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    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors
    4.
    发明授权
    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors 失效
    适合作为酪氨酸激酶抑制剂的环状二芳基脲

    公开(公告)号：US07855215B2

    公开(公告)日：2010-12-21

    申请号：US11575601

    申请日：2005-09-27

    申请人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul W Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    发明人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul W Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    IPC分类号： A61K31/505 ,  A61K31/506 ,  C07D239/02 ,  C07D401/12 ,  C07D413/12

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14

    摘要： The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.

    摘要翻译： 本发明涉及式I的新化合物：其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CRc，S，NRc或O，其中Rc是H或低级烷基; X，Y和Z各自独立地选自N或C-R 3，其中X，Y和Z中的至少两个是N; 并且每个R a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团，其是取代或未取代的，并且可以是五或六元单环或8,9,10,11或12元双环或三环，并且可以含有0,1,2或3个选自 来自O，N和S; 并且其中所述基团的R1，R2，R3和R4具有如本文所定义的含义，其盐，酯，N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用，它们在制备用于治疗所述疾病的药物组合物中的应用，用于治疗所述疾病的日用脲衍生物的使用方法，包含这些新型二芳基脲 衍生物，制备新型二芳基脲衍生物的方法，上述新型二芳基脲衍生物的使用或使用方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。

    Cyclic Diaryl Ureas Suitable as Tyrosine Kinase Inhibitors
    5.
    发明申请
    Cyclic Diaryl Ureas Suitable as Tyrosine Kinase Inhibitors 失效
    适合作为酪氨酸激酶抑制剂的环状二芳基脲

    公开(公告)号：US20080039440A1

    公开(公告)日：2008-02-14

    申请号：US11575601

    申请日：2005-09-27

    申请人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    发明人： Guido Bold ,  Giorgio Caravatti ,  Andreas Floersheimer ,  Pascal Furet ,  Paul Manley ,  Carole Pissot Soldermann ,  Andrea Vaupel

    IPC分类号： A61K31/506 ,  A61K31/496 ,  A61K31/55 ,  A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14

    CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14

    摘要： The invention relates to novel compounds of Formula I: wherein p is 1, 2 or 3; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; A is CRc, S, NRc or O, where Rc is H or lower alkyl; X, Y and Z are each independently selected from N or C—R3, wherein at least two of X, Y and Z are N; and each Ra is independently selected from hydrogen and lower-alkyl; each Rb is hydrogen or lower-alkyl; G is a group Ar or represents CN or unsubstituted or substituted lower alkyl; Ar is a saturated or unsaturated cyclic group, which is substituted or unsubstituted and maybe a five or six membered monocyclic or a 8, 9, 10, 11 or 12 membered bicyclic or tricyclic ring and may contain 0, 1, 2 or 3 heteroatoms selected from O, N and S; and wherein the radicals have R1, R2, R3 and R4 have the meanings as defined herein, to salts, esters, N-oxides or prodrugs thereof; and their use in the treatment of protein kinase dependent diseases, their use in the manufacture of pharmaceutical compositions for use in the treatment of said diseases, methods of use of diary urea derivatives in the treatment of said diseases, pharmaceutical preparations comprising these novel diaryl urea derivatives, processes for the manufacture of the novel diaryl urea derivatives, the use or methods of use of the novel diaryl urea derivatives as mentioned above, and/or these novel diaryl urea derivatives for use in the treatment of the animal or human body.

    摘要翻译： 本发明涉及式I的新化合物：其中p是1,2或3; n为0,1,2或3; m为0,1,2或3; A是CR，C，NR C或O，其中R c是H或低级烷基; X，Y和Z各自独立地选自N或C-R 3，其中X，Y和Z中的至少两个为N; 并且每个R a a独立地选自氢和低级烷基; 每个R b是氢或低级烷基; G是基团Ar或代表CN或未取代或取代的低级烷基; Ar是饱和或不饱和的环状基团，其是取代或未取代的，并且可以是五或六元单环或8,9,10,11或12元双环或三环，并且可以含有0,1,2或3个选自 来自O，N和S; 并且其中基团具有R 1，R 2，R 3和R 4具有如本文所定义的含义 ，其盐，酯，N-氧化物或前药; 以及它们在治疗蛋白激酶依赖性疾病中的应用，它们在制备用于治疗所述疾病的药物组合物中的应用，用于治疗所述疾病的日用脲衍生物的使用方法，包含这些新型二芳基脲 衍生物，制备新型二芳基脲衍生物的方法，上述新型二芳基脲衍生物的使用或使用方法，和/或这些新型二芳基脲衍生物用于动物或人体的治疗。