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    (1H-indol-7-yl)-(pyrimidin-2-ylamino)methanone derivatives and related compounds as IGF-R1 inhibitors for the treatment of cancer
    5.
    发明授权
    (1H-indol-7-yl)-(pyrimidin-2-ylamino)methanone derivatives and related compounds as IGF-R1 inhibitors for the treatment of cancer 失效
    （1H-吲哚-7-基） - （嘧啶-2-基氨基）甲酮衍生物和相关化合物作为治疗癌症的IGF-R1抑制剂

    公开(公告)号：US08114882B2

    公开(公告)日：2012-02-14

    申请号：US11911268

    申请日：2006-03-17

    申请人： Timo Heinrich ,  Andree Blaukat ,  Maria Kordowicz

    发明人： Timo Heinrich ,  Andree Blaukat ,  Maria Kordowicz

    IPC分类号： C07D401/14 ,  C07D403/14 ,  A61K31/506

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

    摘要： The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)9A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH2, NA2, NHA, CH2, CH3, OH, OA, O or S, E: CH2, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH2, O or NH, Q: Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 or X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved.

    摘要翻译： 本发明涉及式（I）化合物，其中Ar表示具有1至4个N，O和/或S原子和5至10个骨架原子的单环或双环芳族均聚或杂环，其可以是未取代的或 羰基氧，Hal，A，OH，OA，NH2，NHA，NA2，NO2，CN，OCN，SCN，COOH，COOA，CONH2，CONHA，CONA2，NHCOA，NHCONH2，NHSO2A，CHO的单，二或三取代 ，COA，SO 2 NH 2和/或S（O）9A，A表示具有1-14个C原子的无支链，支链或环状烷基，其中一个或两个CH 2基团可被O或S原子替代和/或由-CH = CH-基和/或另外1-7个H原子可以被F和/或Cl，Hal，F，Cl，Br或I，D：NH，NH2，NA2，NHA，CH2，CH3，OH，OA ，O或S，E：CH 2，CH，NH或N，Y：E或饱和或不饱和键，X：CH 2，O或NH，Q：Hal，A，OH，OA，NH 2，NHA， ，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA2，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2或XM，用于制备和用于制备治疗药物 疾病，特别是涉及激酶的发展或过程中的肿瘤和/或疾病。

    (1H-Ind0l-7-Yl)-(Pyrimidin-2-Ylamino)Methanone Derivatives and Related Compounds as Igf-R1 Inhibitors for the Treatment of Cancer
    6.
    发明申请
    (1H-Ind0l-7-Yl)-(Pyrimidin-2-Ylamino)Methanone Derivatives and Related Compounds as Igf-R1 Inhibitors for the Treatment of Cancer 失效
    （1H-吲哚-7-基） - （嘧啶-2-基氨基）甲酮衍生物和相关化合物作为Igf-R1抑制剂治疗癌症

    公开(公告)号：US20080194605A1

    公开(公告)日：2008-08-14

    申请号：US11911268

    申请日：2006-03-17

    申请人： Timo Heinrich ,  Andree Blaukat ,  Maria Kordowicz

    发明人： Timo Heinrich ,  Andree Blaukat ,  Maria Kordowicz

    IPC分类号： A61K31/497 ,  C07D401/14 ,  A61P35/04 ,  C07D401/12

    CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

    摘要： The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)9A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CR═CH— groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH2, NA2, NHA, CH2, CH3, OH, OA, O or S, E: CH2, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH2, O or NH, Q: Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 or X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.

    摘要翻译： 本发明涉及式（I）化合物，其中Ar表示具有1至4个N，O和/或S原子和5至10个骨架原子的单环或双环芳族均聚或杂环，其可以是未取代的或 羰基氧，Hal，A，OH，OA，NH 2，NHA，NA 2，NO 2， ，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA 2，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2和/或S（O）9 A，A表示无支链，支链 或具有1-14个C原子的环状烷基，其中一个或两个CH 2基团可以被O或S原子和/或被-CR-CH-基团和/或另外的1- 7 H原子可以被F和/或Cl，Hal：F，Cl，Br或I，D：NH，NH 2，NH 2，NH 2，CH CH 2，CH 3，OH，OA，O或S，E：CH 2，CH，NH或N，Y：E或 饱和或不饱和键，X：CH 2，O或NH，Q：Hal，A，OH，OA，NH 2，NHA，N CN 2，NO 2，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA 2 ，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2或XM， 涉及其制备和用途，用于制备用于治疗疾病，特别是涉及激酶的发展或过程中的肿瘤和/或疾病的药物。