硝喹宗 | 56739-21-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 硝喹宗
• 英文名称: nitraquazone
• 英文别名: 3-ethyl-1-(3-nitrophenyl)-2,4(1H,3H)-quinazolinedione；TVX-2706；1-(m-nitrophenyl)-3-ethylquinazoline-2,4(1H,3H)-dione；3-ethyl-1-(3-nitro-phenyl)-1H-quinazoline-2,4-dione；1-(m-nitrophenyl)-3-ethylquinazoline-2,4 (1H, 3H)-dione；3-ethyl-1-(3-nitrophenyl)quinazoline-2,4-dione
• CAS: 56739-21-0
• 化学式: C₁₆H₁₃N₃O₄
• 分子量: 311.297
• InChiKey: GNWCRBFQZDJFTI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  86.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-(3-nitro-phenyl)-1H-quinazoline-2,4-dione 生成 硝喹宗
  参考文献：
  名称：

  NODA, KANDZI;NAKAGAVA, AKIRA;YATANI, TEHRUMI;FUTAIDEH, XIROYUKI

  摘要：

  DOI：

文献信息

• PHOSPHODIESTERASE IV INHIBITOR CONTAINING PYRIDYLACRYLAMIDE DERIVATIVE
  申请人：TSUMURA & CO.

  公开号：EP1495757A1

  公开（公告）日：2005-01-12

  This invention relates to a phosphodiesterase IV inhibitor containing as an active ingredient a pyridylacrylamide derivative represented by the following formula (I): (wherein Ar1 represents substituted or unsubstituted pyridyl; Ar2 represents phenyl substituted by alkoxy, etc.; R1 represents hydrogen, alkyl, or aryl; R2 represents hydrogen, alkyl, cyano, or alkoxycarbonyl; R3 represents hydrogen or optionally substituted alkyl; X represents oxygen or sulfur; A and B are the same or different and each independently represents hydrogen, hydroxyl, alkoxy, or alkylthio, or A and B together represent oxo, thioxo, etc., or A may be hydroxyl and B may be 1-alkylimidazol-2-yl; and n is an integer from 1 to 3) or a pharmaceutically acceptable salt thereof.

  这项发明涉及一种磷酸二酯酶IV抑制剂，其活性成分为以下式(I)所代表的吡啶丙烯酰胺衍生物：（其中Ar1代表取代或未取代的吡啶；Ar2代表被烷氧基等取代的苯基；R1代表氢、烷基或芳基；R2代表氢、烷基、氰基或烷氧羰基；R3代表氢或可选择取代的烷基；X代表氧或硫；A和B相同或不同，每个独立代表氢、羟基、烷氧基或烷基硫基，或A和B一起代表氧代、硫代等，或A可能是羟基，B可能是1-烷基咪唑-2-基；n为1至3的整数）或其药学上可接受的盐。
• 1-Nitrophenylquinazoline-2,4(1H,3H)-diones
  申请人：Hisamitsu Pharmaceutical Co., Inc.

  公开号：US04016166A1

  公开（公告）日：1977-04-05

  The compounds of the present invention can be represented by the following formula: ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl, unsaturated lower alkyl, substituted lower alkyl and aralkyl; X is selected from the group consisting of O and S, possessing a high degree of pharmacological activities such as anti-inflammatory, analgetic, and central nervous system depressive activities, and certain of them are useful as new anti-inflammatory agents, analgesics and central nervous system depressants.

  本发明的化合物可以用以下公式表示：##STR1## 其中R从氢、低烷基、不饱和低烷基、取代的低烷基和芳基等组成的群体中选择；X从O和S等组成的群体中选择，具有很高程度的药理活性，如抗炎、镇痛和中枢神经系统抑制活性，其中一些可作为新的抗炎药、镇痛剂和中枢神经系统抑制剂。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。
• Nitro-substituted hydroxyindoles, their use as inhibitors of phosphodiesterase 4, and processes for preparing them
  申请人：Norbert Hofgen

  公开号：US20060293362A1

  公开（公告）日：2006-12-28

  The invention relates to nitro-substituted 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).

  本发明涉及硝基取代的7-羟基吲哚，涉及制备它们的方法，涉及包含这些化合物的制药制剂，以及涉及这些化合物的制药用途，这些化合物是磷酸二酯酶4的抑制剂，作为活性化合物用于治疗可以通过使用本发明的化合物来抑制免疫能力细胞（例如巨噬细胞和淋巴细胞）中的磷酸二酯酶4活性而影响的疾病。
• Cancer treatment method
  申请人：——

  公开号：US20030171306A1

  公开（公告）日：2003-09-11

  The invention relates to a method for treating cancer including administering to a mammal therapeutically effective amounts of an anti-neoplastic agent and a PDE4 inhibitor, treatment combinations containing the same as well as a method for attenuating unwanted cancer treatment side effects including myelosuppression and mucositis.

  本发明涉及一种治疗癌症的方法，包括向哺乳动物施用治疗有效量的抗肿瘤剂和PDE4抑制剂，以及包含相同的治疗组合，以及减轻不良癌症治疗副作用，包括骨髓抑制和口腔炎的方法。