(6-methyl-3-pyridyl)(2-propynylamino)methanaldehyde | 1247059-46-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: (6-methyl-3-pyridyl)(2-propynylamino)methanaldehyde
• 英文别名: (6-methyl-3-pyridyl)(2-propynylamino)formaldehyde；6-methyl-N-prop-2-ynylpyridine-3-carboxamide
• CAS: 1247059-46-6
• 化学式: C₁₀H₁₀N₂O
• 分子量: 174.202
• InChiKey: CFFNWDOTMCREEO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (6-methyl-3-pyridyl)(2-propynylamino)methanaldehyde 、 (2S,3S,4R,5R,6R)-3-azido-4,5-bis(benzyloxy)-6-((benzyloxy)methyl)-2-methyltetrahydro-2H-pyran 在 copper(II) sulfate 、 sodium ascorbate 作用下， 以 甲醇 、 水 为溶剂， 生成
  参考文献：
  名称：

  Glycomimetic Ligands for the Human Asialoglycoprotein Receptor

  摘要：

  The asialoglycoprotein receptor (ASGPR) is a high-capacity galactose-binding receptor expressed on hepatocytes that binds its native substrates with low affinity. More potent ligands are of interest for hepatic delivery of therapeutic agents. We report several classes of galactosyl analogues with varied substitution at the anomeric, C2-, C5-, and C6-positions. Significant increases in binding affinity were noted for several trifluoromethyl-acetamide derivatives without covalent attachment to the protein. A variety of new ligands were obtained with affinity for ASGPR as good as or better than that of the parent N-acetylgalactosamine, showing that modification on either side of the key C3,C4-diol moiety is well tolerated, consistent with previous models of a shallow binding pocket. The galactosyl pyranose motif therefore offers many opportunities for the attachment of other functional units or payloads while retaining low-micromolar or better affinity for the ASGPR.

  DOI：

  10.1021/ja2104679

文献信息

• METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
  申请人：PMV Pharmaceuticals, Inc.

  公开号：US20170240525A1

  公开（公告）日：2017-08-24

  Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

  癌基因和肿瘤抑制基因的突变促成了癌症的发展和进展。本公开披露描述了一种化合物和方法，用于恢复p53突变体的野生型功能。本发明的化合物可以结合突变型p53，并恢复p53突变体结合DNA并激活参与肿瘤抑制的下游效应子的能力。所披露的化合物可用于减少含有p53突变的癌症的进展。
• Methods and compounds for restoring mutant p53 function
  申请人：PMV Pharmaceuticals, Inc.

  公开号：US10138219B2

  公开（公告）日：2018-11-27

  Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.

  癌基因和肿瘤抑制因子的突变会导致癌症的发生和发展。本发明公开了使 p53 突变体恢复野生型功能的化合物和方法。本发明的化合物可与突变 p53 结合，恢复 p53 突变体结合 DNA 和激活参与肿瘤抑制的下游效应因子的能力。所公开的化合物可用于减少含有 p53 突变的癌症的恶化。
• PPAR agonists, compounds, pharmaceutical compositions, and methods of use thereof
  申请人：Mitobridge, Inc.

  公开号：US10399958B2

  公开（公告）日：2019-09-03

  Provided herein are compounds I, II or III and compositions useful in increasing PPAR8 activity. The compounds and compositions provided herein are useful for the treatment of PPAR8 related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

  本文提供了可提高 PPAR8 活性的化合物 I、II 或 III 及组合物。本文提供的化合物和组合物可用于治疗 PPAR8 相关疾病（如肌肉疾病、血管疾病、脱髓鞘疾病和代谢性疾病）。
• Crystalline and salt forms of PPAR agonist compounds
  申请人：Mitobridge, Inc.

  公开号：US10927094B2

  公开（公告）日：2021-02-23

  This disclosure relates to salt forms of compounds capable of activating PPARδ for use in drug substance and drug product development, and related compositions and methods.

  本公开涉及能够激活 PPARδ 的化合物的盐形式，用于药物物质和药物产品的开发，以及相关的组合物和方法。
• Nicotinic Acid and Picolinic Acid Derived Near-Infrared Fluorophores
  申请人：VisEn Medical, Inc.

  公开号：US20130272967A1

  公开（公告）日：2013-10-17

  This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.