞内荷载释放。因此，这些连接剂可以与靶向载体协同作用，以在体内提供不同的荷载释放速率，从而提高细胞内荷载释放的选择性并减少非靶向毒性。
• SUBSTITUTED PYRAZINONE DERIVATIVES AS ALPHA2C-ADRENORECEPTOR ANTAGONISTS
  申请人：Janssen Pharmaceutica N.V.

  公开号：EP1966191B1

  公开（公告）日：2010-03-17
• Substituted Pyrazinone Derivatives as Alpha2C-Adrenoreceptor Antagonists
  申请人：Andre-Gil Jose Ignacio

  公开号：US20080269251A1

  公开（公告）日：2008-10-30

  The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1 , having selective α 2C -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.
• Dado; Gellman, Journal of the American Chemical Society, 1994, vol. 116, # 3, p. 1054 - 1062
  作者：Dado、Gellman

  DOI：——

  日期：——