4-(氨基甲基)吡啶-2-甲腈 | 858362-83-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 4-(氨基甲基)吡啶-2-甲腈
• 英文名称: 4-(aminomethyl)pyridine-2-carbonitrile
• 英文别名: reagent C 1-2-24；4-Aminomethyl-pyridine-2-carbonitrile
• CAS: 858362-83-1
• 化学式: C₇H₇N₃
• mdl: MFCD11040589
• 分子量: 133.153
• InChiKey: PXHWVDOUOGBXHW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  62.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(氨基甲基)吡啶-2-甲腈 、 2-hydroxy-4,4-dimethyl-6-oxo-N-phenylcyclohex-1-ene-1-carbothioamide 在 N,N-二异丙基乙胺 作用下， 以29%的产率得到2-{[(2-cyanopyridin-4-yl)methyl]amino}-4,4-dimethyl-6-oxo-N-phenylcyclohex-1-ene-1-carbothioamide
  参考文献：
  名称：

  [EN] 3-AMINO-1,5,6,7-TETRAHYDRO-4H-INDOL-4-ONES
  [FR] 3-AMINO -1,5,6,7-TÉTRAHYDRO-4 H-INDOL-4-ONES

  摘要：

  式(I)的化合物是Bub1激酶的抑制剂，其制备方法及其作为药物的用途。

  公开号：

  WO2015193339A1
• 作为产物：
  描述：

  4-(溴甲基)-2-吡啶甲腈 在 氨 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 2.0h， 以40 mg的产率得到4-(氨基甲基)吡啶-2-甲腈
  参考文献：
  名称：

  Discovery of an N-(2-aminopyridin-4-ylmethyl)nicotinamide derivative: a potent and orally bioavailable NCX inhibitor

  摘要：

  Ca2+ overload in myocardial cells is responsible for arrhythmia. Sodium-calcium exchanger (NCX) inhibitors are more effective than sodium hydrogen exchanger (NHE) inhibitors with regard to modulation of Ca2+ overload, because NCX inhibitors can directly inhibit the influx of Ca2+ into cells. NCX is an attractive target for the treatment of heart failure and ischemia-reper-fusion. We have designed and synthesized a series of N-(2-aminopyridin-4-ylmethyl)nicotinamide derivatives, based on compound 5. We have discovered a novel NCX inhibitor (23h) with an IC50 value of 0.12 mu M against reverse NCX. The inhibitory activities of our NCX inhibitors against cytochrome P450 were also evaluated. The effects on heart failure and the pharmacokinetic profile of compound 23h are discussed. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.03.052

文献信息

• [EN] AZAINDAZOLE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS AZAINDAZOLE EN TANT QU'ANTAGONISTES DES RÉCEPTEURS CCR1
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2010036632A1

  公开（公告）日：2010-04-01

  Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.

  公开的是化合物的公式（I），用于治疗通过CCR1活性介导或维持的多种疾病和疾病，包括自身免疫性疾病，如风湿性关节炎和多发性硬化症。还公开了制备方法和使用方法。
• Pyrazole compounds and their use as antidiabetes agents
  申请人：Takagi Masaki

  公开号：US20070032529A1

  公开（公告）日：2007-02-08

  The present invention provides a pyrazole compound that has liver glycogen phosphorylase inhibitory activity and is useful as a therapeutic or prophylactic agent for diabetes, the pyrazole compound represented by the following general formula (I): wherein Ring Q represents an aryl or heteroaromatic group, R 1 represents a hydrogen atom, a halogen atom, a C 1-6 alkyl group or a C 1-6 alkoxy group, R 2 represents a halogen atom, a C 1-6 alkyl group, a C 1-6 alkoxy group or an azido group, R 3 represents a halogen atom, a hydroxyl group, a C 1-6 alkyl group, a halo C 1-6 alkyl group, a C 1-6 alkoxy group, an azido group, an amino group, an acylamino group or a C 1-6 alkylsulfonylamino group, R 4 and R 5 are identical with or different from each other and represent a hydrogen atom, a substituted or unsubstituted C 1-6 alkyl group, a C 3-8 cycloalkyl group, a substituted or unsubstituted saturated heterocyclic group, a substituted or unsubstituted aryl group, a C 7-14 aralkyl group, a heteroaromatic group, or the like, or a pharmacologically acceptable salt thereof.

  本发明提供了一种具有肝糖原磷酸化酶抑制活性的吡唑化合物，用作糖尿病的治疗或预防剂，所述吡唑化合物由以下通用式（I）表示：其中环Q代表芳基或杂芳基，R1代表氢原子、卤原子、C1-6烷基或C1-6烷氧基，R2代表卤原子、C1-6烷基、C1-6烷氧基或偶氮基，R3代表卤原子、羟基、C1-6烷基、卤代C1-6烷基、C1-6烷氧基、偶氮基、氨基、酰胺基或C1-6烷基磺酰胺基，R4和R5彼此相同或不同，代表氢原子、取代或未取代的C1-6烷基、取代或未取代的C3-8环烷基、取代或未取代的饱和杂环基、取代或未取代的芳基、C7-14芳基烷基、杂芳基等，或其药理学上可接受的盐。
• Pyrimidine derivatives as ghrelin receptor modulators
  申请人：Kosogof Christi

  公开号：US20050070712A1

  公开（公告）日：2005-03-31

  The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by ghrelin including anorexia, cancer cachexia, eating disorders, age-related decline in body composition, weight gain, obesity, and diabetes mellitus.

  本发明涉及式(I)的化合物，或者其治疗上适宜的盐或前药，该化合物的制备、含有该化合物的组合物以及在预防或治疗由生长激素释放素调节的疾病中使用该化合物，包括厌食症、癌症恶病质、进食障碍、与年龄相关的身体组成下降、体重增加、肥胖和糖尿病。
• Diaminopyrimidine derivatives as growth hormone secrectgogue receptor (GHS-R) antagonists
  申请人：Kosogof Christi

  公开号：US20050171131A1

  公开（公告）日：2005-08-04

  The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, the preparation of the compounds, compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the action of ghrelin receptor, including Prader-Willi syndrome, eating disorder, weight gain, weight-loss maintainance following diet and exercise, obesity, and disorders associated with obesity such as noninsulin dependent diabetes mellitus.

  本发明涉及式(I)的化合物，或其治疗上适用的盐或前药，所述化合物的制备，含有所述化合物的组合物以及在预防或治疗由胃泌素受体调节的疾病中使用所述化合物，包括普拉德-威利综合征、进食障碍、体重增加、饮食和锻炼后体重减轻维持、肥胖，以及与肥胖相关的疾病，如非胰岛素依赖型糖尿病。
• [EN] INDAZOLE COMPOUNDS AS CCR1 RECEPTOR ANTAGONISTS<br/>[FR] COMPOSÉS INDAZOLE COMME ANTAGONISTES DES RÉCEPTEURS CCR1
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009134666A1

  公开（公告）日：2009-11-05

  Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

  揭示了吲唑烯化合物，其作为CCR1活性拮抗剂是有用的，因此可用于治疗通过CCR1活性介导或维持的多种疾病和疾病，包括自身免疫疾病，如类风湿性关节炎和多发性硬化症。还披露了包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和疾病的方法，制备这些化合物的过程以及在这些过程中有用的中间体。