N-(3-methoxyphenyl)-2-(1H-pyrazol-4-yl)-1H-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: N-(3-methoxyphenyl)-2-(1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridin-6-amine
• 化学式: C₁₇H₁₅N₅O
• 分子量: 305.339
• InChiKey: FUKZBXVFNPLPCP-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：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  78.6
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• 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。
• [EN] HETEROCYCLIC COMPOUNDS AND THEIR USE FOR PARASITIC DISEASES<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEUR UTILISATION POUR DES MALADIES PARASITAIRES
  申请人：CELGENE CORP

  公开号：WO2022146920A1

  公开（公告）日：2022-07-07

  Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, R3, R4and R5are as defined herein (referred to herein as "Heterocyclic Compounds"), compositions comprising an effective amount of a Heterocyclic Compound, as well as methods of preventing and/or treating cryptosporidiosis and/or inhibiting a parasite or parasitic activity.

  本文提供了公式（I）及其药物可接受的盐、互变异构体、同位素伪构体或立体异构体的化合物，其中R1、R2、R3、R4和R5如本文所定义（在本文中称为“杂环化合物”），包含有效量的杂环化合物的组合物，以及预防和/或治疗隐孢子虫病和/或抑制寄生虫或寄生活动的方法。
• Methods, compositions, and uses of novel Fyn kinase inhibitors
  申请人：Lau Warren C.

  公开号：US10688093B2

  公开（公告）日：2020-06-23

  The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.

  本发明提供了使用 5-3-吡啶-2-胺、6-3-咪唑并[1,2-a]吡嗪、6-3-咪唑并[1,2-b]哒嗪、N-(5-咪唑并[2,1-b][1,3,4]噻二唑-2-基)胺、4-3-1H-吡唑并[3、4-b]吡啶和 N-(3-咪唑并[1,2-b]哒嗪-6-基)胺化合物，以及使用此类化合物治疗、预防、抑制或改善与 Fyn 激酶相关的疾病和病症的方法。
• METHODS, COMPOSITIONS, AND USES OF NOVEL FYN KINASE INHIBITORS
  申请人：Lau, Warren C.

  公开号：EP3347462A1

  公开（公告）日：2018-07-18