1-methyl-2-(1-methylpyrazol-4-yl)-N-phenyl-pyrrolo[3,2-c]pyridin-6-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 1-methyl-2-(1-methylpyrazol-4-yl)-N-phenyl-pyrrolo[3,2-c]pyridin-6-amine
• 英文别名: 1-methyl-2-(1-methylpyrazol-4-yl)-N-phenylpyrrolo[3,2-c]pyridin-6-amine
• 化学式: C₁₈H₁₇N₅
• 分子量: 303.366
• InChiKey: DFGNHXJSUZDQPM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  47.7
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
  申请人：Bavetsias Vassilios

  公开号：US20130345181A1

  公开（公告）日：2013-12-26

  The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them. Formula (I)

  本发明涉及使用特定的吡咯吡啶氨基衍生物（以下简称为“PPA衍生物”），特别是1H-吡咯[3,2-c]吡啶-6-氨基衍生物，直接或间接地通过与Mps激酶本身的相互作用来抑制单丝粒体1（Mps1，也称为TTK）激酶的纺锤体检查点功能。具体而言，本发明涉及将PPA衍生物用作治疗和/或预防增生性疾病，如癌症的治疗剂。本发明还涉及制备PPA衍生物的方法，以及包含它们的药物组合物。公式（I）
• Imidazo[4,5-c]pyridine and pyrrolo[3,2-c]pyridine compounds as G-protein-coupled receptor kinase 5 (GRK5) modulators
  申请人：Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.

  公开号：EP2818472A1

  公开（公告）日：2014-12-31

  The present invention relates to imidazo[5,4-c]pyridine or pyrrolo[3,2-c]pyridine compounds and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds, as well as pharmaceutical compositions containing at least one of these pyridine-based bicyclic compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pyridine-based bicyclic compounds are assumed to be modulators of the GRK5 protein, thereby regulating the expression and/or release of insulin and are useful for the treatment or prophylaxis of a metabolic disease and in particular for the treatment and prophylaxis of diabetes, obesity and impaired adipogenesis.

  本发明涉及咪唑并[5,4-c]吡啶或吡咯并[3,2-c]吡啶化合物及其立体异构体形式、溶剂化合物、水合物和/或这些化合物的药学上可接受的盐，以及包含至少一种这些基于吡啶的双环化合物的药物组合物，与药学上可接受的载体、赋形剂和/或稀释剂一起。所述基于吡啶的双环化合物被假定为GRK5蛋白的调节剂，从而调节胰岛素的表达和/或释放，并可用于治疗或预防代谢性疾病，特别是用于糖尿病、肥胖和受损脂肪生成的治疗和预防。
• [EN] PYRROLO[3,2-C]PYRIDINE COMPOUNDS AS G-PROTEIN-COUPLED RECEPTOR KINASE 5 (GRK5) MODULATORS<br/>[FR] COMPOSÉS PYRROLO[3,2-C]PYRIDINE UTILISÉS COMME MODULATEURS DE KINASE 5 ASSOCIÉE AUX RÉCEPTEURS COUPLÉS À LA PROTÉINE G (GRK5)
  申请人：MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V

  公开号：WO2014207260A1

  公开（公告）日：2014-12-31

  The present invention relates to pyrrolo[3,2-c]pyridine compounds and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds, as well as pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pyrrolo[3,2-c]pyridine compounds are assumed to be modulators of the GRK5 protein, thereby regulating the expression and/or release of insulin and are useful for the treatment or prophylaxis of a metabolic disease and in particular for the treatment and prophylaxis of diabetes, obesity and impaired adipogenesis.

  本发明涉及吡咯并[3,2-c]吡啶化合物及其立体异构体形式、溶剂化物、水合物和/或药学上可接受的盐，以及至少包含其中一种化合物与药学上可接受的载体、辅料和/或稀释剂的制药组合物。所述的吡咯并[3,2-c]吡啶化合物被认为是GRK5蛋白的调节剂，从而调节胰岛素的表达和/或释放，并且对于代谢性疾病的治疗或预防以及特别是糖尿病、肥胖和受损脂肪生成的治疗和预防是有用的。
• US9371319B2
  申请人：——

  公开号：US9371319B2

  公开（公告）日：2016-06-21
• US9458463B2
  申请人：——

  公开号：US9458463B2

  公开（公告）日：2016-10-04