ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4,-THIADIAZOLYL DERIVATIVES

This invention concerns compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R 1 is hydrogen, C 1-6 alkyl, C 1-6 alkyloxy, C 1-6 alkylthio, amino, mono- or di(C 1-6 alkyl)amino, Ar 1 , Ar 1 NH...

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Hauptverfasser: Ceusters, Marc, Stokbroekx, Raymond, Van der Aa, Marcel, Luyckx, Marcel, Willems, Marc, Tuman, Robert
Format: Patent
Sprache:eng
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Zusammenfassung:This invention concerns compounds of formula 1 the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R 1 is hydrogen, C 1-6 alkyl, C 1-6 alkyloxy, C 1-6 alkylthio, amino, mono- or di(C 1-6 alkyl)amino, Ar 1 , Ar 1 NH-, C 3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R 2 is hydrogen, C 1-6 alkyl, amino, aminocarbonyl, mono- or di(C 1-6 alkyl)amino, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonylamino, hydroxy or C 1-6 alkyloxy; R 3 , R 4 and R 5 are each independently selected from hydrogen, halo, C 1-6 alkyl, C 1-6 alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C 1-6 alkyloxyC 1-6 alkyl, C 1-6 alkylthio, C 1-6 alkyloxycarbonyl or Het 1 ; 2 is Ar 2 , Ar 2 CH 2 - or Het 2 ; Ar 1 and Ar 2 optionally substituted phenyl; Het 1 and Het 2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.