1-methyl-3-dimethylaminomethylene-(1H)-quinolin-2,4-dione | 141750-05-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 1-methyl-3-dimethylaminomethylene-(1H)-quinolin-2,4-dione
• 英文别名: 3-(dimethylaminomethylidene)-1-methylquinoline-2,4-dione
• CAS: 141750-05-2
• 化学式: C₁₃H₁₄N₂O₂
• 分子量: 230.266
• InChiKey: AOROXYMOBTZDSW-UHFFFAOYSA-N

物化性质

• 沸点：
  330.4±42.0 °C(Predicted)
• 密度：
  1.270±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-methyl-3-dimethylaminomethylene-(1H)-quinolin-2,4-dione 、 水 在 ice 、 水 作用下， 以to give 1-methyl-3-formyl-4-hydroxy-2(1H)-quinolinone的产率得到4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline-3-carbaldehyde
  参考文献：
  名称：

  Ester and alkoxy substituted benzopyrans

  摘要：

  本发明揭示了一种化合物，可用作降压剂和抗DNA病毒剂，例如疱疹病毒组，该化合物由公式1.0表示：##STR1##以及它们的药学上可接受的盐和溶剂。本发明还揭示了含有由公式1.0表示的化合物的制药组合物。本发明揭示了使用由公式1.0表示的化合物治疗病毒感染的方法。还揭示了使用公式1.0中R选自H、卤素和--C（O）OR.sup.6；R.sup.1选自--OR.sup.14、--O（CH.sub.2）.sub.a C（H）.sub.3-i Z.sub.i和--O（CH.sub.2）.sub.h N（R.sup.15）.sub.2的化合物治疗高血压的方法。

  公开号：

  US05412104A1
• 作为产物：
  描述：

  4-羟基-N-甲基-2-喹啉 以 N,N-二甲基甲酰胺二甲基缩醛 、 二氯甲烷 为溶剂， 反应 1.0h， 以to give 1-methyl-3-dimethylaminomethylene-(1H)-quinolin-2,4-dione的产率得到1-methyl-3-dimethylaminomethylene-(1H)-quinolin-2,4-dione
  参考文献：
  名称：

  Antiviral compounds and antihypertensive compounds

  摘要：

  本发明揭示了一种化合物，其可用作抗高血压药物和抗DNA病毒药物，如单纯疱疹病毒组。该化合物由1.0式表示：##STR1##以及其药学上可接受的盐和溶剂。本发明还揭示了含有由1.0式表示的化合物的制药组合物。本发明还揭示了使用由1.0式表示的化合物治疗病毒感染的方法。此外，本发明还揭示了使用1.0式中R从由H、卤素和--C（O）OR.sup.6组成的群中选择；R.sup.1从由--OR.sup.14、--O（CH.sub.2）.sub.a C（H）.sub.3-i Z.sub.i和--O（CH.sub.2）.sub.h N（R.sup.15）.sub.2组成的群中选择的化合物治疗高血压的方法。

  公开号：

  US05942522A1

文献信息

• Ester and alkoxy substituted benzopyrans
  申请人：Schering Corporation

  公开号：US05412104A1

  公开（公告）日：1995-05-02

  Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.

  抗高血压药物和抗DNA病毒药物，如疱疹病毒等DNA含量病毒的化合物被披露。这些化合物由Formula 1.0代表：##STR1##及其药学上可接受的盐和溶剂。披露了含有由Formula 1.0代表的化合物的药物组合物。披露了使用由Formula 1.0代表的化合物治疗病毒感染的方法。还披露了使用Formula 1.0的化合物治疗高血压的方法，其中R选自H、卤素和--C(O)OR.sup.6的群；R.sup.1选自--OR.sup.14、--O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i和--O(CH.sub.2).sub.h N(R.sup.15).sub.2的群。
• Acyl and alkoxy substituted quinolines
  申请人：Schering Corporation

  公开号：US05378694A1

  公开（公告）日：1995-01-03

  Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 and methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are compounds useful as antihypertensive agents and methods of treating hypertension using such compounds. The antihypertensive agents are compounds represented by Formula 1.0 wherein R.sup.4 is selected from the group consisting of alkyl and aminoalkyl. Preferably R.sup.1 is H.

  抗DNA病毒药物化合物，如单纯疱疹病毒等DNA含量病毒的抗病毒剂被披露。这些化合物由Formula 1.0表示。其中包括Formula 1.0代表的化合物及其药用可接受的盐和溶剂。披露了含有Formula 1.0代表的化合物的药物组合物以及使用Formula 1.0代表的化合物治疗病毒感染的方法。还披露了作为降压药物的化合物以及使用这些化合物治疗高血压的方法。降压药物是由Formula 1.0代表的化合物，其中R.sup.4从由烷基和氨基烷基组成的群体中选择。最好R.sup.1是H。
• Quinoline-diones
  申请人：Schering Corporation

  公开号：US05179093A1

  公开（公告）日：1993-01-12

  Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl); R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl; R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl) are described. These compounds are useful as agents for treating viruses.

  公式##STR1##的化合物或其药用可接受的盐，其中，R为H，卤素，(C.sub.1 -C.sub.6)烷基，N(C.sub.1 -C.sub.6烷基/芳基).sub.2，OH，O-(C.sub.1 -C.sub.6)烷基/芳基，CH.sub.2 OH，COOH，COO-烷基/芳基，SO.sub.2 NH.sub.2，或SO.sub.2 NH (C.sub.1 -C.sub.6烷基/芳基)；R.sub.1为C.sub.1 -C.sub.6烷基，环烷基，C.sub.2 -C.sub.6烯基，杂环芳基，取代的杂环芳基，杂环烷基，--CH.sub.2 -芳基，--CH.sub.2 -取代的芳基，--CH.sub.2 -杂环芳基，或--CH.sub.2 -取代的杂环芳基；R.sub.2为H，C.sub.1 -C.sub.6烷基或芳基；##STR2##为芳香环或杂芳环；X为O或N-(烷基/芳基/烷基-芳基/烷氧基烷氧基芳基)。这些化合物可用作治疗病毒的药剂。
• Alkyl and acyl substituted quinolines
  申请人：Schering Corporation

  公开号：US05382572A1

  公开（公告）日：1995-01-17

  Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates; wherein: (A) X is selected from the group consisting of N--R.sup.3, O, S, and C(R.sup.3).sub.2 ; (B) R.sup.3 is selected from H and a range of substituents; (C) R.sup.1 is an etherifying or esterifying group; (D) R.sup.2 is selected from a range of substituents; (E) m is 0 or an integer from 1 to 4; and (F) R.sup.4 and R.sup.5 are the same and are selected from alkyl and acyl groups; together with the pharmaceutically acceptable salts of the compounds of Formula 1.0 that are acidic or basic. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating a viral infection using compounds represented by Formula 1.0.

  抗DNA病毒药物化合物，如疱疹病毒群，被揭示。这些化合物由Formula 1.0表示：##STR1##及其药学上可接受的盐和溶剂；其中：（A）X选自N-R.sup.3，O，S和C(R.sup.3).sub.2组；（B）R.sup.3选自H和一系列取代基；（C）R.sup.1是醚化或酯化基团；（D）R.sup.2选自一系列取代基；（E）m为0或1至4之间的整数；（F）R.sup.4和R.sup.5相同，选自烷基和酰基；以及Formula 1.0化合物的酸性或碱性药学上可接受的盐。揭示了含有Formula 1.0化合物的药物组合物。还揭示了使用Formula 1.0化合物治疗病毒感染的方法。
• Antiviral compounds and antihypertensive compounds
  申请人：Schering Corporation

  公开号：US05942522A1

  公开（公告）日：1999-08-24

  Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.

  本发明揭示了一种化合物，其可用作抗高血压药物和抗DNA病毒药物，如单纯疱疹病毒组。该化合物由1.0式表示：##STR1##以及其药学上可接受的盐和溶剂。本发明还揭示了含有由1.0式表示的化合物的制药组合物。本发明还揭示了使用由1.0式表示的化合物治疗病毒感染的方法。此外，本发明还揭示了使用1.0式中R从由H、卤素和--C（O）OR.sup.6组成的群中选择；R.sup.1从由--OR.sup.14、--O（CH.sub.2）.sub.a C（H）.sub.3-i Z.sub.i和--O（CH.sub.2）.sub.h N（R.sup.15）.sub.2组成的群中选择的化合物治疗高血压的方法。