MICHELS, MARTIN,FOLLMANN, MARKUS,VAKALOPOULOS, ALEXANDROS,ZIMMERMANN, KATJA,TEUSCH, NICOLE,LOBELL, MARIO,BIERER, DONALD,ENGEL, KAREN,KISSEL, MARIA
申请号：
PE0003842012
公开号：
PE13922012A1
申请日:
2010.10.01
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to compounds derived from diciano - 3.5 - 4 - (1H - indazol - 5 - yl) - 2,6 Dimethyl 1,4 - dihydropyridine fluoro substituted of formula (i) wherein R1 is H, Methyl or Ethyl fluoro, R2 is Methyl, difluorometilo or trifluoromethyl R3 is H or fluoro R4 is H, Methyl or Ethyl R5 is H or Methyl.Preferred compounds are: RAC - 2 - methyl - 4 - (3 - methyl - 5 - 1H - indazol - il) - 6 - (trifluoromethyl) - 1,4 - dihydropyridine - 3.5 - dicarbonitrilo (4R) - 2 - (difluorometil) - 4 - (6 - fluoro - 3 - methyl - 1 - indazol - 5 - il) - 6 - methyl - 1,4 - dihydropyridine - 3.5 - dicarbonitrilo 2,6-bis (difluorometil) - 4 - (6 - fluoro - 3 - methyl - 5 - 1H - indazol - yl) - 1.4 - d Ihidropiridina - 3.5 - dicarbonitrilo among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are inhibitors of protein tyrosine kinase c-met being useful in the treatment of cancerSE REFIERE A COMPUESTOS DERIVADOS DE 3,5-DICIANO-4-(1H-INDAZOL-5-IL)-2,6-DIMETIL-1,4-DIHIDROPIRIDINA FLUORO-SUSTITUIDOS DE FORMULA (I) DONDE R1 ES H, FLUORO, METILO O ETILO R2 ES METILO, DIFLUOROMETILO O TRIFLUOROMETILO R3 ES H O FLUORO R4 ES H, METILO O ETILO R5 ES H O METILO. SON COMPUESTOS PREFERIDOS: rac-2-METIL-4-(3-METIL-1H-INDAZOL-5-IL)-6-(TRIFLUOROMETIL)-1,4-DIHIDROPIRIDINA-3,5-DICARBONITRILO (4R)-2-(DIFLUOROMETIL)-4-(6-FLUORO-3-METIL-1H-INDAZOL-5-IL)-6-METIL-1,4-DIHIDROPIRIDINA-3,5-DICARBONITRILO 2,6-BIS(DIFLUOROMETIL)-4-(6-FLUORO-3-METIL-1H-INDAZOL-5-IL)-1,4-DIHIDROPIRIDINA-3,5-DICARBONITRILO ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA TIROSINA QUINASA c-Met SIENDO UTILES EN EL TRATAMIENTO DE CANCER
