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
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creator Ceusters, Marc
Stokbroekx, Raymond
Van der Aa, Marcel
Luyckx, Marcel
Willems, Marc
Tuman, Robert
description 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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Stokbroekx, Raymond ; Van der Aa, Marcel ; Luyckx, Marcel ; Willems, Marc ; Tuman, Robert</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-uspatents_applications_200400099873</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2004</creationdate><toplevel>online_resources</toplevel><creatorcontrib>Ceusters, Marc</creatorcontrib><creatorcontrib>Stokbroekx, Raymond</creatorcontrib><creatorcontrib>Van der Aa, Marcel</creatorcontrib><creatorcontrib>Luyckx, Marcel</creatorcontrib><creatorcontrib>Willems, Marc</creatorcontrib><creatorcontrib>Tuman, Robert</creatorcontrib><collection>USPTO Published Applications</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Ceusters, Marc</au><au>Stokbroekx, Raymond</au><au>Van der Aa, Marcel</au><au>Luyckx, Marcel</au><au>Willems, Marc</au><au>Tuman, Robert</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4,-THIADIAZOLYL DERIVATIVES</title><date>2004-01-15</date><risdate>2004</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record>
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