公开(公告)号：EP2341049A1

公开(公告)日：2011-07-06

申请号：EP11156123.9

申请日：2003-04-02

申请人： Novartis AG

发明人： Coppola, Gary Mark ,  Davies, John William ,  Jewel, Charles Francis, Jr. ,  Li, Yu-Chin ,  Wareing, James Richard ,  Sperbeck, Donald Mark ,  Stams, Travis Mathew ,  Topiol, Sidney Wolf ,  Vlattas, Isidoros

IPC分类号： C07D285/10 ,  A61K31/433 ,  A61P3/10 ,  C07D417/06

CPC分类号： C07D285/10 ,  C07D417/06 ,  C07D417/10 ,  C07K5/06078

摘要： Compounds of the formula

wherein L 1 , L 2 , L 3 , Q 1 , Q 2 , R 1 , R 2 , X, Y and Z are as decribed in the description fo the invention, provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels. In addition, the compounds of the present invention may be employed to treat or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

摘要翻译： 其中L 1，L 2，L 3，Q 1，Q 2，R 1，R 2，X，Y和Z如本发明描述的化合物提供作为PTP酶抑制剂的药理学试剂， 特别地，式I化合物抑制PTP-1B和TC PTP，因此可用于治疗与PTPase活性相关的病症。 因此，式I化合物可用于预防或治疗与肥胖，葡萄糖不耐受，糖尿病，高血压和大血管和小血管缺血性疾病相关的胰岛素抵抗。 此外，本发明的化合物可用于治疗或预防癌症，骨质疏松症，神经变性和感染性疾病以及涉及炎症和免疫系统的疾病。