3-氨基-N-甲基-2-吡啶甲酰胺 | 99368-19-1

• 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
• 中文名称: 3-氨基-N-甲基-2-吡啶甲酰胺
• 英文名称: 3-amino-N-methylpicolinamide
• 英文别名: 3-amino-N-methylpyridine-2-carboxamide；3-amino-N-methyl-2-pyridinecarboxamide
• CAS: 99368-19-1
• 化学式: C₇H₉N₃O
• 分子量: 151.168
• InChiKey: ACQSXOWTAAETIH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-氨基-N-甲基-2-吡啶甲酰胺 在 劳森试剂 、 六甲基磷酰三胺 作用下， 以21%的产率得到3-amino-N-methylpyridine-2-carbothioamide
  参考文献：
  名称：

  Synthesis and Pharmacological Activity of Triazole Derivatives Inhibiting Eosinophilia

  摘要：

  In order to develop novel antiasthmatic agents based on a new mechanism of action, a series of 3-substituted 5-amino-1-[(methylamino)(thiocarbonyl)]-1H-1,2,4-triazole derivatives were synthesized and evaluated in a model in which eosinophilia was induced in the ah-way through intravenous (iv) injection of Sephadex particles on days 0, 2, and 5. After screening of several hundred derivatives, we finally identified the highly potent eosinophilia inhibitor 5-amino-3-(4-chlorophenyl)-1-[(methylamino)(thiocarbonyl)]-1H-triazole (23c, GCC-AP0341), which had ID50 values of 0.3 and 0.07 mg/kg when administered orally (os) and intraperitoneally tip), respectively. This compound showed complete inhibition of the hypersensitivity induced by ascaris inhalation at an ip dose of 1 mg/kg as well as low toxicity, with an LD(50) value of > 2.0 g/kg in mice. Extensive study of its mechanism of action revealed that 23c inhibited eosinophil survival induced by interleukin-5 (IL-5), but had little or no effect on leukotriene D-4 (LTD(4)) or platelet-activating factor (PAF)-induced responses. Taken together, these results suggest 23e as a novel candidate for the treatment of chronic asthma. Further studies are now underway.

  DOI：

  10.1021/jm9507993
• 作为产物：
  描述：

  2-甲基-3-硝基吡啶 在 palladium 10% on activated carbon potassium permanganate 、 氢气 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 N,N-二异丙基乙胺 作用下， 以 甲醇 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 0.5h， 生成 3-氨基-N-甲基-2-吡啶甲酰胺
  参考文献：
  名称：

  WO2008/115369

  摘要：

  公开号：

文献信息

• [EN] NOVEL CLOSTRIDIUM DIFFICILE TOXIN INHIBITORS<br/>[FR] NOUVEAUX INHIBITEURS DE TOXINE DE CLOSTRIDIUM DIFFICILE
  申请人：VENENUM BIODESIGN LLC

  公开号：WO2017214359A1

  公开（公告）日：2017-12-14

  The present invention relates to benzodiazepine derivative compounds of formula (I), or pharmaceutically acceptable salts thereof. The present benzodiazepine compounds are useful Clostridium difficile inhibitors in the treatment of Clostridium difficile infection in humans. The present invention provides a pharmaceutical composition containing benzodiazepine compounds of formula (I) and a method of making as well as a method of using the same in treating patients infected with Clostridium difficile infection by administering the same. The compounds of the present invention may be used in combination with additional antibiotics or anti-toxin antibody drugs.

  本发明涉及式(I)的苯二氮卓衍生物化合物，或其药学上可接受的盐。目前的苯二氮卓衍生物在治疗人类的克罗斯特氏梭菌感染中是有用的抑制剂。本发明提供了一种含有式(I)的苯二氮卓化合物的药物组合物，以及制备该药物组合物的方法和使用该药物组合物治疗感染克罗斯特氏梭菌的患者的方法。本发明的化合物可以与额外的抗生素或抗毒素抗体药物结合使用。
• NITROGEN CONTAINING HETEROARYL COMPOUNDS
  申请人：Bleicher Konrad

  公开号：US20110306589A1

  公开（公告）日：2011-12-15

  The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A 1 , A 2 , R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.

  这项发明涉及一种新颖的含氮杂环芳基化合物，其化学式为（I），其中A1、A2、R1、R2、R3、R4、R5和R6如描述和索赔中所定义，并且其生理上可接受的盐和酯。这些化合物抑制PDE10A并可用作治疗药物。
• [EN] BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF GLYTL MEDIATED DISORDERS<br/>[FR] DÉRIVÉS DE BENZOXAZINONE POUR TRAITER DES TROUBLES INDUITS PAR GLYTL
  申请人：GLAXO GROUP LTD

  公开号：WO2011012622A1

  公开（公告）日：2011-02-03

  The present invention relates to benzoxazinone derivatives, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in treating disorders mediated by GlyT1, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.

  本发明涉及苯并噁唑酮衍生物，其制备方法，含有它们的药物组合物和药物，以及它们在治疗由GlyT1介导的疾病中的应用，包括神经系统和神经精神疾病，特别是精神病、痴呆或注意力缺陷障碍。
• [EN] NITROGEN CONTAINING HETEROARYL COMPOUNDS<br/>[FR] COMPOSÉS HÉTÉROARYLES CONTENANT DE L'AZOTE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011154327A1

  公开（公告）日：2011-12-15

  The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, (a), R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.

  这项发明涉及一种新颖的含氮杂环化合物，其化学式为（I），其中A1、A2、（a）、R1、R2、R3、R4、R5和R6的定义如描述和索赔中所述，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。
• FUSED BICYCLIC DERIVATIVES OF 2,4-DIAMINOPYRIMIDINE AS ALK AND c-MET INHIBITORS
  申请人：Ahmed Gulzar

  公开号：US20090221555A1

  公开（公告）日：2009-09-03

  The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , A 1 , A 2 , A 3 , A 4 , and A 5 , are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.

  本发明提供公式I或II化合物或其药学上可接受的盐形式，其中R1、R2、R3、R4、R5、A1、A2、A3、A4和A5如本文所定义。公式I或II化合物具有ALK和/或c-Met抑制活性，可用于治疗增殖性疾病。