摘要 |
The invention relates to novel 3(2H)-pyridazinone-derivatives of the general formula (I), pharmaceutical compositions containing them and process for their preparation. In the general formula (I) <IMAGE> (I) stands for an ethyl or propyl group substituted by a terminal halogen atom or a hydroxyl or NR1R2 group, wherein R1 represents hydrogen atom or an unsubstituted or optionally substituted benzyl group; R2 represents hydrogen atom or an unsubstituted or optionally substituted benzo[1,4]dioxan-2-yl-methyl or -ethyl group or a (CH2)n-R3 group, wherein n is 2 or 3; and R3 stands for an unsubstituted or optionally substituted phenoxy or phenylthio group; and X stands for a hydrogen or halogen atom or an unsubstituted or optionally substituted, saturated or unsaturated 5- or 6-membered heterocyclic group containing a nitrogen atom and optionally an additional heteroatom, e.g. an oxygen, sulfur or nitrogen atom, with the proviso that R is different from an ethyl or propyl group substituted terminally by a hydroxyl group or halogen atom when X represents a hydrogen or chlorine atom. The compounds of general formula (I) selectively inhibit the adrenergic alpha1 receptors, have a calcium-antagonistic effect and exert blood pressure lowering action.
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申请人 |
RICHTER GEDEON VEGYESZETI GYAR T.R. |
发明人 |
KASZTREINER, ENDRE;RABLOCSKY, GYOERGY;MAKK, NANDOR;JASZLITS, LASZLO;MATYUS, PETER;CSEH, GYOERGY;PRIBUSZ NEE RAPP, ILDIKO;CZAKO, KLARA;DIESLER, ESZTER;ELEKES, ISTVAN;KAUFER, LASZLO;KUHAR NEE KUERTHY, MARIA;KINCSESSY, JUDIT;KOSARY, JUDIT;NAGY NEE CSOKAS, GYOENGYI |