5-Carbamoyl-picolinsaeure | 24242-18-0

• 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: 5-Carbamoyl-picolinsaeure
• 英文别名: 5-carbamoylpyridine-2-carboxylic Acid
• CAS: 24242-18-0
• 化学式: C₇H₆N₂O₃
• mdl: MFCD04111156
• 分子量: 166.136
• InChiKey: KGBSMDOELQXOBN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  93.3
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-Carbamoyl-picolinsaeure 在 三氯氧磷 作用下， 生成 5-氰基-2-吡啶羧酸
  参考文献：
  名称：

  N-acylamino acid amide compounds and intermediates for preparation thereof

  摘要：

  本发明公开了以下公式（I）所表示的化合物： 其中A代表以下公式（a-1）或以下公式（a-2）： B代表以下公式（b）： （其中符号如规范中所定义）或其药学上可接受的盐，以及用于制备其的中间体，具有优异的血小板聚集抑制活性和其他性质，并且可用作与纤维蛋白原受体、血栓形成、梗塞等疾病相关的预防或治疗剂。

  公开号：

  US06265418B1

文献信息

• 2-AMINO-5,5-DIFLUORO-5,6-DIHYDRO-4H-[1,3]OXAZIN-4-YL)-PHENYL]-AMIDES
  申请人：Banner David

  公开号：US20110144097A1

  公开（公告）日：2011-06-16

  The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的2-氨基-5,5-二氟-5,6-二氢-4H-[1,3]噁唑-4-基)-苯基]-酰胺的化合物，其制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物可用于治疗和/或预防例如阿尔茨海默病和2型糖尿病。
• [EN] 2-AMINO-5, 5-DIFLUORO-5, 6-DIHYDRO-4H-OXAZINES AS BACE 1 AND/OR BACE 2 INHIBITORS<br/>[FR] 2-AMINO-5,5-DIFLUORO-5,6-DIHYDRO-4H-OXAZINES EN TANT QU'INHIBITEURS DE BACE 1 ET/OU BACE 2
  申请人：HOFFMANN LA ROCHE

  公开号：WO2011069934A1

  公开（公告）日：2011-06-16

  The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)- phenyl]-amide derivatives of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

  本发明涉及具有BACE1和/或BACE2抑制活性的2-氨基-5,5-二氟-5,6-二氢-4H-[1,3]噁唑-4-基)-苯基]-酰胺衍生物的化学式(I)，其制备方法，含有它们的药物组合物以及它们作为治疗活性物质的用途。本发明的活性化合物在治疗和/或预防治疗阿尔茨海默病和2型糖尿病等疾病中具有用途。
• Carboxylic acid derivatives having retinoic acid-like activity
  申请人：Shudo, Koichi, Prof. Dr.

  公开号：EP0617020A1

  公开（公告）日：1994-09-28

  Carboxylic acid derivatives having potent retinoid-type pharmacological activities are disclosed. The compounds disclosed are represented by the following formula: wherein R¹, R², and R³ independently represent a hydrogen atom or an alkyl group with the exception that all of R¹, R², and R³ do not simultaneously represent hydrogen atoms and R¹ together with R² optionally represent a cyclic structure formed by the combination thereof; R⁴ represents a hydrogen atom or an alkyl group; X represents a nitrogen atom or C-OH; and A represents -CO-NH- or -NH-CO-.

  揭示了具有强效视黄醇类药理活性的羧酸衍生物。所揭示的化合物由以下公式表示：其中R¹、R²和R³独立地代表氢原子或烷基基团，除非R¹、R²和R³中的所有原子同时代表氢原子，且R¹和R²一起可选地代表由它们的组合形成的环结构；R⁴代表氢原子或烷基基团；X代表氮原子或C-OH；A代表-CO-NH-或-NH-CO-。
• [EN] NOVEL HETEROCYCLIC COMPOUNDS USEFUL IN SIRTUIN BINDING AND MODULATION<br/>[FR] NOUVEAUX COMPOSÉS HÉTÉROCYCLIQUES UTILES POUR LA LIAISON AUX SIRTUINES ET LA MODULATION DE CELLES-CI
  申请人：SMB INNOVATION

  公开号：WO2013090369A1

  公开（公告）日：2013-06-20

  Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, wherein aryl is phenyl or naphthyl, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to ageing.

  提供了一些新型的杂环sirtuin结合剂，例如N-芳基取代的吡啶二酰胺，其中芳基是苯基或萘基，它们可用作sirtuin调节剂。还提供了使用吡啶二酰胺化合物治疗sirtuin介导的疾病和病症，例如糖尿病、癌症、肥胖症和与衰老相关的疾病的方法。
• N-ACYLAMINO ACID AMIDE COMPOUNDS AND INTERMEDIATES FOR PREPARATION THEREOF
  申请人：UBE INDUSTRIES LIMITED

  公开号：EP1020467A1

  公开（公告）日：2000-07-19

  The present invention discloses the compound represented by the formula (I): wherein A represents the following formula (a-1) or the following formula (a-2): B represents the following formula (b): (wherein the symbols are each as defined in the specification) or a pharmaceutically acceptable salts thereof, and intermediates for the preparation thereof, which have excellent platelet aggregation inhibitory activity and other properties and useful as prophylactic or therapeutic agents for diseases associated with a fibrinogen receptor, thrombosis, infarction and the like.

  本发明公开了式 (I) 所代表的化合物： 其中 A 代表下式（a-1）或下式（a-2）： B 代表下式（b）： (其中各符号如说明书中所定义）或其药学上可接受的盐类，以及用于制备它们的中间体，它们具有优异的血小板聚集抑制活性和其他特性，可用作与纤维蛋白原受体、血栓形成、梗塞等相关疾病的预防或治疗药物。