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    2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents
    1.
    发明授权
    2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents 失效
    2-氨基 - 噻唑衍生物，其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号：US07037929B1

    公开(公告)日：2006-05-02

    申请号：US09807962

    申请日：1999-10-27

    申请人： Paolo Pevarello ,  Raffaella Amici ,  Gabriella Traquandi ,  Manuela Villa ,  Anna Vulpetti ,  Antonella Isacchi

    发明人： Paolo Pevarello ,  Raffaella Amici ,  Gabriella Traquandi ,  Manuela Villa ,  Anna Vulpetti ,  Antonella Isacchi

    IPC分类号： A61K31/426 ,  A61K31/495 ,  C07D277/20 ,  C07D413/02 ,  C07D417/02

    CPC分类号： C07D417/12 ,  A61K31/426 ,  A61K31/427 ,  C07D277/46

    摘要： Compounds which are 2-amino-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from i) straight or branched C1–C8 alkyl, C2–C6 alkenyl or C2–C6 alkynyl; ii) C3–C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; R1 is an optionally further substituted group selected from: i) straight or branched C1–C8 alkyl or C2–C6 alkenyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring; iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 8 carbon atoms within the straight or branched alkyl chain; v) arylalkenyl with from 2 to 6 carbon atoms within the straight or branched alkenyl chain; vi) an optionally protected amino acid residue; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

    摘要翻译： 作为式（I）的2-氨基-1,3-噻唑衍生物的化合物，其中R是卤素原子，硝基，任选取代的氨基，或者是任选进一步取代的选自i）直链或 支链C 1 -C 8烷基，C 2 -C 6亚烯基或C 2 -C 6亚烷基， C 6 -C 6炔基; ii）C 3 -C 6环烷基; iii）在直链或支链烷基链中具有1至8个碳原子的芳基或芳基烷基; R 1是任选进一步取代的基团，其选自：i）直链或支链C 1 -C 8烷基或C 2 - / C 1 -C 6链烯基; ii）3至6元碳环或5至7元杂环; iii）芳基或芳基羰基; iv）在直链或支链烷基链中具有1至8个碳原子的芳基烷基; v）直链或支链烯基链中具有2至6个碳原子的芳基烯基; vi）任选保护的氨基酸残基; 或其药学上可接受的盐; 可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。

    Azaindole derivatives, process for their preparation, and their use as antitumor agents
    7.
    发明授权
    Azaindole derivatives, process for their preparation, and their use as antitumor agents 失效
    Azaindole衍生物，其制备方法及其作为抗肿瘤剂的用途

    公开(公告)号：US06335342B1

    公开(公告)日：2002-01-01

    申请号：US09597274

    申请日：2000-06-19

    申请人： Antonio Longo ,  Maria Gabriella Brasca ,  Paolo Orsini ,  Gabriella Traquandi ,  Valeria Pittalà ,  Anna Vulpetti ,  Mario Varasi ,  Paolo Pevarello

    发明人： Antonio Longo ,  Maria Gabriella Brasca ,  Paolo Orsini ,  Gabriella Traquandi ,  Valeria Pittalà ,  Anna Vulpetti ,  Mario Varasi ,  Paolo Pevarello

    IPC分类号： A61K41435

    CPC分类号： C07D471/04

    摘要： Novel 1H-pyrrolo[2,3-b]pyridines which are represented by formula (I): wherein R is a hydrogen or halogen atom or a group selected from —CN, —OH, —OCOR4, —(CH2)nNH2, —(CH2)nNHR4, —(CH2)nNHCOR4, —(CH2)nNHCONR4R5, —(CH2)nNHCOOR4, or —(CH2)nNHSO2R4, wherein n is either 0 or 1, R4 and R5 are as described in the specification; R1 is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted group selected from alkyl or aryl; R3 is hydrogen or a group selected from —CONR4R5, —COOR4, —CONHOR4, —SO2NHR4, alkylsulphonylaminocarbonyl or perfluorinated alkylsulphonylaminocarbonyl; or a pharmaceutically acceptable salt thereof, are disclosed. These compounds are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.

    摘要翻译： 由式（I）表示的新颖的1H-吡咯并[2,3-b]吡啶：其中R是氢或卤素原子或选自-CN，-OH，-OCOR 4， - （CH 2）n NH 2， （CH2）nNHR4， - （CH2）nNHCOR4， - （CH2）nNHCONR4R5， - （CH2）nNHCOOR4或 - （CH2）nNHSO2R4，其中n为0或1，R4和R5如说明书所述; R1是氢或任选取代的烷基; R2是任选取代的选自烷基或芳基的基团; R3是氢或选自-CONR4R5，-COOR4，-CONHOR4，-SO2NHR4，烷基磺酰基氨基羰基或全氟化烷基磺酰基氨基羰基的基团; 或其药学上可接受的盐。 这些化合物可用于治疗与改变的细胞依赖性激酶活性相关的细胞增殖性疾病。