Pyrimidinedione derivatives, pirimidintriona, triacindiona antagonize alpha1-adrenergic receptors.

The present invention relates to novel AGONISTS TO SUB, 3} adrenoceptor of formula (I) wherein: R {SUP, 1} It is acetylamino, amino, cyano, TRIFLUOACETILAMINO, halo, hydro, hydroxy, nitro, methylsulfonylamino, 2-propynyloxy, a group selected from (C SUB {1-6}) alkyl, (C SUB {36}), (C SUB {1-4}) cycloalkyl (C {SUB 3-6 }, alkyloxy (C SUB {1-6}), cycloalkyloxy (C SUB {3-6}, alkyloxy (C SUB {1-4}) cycloalkyl (C SUB {3-6}) and alkylthio ( C SUB {1-4}) (which group is optionally further substituted with 1 to 3 carbon atoms HALO) or a group selected from aryl, (C SUB {1-4}) aryl, heteroaryl, (C SUB {14}) heteroaryl, aryloxy, alkyloxy (C SUB {1-4}) aryl, heteroaryloxy and alkyloxy (C SUB {1-4}) heteroaryl (whose aryl and heteroaryl are further optionally substituted with 1 to 2 radicals independently selected from halo and cyano); R SUP {2} is cyano, halo, hydro, hydroxy or a group selected from alkyl (C SUB {1-6}) and alkyloxy (C {SUB 1-6 }) (which group is A DEMASOPCIONALMENTE substituted with 1 to 3 halogen atoms); R SUP {3} {SUP YR, 4} are both hydro or methyl or together are ethylene; YR {SUP, 5} is a group selected from formulas (A), (B), (C) and (D) GROUP: IN: X is C (O) CH {SUB, 2} O CH (OH) ; Y is CH SUB {2} O CH (OH); Z is NOC (R {SUP, 9}), wherein R SUP {9} is hydro, (C SUB {1-6}) or hydroxy; R SUP {6} is hydro, a group selected from alkyl (C SUB {1-6}) alkyl, (C SUB {3-6}), (C SUB {1-4}) cycloalkyl ( C {SUB, 36}) (which group is optionally substituted with 1 to 3 carbon atoms HALO) or a group selected from aryl, heteroaryl, (C SUB {1-4}) aryl and (C {SUB, } 1-4 heteroaryl (whose aryl and heteroaryl are optionally further substituted by one to three radicals selected from halo, cyano, alkyloxy (C SUB {1-6}) alkyl, (C SUB {1-6}) AND aryl); R SUP {7} is alkanoyl (C SUB {1-6}), carbamoyl, cyano, dialkylamino (C SUB {1-6}), HALO, hydro, hydroxy, hydroxyiminomethyl, (C { SUB, 1-6}) - alkylsulfonyl, (C SUB {1-6}), a group selected from alkyl (C SUB {16}), cycloalkyl (C SUB {3-6}), alkyloxy ( C SUB {1-6}) and (C SUB {1-4}) alkyloxy (C SUB {1-6}) (which group is optionally substituted with one to three radicals selected from halo, hydroxy or alkyloxy (C SUB {1-6})) or a group selected from aryl, heteroaryl, (C SUB {1-4}) alkylaryl and (C SUB {1-4}) heteroaryl (whose aryl and heteroaryl are optionally further substituted by one to three radicals selected from halo, cyano, alkyloxy (C SUB {1-6}) alkyl, (C {SUB, 6/1}) and aryl) OR SUP {7} {SUP YR, 9} together are tetramethylene, and each R {SUP, 8} is independently hydro, hydroxy, methyl or ethyl; AND pharmaceutically acceptable salts and N-oxides thereof.