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    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。

    Pyrido-and pyrimidopyrimidine derivatives as anti-proliferative agents
    9.
    发明授权
    Pyrido-and pyrimidopyrimidine derivatives as anti-proliferative agents 有权
    吡啶并嘧啶并嘧啶衍生物作为抗增殖剂

    公开(公告)号：US08772272B2

    公开(公告)日：2014-07-08

    申请号：US12724203

    申请日：2010-03-15

    申请人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Pierre Henri Storck ,  Virginie Sophie Poncelet ,  Kristof Van Emelen ,  Peter Jacobus Johnnes Antonius Buijnsters ,  Werner Constant Johan Embrechts ,  Timothy Pietro Suren Perera

    发明人： Eddy Jean Edgard Freyne ,  Marc Willems ,  Pierre Henri Storck ,  Virginie Sophie Poncelet ,  Kristof Van Emelen ,  Peter Jacobus Johnnes Antonius Buijnsters ,  Werner Constant Johan Embrechts ,  Timothy Pietro Suren Perera

    IPC分类号： A61K31/33 ,  A61K31/519 ,  C07D487/00 ,  C07D487/18

    CPC分类号： C07D498/16 ,  C07D471/04 ,  C07D487/04 ,  C07D487/16 ,  C07D487/22

    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 a1-a2=a3-a4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的加成盐和立体化学异构体，其中a1-a2 = a3-a4表示选自N-CH = CH-CH，N- CH = N-CH或CH-CH = N-CH; Z表示NH; Y表示-C3-9烷基 - ，-C1-5烷基-NR13-C1-5烷基 - ，C1-6烷基-NH-CO-或-CO-NH-C1-6烷基 - ; X1表示-O-或-NR11-; X2表示-C1-2烷基 - ， - O-C1-2烷基，-O-或-O-CH2-; R1表示氢或卤素; R 2表示氢，氰基，卤素，羟基羰基 - ，C 1-4烷氧基羰基 - ，Het 16 - 羰基 - 或Ar 5; R3表示氢; R 4表示羟基，C 1-4烷氧基 - ，Ar 4 -C 1-4烷氧基或R 4表示被一个或多个可能的两个或多个选自C 1-4烷氧基或Het 2-的取代基取代的C 1-4烷氧基; R11表示氢; R 12表示氢，C 1-4烷基 - 或C 1-4烷基 - 氧基 - 羰基 - ; R13表示Het14-C1-4烷基，特别是吗啉基-C 1-4烷基; Het2表示选自任选被C 1-4烷基，优选甲基取代的吗啉基或哌啶基的杂环; Het14代表吗啉基; Het16表示选自吗啉基或吡咯烷基的杂环; Ar4表示苯基; Ar 5表示任选被氰基取代的苯基。