isopropyl 6-(2-methoxy-4-(1-methyl-1H-pyrazol-4-yl)phenylamino)-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridine-1-carboxylate | 1400285-63-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: isopropyl 6-(2-methoxy-4-(1-methyl-1H-pyrazol-4-yl)phenylamino)-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridine-1-carboxylate
• 英文别名: Propan-2-yl 6-[2-methoxy-4-(1-methylpyrazol-4-yl)anilino]-2-(1-methylpyrazol-4-yl)pyrrolo[3,2-c]pyridine-1-carboxylate
• CAS: 1400285-63-3
• 化学式: C₂₆H₂₇N₇O₃
• 分子量: 485.545
• InChiKey: VINOCKQOWRNHIU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  101
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• [EN] PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS<br/>[FR] DÉRIVÉS PYRROLOPYRIDINEAMINO EN TANT QU'INHIBITEURS DE MPS1
  申请人：CANCER REC TECH LTD

  公开号：WO2012123745A1

  公开（公告）日：2012-09-20

  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）
• [EN] NOVEL PYRROLO[3,2-c]PYRIDINE-6-AMINO DERIVATIVES<br/>[FR] NOUVEAUX DÉRIVÉS DE PYRROLO[3,2-C]PYRIDINE-6-AMINO
  申请人：CANCER RES TECH LTD

  公开号：WO2017109476A1

  公开（公告）日：2017-06-29

  The present invention relates to novel pyrrolo[3,2-c]pyridine-6-amino derivatives that inhibit the spindle checkpoint function of Monospindle 1 (Mps1 – also known as TTK) kinases. In particular, the present invention relates to isopropyl 6-(2-methoxy-4-(1-5 methyl-1H-1,2,3-triazol-5-yl)phenylamino)-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2- c]pyridine-1-carboxylate and isopropyl 6-(2-methoxy-4-(1-methyl-1H-tetrazol-5- yl)phenylamino)-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridine-1-carboxylate and their 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 10 preparation of these compounds and to pharmaceutical compositions comprising them.

  本发明涉及一种新的吡咯并[3,2-c]吡啶-6-氨基衍生物，其抑制单丝粒体1（Mps1 - 也称为TTK）激酶的纺锤体检查点功能。具体而言，本发明涉及异丙基6-(2-甲氧基-4-(1-5 甲基-1H-1,2,3-三唑-5-基)苯胺基)-2-(1-甲基-1H-吡唑-4-基)-1H-吡咯并[3,2-c]吡啶-1-羧酸异丙酯和异丙基6-(2-甲氧基-4-(1-甲基-1H-四唑-5- 基)苯胺基)-2-(1-甲基-1H-吡唑-4-基)-1H-吡咯并[3,2-c]吡啶-1-羧酸异丙酯及其作为治疗和/或预防增殖性疾病（如癌症）的治疗剂的用途。本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。
• PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
  申请人：Cancer Research Technology Ltd

  公开号：EP2686318B1

  公开（公告）日：2016-03-09
• PYRROLO[3,2-C]PYRIDINE-6-AMINO DERIVATIVES
  申请人：Cancer Research Technology Limited

  公开号：EP3394055B1

  公开（公告）日：2019-09-25
• US9371319B2
  申请人：——

  公开号：US9371319B2

  公开（公告）日：2016-06-21