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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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. |
format | Patent |
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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.</description><language>eng</language><creationdate>2004</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://image-ppubs.uspto.gov/dirsearch-public/print/downloadPdf/20040009987$$EPDF$$P50$$Guspatents$$Hfree_for_read</linktopdf><link.rule.ids>230,308,776,869,881,64032</link.rule.ids><linktorsrc>$$Uhttps://patentcenter.uspto.gov/applications/09998975$$EView_record_in_USPTO$$FView_record_in_$$GUSPTO$$Hfree_for_read</linktorsrc></links><search><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><title>ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4,-THIADIAZOLYL DERIVATIVES</title><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.</description><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2004</creationdate><recordtype>patent</recordtype><sourceid>EFI</sourceid><recordid>eNrjZHB19HP39Hd39XMN9gxW8PTz8HTyDPH0c1cw1Q0OdQoO8QwJDXF10TXUMdIx0dEN8fB0dPF0jPL3ifRRcHEN8gxzDPEMcw3mYWBNS8wpTuWF0twMmm6uIc4euqXFBYklqXklxfGJBQU5mcmJJZn5ecXxRgYGJgYGBpaWFubGpKgFANsFMxY</recordid><startdate>20040115</startdate><enddate>20040115</enddate><creator>Ceusters, Marc</creator><creator>Stokbroekx, Raymond</creator><creator>Van der Aa, Marcel</creator><creator>Luyckx, Marcel</creator><creator>Willems, Marc</creator><creator>Tuman, Robert</creator><scope>EFI</scope></search><sort><creationdate>20040115</creationdate><title>ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4,-THIADIAZOLYL DERIVATIVES</title><author>Ceusters, Marc ; 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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language | eng |
recordid | cdi_uspatents_applications_20040009987 |
source | USPTO Published Applications |
title | ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4,-THIADIAZOLYL DERIVATIVES |
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