| 摘要 |
A anti-tumour compounds of formula 1, wherein r is 0 to 2, n is 0 to 2, m is 0 to 4, R1 and R2 (i) are lower alkyl or (ii) together form a bridge in subformula (l*) the binding being achieved via the two terminal carbon atoms, or (iii) together form a bridge in subformula (l**) wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the binding is achieved via T1 and T4 A, B, D, and E are, independently of one another, N or CH, with the stipulation that not more than 2 of these radicals are N; G is lower alkylene, lower alkylene substituted by acyloxy or hydroxy, -CH2-O-, -CH2-S-, -CH2-NH-, oxa (-0-), thia (-S-), or imino (-NH-); Q is lower alkyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or disubstituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfonyl, phenyl-lower alkylsulfinyl or alkylphenylsulfinyl, substituents Z being the same or different from one another if more than 1 radical Z is present; and wherein the bonds characterized, if present, by a wavy line are either single or double bonds; or an N-oxide of the defined compound, wherein 1 or more N atoms carry an oxygen atom; with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, G is selected from the group comprising lower alkylene, -CH2-O-, -CH2-S-, oxa and thia; or a salt thereof. Preferred compounds are selected from the group comprising 1 -(4- Methylanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(3-Chloroaniiino)-4-(4-pyridylmethyl)phthalazine; 1 -Anilino-4- (4-pyridylmethyl)phthalazine; 1 -Benzylamino-4-(4-pyridylmethyl)phthalazine; 1 (4-Methoxyanilino)-4-(4-pyridylmethyl)phthalazine; 1 (3-Benzyloxyanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(3-Methoxyanilino)-4-(4-pyridylmethyl)phthalaxine; 1 -(2-Methoxyanilino)-4-(4-pyridylmethyl)phthalazine; 1- (4-Trifluoromethylanilino)-4- (4-pyridylmethyl)phthalazine; 1 -(4-Fluoroanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(3-Hydroxyanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(4- Hydroxyanilino) -4- (4-pyridylmethyl)phthalazine; 1 -(3-Aminoanilino)-4-(4-pyridylmethyl)phthalazine; 1 - (3,4-Dichloroanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(4-Bromoanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(3-Ohloro-4-methoxyanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(4-Oyanoanilino)-4-(4-pyridylmethyl)phthalazine; 1 -(3-Chloro-4-fluoroanilino)-4-(4-pyridylmethyl)phthazaline; and 1 -(3-Methylanilino)-4-(4-pyridylmethyl)phthalazine. |
