专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06602873B2 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
标题翻译：血管发生抑制噻二唑基哒嗪衍生物
公开(公告)号：US06602873B2
公开(公告)日：2003-08-05
申请号：US09864594
申请日：2001-05-24
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A61K31501
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7-Alk1-X-, NR7-Alk1-X-Alk2-, O-Alk1-X-, O-Alk1-X-Alk2- or S-Alk1-X-; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

2. 发明授权

US06833369B2 Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives 失效
标题翻译：血管发生抑制5-取代-1,2,4-噻二唑衍生物
公开(公告)号：US06833369B2
公开(公告)日：2004-12-21
申请号：US09998975
申请日：2001-10-19
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A61K31496
CPC分类号： C07D213/83 , A61K31/454 , C07D241/26 , C07D285/08 , C07D285/135 , C07D295/155 , C07D417/04 , C07D417/12
摘要： This invention concerns compounds of formula 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 hydrogen, 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, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar 1，Ar 1 NH-，C 3-6环烷基，羟甲基或苄氧基甲基 R 2是氢，C 1-6烷基，氨基，氨基羰基，一或二（C 1-6烷基）氨基，C 1-6烷氧基羰基，C 1-6烷基羰基氨基，羟基或C 1-6烷氧基; R 3，R 4和R 5各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基 C 1-6烷氧基羰基或Het 1; Ar 2，Ar 2 CH 2 - 或Het 2; Ar 1和Ar 2任选取代的苯基; Het 1和Het 2是任选取代的单环杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

3. 发明授权

US07208503B2 Angiogenesis inhibiting 5-substituted-1,2,4-thiadiazolyl derivatives 失效
标题翻译：血管发生抑制5-取代-1,2,4-噻二唑衍生物
公开(公告)号：US07208503B2
公开(公告)日：2007-04-24
申请号：US10387703
申请日：2003-03-13
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A01N43/40 , A61K31/445 , C07D211/68
CPC分类号： C07D285/08 , A61K31/454 , A61K31/496 , C07D285/135 , C07D417/04
摘要： This invention concerns compounds of formula 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 benzoyloxymethyl; R2 is hydrogen, 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, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; is Ar2, Ar2CH2— or Het2; Ar1 and Ar2 optionally substituted phenyl; Het1 and Het2 are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar 1，Ar 1，NH 3，C 3 -6个环烷基，羟甲基或苯甲酰氧基甲基; R 2是氢，C 1-6烷基，氨基，氨基羰基，一或二（C 1-6烷基）氨基，C C 1-6烷氧基羰基，C 1-6烷基羰基氨基，羟基或C 1-6烷氧基; R 3，R 4和R 5各自独立地选自氢，卤素，C 1-6烷基 C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷基氧基C 1-6烷基，C 1〜 C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 是Ar 2，Ar 2，CH 2或Het 2; Ar 1和Ar 2任选取代的苯基; Het 1和H 2 2是任选取代的单环杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

4. 发明授权

US06265407B1 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives 失效
标题翻译：血管发生抑制噻二唑基哒嗪衍生物
公开(公告)号：US06265407B1
公开(公告)日：2001-07-24
申请号：US09446495
申请日：2000-08-14
申请人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
发明人： Raymond Antoine Stokbroekx , Marc André Ceusters , Marcel Jozef Maria Van der Aa , Marcel Gerebernus Maria Luyckx , Marc Willems , Robert W. Tuman
IPC分类号： A61K31501
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1—NH—, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula —CH═CH—CH═CH—; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula —CH═CH—CH═CH—; A is a bivalent radical of formula NR7, NR7—Alk1—X—, NR7—Alk1—X—Alk2—, O—Alk1—X—, O—Alk1—X—Alk2— or S—Alk1—X—; wherein X is a direct bond, —O—, —S—, C═O, —NR8— or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中R 1是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，氨基，单或二（C 1-6烷基）氨基，Ar1，Ar1-NH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; R4，R5和R6各自独立地选自氢，卤素，C 1-6烷基，C 1-6烷氧基，三氟甲基，硝基，氨基，氰基，叠氮基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基，C 1-6烷氧基羰基或Het 1; 或当R 4和R 5彼此相邻时，它们可以一起形成式-CH = CH-CH = CH-的基团; A是式NR7，NR7-Alk1-X，NR7-Alk1-X-Alk2-，O-Alk1-X，O-Alk1-X-Alk2-或S-Alk1-X-2的二价基; 其中X是直接键，-O - ， - S - ，C = O，-NR 8 - 或Het 2; R 7为氢，C 1-6烷基或Ar 2甲基; R8是氢，C1-6烷基或Ar2甲基; Alk1是C1-6烷二基; Alk2是C1-4烷二基; Ar1和Ar2是任选取代的苯基; 苯基; Het1和Het2是任选取代的杂环; 具有血管生成抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式