4-[4-amino-1-(1-but-2-ynoylpiperidin-2-yl)imidazo[1,5-a]pyrazin-4-ium-3-yl]-2-methoxy-N-(4-propylpyridin-2-yl)benzamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-[4-amino-1-(1-but-2-ynoylpiperidin-2-yl)imidazo[1,5-a]pyrazin-4-ium-3-yl]-2-methoxy-N-(4-propylpyridin-2-yl)benzamide
• 化学式: C31H34N7O3+
• 分子量: 552.6
• InChiKey: IUSWBPHQZDTWFT-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  41
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS
  申请人：Merck Sharp & Dohme B.V.

  公开号：US20160159810A1

  公开（公告）日：2016-06-09

  The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

  本发明涉及公式(I)所示的6-5成员融合吡啶环化合物，或其药学上可接受的盐，以及包含这些化合物的制药组合物及其在治疗中的用途。特别地，本发明涉及使用公式(I)所示的6-5成员融合吡啶环化合物治疗布鲁顿酪氨酸激酶（Btk）介导的疾病。
• (S)-4-(8-AMINO-3-(1-(BUT-2-YNOYL)PYRROLIDIN-2-YL)IMIDAZO[1,5-A]PYRAZIN-1-YL)-2-METHOXY-N-(PYRIDIN-2-YL)BENZAMIDE AS BTK-INHIBITOR
  申请人：Merck Sharp & Dohme B.V.

  公开号：EP3495368A1

  公开（公告）日：2019-06-12

  The present invention relates to 6-5 membered fused pyridine ring compounds according to formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

  本发明涉及符合式 I 的 6-5 分子融合吡啶环化合物 或其药学上可接受的盐，或包含这些化合物的药物组合物，以及它们在治疗中的用途。特别是，本发明涉及根据式 I 的 6-5 位融合吡啶环化合物在治疗布鲁顿酪氨酸激酶（Btk）介导的疾病中的用途。
• 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK-INHIBITORS
  申请人：Merck Sharp & Dohme B.V.

  公开号：EP3689878A1

  公开（公告）日：2020-08-05

  The present invention relates to 6-5 membered fused pyridine ring compounds according to formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

  本发明涉及符合式 I 的 6-5 分子融合吡啶环化合物 或其药学上可接受的盐，或包含这些化合物的药物组合物，以及它们在治疗中的用途。特别是，本发明涉及根据式 I 的 6-5 位融合吡啶环化合物在治疗布鲁顿酪氨酸激酶（Btk）介导的疾病中的用途。
• BTK INHIBITORS FOR TREATING SPLENOMEGALY
  申请人：Telios Pharma, Inc.

  公开号：EP4000624A1

  公开（公告）日：2022-05-25

  Therapeutic methods and pharmaceutical compositions for treating splenomegaly in a human subject are described. In certain embodiments, the invention includes therapeutic methods of treating splenomegaly using a BTK inhibitor.

  本发明描述了治疗人类脾肿大的治疗方法和药物组合物。在某些实施方案中，本发明包括使用 BTK 抑制剂治疗脾肿大的治疗方法。
• 4-imidazopyridazin-1-yl-benzamides as BTK inhibitors
  申请人：Merck Sharp & Dohme B.V.

  公开号：US10239883B2

  公开（公告）日：2019-03-26

  The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.

  本发明涉及符合式 (I) 的 6-5 位融合吡啶环化合物 或其药学上可接受的盐，或包含这些化合物的药物组合物，以及它们在治疗中的用途。特别是，本发明涉及根据式（I）的 6-5 位融合吡啶环化合物在治疗布鲁顿酪氨酸激酶（Btk）介导的疾病中的用途。