公开(公告)号：US20050075365A1

公开(公告)日：2005-04-07

申请号：US10776953

申请日：2004-02-11

申请人： John Braganza ,  Michael Letavic ,  Kim McClure

发明人： John Braganza ,  Michael Letavic ,  Kim McClure

IPC分类号： A61K31/4745 ,  A61P29/00 ,  C07D471/02 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S═O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S═O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C═O)—, R5—(NR6)—(C═O)—, R5—(C═O)—NR6—, R5—O—(C═O)—, R5—(C═O)—O—, R5—CR7═CR8— or R5—C≡C_; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

摘要翻译： 本发明涉及下式的新的三唑并 - 吡啶：其中X是> CH2，> NH，硫，> S = O，> SO2或氧; 其中所述> CH 2和> NH可以任选地被合适的取代基取代; R 1选自氢，（C 1 -C 6）烷基和其它合适的取代基; R 2选自氢，（C 1 -C 6）烷基和其它合适的取代基; s是0-4的整数; R 3是R 4，R 5 - （NR 6） - ，R 5 -S-，R 5 - （S = O） - ，R 5 - （SO 2 ） - ，R 5 -SO 2 -NR 6 - ，R 5 - （NR 6）-SO 2 - ，R 5 -O-，R 5 - （C = O） R 5 - （NR 6） - （C = O） - ，R 5 - （C = O）-NR 6 - ，R 5 -O-（C = O） R 5 - （C = O）-O-，R 5 -CR 7 = CR 8 - 或R 5 -C = C = 使得R 3的分子量小于500AMU，优选小于250MAU; R 4，R 5和R 6各自选自氢，（C 1 -C 6）烷基和其它合适的取代基; 或其药学上可接受的盐; 制备中间体，含有它们的药物组合物及其药物用途。 本发明的化合物是MAP激酶的有效抑制剂。 它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫性疾病和其他疾病。