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    MTKI quinazoline derivatives
    7.
    发明授权
    MTKI quinazoline derivatives 有权
    MTKI喹唑啉衍生物

    公开(公告)号：US08492377B2

    公开(公告)日：2013-07-23

    申请号：US12373404

    申请日：2007-07-12

    申请人： Alexandra Papanikos ,  Eddy Jean Edgard Freyne ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Pierre-Henri Storck

    发明人： Alexandra Papanikos ,  Eddy Jean Edgard Freyne ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Pierre-Henri Storck

    IPC分类号： A61K31/54 ,  A61K31/535 ,  A61K31/497 ,  C07D471/04

    CPC分类号： C07D498/14 ,  C08K5/544

    摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O —; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(═O)2—C1-4alkyl-C(═O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(═O)2—C1-4alkyl-.

    摘要翻译： 本发明涉及式I化合物的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Y代表-C3-9烷基 - ， - C1-5烷基-NR6-C1-5烷基 - 或-C1- 5烷基-NR 7 -CO-C 1-5烷基 - ; X1表示-O - ; X2表示NR5-C1-2烷基 - ; R1代表氢，卤素或Het3-O-; R2表示氢; R 3表示羟基，被一个或两个独立地选自Het4，羟基，C 1-4烷氧基 - ，C 1-4烷氧基-C 1-4烷氧基和NR 9 R 10的取代基取代的C 1-4烷氧基 - 或C 1-4烷氧基; R5代表氢或C1-4烷基; R6代表氢或C1-4烷基; R7代表氢; R9和R10各自独立地表示氢; C 1-4烷基-S（= O）2 -C 1-4烷基-C（= O） - ; 被羟基取代的C 1-4烷基或C 1-4烷基; Het3表示任选被C 1-4烷基取代的吡啶基; Het4表示吗啉基，哌啶基或哌嗪基，其中所述Het4任选被羟基-C 1-4烷基或C 1-4烷基-S（= O）2 -C 1-4烷基取代。

    MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI
    8.
    发明申请
    MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI 审中-公开
    大分子喹唑啉衍生物及其作为MTKI的用途

    公开(公告)号：US20100152174A1

    公开(公告)日：2010-06-17

    申请号：US11720693

    申请日：2005-12-08

    申请人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Peter Ten Holte ,  Alexandra Papanikos ,  Werner Constant John Embrechts ,  Pierre Henri Storck ,  Virginie Sophie Poncelet ,  Werner Constant Johan Embrechts ,  Pierre Henri Storck ,  Virginie Sophie Poncelet

    发明人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Peter Ten Holte ,  Alexandra Papanikos ,  Werner Constant John Embrechts ,  Pierre Henri Storck ,  Virginie Sophie Poncelet ,  Werner Constant Johan Embrechts ,  Pierre Henri Storck ,  Virginie Sophie Poncelet

    IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/517 ,  C07D498/04 ,  A61P35/00

    CPC分类号： C07D498/06 ,  C07D498/08

    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 Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydrogen, C1-4alkyl or R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R23 represents C1-4alkyl and R23 represents hydrogen when R16 and R17 taken together with the carbon atom to which they are attached from a C3-6cycloalkyl; R25, R26, R27 and R28 each independently represent hydrogen or C1-4alkylcarbonyl; Het1 represents 2-bora-1,3-dioxolanyl; Het represents piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl wherein said Het2 is optionally substituted with C1-4alkyloxycarbonyl or NR27R28—C1-4alkyl; Ar4 and Ar5 represents phenyl; Ar6 represents phenyl optionally substituted with nitro.

    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Z表示NH; Y表示-C3-9烷基，-C1-5烷基-NR13-C1-5烷基，-C1-5烷基-NR14-CO-C1-5烷基，-C1-2烷基-NR21-H2-CO-NH-C1-3烷基 - 或-C1-2烷基-NR23-CO-CR16R17-NH-; X 1表示O或-O-C 1-2烷基 - ; X2表示直接键，C1-2烷基，-CO-C1-2烷基或NR12-​​C1-2烷基; R1表示氢或卤素; R2代表卤代，乙炔或Het1; R3表示氢或氰基; R 4表示被一个或多个可能的两个或多个选自Het 2，NR 7 R 8，羟基和C 1-4烷氧基-C 1-4烷氧基 - 的取代基取代的Ar 4 -C 1-4烷氧基 - ，C 1-4烷氧基 - 或C 1-4烷氧基。 R7代表氢或C1-4烷基; R8表示被NR25R26或C1-4烷基磺酰基取代的C1-4烷基; R 12表示氢或C 1-4烷基 - ; R 13表示Ar 6 - 磺酰基或任选被苯基取代的C 1-6烷氧基羰基; R 16和R 17表示氢，C 1-4烷基或R 16和R 17与它们与C 3-6环烷基连接的碳原子一起; 当R 16和R 17与C 3-6环烷基连接的碳原子一起时，R 23表示C 1-4烷基，R 23表示氢; R 25，R 26，R 27和R 28各自独立地表示氢或C 1-4烷基羰基; Het1代表2-硼-1,3-二氧戊环基; Het表示哌啶基，哌嗪基，吗啉基，硫代吗啉基或1,1-二氧代硫代吗啉基，其中所述Het2任选被C 1-4烷氧基羰基或NR 27 R 28 -C 1-4烷基取代; Ar 4和Ar 5表示苯基; Ar 6表示任选被硝基取代的苯基。

    MTKI QUINAZOLINE DERIVATIVES
    9.
    发明申请
    MTKI QUINAZOLINE DERIVATIVES 有权
    MTKI喹诺酮衍生物

    公开(公告)号：US20100029627A1

    公开(公告)日：2010-02-04

    申请号：US12373404

    申请日：2007-07-12

    申请人： Alexandra Papanikos ,  Freyne Eddy Jean Edgard ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Fierre-Henri Storck

    发明人： Alexandra Papanikos ,  Freyne Eddy Jean Edgard ,  Peter Ten Holte ,  Marc Willems ,  Werner Constant Johan Embrechts ,  Laurence Anne Mevellec ,  Fierre-Henri Storck

    IPC分类号： A61K31/541 ,  C07D271/12 ,  A61K31/519 ,  A61K31/496 ,  A61K31/5377 ,  A61P9/10 ,  A61P35/00 ,  A61P29/00

    CPC分类号： C07D498/14 ,  C08K5/544

    摘要： The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O—; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(═O)2—C1-4alkyl-C(═O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(═O)2—C1-4alkyl-.

    摘要翻译： 本发明涉及式I化合物的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Y代表-C3-9烷基 - ， - C1-5烷基-NR6-C1-5烷基 - 或-C1- 5烷基-NR 7 -CO-C 1-5烷基 - ; X1表示-O-; X2表示NR5-C1-2烷基 - ; R1代表氢，卤素或Het3-O-; R2表示氢; R 3表示羟基，被一个或两个独立地选自Het4，羟基，C 1-4烷氧基 - ，C 1-4烷氧基-C 1-4烷氧基和NR 9 R 10的取代基取代的C 1-4烷氧基 - 或C 1-4烷氧基; R5代表氢或C1-4烷基; R6代表氢或C1-4烷基; R7代表氢; R9和R10各自独立地表示氢; C 1-4烷基-S（-O）2 -C 1-4烷基-C（-O） - ; 被羟基取代的C 1-4烷基或C 1-4烷基; Het3表示任选被C 1-4烷基取代的吡啶基; Het4表示吗啉基，哌啶基或哌嗪基，其中所述Het4任选被羟基-C 1-4烷基或C 1-4烷基-S（-O）2 -C 1-4烷基取代。