公开(公告)号：US07943654B2

公开(公告)日：2011-05-17

申请号：US11988528

申请日：2006-07-10

申请人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tizizno Bandiera

发明人： Daniele Fancelli ,  Jurgen Moll ,  Maurizio Pulici ,  Francesca Quartieri ,  Tizizno Bandiera

IPC分类号： A01N43/56 ,  A01N43/06 ,  A61K31/415 ,  A61K31/38 ,  C07D487/02 ,  C07D231/54 ,  C07D333/00

CPC分类号： C07D495/04

摘要： There are provided thieno[2,3-c]pyrazole derivatives of formula (I), wherein A is an aryl or heteroaryl ring, on which the substituent-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 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 organic group; or isomers, tautomers, carriers, metabolites, prodrugs, and pharamaceutically acceptable salts thereof. A process for their preparation and pharamaceutical compositions comprising them are also disclosed; the compounds of the invention may be useful, in theraphy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

摘要翻译： 提供式（I）的噻吩并[2,3-c]吡唑衍生物，其中A是芳基或杂芳基环，取代基-NHZR5在其上与CONH连接体的邻位; R1和R2相同或不同，彼此独立地表示氢原子或有机基团; 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是氢或有机基团; 或异构体，互变异构体，载体，代谢物，前药和药物上可接受的盐。 还公开了其制备方法和包含它们的药用组合物; 本发明的化合物在治疗与失调的蛋白激酶活性相关的疾病（例如癌症）中可能是有用的。