会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 8. 发明申请
    • BENZISOXAZOLES
    • 苯并异恶唑
    • WO2005089753A2
    • 2005-09-29
    • PCT/EP2005/051105
    • 2005-03-11
    • JANSSEN PHARMACEUTICA N.V.KENNIS, Ludo, Edmond, JosephineVANHOOF, Greta, Constantia, PeterBONGARTZ, Jean-Pierre, André, MarcLUYCKX, Marcel, Gerebernus, MariaMINKE, Wenda, Eveline
    • KENNIS, Ludo, Edmond, JosephineVANHOOF, Greta, Constantia, PeterBONGARTZ, Jean-Pierre, André, MarcLUYCKX, Marcel, Gerebernus, MariaMINKE, Wenda, Eveline
    • A61K31/423
    • A61K31/423A61K31/42A61K31/425A61K31/426A61K31/428C07D261/20
    • 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-.
    • 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。