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178 条记录 (耗时 0.09 秒)

    1,3-dihydro-imidazo[4,5-c]quinolin-2-ones as lipid kinase inhibitors
    82.
    发明授权
    1,3-dihydro-imidazo[4,5-c]quinolin-2-ones as lipid kinase inhibitors 有权
    1,3-二氢 - 咪唑并[4,5-c]喹啉-2-酮作为脂质激酶抑制剂

    公开(公告)号：US08431592B2

    公开(公告)日：2013-04-30

    申请号：US13165144

    申请日：2011-06-21

    申请人： Carlos Garcia-Echeverria ,  Frederic Stauffer ,  Pascal Furet

    发明人： Carlos Garcia-Echeverria ,  Frederic Stauffer ,  Pascal Furet

    IPC分类号： A61K31/4188

    CPC分类号： C07D471/04

    摘要： The invention relates to methods of treatment of a proliferative disease which responds to inhibition of PI3-Kinase-related protein kinases, particularly the PI3-kinase, by administration of a novel organic compound of formula (I) to a human or animal requiring such treatment; and methods of treatment of inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease, by administration of such compound.

    摘要翻译： 本发明涉及通过向需要这种治疗的人或动物施用式（I）的新型有机化合物来治疗对PI3-激酶相关蛋白激酶，特别是PI3激酶的抑制作用的增殖性疾病的治疗方法 ; 以及通过施用该化合物治疗炎性或阻塞性气道疾病如哮喘，通常与移植相关的疾病或增生性疾病如肿瘤疾病的治疗方法。

    Cyclic diaryl ureas suitable as tyrosine kinase inhibitors
    85.
    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。

    1,3-DIHYDRO-IMIDAZO[4,5-C]QUINOLIN-2-ONES AS LIPID KINASE INHIBITORS
    88.
    发明申请
    1,3-DIHYDRO-IMIDAZO[4,5-C]QUINOLIN-2-ONES AS LIPID KINASE INHIBITORS 有权
    1,3-二氢-1H-咪唑并[4,5-C]喹啉-2-酮作为脂质激酶抑制剂

    公开(公告)号：US20100056558A1

    公开(公告)日：2010-03-04

    申请号：US12577268

    申请日：2009-10-12

    申请人： Carlos Garcia-Echeverria ,  Frédéric Stauffer ,  Pascal Furet

    发明人： Carlos Garcia-Echeverria ,  Frédéric Stauffer ,  Pascal Furet

    IPC分类号： A61K31/437 ,  C07D471/04 ,  A61P11/00 ,  A61P35/00 ,  A61P29/00

    CPC分类号： C07D471/04

    摘要： The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for 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 an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.

    摘要翻译： 本发明涉及式（I）的新型有机化合物，其制备方法，其在治疗人或动物体的方法中的应用，其用途单独或与一种或多种其它药学活性化合物 用于治疗炎性或阻塞性气道疾病，例如哮喘，通常与移植相关的疾病，或增生性疾病如肿瘤疾病。

    Benzoxazoles and Oxazolopyridines Being Useful as Janus Kinases Inhibitors
    89.
    发明申请
    Benzoxazoles and Oxazolopyridines Being Useful as Janus Kinases Inhibitors 失效
    苯并恶唑和唑吡吉因作为Janus激酶抑制剂有用

    公开(公告)号：US20100009978A1

    公开(公告)日：2010-01-14

    申请号：US12440298

    申请日：2007-09-13

    申请人： Marc Gerspacher ,  Pascal Furet ,  Eric Vangrevelinghe

    发明人： Marc Gerspacher ,  Pascal Furet ,  Eric Vangrevelinghe

    IPC分类号： A61K31/423 ,  C07D263/58 ,  C07D413/14 ,  C07D417/14 ,  A61K31/5377 ,  A61K31/541 ,  A61P35/00

    CPC分类号： C07D263/58 ,  C07D413/04

    摘要： The invention relates to 2,7-disubstituted benzoxazole and 2,4-disubstituted oxazolo[5,4-c]pyridine compounds of the formula I given below, as well as salts thereof, processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, these compounds for use in the treatment (including prophylaxis) of the animal, especially human, body (especially with regard to a proliferative disease), the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a protein tyrosine kinase mediated disease (such as a tumor disease) or for the manufacture of a pharmaceutical preparation for use in the treatment of such a disease, a method for the treatment of such a disease and a pharmaceutical preparation for the treatment of a disease as mentioned. The compounds are of the formula I, wherein the symbols are as defined in the description. The compounds inhibit, for example, JAK2 and JAK3.

    摘要翻译： 本发明涉及以下给出的式I的2,7-二取代苯并恶唑和2,4-二取代的恶唑并[5,4-c]吡啶化合物及其盐，其制备方法及其在 用于治疗人或动物体的方法，这些化合物用于动物，特别是人体（特别是关于增殖性疾病）的治疗（包括预防）中，单独使用或与一种 或更多其它药物活性化合物 - 用于治疗特别是蛋白质酪氨酸激酶介导的疾病（例如肿瘤疾病）或用于制备用于治疗这种疾病的药物制剂的治疗方法 用于治疗所述疾病的疾病和药物制剂。 所述化合物具有式I，其中符号如说明书中所定义。 该化合物抑制例如JAK2和JAK3。