FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel derivatives of pyrimidinedione, triazinedione and tetrahydroquinazolinedione of the general formula (I) α1 where 
means halogen, hydrogen atom, hydroxy-group, nitro-group taken among R1-alkyl, C1-C6-alkoxy-group being the indicated group, except for, is substituted optionally with one-three halogen atoms or a group taken among phenyl, phenyl- -C1-C6-alkyl, furyl, oxazolyl or pyrrolyl; C1-C4 means halogen, hydrogen atom, hydroxy-group or a group taken among R2-alkyl and C1-C6-alkoxy-group being the indicated group, except for, is substituted optionally with one-three halogen atoms; C1-C6 and R3 each means hydrogen atom or methyl or they in common mean ethylene; and R4 means a group taken among the formulas (a) R5, (b) 
, (c) 
and (d) 
where X means C(O), 
or CH(OH); Y means CH2/ or CH(OH); Z means N or CH2 where C(R9) means hydrogen atom or R9-alkyl; C1-C6 means hydrogen atom, group taken among R6-alkyl, C1-C6-cycloalkyl-C3-C6-alkyl or group taken among phenyl, phenyl-C1-C4-alkyl, thienyl, pyridyl, furyl, pyrrolyl or pyrazinyl, heteroaryl-C1-C4-alkyl being the indicated aryl and heteroaryl, except for, are substituted optionally with one-three radicals taken among halogen atom, C1-C4-alkoxy-group, C1-C6-alkyl and phenyl; C1-C6 means carbamoyl-group, cyano-group, di-R7-alkylamino-group, halogen, hydrogen atom, hydroxy-group, hydroxyiminomethyl-group, a group taken among C1-C6-alkyl, C1-C6-cycloalkyl and C3-C6-alkoxy-group being the indicated group is substituted optionally with one-three radicals taken among halogen atom, hydroxy-group or C1-C6-alkoxy-group, or a group taken among phenyl, furyl, phenyl-C1-C6-alkyl being the indicated aryl and heteroaryl, except for, are substituted optionally with one-three radicals taken among halogen atom, C1-C4-alkyl and phenyl; or C1-C6 and R7 in common mean tetramethylene-group; and each R9 means independently hydrogen atom, hydroxy-group, methyl or ethyl; and their pharmaceutically acceptable salts and N-oxides. New compounds of the formula (I) can be used as antagonists of R8-adrenceptors. Invention describes also methods of synthesis of indicated compounds and pharmaceutical composition based on thereof. EFFECT: valuable pharmacological properties. 22 cl, 1 tbl, 42 ex
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