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33 条记录 (耗时 0.023 秒)

    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis
    5.
    发明授权
    Amino anthracyclinone derivatives and their use in the treatment of amyloidosis 失效
    氨基蒽环类衍生物及其在治疗淀粉样变性中的应用

    公开(公告)号：US06268362B1

    公开(公告)日：2001-07-31

    申请号：US09622921

    申请日：2000-09-07

    申请人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    发明人： Tiziano Bandiera ,  Daniele Fancelli ,  Mario Varasi ,  Michele Caruso ,  Jacqueline Lansen ,  Antonino Suarato

    IPC分类号： A61K315377

    CPC分类号： C07D405/06 ,  C07D211/70

    摘要： A compound of formula (1), wherein R1 represents hydrogen, hydroxy, a group of formula OR7, wherein R7 is C1-C6 alkyl, C2-C6 alkenyl; R2 represents hydrogen, hydroxy, diethylamino, piperidino, tetrahydropyridino or morpholino, and either R3, taken alone, represtnts hydrogen or hydroxy, and R4 and R5, taken alone, independently represent hydrogen, hydroxy or, taken together with the carbon atom, represent a carbonyl group; or R3 and R4, taken together, represent a group of formula (A), wherein R8 and R9 represent a C1-C6 alkyl and R5 represents hydrogen; R6 represents hydrogen or a phenyl group, optionally substituted by methyl, methoxy or halogen and the pharnaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

    摘要翻译： 式（1）的化合物，其中R 1表示氢，羟基，式OR 7的基团，其中R 7是C 1 -C 6烷基，C 2 -C 6烯基; R2代表氢，羟基，二乙基氨基，哌啶子基，四氢吡啶基或吗啉代，独立的R 3独立地代表氢或羟基，独立地，R 4和R 5独立地表示氢，羟基或与碳原子一起代表 羰基; 或R 3和R 4一起表示式（A）的基团，其中R 8和R 9表示C 1 -C 6烷基，R 5表示氢; R6代表氢或任选被甲基，甲氧基或卤素取代的苯基及其药物上可接受的盐，可用于治疗淀粉样变性。 还描述了制备方法和药物组合物。

    Heterocyclyl anthracyclinone derivatives
    9.
    发明授权
    Heterocyclyl anthracyclinone derivatives 失效
    杂环蒽环类衍生物

    公开(公告)号：US06316451B1

    公开(公告)日：2001-11-13

    申请号：US09623859

    申请日：2000-09-26

    申请人： Sergio Mantegani ,  Gabriella Traquandi ,  Tiziano Bandiera ,  Jacqueline Lansen ,  Mario Varasi

    发明人： Sergio Mantegani ,  Gabriella Traquandi ,  Tiziano Bandiera ,  Jacqueline Lansen ,  Mario Varasi

    IPC分类号： C07D27742

    CPC分类号： C07D417/04 ,  C07D233/88 ,  C07D277/40 ,  C07D277/42

    摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.

    摘要翻译： 式（1）的化合物，其中R 1是氢，羟基，式OR 5的基团，其中R 5是C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可被未被取代或被C1单或二取代的氨基 C 6烷基，C 2 -C 6烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，NR 6 R 7基团，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起代表任选取代的C 3 -C 8 杂环 R3是氢，羟基，R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。 还描述了制备方法和药物组合物。

    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
    10.
    发明授权
    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors 有权
    可用作激酶抑制剂的1H-呋喃并[3,2-C]吡唑化合物

    公开(公告)号：US08119641B2

    公开(公告)日：2012-02-21

    申请号：US12302569

    申请日：2007-05-25

    申请人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    发明人： Daniele Fancelli ,  Maurizio Pulici ,  Jürgen Moll ,  Tiziano Bandiera

    IPC分类号： A61K31/4162 ,  A61K31/427 ,  A61K31/496 ,  C07D491/048 ,  C07D277/44 ,  C07D295/135 ,  C07D417/10 ,  C07D403/14

    CPC分类号： C07D491/048

    摘要： Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 are the same or different and, independently from each other, represent a hydrogen atom, or an organic residue; R3 is a hydrogen or halogen atom or an organic group; R4 is a hydrogen or halogen atom or an organic group; Z is direct bond, >C═O, or —C(═O)NH—; —R5 is hydrogen or an optionally substituted organic group or isomers, tautomers, carriers, metabolites, prodrugs, and pharmaceutically acceptable salts thereof. A process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Aurora kinases activity or IGF-1R activity, like cancer.

    摘要翻译： 如描述中定义的式（I）的呋喃并[3,2-c]吡唑衍生物及其药学上可接受的盐，其中A是芳基或杂芳基环，-NHZR5位于与CONH接头的邻位; -R 1和R 2相同或不同，彼此独立地表示氢原子或有机残基; R3是氢或卤素原子或有机基团; R4是氢或卤素原子或有机基团; Z是直接键合，> C = O或-C（= O）NH-; -R5是氢或任选取代的有机基团或其异构体，互变异构体，载体，代谢物，前药及其药学上可接受的盐。 公开了其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性，特别是Aurora激酶活性或IGF-1R活性相关的疾病，如癌症。