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    Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
    27.
    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。