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

This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH-, C3-6cyc...

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Hauptverfasser: STOKBROEKX, RAYMOND ANTOINE, LUYCKX, MARCEL GEREBERNUS MARIA, WILLEMS, MARC, CEUSTERS, MARC ANDRE, TUMAN, ROBERT W, VAN DER AA, MARCEL JOZEF MARIA
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 is hydroge n, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R3, R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitr o, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; formula (1) is Ar2, Ar2CH2- or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 ar e optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity ; their preparation, compositions containing them and their use as a medicine.