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Invention Grant
US4855320A 5-arylalkyl-4-alkoxy-2(5H)-furanones, intermediates and processes for the preparation thereof and medicaments containing them 失效
5-芳基烷基-4-烷氧基-2（5H） - 呋喃酮，其制备方法及其制备方法和含有它们的药物

5-arylalkyl-4-alkoxy-2(5H)-furanones, intermediates and processes for the preparation thereof and medicaments containing them
Abstract:
The present invention provides 5-arylalkyl-4-alkoxy-2(5H)-furanones of the formula: ##STR1## 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 R.sup.2 is H or CH.sub.3 when n=0 or 2, R.sup.o =H, R.sup.1 =CH.sub.3, R.sup.3 =H and R.sup.4 =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.
Abstract(Chinese):

本发明提供下式的5-芳基烷基-4-烷氧基-2（5H） - 呋喃酮：其中C-5和C-α上的氧原子相对于彼此处于苏打 位置，排除那些当n = 0或2时R 2为H或CH 3的式（I）化合物，Ro = H，R 1 = CH 3，R 3 = H和R 4 = H。 本发明还提供其制备方法，以及作为制备新的呋喃酮衍生物的反应中间体的新的3-烷氧基-5-（低级） - 苯基-2（E），4（E） - 戊二酸二乙酯。 苏氨酸系列的新呋喃酮衍生物作为抗惊厥药/抗癫痫药物是有活性的。 因此，本发明还提供含有这些新的呋喃酮衍生物的药物以及已知的呋喃酮，其首次发现其抗惊厥/抗癫痫效果。

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