tert-butyl 4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidine-1-carboxylate | 1452520-72-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: tert-butyl 4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidine-1-carboxylate
• 英文别名: Tert-butyl 4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidine-1-carboxylate；tert-butyl 4-[[(5-methoxy-1H-indazole-3-carbonyl)amino]methyl]piperidine-1-carboxylate
• CAS: 1452520-72-7
• 化学式: C₂₀H₂₈N₄O₄
• 分子量: 388.467
• InChiKey: NWIPTCPSVRLQAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  96.6
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidine-1-carboxylate 在 盐酸 、 potassium carbonate 作用下， 以 甲醇 、 乙醚 、 丙酮 为溶剂， 反应 4.0h， 生成 ethyl 4-[4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidin-1-yl]butanoate
  参考文献：
  名称：

  [EN] 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS
  [FR] COMPOSÉS 1H-INDAZOLE-3-CARBOXAMIDE EN TANT QU'INHIBITEURS DE LA GLYCOGÈNE SYNTHASE KINASE 3 BÊTA

  摘要：

  本发明涉及具有以下一般式（I）的1H-吲唑-3-羧酰胺化合物作为糖原合成酶激酶3β（GSK-3ß）抑制剂，并且涉及它们在治疗GSK-3β相关疾病中的用途，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症障碍；（v）癌症性疾病；（vi）炎症；（vii）物质滥用障碍；（viii）癫痫病；和（ix）神经病性疼痛。

  公开号：

  WO2013124158A1
• 作为产物：
  描述：

  5-甲氧基-3-吲唑羧酸 、 1-叔丁氧羰基-4-氨甲基哌啶 在 1-羟基苯并三唑 、 N,N'-二环己基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 以96%的产率得到tert-butyl 4-({[(5-methoxy-1H-indazol-3-yl)carbonyl]amino}methyl)piperidine-1-carboxylate
  参考文献：
  名称：

  NEW USE OF 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS

  摘要：

  1H-吲唑-3-羧酰胺类化合物作为糖原合成酶激酶3β抑制剂。本发明涉及用作糖原合成酶激酶3β（GSK-33）抑制剂的1H-吲唑-3-羧酰胺类化合物，并且涉及它们在治疗GSK-3β相关疾病中的用途，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症性障碍；（v）癌症性障碍；（vi）炎症；（vii）物质滥用障碍；以及（viii）癫痫。

  公开号：

  US20140378455A1

文献信息

• [EN] USE OF 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS<br/>[FR] UTILISATION DES COMPOSÉS 1H-INDAZOLE-3-CARBOXAMIDE EN TANT QU'INHIBITEURS DE LA GLYCOGÈNE SYNTHASE KINASE 3 BÊTA
  申请人：ACRAF

  公开号：WO2013124169A1

  公开（公告）日：2013-08-29

  1 H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1 H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-33) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.

  1- H-吲唑-3-羧酰胺化合物作为糖原合成酶激酶3β抑制剂。本发明涉及用于作为糖原合成酶激酶3β（GSK-33）抑制剂的1- H-吲唑-3-羧酰胺化合物，以及它们在治疗GSK-3β相关疾病中的应用，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症性障碍；（v）癌症性障碍；（vi）炎症；（vii）物质滥用障碍；以及（viii）癫痫。
• NEW USE OF 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS
  申请人：AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.

  公开号：US20140378455A1

  公开（公告）日：2014-12-25

  1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-33) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.

  1H-吲唑-3-羧酰胺类化合物作为糖原合成酶激酶3β抑制剂。本发明涉及用作糖原合成酶激酶3β（GSK-33）抑制剂的1H-吲唑-3-羧酰胺类化合物，并且涉及它们在治疗GSK-3β相关疾病中的用途，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症性障碍；（v）癌症性障碍；（vi）炎症；（vii）物质滥用障碍；以及（viii）癫痫。
• 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS
  申请人：AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.

  公开号：US20150057294A1

  公开（公告）日：2015-02-26

  The present invention relates to the 1H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3p-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.

  本发明涉及具有以下一般式（I）的1H-吲唑-3-羧酰胺化合物作为糖原合成酶激酶3β（GSK-3β）抑制剂，并且涉及它们在治疗GSK-3β相关疾病中的应用，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症；（v）癌症性疾病；（vi）炎症；（vii）物质滥用障碍；（viii）癫痫；和（ix）神经病理性疼痛。
• Use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
  申请人：AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.

  公开号：US09163013B2

  公开（公告）日：2015-10-20

  1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors. The present invention relates to the 1H-indazole-3-carboxamide compounds for use as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3β-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.

  1H-吲唑-3-羧酰胺类化合物作为糖原合酶激酶3β抑制剂。本发明涉及1H-吲唑-3-羧酰胺类化合物，用作糖原合酶激酶3β（GSK-3β）抑制剂，并用于治疗GSK-3β相关疾病，例如（i）胰岛素抵抗性疾病；（ii）神经退行性疾病；（iii）情绪障碍；（iv）精神分裂症；（v）癌症性疾病；（vi）炎症，（vii）物质滥用障碍；和（viii）癫痫病。
• 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
  申请人：AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.

  公开号：US10160746B2

  公开（公告）日：2018-12-25

  The present invention relates to the 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3β) inhibitors and to their use in the treatment of GSK-3β-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; (viii) epilepsies; and (ix) neuropathic pain.

  本发明涉及作为糖原合酶激酶3β（GSK-3β）抑制剂的1H-吲唑-3-甲酰胺化合物，以及它们在治疗GSK-3β相关疾病中的用途，例如，(i) 胰岛素抵抗性疾病；(ii) 神经退行性疾病；(iii) 情绪障碍；(iv) 精神分裂症；(v) 癌症；(vi) 炎症；(vii) 药物滥用障碍；(viii) 癫痫；以及 (ix) 神经性疼痛。