| 摘要 |
1,3-Diacyl-2-oxo-indole cpds. of formula (I) and pharmaceutically acceptable base salts are new. Also claimed are intermediate 1-acyl cpds. of formula (II). In (I), X = H, F, Cl, Br, 1-4C alkyl, alkoxy, alkylthio, alkylsulphinyl or alkylsulphonyl, 3-7C cycloalkyl, CF3, NO2, phenyl, 2-4C alkanoyl, benzoyl, thenoyl, 2-4C alkanamido, benzamido or N,N-di(1-3C alkyl)sulphamoyl; Y = H, F, Cl, Br, CF3, 3-7C cycloalkyl or 1-4C alkyl, alkoxy or alkylthio; R1 = 1-6C alkyl, 3-7C cycloalkyl, 4-7C cycloalkenyl, phenyl, phenyl-(1-3C)alkyl, phenoxy-(1-3C)alkyl, thiophenoxy-(1-3C)alkyl, naphthyl or -(CH2)n-Q-R, where phenyl gps. in R1 (except thiophenoxy) are opt. substd. by an F, Br, Cl, 1-4C alkyl, 1-4C alkoxy or CF3 gp.; n = 0, 1 or 2; Q = divalent residue of a furan, thiophene, pyrrole, pyrazole, imidazole, thiazole, isothiazole, oxazole, isoxazole, 1,2,3-thiadiazole, 1,3,4-thiadiazole, 1,2,5-thiadiazole, THF, tetrahydrothiophene, tetrahydropyran, tetrahydrothiopyran, pyridine, pyrimidine or pyrazine ring; R = H or 1-3C alkyl; and R2 = 1-5C alkyl. In (II), X1 = H, 5-F, 5-Cl or 5-CF3; Y1 = H, 6-F, 6-Cl or 6-CF3; provided both X1 and Y1 are not H; and R2 = 1-5C alkyl. |
