Pyrimidineamide derivatives and the use thereof
    122.
    发明授权
    Pyrimidineamide derivatives and the use thereof 失效
    嘧啶酰胺衍生物及其用途

    公开(公告)号:US07655669B2

    公开(公告)日:2010-02-02

    申请号:US10528913

    申请日:2003-09-26

    IPC分类号: C07D401/14 A61K31/506

    CPC分类号: C07D401/04

    摘要: The invention relates to novel substituted N-(3-benzoylaminophenyl)-4-pyridyl-2-pyrimidinamine derivatives, processes for the preparation thereof, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, and a method for the treatment of such a disease.

    摘要翻译: 本发明涉及新的取代的N-(3-苯甲酰氨基苯基)-4-吡啶基-2-嘧啶胺衍生物,其制备方法,含有它们的药物组合物,其用途任选与一种或多种其它药物活性化合物组合用于 治疗对抑制蛋白激酶活性,特别是肿瘤性疾病作出反应的疾病,以及治疗这种疾病的方法。

    3 Substituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors
    123.
    发明申请
    3 Substituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors 审中-公开
    3取代的N-(芳基 - 或杂芳基) - 吡唑并[1,5-a]嘧啶作为激酶抑制剂

    公开(公告)号:US20090275593A1

    公开(公告)日:2009-11-05

    申请号:US12296154

    申请日:2007-04-02

    IPC分类号: A61K31/519 C07D487/04

    CPC分类号: C07D487/04

    摘要: The invention relates to 3-substituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.

    摘要翻译: 本发明涉及3-取代的N-(芳基 - 或杂芳基) - 吡唑并[1,5-a]嘧啶化合物,它们作为激酶抑制剂的用途,包含所述化合物的新药物制剂,用于诊断或治疗性治疗的所述化合物 温血动物,特别是人类,其用于治疗疾病或用于制备可用于治疗响应于激酶调节的疾病的药物制剂,特别是tie-2激酶,活性,治疗方法,包括施用 所述化合物与温血动物,特别是人类,以及所述化合物的制备方法。

    Sulphonamidoaniline Derivatives Being Janus Kinase Inhibitors
    126.
    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

    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。