Process for preparing aminocrotonylamino-substituted quinazoline derivatives
    1.
    发明授权
    Process for preparing aminocrotonylamino-substituted quinazoline derivatives 有权
    制备氨基羰基氨基取代喹唑啉衍生物的方法

    公开(公告)号:US08188274B2

    公开(公告)日:2012-05-29

    申请号:US13101195

    申请日:2011-05-05

    IPC分类号: C07D239/72

    CPC分类号: C07D293/04

    摘要: The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

    摘要翻译: 本发明涉及一种制备通式(I)的氨基巴豆酰氨基取代的喹唑啉衍生物的改进方法,其中基团R a,R b,R c和R d具有权利要求中给出的含义,以及式的磺酰基衍生物及其作为 用于制备式(I)的喹唑啉的合成组分。 式(I)的喹唑啉衍生物是由酪氨酸激酶和表皮生长因子受体(EGF-R)介导的信号转导抑制剂,因此特别适用于治疗肿瘤疾病。

    PROCESS FOR PREPARING AMINOCROTONYLAMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES
    2.
    发明申请
    PROCESS FOR PREPARING AMINOCROTONYLAMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES 有权
    制备氨基磺酰胺取代的喹唑啉衍生物的方法

    公开(公告)号:US20090306378A1

    公开(公告)日:2009-12-10

    申请号:US12162037

    申请日:2007-01-25

    IPC分类号: C07D239/94

    CPC分类号: C07D293/04

    摘要: The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

    摘要翻译: 本发明涉及一种制备通式(I)的氨基巴豆酰氨基取代的喹唑啉衍生物的改进方法,其中基团R a,R b,R c和R d具有权利要求中给出的含义,以及式(ⅩⅢ)的磺酰基衍生物和式 其用作制备式(I)的喹唑啉的合成组分。 式(I)的喹唑啉衍生物是由酪氨酸激酶和表皮生长因子受体(EGF-R)介导的信号转导抑制剂,因此特别适用于治疗肿瘤疾病。

    Process for preparing aminocrotonylamino-substituted quinazoline derivatives
    3.
    发明授权
    Process for preparing aminocrotonylamino-substituted quinazoline derivatives 有权
    制备氨基羰基氨基取代喹唑啉衍生物的方法

    公开(公告)号:US07960546B2

    公开(公告)日:2011-06-14

    申请号:US12162037

    申请日:2007-01-25

    IPC分类号: C07D239/72

    CPC分类号: C07D293/04

    摘要: The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well as sulphonyl derivatives of formula (XIII) and the use thereof as synthesis components for preparing quinazolines of formula (I). The quinazoline derivatives of formula (I) are inhibitors of signal transduction mediated by tyrosinekinases and by the Epidermal Growth Factor-Receptor (EGF-R) and are therefore particularly suitable for the treatment of tumoral diseases.

    摘要翻译: 本发明涉及一种制备通式(I)的氨基巴豆酰氨基取代的喹唑啉衍生物的改进方法,其中基团R a,R b,R c和R d具有权利要求中给出的含义,以及式(ⅩⅢ)的磺酰基衍生物和式 其用作制备式(I)的喹唑啉的合成组分。 式(I)的喹唑啉衍生物是由酪氨酸激酶和表皮生长因子受体(EGF-R)介导的信号转导抑制剂,因此特别适用于治疗肿瘤疾病。

    INDOLINONE DERIVATIVES AND PROCESS FOR THEIR MANUFACTURE
    9.
    发明申请
    INDOLINONE DERIVATIVES AND PROCESS FOR THEIR MANUFACTURE 有权
    吲哚啉酮衍生物及其制备方法

    公开(公告)号:US20100311985A1

    公开(公告)日:2010-12-09

    申请号:US12745788

    申请日:2008-12-02

    IPC分类号: C07D209/34

    CPC分类号: C07D209/34

    摘要: The present invention relates to specific indolinone derivatives, namely the compounds of formula, in which R1 represents an hydrogen atom or a group, and R2 and R3 each represent an hydrogen atom or R2 and R3 taken together represent a group, with the proviso that when R1 represents an hydrogen atom R2 and R3 taken together represent a group, and to a process for their manufacture.

    摘要翻译: 本发明涉及特定的二氢吲哚酮衍生物,即其中R 1表示氢原子或基团的化合物,R 2和R 3各自表示氢原子,或者R 2和R 3一起表示基团,条件是当 R1表示氢原子R2和R3一起表示基团,并且涉及其制造方法。