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2. 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。

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