4,6-二氯-3-(三氟甲基)-1H-吡咯并[2,3-b]吡啶 | 1256801-93-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 中文名称: 4,6-二氯-3-(三氟甲基)-1H-吡咯并[2,3-b]吡啶
• 英文名称: 4,6-Dichloro-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine
• 英文别名: 4,6-dichloro-3-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridine
• CAS: 1256801-93-0
• 化学式: C₈H₃Cl₂F₃N₂
• 分子量: 255.02
• InChiKey: TXPTXMVVDABNAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  28.7
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES<br/>[FR] DÉRIVÉS DE PYRROLOPYRIDINE SUBSTITUÉS
  申请人：BAYER PHARMA AG

  公开号：WO2018228920A1

  公开（公告）日：2018-12-20

  The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

  本发明涉及公式（I）中X、Y、R1、R2、R3和R4如本文所定义的蛋白抑制取代吡咯吡啶衍生物，涉及包含根据本发明的化合物的药物组合物和制剂，以及创新化合物的预防和治疗用途，分别用于制造用于治疗或预防疾病的药物组合物，特别是用于恶性肿瘤障碍，癌症或与MAP4K1信号异常相关的其他疾病，作为唯一药剂或与其他活性成分组合使用。本发明还涉及用途，分别用于制造药物组合物，用于治疗或预防良性增生中的蛋白酶抑制剂，在动脉粥样硬化疾病、败血症、自身免疫疾病、血管疾病、病毒感染、神经退行性疾病、炎症性疾病、动脉粥样硬化疾病和男性生育控制方面。
• [EN] SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES AS MAP4K1 MODULATORS FOR THE TREATMENT OF CANCER DISEASES<br/>[FR] DÉRIVÉS DE PYRROLOPYRIDINE SUBSTITUÉS UTILISÉS EN TANT QUE MODULATEURS DE MAP4K1 POUR LE TRAITEMENT DE MALADIES CANCÉREUSES
  申请人：BAYER PHARMA AG

  公开号：WO2018228923A1

  公开（公告）日：2018-12-20

  The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I) in which X, Y, R1, R2a, R2b, R3 and R4 are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, repectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients. The present invention further relates to the use, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control.

  本发明涉及公式（I）的蛋白抑制取代吡咯吡啶衍生物，其中X，Y，R1，R2a，R2b，R3和R4如本文所定义，以及包含本发明化合物的制药组合物和制药组合物的制备方法，以及本发明化合物的预防和治疗用途，分别用于制造治疗或预防疾病的制药组合物，特别是用于肿瘤性疾病，或与MAP4K1信号异常相关的疾病或其他与异常MAP4K1信号相关的疾病，作为唯一的药剂或与其他活性成分组合使用。本发明还涉及使用该化合物制造治疗或预防良性增生、动脉粥样硬化疾病、败血症、自身免疫性疾病、血管疾病、病毒感染、神经退行性疾病、炎症性疾病、动脉粥样硬化疾病和男性生育控制的制药组合物的用途。
• SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：EP3638669A1

  公开（公告）日：2020-04-22
• SUBSTITUTED PYRROLOPYRIDINE-DERIVATIVES AS MAP4K1 MODULATORS FOR THE TREATMENT OF CANCER DISEASES
  申请人：Bayer Pharma Aktiengesellschaft

  公开号：EP3638670A1

  公开（公告）日：2020-04-22