6-甲基咪唑并[1,2-a]吡嗪-2-羧酸 | 190381-48-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡嗪类
• 中文名称: 6-甲基咪唑并[1,2-a]吡嗪-2-羧酸
• 英文名称: 6-methylimidazo[1,2-a]pyrazine-2-carboxylic acid
• CAS: 190381-48-7
• 化学式: C₈H₇N₃O₂
• 分子量: 177.162
• InChiKey: KENGYTNARRJVIB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  67.5
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氨基-5-甲基吡嗪 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 6.0h， 生成 6-甲基咪唑并[1,2-a]吡嗪-2-羧酸
  参考文献：
  名称：

  Research on heterocyclic compounds. XXXVII. Synthesis and antiinflammatory activity of methyl-substituted imidazo[1,2-a]pyrazine derivatives

  摘要：

  A series of methyl-substituted imidazo[1,2-a]pyrazines 8 bearing a carboxylic acid group on the imidazole ring were synthesized. The structures of new compounds were confirmed by H-1- and C-13-NMR spectral data; the correct assignment of carbon resonances was made by means of HETCOR and COLOC experiments. Antiinflammatory, analgesic and ulcerogenic activities in vivo were evaluated and compared with those of antiinflammatory imidazopyrazines (2 and 3) and indomethacin. The inhibitory action on cyclooxygenase activity was evaluated in vitro. Compounds 8 were found to be less potent than indomethacin in these assays. SARs are discussed.

  DOI：

  10.1016/s0223-5234(97)83971-2

文献信息

• [EN] HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE PRMT5
  申请人：JUBILANT BIOSYS LTD

  公开号：WO2019102494A1

  公开（公告）日：2019-05-31

  The compounds of Formula I, Formula Ia, and Formula Ib are described herein along with their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds inhibit PRMT5 and are useful as therpeautic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, Parkinson's disease and the like.

  公式I、公式Ia和公式Ib的化合物以及它们的类似物、互变异构体、对映异构体、多态性、水合物、溶剂化物、药物可接受的盐、药物组合物、代谢物和前药在本文件中进行了描述。这些化合物抑制PRMT5，并可作为治疗或改善与细胞生长相关的疾病，如恶性肿瘤、精神分裂症、阿尔茨海默病、帕金森病等的治疗或改善剂。
• PEPTIDE COMPOUND AND METHOD FOR PRODUCING SAME, COMPOSITION FOR SCREENING USE, AND METHOD FOR SELECTING PEPTIDE COMPOUND
  申请人：FUJIFILM Corporation

  公开号：EP3604326A1

  公开（公告）日：2020-02-05

  An object of the present invention is to provide a novel cyclic peptide compound excellent in cell membrane permeability, a method for producing the same, a composition for screening use, and a method for selecting a cyclic peptide compound that binds to a target substance. According to the present invention, a peptide compound represented by Formula (1) or a salt thereof is provided. In the formula, the symbols have the meanings as defined in the specification of the present application.

  本发明的目的是提供一种细胞膜渗透性极佳的新型环肽化合物、一种生产该化合物的方法、一种用于筛选的组合物以及一种选择与目标物质结合的环肽化合物的方法。根据本发明，提供了一种由式（1）表示的多肽化合物或其盐。式中的符号具有本申请说明书中定义的含义。
• HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS
  申请人：JUBILANT EPISCRIBE LLC

  公开号：US20210371431A1

  公开（公告）日：2021-12-02

  The compounds of Formula I, Formula Ia, and Formula Ib are described herein along with their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds inhibit PRMT5 and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, Parkinson's disease and the like.