| 摘要 |
In the present invention, there is disclosed 5-substituted 1,2,4-thiadiazolyl derivative of the general formula I, in which X represents CH or nitrogen; Re1 represents hydrogen, alkyl containing 1 to 6 carbon atoms, alkyloxy containing 1 to 6 carbon atoms, alkylthio containing 1 to 6 carbon atoms, amino, mono- or dialkyl-amino containing 1 to 6 carbon atoms in the alkyl moiety, Are1, Are1-.NY..ETA.-, cycloalkyl containing 3 to 6 carbon atoms, hydroxymethyl or benzyloxymethyl; Re2 denotes hydrogen, alkyl containing 1 to 6 carbon atoms, amino, aminocarbonyl, mono or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, alkyloxycarbonyl containing 1 to 6 carbon atoms in the alkyl moiety, alkylcarbonylamino containing 1 to 6 carbon atoms in the alkyl moiety, OH or alkyloxy containing 1 to 6 carbon atoms; Re3, Re4 and Re5 represent independently on each other hydrogen, halogen, alkyl containing 1 to 6 carbon atoms, alkyloxyl containing 1 to 6 carbon atoms in the alkyl moiety, trifluoromethyl, nitro, amino, cyano, azido, alkyloxy containing 1 to 6 carbon atoms, alkyl containing 1 to 6 carbon atoms, alkylthio containing 1 to 6 carbon atoms in the alkyl moiety, alkyloxycarbonyl containing 1 to 6 carbon atoms in the alkyl moiety or Hete1; - A - denotes Are2, Are2CHi2- or Hete2; Are1 represents an optionally substituted phenyl; Are2 represents an optionally substituted phenyl; Hete1 and Hete2 represent monocyclic, heterocyclic radicals; N-oxide form thereof, pharmaceutically acceptable acid addition salt and stereochemically isomeric form. Disclosed is also process and intermediate for its preparation, further its use and pharmaceutical composition intended particularly for treating angiogenesis-dependent diseases, in which the derivative is comprised. |
