3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine | 1788906-96-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine
• 英文别名: Unii-XX8E5WP7FS；3-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]-6-(1-methylpyrazol-4-yl)imidazo[4,5-b]pyridin-2-amine
• CAS: 1788906-96-6
• 化学式: C₂₆H₂₆N₆O₃
• 分子量: 470.531
• InChiKey: HVRWZFQFSQUILC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  35
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  102
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  5-溴-2-氯-3-硝基吡啶 在 potassium phosphate 、 sodium dithionite 、 palladium diacetate 、 N,N-二异丙基乙胺 、 三环己基膦 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 甲醇 、 乙醇 、 二氯甲烷 、 水 、 乙腈 为溶剂， 反应 140.08h， 生成 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine
  参考文献：
  名称：

  [EN] PHARMACEUTICAL FORMULATIONS OF TROPOMYOSIN RELATED KINASE (TRK) INHIBITORS
  [FR] FORMULATIONS PHARMACEUTIQUES D'INHIBITEURS DE KINASE ASSOCIÉE À LA TROPOMYOSINE (TRK)

  摘要：

  公开号：

  WO2016100677A3

文献信息

• TROPOMYOSIN-RELATED KINASE (TRK) INHIBITORS
  申请人：Genzyme Corporation

  公开号：US20150158847A1

  公开（公告）日：2015-06-11

  Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

  Tropomyosin相关激酶抑制剂（Trk抑制剂）是治疗疾病的小分子化合物。Trk抑制剂可用作药物代理和药物组合物。Trk抑制剂在治疗炎症性疾病、自身免疫疾病、骨代谢缺陷和/或癌症方面非常有用，特别适用于骨关节炎（OA）、疼痛以及与OA相关的疼痛的治疗。Trk抑制剂还可用于抑制与肌浆蛋白相关的激酶A（TrkA）、与肌浆蛋白相关的激酶B（TrkB）、与肌浆蛋白相关的激酶C（TrkC）和/或c-FMS（促红细胞生成因子-1（CSF-1）的细胞受体）有关的作用。
• PHARMACEUTICAL FORMULATIONS OF TROPOMYOSIN RELATED KINASE (TRK) INHIBITORS
  申请人：GENZYME CORPORATION

  公开号：US20180000728A1

  公开（公告）日：2018-01-04

  Pharmaceutical formulations with a tropomyosin-related kinase inhibitor (“Trk inhibitor”) are disclosed. The pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine in microcrystalline suspension formulations in its monohydrate form, which shows improved characteristics over the anhydrate form, and in extended release formulations. The extended release pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine-loaded microspheres.

  本发明揭示了含有肌动蛋白相关激酶抑制剂（“Trk抑制剂”）的制药配方。这些制药配方包括以其单水合物形式呈微晶悬浮制剂的3-（3-甲氧基-4-（（4-甲氧基苄基）氧基）苯基）-6-（1-甲基-1H-吡唑-4-基）-3H-咪唑并[4,5-b]吡啶-2-胺，该单水合物形式具有比无水合物形式更好的特性，并且还包括延长释放制剂。延长释放的制药配方包括3-（3-甲氧基-4-（（4-甲氧基苄基）氧基）苯基）-6-（1-甲基-1H-吡唑-4-基）-3H-咪唑并[4,5-b]吡啶-2-胺负载的微球。
• Tropomyosin-related kinase (TRK) inhibitors
  申请人：Genzyme Corporation

  公开号：US09067914B1

  公开（公告）日：2015-06-30

  Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

  Tropomyosin-related kinase inhibitors (Trk抑制剂)是一种小分子化合物，可用于治疗疾病。Trk抑制剂可作为药物剂量和药物组成部分使用。Trk抑制剂在治疗炎症性疾病、自身免疫疾病、骨代谢缺陷和/或癌症方面非常有用，尤其在治疗骨关节炎（OA）、疼痛以及与OA相关的疼痛方面特别有用。Trk抑制剂还可用于抑制与肿瘤相关的蛋白激酶A、B、C和/或c-FMS（促红细胞生成素-1（CSF-1）的细胞受体）。
• Tropomyosin-related kinase (Trk) inhibitors
  申请人：Genzyme Corporation

  公开号：US09174986B2

  公开（公告）日：2015-11-03

  Tropomyosin-related kinase inhibitors (Trk inhibitors) are small molecule compounds useful in the treatment of disease. Trk inhibitors can be used as pharmaceutical agents and in pharmaceutical compositions. Trk inhibitors are useful in the treatment of inflammatory diseases, autoimmune disease, defects of bone metabolism and/or cancer, and are particularly useful in the treatment of osteoarthritis (OA), pain, and pain associated with OA. Trk inhibitors are also useful for inhibiting tropomyosin-related kinase A (TrkA), tropomyosin-related kinase B (TrkB), tropomyosin-related kinase C (TrkC), and/or c-FMS (the cellular receptor for colony stimulating factor-1 (CSF-1)).

  Tropomyosin-related kinase抑制剂（Trk抑制剂）是治疗疾病的小分子化合物。Trk抑制剂可用作制药剂和制药组合物。Trk抑制剂对治疗炎症性疾病、自身免疫疾病、骨代谢缺陷和/或癌症有用，尤其对于治疗骨关节炎（OA）、疼痛和与OA相关的疼痛特别有用。Trk抑制剂还可用于抑制肌动蛋白相关激酶A（TrkA）、肌动蛋白相关激酶B（TrkB）、肌动蛋白相关激酶C（TrkC）和/或c-FMS（集落刺激因子-1（CSF-1）的细胞受体）。
• Pharmaceutical formulations of tropomyosin related kinase (Trk) inhibitors
  申请人：GENZYME CORPORATION

  公开号：US10219998B2

  公开（公告）日：2019-03-05

  Pharmaceutical formulations with a tropomyosin-related kinase inhibitor (“Trk inhibitor”) are disclosed. The pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine in microcrystalline suspension formulations in its monohydrate form, which shows improved characteristics over the anhydrate form, and in extended release formulations. The extended release pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine-loaded microspheres.

  本发明公开了含有肌球蛋白相关激酶抑制剂（"Trk 抑制剂"）的药物制剂。这些药物制剂包括 3-(3-甲氧基-4-((4-甲氧基苄基)氧基)苄基)-6-(1-甲基-1H-吡唑-4-基)-3H-咪唑并[4,5-b]吡啶-2-胺的微晶悬浮制剂，其一水合物形式的特性比二水合物形式的特性更好，还包括缓释制剂。缓释制剂包括 3-(3-甲氧基-4-((4-甲氧基苄基)氧基)苄基)-6-(1-甲基-1H-吡唑-4-基)-3H-咪唑并[4,5-b]吡啶-2-胺负载微球。