3-氰基吡啶-2-羧胺 | 23590-00-3

• 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-氰基吡啶-2-羧胺
• 英文名称: 3-cyanopyridine-2-carboxamide
• 英文别名: 3-Cyano-picolinamid
• CAS: 23590-00-3
• 化学式: C₇H₅N₃O
• mdl: MFCD07368150
• 分子量: 147.136
• InChiKey: PFKPTCLDFSITFB-UHFFFAOYSA-N

物化性质

• 熔点：
  275 °C(Solv: acetone (67-64-1))
• 沸点：
  369.4±27.0 °C(Predicted)
• 密度：
  1.33±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  79.8
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2933399090

反应信息

• 作为产物：
  描述：

  3-氰基吡啶-2-羧酸 在 氨 、 氯甲酸乙酯 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 3-氰基吡啶-2-羧胺
  参考文献：
  名称：

  Spiessens, Luc I. M.; Anteunis, Marc J. O., Bulletin des Societes Chimiques Belges, 1980, vol. 89, # 3, p. 205 - 232

  摘要：

  DOI：

文献信息

• [EN] PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE<br/>[FR] COMPOSÉS À BASE DE 1,3-OXAZIN-2-AMINE FUSIONNÉE AVEC DU CYCLOPROPYLE PERFLUORÉ UTILISABLES EN TANT QU'INHIBITEURS DE LA BÊTA-SÉCRÉTASE ET LEURS PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2014138484A1

  公开（公告）日：2014-09-12

  PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: INSERT STRUCTURE HERE} I wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

  本发明提供了一类新的化合物，用于调节β-分泌酶（BACE）活性。这些化合物具有一般的化学式I：在此插入结构} I，其中变量A4、A5、A6、A8，以及化学式I中的每个Ra、Rb、R1、R2、R3和R7，在本文中分别定义。该发明还提供了包含这些化合物的药物组合物，以及用于治疗与A-beta斑块形成和沉积相关的疾病和/或症状的化合物和组合物的用途，这些疾病和症状是由BACE的生物活性引起的。这种由BACE介导的疾病包括阿尔茨海默病、认知缺陷、认知障碍、精神分裂症和其他中枢神经系统疾病。该发明还提供了化学式II和III的化合物，以及其亚式化合物、中间体和制备本发明化合物的方法。
• PERFLUORINATED 5,6-DIHYDRO-4H-1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
  申请人：AMGEN INC.

  公开号：US20140249104A1

  公开（公告）日：2014-09-04

  The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A 4 , A 5 , A 6 , A 8 , each of R 1 and R 2 , R 3 and R 7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.

  本发明提供了一类新的化合物，用于调节β-分泌酶（BACE）活性。这些化合物的通用公式为I： 其中变量A4，A5，A6，A8，公式I中的R1和R2，R3和R7各自独立定义如下。本发明还提供了包含这些化合物的药物组合物，以及使用这些化合物和组合物治疗与A-β斑块形成和沉积相关的疾病和/或状况，这些疾病和/或状况是由BACE的生物活性引起的。这样的BACE介导的疾病包括，例如，阿尔茨海默病，认知缺陷，认知障碍，精神分裂症和其他中枢神经系统疾病。本发明进一步提供了公式II和III的化合物，以及其子公式的实施例，中间体和用于制备公式I-III化合物的过程和方法。
• Novel pyridopyprimidinone derivatives which are HM74A agonists
  申请人：Conte Aurelia

  公开号：US20070275987A1

  公开（公告）日：2007-11-29

  The invention is concerned with novel pyridopyrimidinone derivatives of formula (I): wherein R 1 to R 8 , X, Y, m and n are as defined in the description and in the claims. The compounds of the present invention are HM74A agonists with improved properties compared to niacin and can be used for the treatment and/or prevention of diseases such as dyslipidemia, atherosclerosis, diabetes, metabolic syndrome, and other related diseases associated with HM74A.

  这项发明涉及式(I)的新型吡啶吡嘧啶酮衍生物：其中R1至R8、X、Y、m和n如描述和索赔中所定义。本发明的化合物是HM74A激动剂，与烟酸相比具有改进的性能，并可用于治疗和/或预防与HM74A相关的疾病，如脂质代谢异常、动脉粥样硬化、糖尿病、代谢综合征和其他与HM74A相关的疾病。
• [EN] TRIAZOLE BENZAMIDE DERIVATIVES AND THE COMPOSITIONS AND METHODS OF TREATMENT REGARDING THE SAME<br/>[FR] DÉRIVÉS DE TRIAZOLE BENZAMIDE ET COMPOSITIONS ET PROCÉDÉS DE TRAITEMENT ASSOCIÉS
  申请人：AN2H DISCOVERY LTD

  公开号：WO2017210694A1

  公开（公告）日：2017-12-07

  The present disclosure is directed to triazole benzamide compounds of formula (I) and formula (II), pharmaceutical compositions thereof and methods for modulating or activating a Parkin ligase The present disclosure is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase. R1, R2, R3, M1, M2, M3, L1, L2, and L3 are as defined herein.

  本公开涉及式(I)和式(II)的三唑苯甲酰胺化合物，以及其药物组合物和调节或激活Parkin连接酶的方法。本公开还涉及治疗和/或减少与激活Parkin连接酶相关的疾病或症状的方法。R1、R2、R3、M1、M2、M3、L1、L2和L3如本文所定义。
• Carboximidamide derivatives
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP0388528A2

  公开（公告）日：1990-09-26

  Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboximidate compounds represented by the following formula (II) whiich are the intermediates for preparing of N-cyano-N′-substituted-­pyridinecarboximidamide derivatives wherein the substituent B in the above described formula (A) is pyridine are also disclosed: wherein all the substituents have the same meanings as defined above. The process for preparing the compounds, the pharmaceutical agents comprising the compound having vasodilating effect, and the therapeutic method of dosing the compound on patients for therapy are also disclosed.

  本发明公开了由下式（A）代表的新型羧亚酰胺衍生物及其酸加成盐： 其中所有取代基的含义与上述定义相同。 还公开了下式(II)代表的 N-氰基吡啶甲脒化合物，它们是制备 N-氰基-N′-取代的吡啶甲脒衍生物的中间体，其中上述式(A)中的取代基 B 为吡啶： 其中所有取代基的含义与上述定义相同。 本发明还公开了制备上述化合物的工艺、包含具有血管扩张作用的化合物的药物制剂以及将该化合物用于患者治疗的治疗方法。