(N-methyl)indole-4-carboxamide | 1154383-44-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (N-methyl)indole-4-carboxamide
• 英文别名: N-methyl-1H-indole-4-carboxamide
• CAS: 1154383-44-4
• 化学式: C₁₀H₁₀N₂O
• 分子量: 174.202
• InChiKey: SLFIWTNAKPDBJR-UHFFFAOYSA-N

物化性质

• 沸点：
  464.5±18.0 °C(Predicted)
• 密度：
  1.224±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  44.9
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (N-methyl)indole-4-carboxamide 在 sodium hydroxide 作用下， 生成 1-(1H-吲哚-5-基)-N-甲基甲胺
  参考文献：
  名称：

  Indole and indazole derivatives, for the treatment and prophylaxis of cerebral disorders, their preparation and their use

  摘要：

  化合物的化学式（I）：[其中R¹和R²分别为氢或不同的有机基团，p为0、1、2或3，U为-CO-或-CH(OR³)-其中R³为氢或羟基保护基团，V为可选的不饱和脂肪烃基团，W为含氮基团] 在治疗和预防痴呆症，尤其是阿尔茨海默病类型的痴呆症方面是有用的。

  公开号：

  EP0562832A1

文献信息

• [EN] INHIBITORS OF BRUTON'S TYROSINE KINASE<br/>[FR] INHIBITEURS DE LA TYROSINE KINASE DE BRUTON
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015086635A1

  公开（公告）日：2015-06-18

  This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.

  本申请揭示了根据通用式（I）定义的化合物，其中所有变量如本文所述，这些化合物抑制Btk。本文披露的化合物可用于调节Btk的活性并治疗与过度Btk活性相关的疾病。这些化合物可用于治疗由异常B细胞激活引起的肿瘤学、自身免疫和炎症性疾病。还披露了包含通用式（I）化合物和至少一种载体、稀释剂或赋形剂的组合物。
• Substituted indole derivatives
  申请人：Schunk Stefan

  公开号：US20090215828A1

  公开（公告）日：2009-08-27

  Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.

  取代吲哚衍生物，其制备方法，含有这些化合物的药品和药物组合物，以及利用取代吲哚衍生物治疗疼痛和其他症状以及其他医学用途。
• [EN] MONOCYCLIC PYRIMIDINE/PYRIDINE COMPOUNDS AS INHIBITORS OF P97 COMPLEX<br/>[FR] COMPOSÉS MONOCYCLIQUES PYRIMIDINE/PYRIDINE COMME INHIBITEURS DU COMPLEXE P97
  申请人：WUSTROW DAVID

  公开号：WO2015089218A1

  公开（公告）日：2015-06-18

  Monocyclic pyrimidine and pyridine compounds having a benzyl amine substituent at the 4 position and a 5:6 bicyclic heteroaryl substituent at the 2 position of the pyrimidine or pyridine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

  在4位上具有苄胺取代基的单环嘧啶和吡啶化合物，以及在2位上具有5:6双环杂芳基取代基的嘧啶或吡啶环，还可以在环的其他位置取代烷基、官能基和/或芳香基成分。这些化合物是含有p97的AAA蛋白酶复合物的抑制剂，并且是用于治疗与p97生物活性相关的疾病如癌症的有效药物。
• NITROGEN HEXACYCLE COMPOUNDS AS INHIBITORS OF p97 COMPLEX
  申请人：Cleave Biosciences, Inc.

  公开号：US20160355503A1

  公开（公告）日：2016-12-08

  Nitrogen hexacycle compounds having an arylalkyl amine substituent at the P4 position and a substituted 5:6 bicyclic group at the P2 position of the nitrogen hexacycle as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the nitrogen hexacycle, the aryl alkyl group and the 5:6 bicyclic group are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

  本发明涉及一种氮六环化合物，其在P4位置具有芳基烷基胺取代基，在氮六环的P2位置具有取代的5:6双环基团，并在氮六环的其他位置，芳基烷基基团和5:6双环基团的其他位置上可选地取代有脂肪族、功能性和/或芳香性组分。这些化合物是AAA蛋白酶体复合物的p97抑制剂，并且是治疗与p97生物活性相关的疾病，如癌症的有效药物。
• FUSED PYRIMIDINES AS INHIBITORS OF P97 COMPLEX
  申请人：Cleave Biosciences, Inc.

  公开号：US20170258795A1

  公开（公告）日：2017-09-14

  Fused pyrimidine compounds having a saturated, unsaturated or aromatic A ring fused to a pyrimidine ring and having a complex substituents at the 2 position and a substituted amine at the 4 position of the pyrimidine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine ring and A ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.

  本发明公开了一种融合嘧啶化合物，其具有饱和，不饱和或芳香性A环融合到嘧啶环上，并在嘧啶环的2位位置具有复杂的取代基和取代胺在嘧啶环的4位位置，以及可选的脂肪烷基，功能性和/或芳香基组分取代在嘧啶环和A环的其他位置。这些化合物是AAA蛋白酶复合物的抑制剂，包含p97，并且是用于治疗与p97生物活性相关的疾病的有效药物，例如癌症。