| 摘要 |
Described are compounds of formula I which are phthalazinone-derivatives and used in the pharmaceutical industry for the production of medicaments. Described are compounds of formula I in which, R1 is methoxy or ethoxy, R2 is fluorine, bromine or chlorine, R3 and R4 together form an additional bond, R5 is R6, -CmH2m-R7, -CpH2p-Y-Aryl1, R12 or R26, in which R6 , 3-6C-cycloalkyl, 3-7C-cycloalkylmethyl, quinoxalinyl, indazolyl, benzothiazolyl, 6-methyl-3-trifluoromethyl-pyridin-2-yl, 1,3,4-trimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl, 3-thiophen-2-yl[1,2,4]-thiadiazol-5-yl, 1,1-dioxide-tetrahydrothiophen-3-yl, 1-oxo-1,3-dihydro-isobenzofuran-5-yl, 4-(4-yl-but-1-oxy)-benzoic acid, or an unsubstituted or by R61 substituted phenyl radical, in which R61 is 1-4C-alkyl, 1-4C-alkoxy, carboxyl or 1-4C-alkoxycarbonyl, R7 is carboxyphenyloxy, Y is a bond, Aryl1 is imidazolyl m is an integer from 1 to 4, p is an integer from 1 to 4, R12 is a radical of formula (a) wherein R13 is-S(0)2-R14, -C(O)R17 or Aryl3-1-4C-alykl, R14 is phenyl or phenyl substituted by R22, R17 is 1-4C-alkyl, 2-oxo-imidazoidin-1-yl or -N(R20)R21, R20 and R21 are independent from each other, 1-7C-alkyl or R20 and R21 together and with inclusion of the nitrogen atom to which they are bonded, form a 4-morpholinyl-ring, 1-pyrrolidinyl-ring, 1-piperidinyl-ring or a 1-piperazinyl-ring, R22 is 1-4C-alkyl, Aryl3 is pyridyl, R26 is a radical of formula (c) wherein R27 is -(CH2)UR30, R30 is -N(R32)R33, R32 is 1-4C-alkyl, or R32 and R33 together and with inclusion of the nitrogen atom to which they are bonded, form a 4-morpholinyl-,1-pyrrolidinyl-, 1-piperidinyl-or 1-hexahydroazepinyl-ring, u is an integer from 1 to 4, v is 1, X is -C(O)- or a salt hydrate solvate, hydrate of a salt or solvate of a salt thereof..
|
