N-(4-piperidyl)methyl-1H-indazole-3-carboxamide | 1281364-19-9

• 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: N-(4-piperidyl)methyl-1H-indazole-3-carboxamide
• 英文别名: N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamide
• CAS: 1281364-19-9
• 化学式: C₁₄H₁₈N₄O
• 分子量: 258.323
• InChiKey: UGJWSQNGPPNYLP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  69.8
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

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

  公开号：WO2013124158A1

  公开（公告）日：2013-08-29

  The present invention relates to the 1 H-indazole-3-carboxamide compounds having the following general formula (I) as glycogen synthase kinase 3 beta (GSK-3ß) 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-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。
• [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。
• INDAZOLE DERIVATIVES HAVING MONOCYCLIC AMINO GROUP
  申请人：NISSHIN FLOUR MILLING CO., LTD.

  公开号：EP0829474A1

  公开（公告）日：1998-03-18

  An indazole derivative having a monocyclic amine of formula () wherein R1 is a hydrogen atom, a C1-C6 alkyl group, a C3-C6 alkenyl group or a C3-C6 cycloalkyl group, Q is a carbonyl group, a thiocarbonyl group or a methylene group, and R2 represents a group of formula (), (), () or () wherein R3 is a C1-C6 alkyl group, a C3-C6 alkenyl group or a benzyl group, of which a phenyl ring may be mono- or di-substituted by the same or different halogen atom or methoxy group, m is 0-2, n is 2 or 3, o is 1 or 2, and p is 2-4. The compound per se or a pharmaceutically acceptable salt thereof possesses a 5-HT4 receptor agonist activity and is useful as a medicine.

  具有式（）单环胺的吲唑衍生物 其中 R1 是氢原子、C1-C6 烷基、C3-C6 烯基或 C3-C6 环烷基、 Q 是羰基、硫代羰基或亚甲基，以及 R2 代表式（）、（）、（）或（）的基团 其中 R3 是 C1-C6 烷基、C3-C6 烯基或苄基，其中一个苯基环可以被相同或不同的卤原子或甲氧基单取代或二取代，m 是 0-2，n 是 2 或 3，o 是 1 或 2，p 是 2-4。该化合物本身或其药学上可接受的盐具有 5-HT4 受体激动剂活性，可用作药物。