1-(1,3-Benzodioxol-5-ylmethyl)-2-methyl-5-phenylpyrrole-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 1-(1,3-Benzodioxol-5-ylmethyl)-2-methyl-5-phenylpyrrole-3-carboxamide
• 化学式: C₂₀H₁₈N₂O₃
• 分子量: 334.4
• InChiKey: GQGBHQKKJDARDI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  66.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• COMPOUNDS FOR TREATING CNS- AND NEURODEGENERATIVE DISEASES
  申请人：ETH Zurich

  公开号：EP3543231A1

  公开（公告）日：2019-09-25

  SUMMARY The present invention is directed to compounds and corresponding pharmaceutical formulations for use in the medical treatment of CNS- and neurodegenerative diseases, for example, for use in the treatment and prophylaxis of familial or sporadic Alzheimer's disease. The invention further relates to corresponding methods of treatment.

  本发明涉及化合物和相应的药物配方，用于治疗中枢神经系统和神经退行性疾病，例如用于治疗和预防家族性或散发性阿尔茨海默病。该发明还涉及相应的治疗方法。
• [EN] CELL-PROTECTIVE COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS PROTECTEURS DE CELLULES ET LEUR UTILISATION
  申请人：ETH ZUERICH

  公开号：WO2018130537A1

  公开（公告）日：2018-07-19

  The present invention is directed to cell-protective, in particular, cardio- and renal-protective organic compounds, preferably to organic compounds that inhibit substrate phosphorylation by the G-protein-coupled receptor kinase 2 (GRK2, ADRBK1). Preferably, the organic compounds inhibit the GRK2-mediated phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1, ASF- 1, SF2) and/or phosducin for treating hypertension, heart diseases, heart dysfunction or failure and heart disease-associated pathologies, e.g. cardiomyocyte necrosis, ischemic cardiac disease and/or ischemic heart damage or ageing. Furthermore, the present invention is directed to a method for the identification of inhibitors of the (GRK2)-mediated phosphorylation of (SRSF1) and/or phosducin.

  本发明涉及细胞保护性，特别是心脏和肾脏保护性的有机化合物，优选地指向抑制G蛋白偶联受体激酶2（GRK2，ADRBK1）对底物的磷酸化的有机化合物。优选地，这些有机化合物抑制GRK2介导的丝氨酸/精氨酸富集剪接因子1（SRSF1，ASF-1，SF2）和/或磷酸鸟杜辛的磷酸化，用于治疗高血压、心脏疾病、心脏功能障碍或衰竭以及心脏疾病相关的病理，例如心肌细胞坏死、缺血性心脏病和/或缺血性心脏损伤或衰老。此外，本发明还涉及一种用于识别抑制剂（GRK2）介导的（SRSF1）和/或磷酸鸟杜辛磷酸化的方法。
• CELL-PROTECTIVE COMPOUNDS AND THEIR USE
  申请人：ETH ZÜRICH

  公开号：US20190343802A1

  公开（公告）日：2019-11-14

  The present invention is directed to cell-protective, in particular, cardio- and renal-protective organic compounds, preferably to organic compounds that inhibit substrate phosphorylation by the G-protein-coupled receptor kinase 2 (GRK2, ADRBK1). Preferably, the organic compounds inhibit the GRK2-mediated phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1, ASF-1, SF2) and/or phosducin for treating hypertension, heart diseases, heart dysfunction or failure and heart disease-associated pathologies, e.g. cardiomyocyte necrosis, ischemic cardiac disease and/or ischemic heart damage or ageing. Furthermore, the present invention is directed to a method for the identification of inhibitors of the (GRK2)-mediated phosphorylation of (SRSF1) and/or phosducin.
• [EN] COMPOUNDS FOR TREATING CNS- AND NEURODEGENERATIVE DISEASES<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE MALADIES DU SNC ET DE MALADIES NEURODÉGÉNÉRATIVES
  申请人：ETH ZUERICH

  公开号：WO2019179890A1

  公开（公告）日：2019-09-26

  The present invention is directed to compounds and corresponding pharmaceutical formulations for use in the medical treatment of CNS- and neurodegenerative diseases, for example, for use in the treatment and prophylaxis of familial or sporadic Alzheimer's disease. The invention further relates to corresponding methods of treatment and to a method for determining treatment progression or outcome of senescence and anti-aging treatment based on the detection and/or quantification of Membrane Palmitoylated Protein 1 (MPP1).