2-formylaminomethyl-5-methylpyrazine | 864868-47-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-formylaminomethyl-5-methylpyrazine
• 英文别名: N-[(5-methylpyrazin-2-yl)methyl]formamide
• CAS: 864868-47-3
• 化学式: C₇H₉N₃O
• 分子量: 151.168
• InChiKey: DJRVCDMUZCSGSM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  54.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-formylaminomethyl-5-methylpyrazine 在 sodium iodide 、 三氯氧磷 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  CP0569, A New Broad-Spectrum Injectable Carbapenem. Part 1: Synthesis and Structure–Activity Relationships

  摘要：

  A series of 10-methylcarbapenems bearing an (imidazo[5,1-b]thiazolium-6-yl)methyl moiety, a 5,5-fused heterobicycle, at the C-2 position was synthesized and evaluated for in vitro antibacterial activities. CP0569 (1r) and its analogues showed potent antibacterial activities against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative bacteria, including Pseudomonas aeruginosa. Moreover, CP0569 (1r) exhibited stronger antibacterial activity against MRSA and higher resistance to renal dehydropeptidase-1 (DHP-1) than any currently marketed carbapenems, that is, imipenem (IPM), panipenem (PAPM), and meropenem (MEPM). (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(03)00304-3
• 作为产物：
  描述：

  甲酸 、 2-氨甲基-5-甲基吡嗪 在 乙酸酐 作用下， 以 二氯甲烷 为溶剂， 以69%的产率得到2-formylaminomethyl-5-methylpyrazine
  参考文献：
  名称：

  CP0569, A New Broad-Spectrum Injectable Carbapenem. Part 1: Synthesis and Structure–Activity Relationships

  摘要：

  A series of 10-methylcarbapenems bearing an (imidazo[5,1-b]thiazolium-6-yl)methyl moiety, a 5,5-fused heterobicycle, at the C-2 position was synthesized and evaluated for in vitro antibacterial activities. CP0569 (1r) and its analogues showed potent antibacterial activities against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative bacteria, including Pseudomonas aeruginosa. Moreover, CP0569 (1r) exhibited stronger antibacterial activity against MRSA and higher resistance to renal dehydropeptidase-1 (DHP-1) than any currently marketed carbapenems, that is, imipenem (IPM), panipenem (PAPM), and meropenem (MEPM). (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0968-0896(03)00304-3

文献信息

• [EN] PYRROLE BASED INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3<br/>[FR] INHIBITEURS DE LA GLYCOGENE SYNTHASE KINASE 3 A BASE DE PYRROLE
  申请人：CHIRON CORP

  公开号：WO2004018455A1

  公开（公告）日：2004-03-04

  New pyrrole based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

  提供了基于新吡咯烷基化合物的方法、组合物以及抑制体外糖原合成酶激酶（GSK3）活性和治疗体内GSK3介导的疾病的方法。该发明的方法、化合物和组合物可单独使用，也可与其他药理活性剂结合在一起，用于治疗由GSK3活性介导的疾病，如糖尿病、阿尔茨海默病和其他神经退行性疾病、肥胖、动脉粥样硬化心血管疾病、原发性高血压、多囊卵巢综合征、X综合征、缺血、创伤性脑损伤、躁狂抑郁症、免疫功能缺陷或癌症。
• [EN] 2,4,6-TRISUBSTITUTED PYRIMIDINES AS PHOSPHOTIDYLINOSITOL (PI) 3-KINASE INHIBITORS AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] PYRIMIDINES 2,4,6-TRISUBSTITUTEES UTILISEES COMME INHIBITEURS DE PHOSPHOTIDYLINOSITOL (PI) 3-KINASE ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：CHIRON CORP

  公开号：WO2004048365A1

  公开（公告）日：2004-06-10

  Compounds having formula I are provided where the variables have the values described herein. (I). Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.

  提供具有I式的化合物，其中变量具有所述的值。药物配方包括该化合物或药物可接受的盐以及药物可接受的载体和与其他药物的组合。治疗患者的方法包括向需要该药物的患者投予本发明的药物配方。
• [EN] DEXAMETHASONE COMBINATION THERAPY<br/>[FR] POLYTHÉRAPIE À LA DEXAMÉTHASONE
  申请人：UNIV TEXAS

  公开号：WO2012065021A1

  公开（公告）日：2012-05-18

  The present invention relates to a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I), as described herein, and/or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and an amount of (2) dexamethasone and/or a pharmaceutically acceptable salt, solvate, metabolite or racemate thereof, such that the subject is treated. In another aspect, provided herein is a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I) and an amount of (2) dexamethasone, such that the subject is treated; pharmaceutical formulations comprising said combination for the treatment of multiple myelom; and compositions thereof.

  本发明涉及一种治疗多发性骨髓瘤的方法，包括向受试者注射(1)公式(I)所述的化合物和/或其立体异构体、互变异构体或药学上可接受的盐，以及(2)地塞米松和/或其药学上可接受的盐、溶剂、代谢物或外消旋体的剂量，以使受试者得到治疗。在另一方面，本发明提供了一种治疗多发性骨髓瘤的方法，包括向受试者注射(1)公式(I)的化合物和(2)地塞米松的剂量，以使受试者得到治疗；以及用于治疗多发性骨髓瘤的该组合的制剂和组成物。
• DEXAMETHASONE COMBINATION THERAPY
  申请人：Yi Qing

  公开号：US20130310352A1

  公开（公告）日：2013-11-21

  The present invention relates to a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I), as described herein, and/or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, and an amount of (2) dexamethasone and/or a pharmaceutically acceptable salt, solvate, metabolite or racemate thereof, such that the subject is treated. In another aspect, provided herein is a method of treating multiple myeloma in a subject comprising administering to the subject an amount of (1) a compound of formula (I) and an amount of (2) dexamethasone, such that the subject is treated; pharmaceutical formulations comprising said combination for the treatment of multiple myelom; and compositions thereof.

  本发明涉及一种治疗多发性骨髓瘤的方法，包括向患者施用（1）公式（I）所述的化合物及/或其立体异构体，互变异构体或其药学上可接受的盐的量，以及（2）地塞米松和/或其药学上可接受的盐，溶剂，代谢物或外消旋体的量，从而治疗患者。在另一个方面，本发明提供了一种治疗多发性骨髓瘤的方法，包括向患者施用（1）公式（I）的化合物的量和（2）地塞米松的量，从而治疗患者；用于治疗多发性骨髓瘤的上述组合物的药物制剂；以及它们的组成物。
• [EN] MANUFACTURING PROCESS FOR PYRIMIDINE DERIVATIVES<br/>[FR] PROCÉDÉ DE FABRICATION DE DÉRIVÉS DE PYRIMIDINE
  申请人：NOVARTIS AG

  公开号：WO2012044727A2

  公开（公告）日：2012-04-05

  The invention relates to processes for manufacturing a compound of formula (5) or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of said solid forms for the therapeutic treatment of warm-blooded animals.

  本发明涉及制造化合物式（5）或其立体异构体、互变异构体或盐的过程，其中取代基如规范中所定义。本发明还涉及化合物A及其盐的特定固态形式的新制造工艺，以及使用所述固态形式治疗温血动物的方法。