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    Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
    22.
    发明授权
    Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention 失效
    噻吩化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US06414013B1

    公开(公告)日：2002-07-02

    申请号：US09596550

    申请日：2000-06-19

    申请人： Daniele Fancelli ,  Paolo Pevarello ,  Mario Varasi

    发明人： Daniele Fancelli ,  Paolo Pevarello ,  Mario Varasi

    IPC分类号： A61K3138

    CPC分类号： C07D409/12 ,  C07D333/38 ,  C07D333/68 ,  C07D413/12 ,  C07D473/00 ,  C07D495/04

    摘要： Compounds which are 3-aminocarbonyl-2-carboxamido-thiophene derivatives of formula (I): wherein R1 and R2 are, independently from each other, hydrogen, halogen or an optionally substituted group selected from aryl, straight or branched C1-C6 alkyl or aryl C1-C6 alkyl; or, taken together with the thiophene bond to which they are linked, R1 and R2 form a —(CH2)m—(NR4)n—(CH2)p— group wherein m and p are, each independently, an integer form 1 to 3, n is 0 or 1 and m+n+p is an integer from 3 to 5; and R4 is hydrogen or an optionally substituted straight or branched C1-C6 alkyl group; R3 is a group, optionally further substituted, selected from: i) straight or branched C1-C8 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C2-C6 alkylcarbonyl; ii) aryl; iii) 3 to 7 membered carbocycle; iv) 5 to 7 membered heterocycle with from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; or a pharmaceutically acceptable salt thereof; are useful in the treatment of diseases associated with an altered protein kinase activity such as cancer, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders.

    摘要翻译： 作为式（I）的3-氨基羰基-2-甲酰氨基 - 噻吩衍生物的化合物：其中R 1和R 2彼此独立地为氢，卤素或任选取代的基团，其选自芳基，直链或支链C 1 -C 6烷基或 芳基C1-C6烷基; 或者与它们所连接的噻吩键一起，R 1和R 2形成 - （CH 2）m - （NR 4）n - （CH 2）p - 基团，其中m和p各自独立地是1〜 3，n为0或1，m + n + p为3〜5的整数， 且R 4为氢或任选取代的直链或支链C 1 -C 6烷基; R 3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烯基，C 2 -C 6炔基或C 2 -C 6烷基羰基; ii）芳基; iii）3至7元碳环; iv）具有1至3个选自氮，氧和硫的杂原子的5至7元杂环; 或其药学上可接受的盐; 可用于治疗与改变的蛋白激酶活性如癌症，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病相关的疾病。

    1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
    26.
    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。