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. 发明申请

WO2005089753A2 BENZISOXAZOLES 审中-公开
标题翻译：苯并异恶唑
公开(公告)号：WO2005089753A2
公开(公告)日：2005-09-29
申请号：PCT/EP2005/051105
申请日：2005-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , KENNIS, Ludo, Edmond, Josephine , VANHOOF, Greta, Constantia, Peter , BONGARTZ, Jean-Pierre, André, Marc , LUYCKX, Marcel, Gerebernus, Maria , MINKE, Wenda, Eveline
发明人： KENNIS, Ludo, Edmond, Josephine , VANHOOF, Greta, Constantia, Peter , BONGARTZ, Jean-Pierre, André, Marc , LUYCKX, Marcel, Gerebernus, Maria , MINKE, Wenda, Eveline
IPC分类号： A61K31/423
CPC分类号： A61K31/423 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , C07D261/20
摘要： The present invention concerns the compounds of formula (I), the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R 1 ; Y is absent when X represents -Z-R 1 and -(C=O)-R 6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR 5 -carbonyl-; R 1 represents C 1 - 4 alkyl, Ar 1 , Ar 1 -C 1-4 a1ky1-, -NR 3 R 4 or -Het 1 ; R 2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C 1-4 alkyloxy or C 1-4 alkyl; R 3 and R 4 are each independently selected from hydrogen, Ar 3 or C 1-4 alkyl; R 5 represents hydrogen, C 1-4 alkylcarbonyl- or Ar 4 -carbonyl-; R 6 represents a substituent selected from the group consisting of C 1 . 4 alkyl, Ar 5 , Ar 6 -C 1-4 alkyl- or NR 7 R 8 ; R 7 and R 8 are each independently selected from hydrogen, Het 4 or C 1-4 alkyl; Het 1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substituents selected from the group consisting of amino, C 1-4 alkyl, hydroxy-C 1-4 alkyl, phenyl, phenyl-C 1-4 alkyl- and phenyl substituted with one or more halo substituents; Het 4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substituents selected from the group consisting of amino, C 1-4 alkyl, hydroxy-C 1-4 alkyl-, phenyl, phenyl-C l-4 alkyl and phenyl substituted with one or more halo substituents; and Ar 1 , Ar 2 , Ar 3 , Ar 4 , Ar 5 or Ar 6 each independently represents phenyl optionally substituted one or where possible two or more substituents selected from halo, nitro, C 1-4 alkyl, hydroxy or C 1-4 alkyloxy-.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示1至3的整数; X代表氨基，羟基，-oxo或-Z-R 1; 当X表示氧代时，当X表示-Z-R 1和 - （C = O）-R 6时，Y不存在; Z表示羰基， - 氧基 - 羰基 - 或-NR 5 - 羰基 - ; R 1表示C 1-4烷基，Ar 1，Ar 1 -C 1-4烷基，-NR 3 R 4或-Het 1; R 2表示氢，卤素，硝基，羟基羰基 - ，C 1-4烷氧基或C 1-4烷基; R 3和R 4各自独立地选自氢，Ar 3或C 1-4烷基; R 5表示氢，C 1-4烷基羰基 - 或Ar 4 - 羰基 - ; R 6表示选自C 1-4烷基，Ar 5，Ar 6 -C 1-4烷基或NR 7 R 8中的取代基。 R 7和R 8各自独立地选自氢，Het 4或C 1-4烷基; Het 1表示选自恶唑基，异恶唑基，咪唑基或吡唑基的杂环，其中所述杂环任选被一个，两个或三个选自以下的取代基取代：氨基，C 1-4烷基，羟基-C 1-4烷基，苯基，苯基 C 1-4烷基 - 和被一个或多个卤素取代基取代的苯基; Het 4表示选自恶唑基或异恶唑基的杂环，其中所述杂环任选被一个或多个选自以下的取代基取代：氨基，C 1-4烷基，羟基-C 1-4烷基 - ，苯基，苯基-C 1-4烷基和被一个或多个卤素取代基取代的苯基; Ar 1，Ar 2，Ar 3，Ar 4，Ar 5或Ar 6各自独立地表示任选被取代的苯基，或者可能的两个或多个选自卤素，硝基， C 1-4烷基，羟基或C 1-4烷氧基。

2. 发明公开

EP1746991A2 DAAO INHIBITING BENZISOXAZOLES FOR TREATING MENTAL DISORDERS 审中-公开
标题翻译：大坳耐苯并异恶唑精神疾病的治疗
公开(公告)号：EP1746991A2
公开(公告)日：2007-01-31
申请号：EP05731936.0
申请日：2005-03-11
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： KENNIS, Ludo, Edmond, Josephine , VANHOOF, Greta, Constantia, Peter , BONGARTZ, Jean-Pierre, André, Marc , LUYCKX, Marcel, Gerebernus, Maria , MINKE, Wenda, Eveline
IPC分类号： A61K31/423 , C07D413/12 , C07D261/20 , A61P25/18
CPC分类号： A61K31/423 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , C07D261/20
摘要： The present invention concerns the compounds of formula (I) , the substituents being specified in the description, (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemical Iy isomeric forms thereof , and their use for the manufacture of a medicament for the treatment of mental disorders, preferably schizophrenia.

3. 发明公开

EP0993452A1 ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4-THIADIAZOLYL DERIVATIVES 失效
标题翻译：血管生成抑制5-取代的-1,2,4- THIADIAZOLYLDERIVATE
公开(公告)号：EP0993452A1
公开(公告)日：2000-04-19
申请号：EP98937560.5
申请日：1998-06-22
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： STOKBROEKX, Raymond, Antoine , CEUSTERS, Marc, André , VAN DER AA, Marcel, Jozef, Maria , LUYCKX, Marcel, Gerebernus, Maria , WILLEMS, Marc , TUMAN, Robert, W.
IPC分类号： C07D285/08 , C07D285/135 , C07D417/04 , A61K31/41 , A61K31/495 , C07D213/83 , C07D241/28 , C07D295/155
CPC分类号： C07D285/135 , C07D213/83 , C07D241/26 , C07D241/28 , C07D285/08 , C07D295/155 , C07D417/04 , C07D417/12
摘要： 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, C¿1-6?alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar?1, Ar1¿NH-, C¿3-6?cycloalkyl, hydroxymethyl or benzyloxymethyl; R?2¿ is hydrogen, C¿1-6?alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R?3, R4 and R5¿ are each independently selected from hydrogen, halo, C¿1-6?alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het?1¿; formula (1) is Ar?2, Ar2CH¿2- or Het?2; 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.

4. 发明授权

EP0993452B1 ANGIOGENESIS INHIBITING 5-SUBSTITUTED-1,2,4-THIADIAZOLYL DERIVATIVES 失效
标题翻译：血管生成抑制5-取代的-1,2,4- THIADIAZOLYLDERIVATE
公开(公告)号：EP0993452B1
公开(公告)日：2007-09-05
申请号：EP98937560.5
申请日：1998-06-22
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： STOKBROEKX, Raymond, Antoine , CEUSTERS, Marc, André , VAN DER AA, Marcel, Jozef, Maria , LUYCKX, Marcel, Gerebernus, Maria , WILLEMS, Marc , TUMAN, Robert, W.
IPC分类号： C07D285/08 , C07D285/135 , C07D417/04 , A61K31/41 , A61K31/495 , C07D213/83 , C07D241/28 , C07D295/155
CPC分类号： C07D285/135 , C07D213/83 , C07D241/26 , C07D241/28 , C07D285/08 , C07D295/155 , C07D417/04 , C07D417/12
摘要： 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; R is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar , Ar NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R is hydrogen, C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbonyl, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; R , R and R are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het ; formula (1) is Ar , Ar CH2- or Het ; Ar and Ar optionally substituted phenyl; Het and Het are optionally substituted monocyclic heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

5. 发明授权

EP0991649B1 ANGIOGENESIS INHIBITING THIADIAZOLYL PYRIDAZINE DERIVATIVES 失效
标题翻译：血管生成抑制剂THIADIAZOLYPYRIDAZINE衍生物
公开(公告)号：EP0991649B1
公开(公告)日：2003-03-26
申请号：EP98940098.1
申请日：1998-06-22
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： STOKBROEKX, Raymond, Antoine , CEUSTERS, Marc, André , VAN DER AA, Marcel, Jozef, Maria , LUYCKX, Marcel, Gerebernus, Maria , WILLEMS, Marc , TUMAN, Robert, W.
IPC分类号： C07D417/04 , C07D417/14 , A61K31/41
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar , Ar -NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R and R are hydrogen, or taken together may form a bivalent radical of formula -CH=CH-CH=CH-; R , R and R are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het ; or when R and R 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 NR , NR -Alk -X-, NR -Alk -X-Alk -, O-Alk -X-, O-Alk -X-Alk - or S-Alk -X-; wherein X is a direct bond, -O-, -S-, C=O, -NR - or Het ; R is hydrogen, C1-6alkyl or Ar methyl; R is hydrogen, C1-6alkyl or Ar methyl; Alk is C1-6alkanediyl; Alk is C1-4alkanediyl; Ar and Ar are optionally substituted phenyl; phenyl; Het and Het are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.

6. 发明公开

EP0991649A1 ANGIOGENESIS INHIBITING THIADIAZOLYL PYRIDAZINE DERIVATIVES 失效
标题翻译：血管生成抑制剂THIADIAZOLYPYRIDAZINE衍生物
公开(公告)号：EP0991649A1
公开(公告)日：2000-04-12
申请号：EP98940098.1
申请日：1998-06-22
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： STOKBROEKX, Raymond, Antoine , CEUSTERS, Marc, André , VAN DER AA, Marcel, Jozef, Maria , LUYCKX, Marcel, Gerebernus, Maria , WILLEMS, Marc , TUMAN, Robert, W.
IPC分类号： C07D417/04 , C07D417/14 , A61K31/41
CPC分类号： C07D417/04 , C07D417/14
摘要： This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C¿1-6?alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar?1, Ar1¿-NH-, C¿3-6?cycloalkyl, hydroxymethyl or benzyloxymethyl; R?2 and R3¿ are hydrogen, or taken together may form a bivalent radical of formula -CH=CH-CH=CH-; R?4, R5 and R6¿ are each independently selected from hydrogen, halo, C¿1-6?alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het?1¿; or when R?4 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 NR?7, NR7-Alk1-X-, NR7-Alk1-X-Alk2¿-, O-Alk1-X-, O-Alk?1-X-Alk2¿- or S-Alk1-X-; wherein X is a direct bond, -O-, -S-, C=O, -NR8- or Het2; R7 is hydrogen, C¿1-6?alkyl or Ar?2¿methyl; R8 is hydrogen, C¿1-6?alkyl or Ar?2¿methyl; Alk1 is C¿1-6?alkanediyl; Alk?2¿ is C¿1-4?alkanediyl; Ar?1 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.

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