New aminosulfonyl-substituted 3H-imidazo (1,5-a) (1,3,5) triazin-4-one derivatives, are phosphodiesterase inhibitors, useful for treating cardiovascular, cerebrovascular or urogenital disorders

摘要

2-(2-Oxy-5-(amino-sulfonyl)-phenyl)-3H-imidazo (1,5-a) (1,3,5) triazin-4-ones (I), their salts, N-oxides or isomers are new. 2-(2-Oxy-5-(amino-sulfonyl)-phenyl)-3H-imidazo (1,5-a) (1,3,5) triazin-4-ones of formula (I), their salts, N-oxides or isomers are new. R1 = 1-4C alkyl; R2 = 1-4C alkyl or 3-8C cycloalkyl; R3 = H or 1-4C alkyl; R4, R5 = H, alkoxy, 1-6C alkoxy, OH or 1-8C alkyl (optionally substituted by 1-3 of OH, alkoxy, tetrahydrofuran-2-yl, morpholino, pyrrolidino or NR6R7; or phenyl or phenoxy (themselves optionally substituted by halo, OH, 1-6C alkoxy, 1-6C alkyl or SO2NR8R9)); or R4 = H or Me; and R4 = 1,1-dioxo-tetrahydro-3-thienyl, 2-oxo-perhydroazepin-3-yl or phenyl (optionally substituted by 1-3 of halo, COMe, alkoxy, cyclopentyloxy, NR10R11 or CH2P(O)(OR12)(OR13)); or NR4R5 = piperidino substituted by R14 and R15, 4-(R16)-piperazino or morpholino; R6-R9, R12, R13 = H or alkyl; R10, R11 = H or 1-4C alkyl; R14, R5 = H, OH or 1-4C alkyl (optionally substituted by OH); or R14 = H; and R15 = 5,6-dihydro-1,4,2-dioxazin-3-yl or CR14R15 = C=NOMe; R16 = H, 1-6C alkyl (optionally substituted by OH) or 5- or 6-membered aromatic heterocycle containing 1-3 of O, N and S as heteroatom(s); alkyl moieties have 1-6C unless specified otherwise. An Independent claim is included for the preparation of (I).