| 摘要 |
<p>7-phenylamino-(aza)-quinolone derivatives (I) and their salts are new. 7-phenylamino-(aza)-quinolone derivatives of formula (I) and their salts are new. R1 : hydroxy or 1-6C alkoxy, optionally substituted by 1-6C alkoxycarbonyl; R2 : hydrogen, 1-6C alkyl or phenyl; R3 : hydrogen, 1-8C alkyl (optionally substituted by R9), 3-7C cycloalkyl, pyridyl or phenyl (both optionally substituted by R10); R9 : amino, (di)1-6C alkylamino, carboxy, 1-6C alkoxycarbonyl, 3-7C cycloalkyl, heteroalkyl, heteroaryl, phenyl or phenoxy, where phenyl and heteroaryl may be substituted by R11; R10 : fluoro, chloro, bromo, 1-6C alkyl or alkoxy, carboxy, 1-6C alkoxycarbonyl, amino or (di)1-6C alkylamino; R11 : fluoro, chloro, 1-6C alkyl or alkoxy, amino, (di)1-6C alkylamino, carboxy or 1-4C alkoxycarbonyl; X : CR4 or N; R4 and R5 : hydrogen, floro, chloro, bromo, hydroxy, nitro, cyano, 1-6C alkyl or alkoxy, where alkyl may be substituted by chloro, fluoro or bromo; R6 : R4 but not hydroxy; R7 : hydrogen or 1-6C alkyl; R8 : phenyl, optionally substituted by up to 5 of fluoro, chloro, bromo, cyano, nitro, 1-8C alkyl, alkoxy or alkylthio, 2-8C alkenyl, 3-7C cycloalkyl, phenyl, benzyl, benzoyl, amino, (di)1-6C alkylamino, -P(O)(1-4C alkoxy) 2 or heteroalkyl, where alkyl and alkenyl may be substituted by fluoro, chloro, bromo, carboxy or 1-4C alkoxycarbonyl; heteroalkyl : heterocyclic, (un)saturated 4-7 membered ring with up to 3 heteroatoms (N, O or S) and optionally ring-substituted by fluoro, chloro, bromo, cyano, nitro, 1-4C alkyl, hydroxy, carboxy or 1-4C alkoxycarbonyl; proviso: excluded are compounds where X : N; R1 = hydroxy; R2-R5 and R7 = hydrogen and R8 = unsubstituted phenyl . [Image] ACTIVITY : Antidiabetic; Antiarteriosclerotic. MECHANISM OF ACTION : Glycogen Phosphorylase (GP) inhibitor. The compound ethyl 1-ethyl-6-(4-ethylphenylamino)-7-methyl-4-oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylate when tested at 10 mu M in vitro, caused 14% inhibition of GP.</p> |
