| 摘要 |
In the present invention there are disclosed tetracyclic azepine derivatives of the general formula I, in which Re1 and Re2 represent hydrogen, alkyl, alkylcarbonyl, trihalomethylcarbonyl, alkyl being substituted with hydroxyl, alkoxyl, carbonyl, alkylcarbonyloxy group containing 1 to 6 carbon atoms in the alkyl moiety, alkoxycarbonyl or aryl or Re1 and Re2 together with a nitrogen atom to which they are attached can form a morpholine radical, Re3, Re4, Re5, Re6, Re9, Re10, Re11 and Re12 represent independently on each other hydrogen, halogen, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxy, nitro, amino, mono- or diamino, alkylcarbonylamino, aminosulfonyl, mono- or diaminosulfonyl, alkyl, alkoxy, alkylcarbonyl, or alkoxycarbonyl, Re7 and Re8 represent independently on each other hydrogen, OH, alkyl or alkoxy containing 1 to 6 carbon atoms or Re7 and Re8 together can form methylidene, mono or di(cyano)methylene, the group -(CHi2)i2-, -(CHi2)i3-, -(CHi2)i4-, -(CHi2)i5-, -O-(CHi2)i2-O-, or O-(CHi2)i3-O or together with a carbon atom to which they are attached they can represent carbonyl, Re13 represents hydrogen, alkyl or trifluoromethyl, Re14 represents alkyl, cyano or trifluoromethyl, a is 0 to 6, aryl can be optionally a substituted phenyl, as well as their pharmaceutically acceptable addition salts with acids or bases, their stereochemically isomeric forms and A-oxides. In the present invention there are also claimed process and intermediates for their preparation as well as pharmaceutical preparations based thereon. The compounds are mCPP-antagonists and they can be therefore used for treating or prevention of central nervous system diseases, cardiovascular diseases or gastrointestinal disorders. |
