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    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors
    1.
    发明申请
    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors 审中-公开
    磺酰胺苯胺衍生物作为Janus激酶抑制剂

    公开(公告)号：US20080261973A1

    公开(公告)日：2008-10-23

    申请号：US12158764

    申请日：2006-12-20

    申请人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    发明人： Hans-Georg Capraro ,  Bernard Coupez ,  Pascal Furet ,  Paul W. Manley ,  Carole Pissot Soldermann

    IPC分类号： C07D473/32 ,  C07D487/04 ,  A61K31/52 ,  A61K31/5377

    CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D487/04 ,  C07D519/00

    摘要： The invention relates to sulphonamidoanilines of formula I, wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R1 represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alky, or R4 and R5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R2 is hydrogen, lower alkenyl or alkyl, R3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.

    摘要翻译： 本发明涉及式I的磺酰氨基苯胺，其中A是N或CH，W，X，Y和Z是N或CH，条件是三个符号W，X和Y中的至少一个表示CH， 1表示NR 4 R 5或OR 4，其中R 4表示任选取代的烷基， 任选包含一个或两个氮原子或氧原子的任选取代的环烷基或取代的芳基，R 5表示氢或未取代或取代的烷基，或R 4和R 3， 与它们所连接的氮一起代表任选取代的五元或六元含氮单环，任选取代的含氮完全饱和双环，或含有一个或两个 氮原子，R 2是氢，低级烯基或烷基，R 3是未被取代的或被卤素单 - ，二 - 或三取代的烷基; 烯基或芳基，及其盐; 其制备方法，它们在人体或动物体内的治疗中的应用，单独使用或与一种或多种其它药学活性化合物组合用于治疗疾病，治疗这种疾病的方法和 使用这种化合物单独或与一种或多种其它药学活性化合物组合，用于制备用于治疗增殖性疾病的药物制剂。

    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
    9.
    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。

    1H-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases
    10.
    发明授权
    1H-imidazo[4,5-c]quinoline derivatives in the treatment of protein kinase dependent diseases 有权
    1H-咪唑并[4,5-c]喹啉衍生物在治疗蛋白激酶依赖性疾病中的应用

    公开(公告)号：US07998972B2

    公开(公告)日：2011-08-16

    申请号：US10515126

    申请日：2003-05-20

    申请人： Carlos Garcia-Echeverria ,  Hans-Georg Capraro ,  Pascal Furet

    发明人： Carlos Garcia-Echeverria ,  Hans-Georg Capraro ,  Pascal Furet

    IPC分类号： A61K31/4166 ,  A61K31/4188 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoloquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.

    摘要翻译： 本发明涉及咪唑并喹啉及其盐在治疗蛋白激酶依赖性疾病中的用途，以及用于制备用于治疗所述疾病的药物制剂，用于治疗蛋白激酶依赖性疾病的咪唑并喹啉， 所述疾病包括将咪唑并喹啉给予包含咪唑并喹啉的温血动物，特别是用于治疗蛋白激酶依赖性疾病的新型咪唑并喹啉的药物制剂，以及制备新的咪唑并喹啉的方法。