Aminoalkyl substituted benzodioxan derivatives
本发明是有关式(I)化合物∴其立体化学异构型、其N-氧化物型或医药上可接受的酸加成盐,其中-Z#+[1]-Z#+[2]-为二价基;R#+[1]、R#+[2]与R#+[3]分别选自:氢、C#-[1-6]烷基、羟基、卤素,等等;或当R#+[1]与R#+[2]位于相邻碳原子上时,R#+[1]与R#+[2]共同形成如式的二价基;Alk#+[1]与Alk#+[2]为可视需要经取代的C#-[1-6]烷二基;R#+[6]为氢或苯甲基;R#+[5]为如下式基团:∴其中n为1或2;p#+[1]为0,且p#+[2]为1或2;或p#+[1]为1或2,且p#+[2]为0;X为氧、硫或=NR#+[9];Y为氧或硫;R#...
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Zusammenfassung: | 本发明是有关式(I)化合物∴其立体化学异构型、其N-氧化物型或医药上可接受的酸加成盐,其中-Z#+[1]-Z#+[2]-为二价基;R#+[1]、R#+[2]与R#+[3]分别选自:氢、C#-[1-6]烷基、羟基、卤素,等等;或当R#+[1]与R#+[2]位于相邻碳原子上时,R#+[1]与R#+[2]共同形成如式的二价基;Alk#+[1]与Alk#+[2]为可视需要经取代的C#-[1-6]烷二基;R#+[6]为氢或苯甲基;R#+[5]为如下式基团:∴其中n为1或2;p#+[1]为0,且p#+[2]为1或2;或p#+[1]为1或2,且p#+[2]为0;X为氧、硫或=NR#+[9];Y为氧或硫;R#+[7]为氢、C#-[1-6]烷基、C#-[3-6]环烷基、苯基或苯甲基;R#+[8]为C#-[1-6]烷基、C#-[3-6]环烷基、苯基或苯甲基;R#+[9]为氰基、C#-[1-6]烷基、C#-[3-6]环烷基、C#-[1-6]烷氧羰基或氨基羰基;R#+[10]为氢或C#-[1-6]烷基;且Q为二价基。本发明并揭示制备该产物的方法、含该产物的调配物及其作为医药的用途,特别是用于治疗与胃底放松作用受损有关的病症。
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or -NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation. |
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