| abstract |
The present invention relates to novel α 1 -adrenoceptor antagonists of the formula In in which:n R 1 is acetylamino, amino, cyano, trifluoroacetylamino, halo, hydro, hydroxy, nitro, methylsulfonylamino, 2-propynyloxy, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl, (C 1-6 )alkyloxy, (C 3-6 )cycloalkyloxy, (C 3-6 )cycloalkyl(C 1-4 )alkyloxy and (C 1-4 )alkylthio (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, aryl(C 1-4 )alkyl, heteroaryl, heteroaryl(C 1-4 )alkyl, aryloxy, aryl(C 1-4 )alkyloxy, heteroaryloxy and heteroaryl(C 1-4 )alkyloxy (which aryl and heteroaryl are optionally further substituted with one to two radicals independently selected from halo and cyano); R 2 is cyano, halo, hydro, hydroxy or a group selected from (C 1-6 )alkyl and (C 1-6 )alkyloxy (which group is optionally further substituted with one to three halogen atoms); R 3 and R 4 are both hydro or methyl or together are ethylene; and R 5 is a group selected from Formulae (a), (b), (c) and (d):n in which:n X is C(O), CH 2 or CH(OH); Y is CH 2 or CH(OH); Z is N or C(R 9 ), wherein R 9 is hydro, (C 1-6 )alkyl or hydroxy; R 6 is hydro, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 3-6 )cycloalkyl(C 1-4 )alkyl (which group is optionally further substituted with one to three halo atoms) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl); R 7 is (C 1-6 )alkanoyl, carbamoyl, cyano, di(C 1-6 )alkylamino, halo, hydro, hydroxy, hydroxyiminomethyl, (C 1-6 )alkylsulfonyl, (C 1-6 )alkylthio, a group selected from (C 1-6 )alkyl, (C 3-6 )cycloalkyl, (C 1-6 )alkyloxy and (C 1-6 )alkyloxy(C 1-4 )alkyl (which group is optionally further substituted with one to three radicals selected from halo, hydroxy or (C 1-6 )alkyloxy) or a group selected from aryl, heteroaryl, aryl(C 1-4 )alkyl and heteroaryl(C 1-4 )alkyl (which aryl and heteroaryl are optionally further substituted with one to three radicals selected from halo, cyano, (C 1-6 )alkyloxy, (C 1-6 )alkyl and aryl) or R 7 and R 9 together are tetramethylene; and each R 8 is independently hydro, hydroxy, methyl or ethyl; and the pharmaceutically acceptable salts and N -oxides thereof. |