N-methyl-3,4-pyridinedicarboximide | 20743-46-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: N-methyl-3,4-pyridinedicarboximide
• 英文别名: N-methylpyridine-3,4-dicarboximide；2-methyl-pyrrolo[3,4-c]pyridine-1,3-dione；2-methyl-pyrrolo[3,4-c]pyridine-1,3-dione；Cinchomeronsaeure-N-methyl-imid；N-Methyl-isochinolinsaeureimid；5H-Pyrrolo(3,4-b)pyridine-5,7(6H)-dione, 6-methyl-；2-methylpyrrolo[3,4-c]pyridine-1,3-dione
• CAS: 20743-46-8
• 化学式: C₈H₆N₂O₂
• mdl: MFCD00972198
• 分子量: 162.148
• InChiKey: UNNHKPOHFLHRCV-UHFFFAOYSA-N

物化性质

• 熔点：
  94-95 °C
• 沸点：
  297.2±13.0 °C(Predicted)
• 密度：
  1.400±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.125
• 拓扑面积：
  50.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-methyl-3,4-pyridinedicarboximide 在 甲基磺酰氯 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 生成 、
  参考文献：
  名称：

  吡啶-3,4-二羧酰亚胺作为天然产物eupolauramine和其异构体的总合成起始原料异-eupolauramine赋予抗-tubercular活动

  摘要：

  描述了直接和方便的合成途径，用于制备关键中间体氮杂-异吲哚满酮4a / 4b，该中间体可从吡啶-3,4-二羧酸二酰亚胺中直接制得。在天然产物eupolauramine 7b的全合成和位置类似物异-eupolauramine 7a的第一个合成中，均采用这种方法，经过6个步骤获得，总产率为13％。所开发的策略代表了第一种合成方法，该方法采用了已嵌入氮杂菲内酰胺骨架的吡啶和内酰胺循环（分别为循环D和C）的原料。这些化合物，主要是新的非天然产物，对结核分枝杆菌的生长表现出良好的抑制活性。

  DOI：

  10.1016/j.tet.2015.01.034
• 作为产物：
  描述：

  3,4-吡啶二酰亚胺 、 碘甲烷 在 potassium carbonate 作用下， 以 丙酮 为溶剂， 反应 3.0h， 以75%的产率得到N-methyl-3,4-pyridinedicarboximide
  参考文献：
  名称：

  吡啶-3,4-二羧酰亚胺作为天然产物eupolauramine和其异构体的总合成起始原料异-eupolauramine赋予抗-tubercular活动

  摘要：

  描述了直接和方便的合成途径，用于制备关键中间体氮杂-异吲哚满酮4a / 4b，该中间体可从吡啶-3,4-二羧酸二酰亚胺中直接制得。在天然产物eupolauramine 7b的全合成和位置类似物异-eupolauramine 7a的第一个合成中，均采用这种方法，经过6个步骤获得，总产率为13％。所开发的策略代表了第一种合成方法，该方法采用了已嵌入氮杂菲内酰胺骨架的吡啶和内酰胺循环（分别为循环D和C）的原料。这些化合物，主要是新的非天然产物，对结核分枝杆菌的生长表现出良好的抑制活性。

  DOI：

  10.1016/j.tet.2015.01.034

文献信息

• HIGHLY-FLUORESCENT AND PHOTO-STABLE CHROMOPHORES FOR ENHANCED SOLAR HARVESTING EFFICIENCY
  申请人：NITTO DENKO CORPORATION

  公开号：US20130074927A1

  公开（公告）日：2013-03-28

  The invention provides highly fluorescent materials comprising a single (n=0) or a series (n=1, 2, etc.) of benzo heterocyclic systems. The photo-stable highly luminescent chromophores are useful in various applications, including in wavelength conversion films. Wavelength conversion films have the potential to significantly enhance the solar harvesting efficiency of photovoltaic or solar cell devices.

  这项发明提供了包括单个（n=0）或一系列（n=1、2等）苯并杂环系统的高荧光材料。这种光稳定的高发光色团在各种应用中很有用，包括波长转换膜。波长转换膜有潜力显著提高光伏或太阳能电池器件的太阳能收集效率。
• Dipeptide derivatives as growth hormone secretagogues
  申请人：Pfizer Inc.

  公开号：US06251902B1

  公开（公告）日：2001-06-26

  This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

  本发明涉及公式化合物及其药用盐，其中取代基如规范中定义，这些化合物是生长激素分泌素，能增加内源性生长激素水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱、充血性心力衰竭、与衰老有关的虚弱、肥胖；加速骨折修复、减轻重大手术后蛋白质分解反应、减少慢性疾病导致的消瘦和蛋白质丢失、加速伤口愈合，或加速烧伤患者或接受重大手术的患者的康复；改善肌肉力量、运动能力、皮肤厚度的维持、代谢稳态或肾脏稳态。本发明的化合物在与：双膦酸盐类化合物如阿伦膦酸盐；雌激素、前马品、以及可选的孕激素；雌激素拮抗剂或激动剂；或降钙素结合使用时，也可用于治疗骨质疏松症和/或虚弱；及其药用组合物。此外，本发明涉及药用组合物，用于增加人类或其他动物内源性生长激素的产生或释放，包括本发明的化合物和从GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-HT920中选择的生长激素分泌素的有效量。该发明还涉及在制备公式I化合物中有用的中间体。
• Dipeptide derivatives
  申请人：——

  公开号：US20010041703A1

  公开（公告）日：2001-11-15

  This invention is directed to compounds of the formula 1 and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-H-T920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

  本发明涉及公式1的化合物及其药学上可接受的盐，其中取代基如规范中所定义，这些化合物是生长激素分泌促进剂，可以增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松和/或衰弱、充血性心力衰竭、与衰老有关的衰弱、肥胖症；加速骨折修复、减轻重大手术后的蛋白质分解反应、减少慢性疾病引起的消瘦和蛋白质流失、加速伤口愈合或加速烧伤患者或接受重大手术的患者的恢复；改善肌肉力量、运动能力、皮肤厚度维持、代谢稳态或肾脏稳态。本发明的化合物在与双磷酸盐化合物（如阿伦膦酸）、雌激素、预马林和可选孕激素、雌激素激动剂或拮抗剂或降钙素联合使用时，也可用于治疗骨质疏松和/或衰弱，以及用于该用途的药物组合物。此外，本发明还涉及用于增加人类或其他动物内源性生长激素的产生或释放的药物组合物，该组合物包括本发明化合物的有效量和从GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-H-T920中选择的生长激素分泌促进剂。本发明还涉及用于制备公式I化合物的中间体。
• PYRROLE BASED INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3
  申请人：Desai C. Manoj

  公开号：US20070244109A1

  公开（公告）日：2007-10-18

  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.

  提供了基于新的吡咯基化合物、组合物和方法，用于体外抑制糖原合成酶激酶(GSK3)的活性和治疗GSK3介导的疾病。该发明的方法、化合物和组合物可单独应用，或与其他药理活性剂联合治疗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、肥胖症、动脉粥样硬化性心血管疾病、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、双相情感障碍、免疫缺陷或癌症。
• Pyrrolo Pyrimidines as Agents for the Inhibition of Cystein Proteases
  申请人：Betschart Claudia

  公开号：US20090054467A1

  公开（公告）日：2009-02-26

  The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

  本发明提供了公式I的化合物，或其药理学上可接受的盐或酯，其中符号具有定义的含义，这些化合物是卡特普西林K的抑制剂，并在药学上用于治疗与卡特普西林K有关的疾病和医疗条件，例如各种疾病，包括炎症，类风湿性关节炎，骨关节炎，骨质疏松和肿瘤。