INHIBITORS OF TYROSINE KINASES
    11.
    发明申请
    INHIBITORS OF TYROSINE KINASES 有权
    TYROSINE KINASES的抑制剂

    公开(公告)号:US20090286821A1

    公开(公告)日:2009-11-19

    申请号:US12489049

    申请日:2009-06-22

    IPC分类号: A61K31/506 C07D401/04

    CPC分类号: C07D401/14 C07D405/14

    摘要: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, 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, in particular leukaemia, and a method for the treatment of such a disease.

    摘要翻译: 本发明涉及下式的化合物,其中取代基R 1,R 2和R 4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物,其任选组合的用途 与一种或多种用于治疗对蛋白激酶活性,特别是肿瘤性疾病,特别是白血病的抑制作出反应的疾病的其它药学活性化合物,以及治疗这种疾病的方法。

    4-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives
    13.
    发明授权
    4-Amino-5-phenyl-7-cyclobutyl-pyrrolo(2,3-d)pyrimidine derivatives 失效
    4-氨基-5-苯基-7-环丁基 - 吡咯并(2,3-d)嘧啶衍生物

    公开(公告)号:US07326699B2

    公开(公告)日:2008-02-05

    申请号:US10477594

    申请日:2002-05-13

    CPC分类号: C07D487/04

    摘要: The invention relates to new 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives, 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 a disease, especially a proliferative disease, such as a tumour disease, a method for the treatment of such diseases in mammals, especially in humans, and the use of such a compound-alone or in combination with one or more other pharmaceutically active compounds-for the preparation of a pharmaceutical composition (medicament) for the treatment especially of a proliferative disease, such as a tumour.

    摘要翻译: 本发明涉及新的4-氨基-5-苯基-7-环丁基 - 吡咯并[2,3-d]嘧啶衍生物,其制备方法及其在治疗人或动物体的方法中的应用, 其用途 - 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,特别是增殖性疾病,例如肿瘤疾病,哺乳动物,特别是人类中的这些疾病的治疗方法, 以及这种化合物单独使用或与一种或多种其它药学活性化合物组合的用途,用于制备特别是增殖性疾病如肿瘤的药物组合物(药物)。

    INHIBITORS OF TYROSINE KINASES
    14.
    发明申请
    INHIBITORS OF TYROSINE KINASES 有权
    TYROSINE KINASES的抑制剂

    公开(公告)号:US20080188451A1

    公开(公告)日:2008-08-07

    申请号:US12061334

    申请日:2008-04-02

    CPC分类号: C07D401/14 C07D405/14

    摘要: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, 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, in particular leukaemia, and a method for the treatment of such a disease.

    摘要翻译: 本发明涉及下式的化合物,其中取代基R 1,R 2和R 4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物,其任选组合的用途 与一种或多种用于治疗对蛋白激酶活性,特别是肿瘤性疾病,特别是白血病的抑制作出反应的疾病的其它药学活性化合物,以及治疗这种疾病的方法。

    Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase
    15.
    发明授权
    Pyridine derivatives inhibiting angiogenesis and/or VEGF receptor tyrosine kinase 失效
    抑制血管发生和/或VEGF受体酪氨酸激酶的吡啶衍生物

    公开(公告)号:US06706731B2

    公开(公告)日:2004-03-16

    申请号:US10203579

    申请日:2002-10-11

    IPC分类号: C07D47104

    CPC分类号: C07D401/06 C07D471/04

    摘要: The invention relates to pyridine derivatives of formula I: wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds.

    摘要翻译: 本发明涉及式I的吡啶衍生物:其中取代基和符号如说明书所述定义,其制备方法,它们在制备用于治疗对抑制作用的疾病的药物组合物中的用途 血管生成和含有这些化合物的药物组合物。

    2-amino-nicotinamide derivatives and their use as VEGF-receptor tyrosine kinase inhibitors
    16.
    发明授权
    2-amino-nicotinamide derivatives and their use as VEGF-receptor tyrosine kinase inhibitors 有权
    2-氨基 - 烟酰胺衍生物及其作为VEGF-受体酪氨酸激酶抑制剂的用途

    公开(公告)号:US06624174B2

    公开(公告)日:2003-09-23

    申请号:US10181005

    申请日:2002-07-11

    IPC分类号: C07D21382

    摘要: The invention relates to the use of 2 amino-nicotinamide derivatives of formula I wherein n is from 1 up to and including 6; W is O or S; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R′ are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptable salt of such a compound, alone or in combination with one or more other pharmaceutically active compounds for the preparation of a pharmaceutical composition for use for therapy of a disease which responds to an inhibition of the VEGF-receptor tyrosine kinase activity; and to new 2-amino-nicotinamide derivatives of formula I and processes for the preparation thereof.

    摘要翻译: 本发明涉及式I的2种氨基 - 烟酰胺衍生物的用途,其中n为1至6,W为O或S; R 1和R 3彼此独立地为氢,低级烷基或低级酰基; R 2表示 环烷基,芳基或包含一个或多个环氮原子和0,1或2个彼此独立地选自氧和硫的杂原子的单环或双环杂芳基,这些基团在每种情况下是未取代的 或单取代或多取代; R和R'彼此独立地为氢或低级烷基; X表示芳基,或单环或双环杂芳基,其包含一个或多个环氮原子和0,1或2个独立地为 彼此选自氧和硫,这些基团在每种情况下都是未取代的或单取代或多取代的;或N-氧化物,其可能的互变异构体或这种化合物的药学上可接受的盐,alo ne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对VEGF-受体酪氨酸激酶活性的抑制作出反应的疾病的药物组合物;以及新的2-氨基 - 烟酰胺衍生物 式I及其制备方法。

    Pyrimidineamide derivatives and the use thereof
    20.
    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。