6-Quinoxalineacetaldehyde | 545424-00-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-Quinoxalineacetaldehyde
• 英文别名: 2-quinoxalin-6-ylacetaldehyde
• CAS: 545424-00-8
• 化学式: C₁₀H₈N₂O
• 分子量: 172.18
• InChiKey: IHEGPKBBLFPXHA-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：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  42.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] MONOCYCLIC OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA MONOCYCLIQUE
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2018109202A1

  公开（公告）日：2018-06-21

  The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

  本发明涉及O-GlcNAc水解酶（OGA）抑制剂。该发明还涉及包含这类化合物的药物组合物，用于制备这类化合物和组合物的方法，以及这类化合物和组合物在抑制OGA有益的疾病的预防和治疗中的用途，例如tau病变，特别是阿尔茨海默病或进行性上核性麻痹症；以及伴有tau病理的神经退行性疾病，特别是由C9ORF72突变引起的肌萎缩侧索硬化症或前颞叶痴呆症。
• [EN] OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2018141984A1

  公开（公告）日：2018-08-09

  The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors of Formulas (I) and (II). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.

  本发明涉及具有式(I)和(II)的O-GlcNAc水解酶（OGA）抑制剂。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的过程，以及利用这些化合物和组合物预防和治疗OGA抑制对其有益的疾病的用途，如tau病变，特别是阿尔茨海默病或进行性上行性麻痹; 伴有tau病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩性侧索硬化或额颞叶痴呆。
• [EN] 6-O-ACYL KETOLIDE DERIVATIVES OF ERYTHROMYCINE USEFUL AS ANTIBACTERIALS<br/>[FR] DERIVES DE 6-O-ACYL CETOLIDE D'ERYTHROMYCINE UTILES COMME AGENTS ANTI-BACTERIENS
  申请人：ORTHO MCNEIL PHARM INC

  公开号：WO2003050132A1

  公开（公告）日：2003-06-19

  6-O-Acyl ketolide antibacterials of formula (I): wherein R?1, R2, R3, R4¿, W, X, X', Y, and Y' are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

  公式（I）中的6-O-Acyl ketolide抗菌剂：其中R?1，R2，R3，R4¿，W，X，X'，Y和Y'如本文所述，并且其中取代基的含义如说明中所示。这些化合物可用作抗菌剂。
• NOVEL PYRAZOLE DERIVATIVE AS ALK5 INHIBITOR AND USES THEREOF
  申请人：Hanmi Pharmaceutical Co., Ltd.

  公开号：EP3480193A1

  公开（公告）日：2019-05-08

  The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.

  本公开涉及一种新型取代的吡唑衍生物，该衍生物具有抑制以 TGF-β 受体 ALK5 为靶点的丝氨酸/苏氨酸激酶活性的作用，包括本公开化合物作为活性成分的药物组合物可用于预防和/或治疗癌症、自身免疫性疾病、纤维化疾病、炎症性疾病、神经退行性疾病、传染性疾病、肺部疾病、心血管疾病或代谢性疾病，或其他与 TGF 家族信号活性降低有关的疾病。
• Pyrazole derivative as ALK5 inhibitor and uses thereof
  申请人：HANMI PHARMACEUTICAL CO., LTD.

  公开号：US10954232B2

  公开（公告）日：2021-03-23

  The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.

  本公开涉及一种新型取代的吡唑衍生物，该衍生物具有抑制以 TGF-β 受体 ALK5 为靶点的丝氨酸/苏氨酸激酶活性的作用，包括本公开化合物作为活性成分的药物组合物可用于预防和/或治疗癌症、自身免疫性疾病、纤维化疾病、炎症性疾病、神经退行性疾病、传染性疾病、肺部疾病、心血管疾病或代谢性疾病，或其他与 TGF 家族信号活性降低有关的疾病。