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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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. |
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