首页> 外国专利> 5-Arylalkyl-4-alkoxy-2(5H)-furanones, intermediates and process for their preparation as well as their application as therapeutically active ingredients.

5-Arylalkyl-4-alkoxy-2(5H)-furanones, intermediates and process for their preparation as well as their application as therapeutically active ingredients.

机译:5-芳烷基-4-烷氧基-2(5H)-呋喃酮,中间体及其制备方法以及作为治疗活性成分的应用。

摘要

The present invention provides 5-arylalkyl-4-alkoxy-2(5H)-furanones of the formula: IMAGE (I) wherein the oxygen atoms on C-5 and C- alpha , relative to one another, are in the threo-position, with the exclusion of those compounds of the formula (I) wherein R2 is H or CH3 when n=0 or 2, Ro=H, R1=CH3, R3=H and R4=H. The present invention also provides processes for their preparation, as well as new 3-alkoxy-5-(subst.)-phenyl-2(E), 4(E)-pentadienoates as reactive intermediates for the preparation of the new furanone derivatives. The new furanone derivatives of the threo series are active as anticonvulsives/anti-epileptics. Therefore, the present invention also provides medicaments which contain these new furanone derivatives, as well as known furanones, the anticonvulsive/anti-epileptic effectiveness of which has been found for the first time.
机译:本发明提供下式的5-芳基烷基-4-烷氧基-2(5H)-呋喃酮:(I)其中C-5和C-α上的氧原子彼此相对。 -位置,但当n = 0或2时,其中R 2为H或CH 3的式(I)化合物除外,Ro = H,R 1 = CH 3,R 3 = H和R 4 = H。本发明还提供了它们的制备方法,以及作为反应性中间体的新的3-烷氧基-5-(取代)-苯基-2(E),4(E)-戊二烯酸酯,用于制备新的呋喃酮衍生物。苏氨酸系列的新呋喃酮衍生物具有抗惊厥药/抗癫痫药的活性。因此,本发明还提供了包含这些新的呋喃酮衍生物以及已知的呋喃酮的药物,其首次发现了其抗惊厥/抗癫痫的功效。

著录项

  • 公开/公告号ES2003293A6

    专利类型

  • 公开/公告日1988-10-16

    原文格式PDF

  • 申请/专利权人 DR. WILLMAR SCHWABE GMBH & CO.;

    申请/专利号ES19870001330

  • 发明设计人 SUNDER CHATTERJEE SHYAM;KLESSING KLAUS;

    申请日1987-05-04

  • 分类号C07D307/60;C07C59/64;C07C69/734;A61K31/34;

  • 国家 ES

  • 入库时间 2022-08-22 06:57:28

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