| 摘要 |
A compound of formula 1 is described wherein: R1 is hydrogen, 1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl or hydroxy-1-4C-alkyl, R2 is hydrogen, 1-4C-alkyl, hydroxy-1-4C-alkyl, halogen, 2-4C-alkenyl or 2-4C-alkynyl, R3 is hydrogen, halogen, trifluoromethyl, 1-4C-alkyl, 2-4C-alkenyl, 2-4C-alkynyl, carboxyl, -CO-1-4C-alkoxy, hydroxy-1-4C-alkyl, 1-4C-alkoxy-1-4C-alkyl, fluoro-1-4C-alkoxy-1-4C-alkyl or the radical -CO-NR3aR3b, one of the substituents R4a and R4b is hydrogen, 1-7C-alkyl, 2-7C-alkenyl, phenyl or phen-1-4C-alkyl and the other is hydroxyl, 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkoxy,1-4C- alkylcarbonyloxy or the radical R4', or R4a and R4b together are O (oxygen) or 1-7C-alkylidene, where R4' is a radical from which a hydroxyl group is formed under physiological conditions, one of the substituents R5a and R5b is hydrogen, 1-7C-alkyl,2-7C-alkenyl, phenyl or phen-1- 4C-alkyl and the other is hydrogen, hydroxyl, 1-4C-alkoxy,1-4C-alkoxy-1-4C-alkoxy, 1-4C- alkycarbonyloxy or the radical R5', or R5a and R5b together are O (oxygen) or 1-7C-alkylidene, where R5' is a radical from which a hydroxyl group is formed under physiological conditions, or one of the substituents R4a and R4b on the one hand and one of the substituents R5a and R5b on the other hand is in each case hydrogen, 1-7C-alkyl, 2-7C-alkenyl, phenyl or phen-1-4C-alkyl, and the other substituents in each case together form a 1-4C-alkylenedioxy radical, where at least one of the substituents R4a, R4b, R5a and R5b must have the meaning 1-7Calkyl, 1-7C-alkenyl, phenyl or phen-1-4C-alkyl or where either R4a and R4b or R5aC R5b together must be 1-7C-alkylidene; R6 is hydrogen, halogen, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonylamino, 1-4C-alkoxy-1-4C-alkoxycarbonylamino or trifluoromethyl, R7 is hydrogen, halogen, 1-4C-alkyl or 1-4C-alkoxy and X is O (oxygen) or NH R3a and R3b are hydrogen, 1-7C-alkyl, hydroxy-1-4C-alkyl or 1-4C-alkoxy-1-4C-alkyl or R3a and R3b together, including the nitrogen atom to which both are bonded, are a pyrrolidino, piperidino or morpholino radical. A medicament comprising compound 1 is useful in the prevention and treatment of gastrointestinal diseases. |
