N,N-dimethyl-1,2,3,4-tetrahydro-2,3-dioxo-6-quinoxaline sulfonamide | 153504-94-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N,N-dimethyl-1,2,3,4-tetrahydro-2,3-dioxo-6-quinoxaline sulfonamide
• 英文别名: N,N-dimethyl-2,3-dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamide；N,N-dimethyl-2,3-dioxo-1,4-dihydroquinoxaline-6-sulfonamide
• CAS: 153504-94-0
• 化学式: C₁₀H₁₁N₃O₄S
• mdl: MFCD13547102
• 分子量: 269.281
• InChiKey: FIIHFCGZSMNUAP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2,3-二氧代-1,2,3,4-四氢喹噁啉-6-磺酰氯 、 二甲胺 在 水 、 丙酮 作用下， 反应 6.0h， 以Thus 1.40 g (35%) of N,N-dimethyl-1,2,3,4-tetrahydro-2,3-dioxo-6-quinoxaline sulfonamide is obtained的产率得到N,N-dimethyl-1,2,3,4-tetrahydro-2,3-dioxo-6-quinoxaline sulfonamide
  参考文献：
  名称：

  Acid amide derivatives and process for the preparation thereof

  摘要：

  本发明涉及一种酸酰胺，其化学式为##STR1##其中R.sup.1代表氢或硝基，R.sup.2和R.sup.3分别代表氢、较低的烷基或较低的烯基，每个基还可以携带从卤素、羟基、较低的烷氧基、二（较低的烷基）氨基、苯基-较低的烷氧羰基和选自哌啶基、吡咯啉基、哌嗪基和吗啡啉的5-至6-成员饱和杂环中选取的取代基；或者R.sup.2和R.sup.3与相邻的氮原子一起形成选自哌啶基、吡咯啉基、哌嗪基和吗啡啉的6-成员饱和杂环，该杂环还可以携带羟基或羟基-较低的烷基基团；或其药学上可接受的盐；制备方法和用于治疗的制药组合物和方法。

  公开号：

  US05912245A1

文献信息

• Acid amide derivatives and process for the preparation thereof
  申请人：Egis Gyogyszergyar RT.

  公开号：US05912245A1

  公开（公告）日：1999-06-15

  The present invention is directed to an acid amide of the formula ##STR1## wherein R.sup.1 represents hydrogen or nitro, R.sup.2 and R.sup.3 stand for, independently from each other, hydrogen, lower alkyl or lower alkenyl each optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated hetero-ring selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino; or R.sup.2 and R.sup.3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino, said heterocyclic group optionally carrying a hydroxy or a hydroxy-lower alkyl group; or a pharmaceutically acceptable salt thereof; process of making and pharmaceutical compositions and methods of treating.

  本发明涉及一种酸酰胺，其化学式为##STR1##其中R.sup.1代表氢或硝基，R.sup.2和R.sup.3分别代表氢、较低的烷基或较低的烯基，每个基还可以携带从卤素、羟基、较低的烷氧基、二（较低的烷基）氨基、苯基-较低的烷氧羰基和选自哌啶基、吡咯啉基、哌嗪基和吗啡啉的5-至6-成员饱和杂环中选取的取代基；或者R.sup.2和R.sup.3与相邻的氮原子一起形成选自哌啶基、吡咯啉基、哌嗪基和吗啡啉的6-成员饱和杂环，该杂环还可以携带羟基或羟基-较低的烷基基团；或其药学上可接受的盐；制备方法和用于治疗的制药组合物和方法。
• ACID AMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
  申请人：EGIS GYOGYSZERGYAR RT.

  公开号：EP0759910A1

  公开（公告）日：1997-03-05
• US5912245A
  申请人：——

  公开号：US5912245A

  公开（公告）日：1999-06-15
• [EN] ACID AMIDE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF<br/>[FR] DERIVES D'AMIDE ACIDE ET LEUR PROCEDE DE PREPARATION
  申请人：EGIS GYÓGYSZERGYÁR RT.

  公开号：WO1995031443A1

  公开（公告）日：1995-11-23

  (EN) The invention relates to new acid amide derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said acid amide derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases. The new compounds according to the invention can be characterized by formula (I), wherein R1 represents hydrogen or nitro, R2 and R3 stand, independently from each other, for hydrogen, lower alkyl or lower alkenyl optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated heteroring containing 1 or 2 nitrogen and/or oxygen atom(s); or R2 and R3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group containing optionally 1 or 2 additional nitrogen atoms and/or oxygen atom(s), said ring optionally carrying a hydroxy or a hydroxy-lower alkyl group, and possess valuable AMPA and kainate antagonizing properties, so they can be used to advantage in the therapy.(FR) Nouveaux dérivés d'amide acide, leur procédé de préparation, compositions pharmaceutiques les comportant, et application desdits dérivés d'amide acide au traitement de maladies et à la préparation de compositions pharmaceutiques utilisables dans le traitement de maladies. Ces nouveaux composés peuvent être caractérisés par la formule (I), dans laquelle R1 représente hydrogène ou nitro; R2 et R3, indépendamment l'un de l'autre, représentent hydrogène, alkyle inférieur ou alcényle inférieur portant éventuellement un substituant sélectionné dans le groupe constitué d'halogène, hydroxy, alcoxy inférieur, di(alkyle inférieur)amino, phénylalcoxy inférieur-carbonyle et un hétérocycle saturé pentagonal ou hexagonal contenant 1 ou 2 atomes d'azote et/ou d'oxygène; ou R2 et R3, pris ensemble avec l'atome d'azote adjacent, forment un groupe hétérocyclique saturé hexagonal contenant éventuellement 1 ou 2 atomes supplémentaires d'azote et/ou d'oxygène, ledit cycle portant éventuellement un groupe hydroxy-alkyle inférieur ou hydroxy; et ces nouveaux composés présentent de précieuses propriétés antagonistes d'AMPA et de kaïnate, ce qui les rend avantageux dans le domaine thérapeutique.