申请人:Dr. Willmar Schwabe GmbH & Company
公开号:US04855320A1
公开(公告)日:1989-08-08
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.
本发明提供了式为:##STR1##的5-芳基烷基-4-烷氧基-2(5H)-呋喃酮,其中相对于彼此的C-5和C-.alpha.上的氧原子处于threo位,不包括当n=0或2,R.sup.2为H或CH.sub.3,R.sup.o=H,R.sup.1=CH.sub.3,R.sup.3=H和R.sup.4=H的化合物。本发明还提供了它们的制备方法,以及用于制备新的呋喃酮衍生物的新的3-烷氧基-5-(取代基)-苯基-2(E),4(E)-戊二烯酸酯作为反应中间体。threo系列的新呋喃酮衍生物作为抗惊厥/抗癫痫剂具有活性。因此,本发明还提供含有这些新呋喃酮衍生物的药物,以及首次发现具有抗惊厥/抗癫痫功效的已知呋喃酮。