DORSCH, DIETER,JONCZYK, ALFRED,HOELZEMANN, GUENTER,AMENDT, CHRISTIANE,ZENKE, FRANK
申请号：
PE0025142012
公开号：
PE03762013A1
申请日:
2011.05.31
申请国别(地区):
PE
年份:
2013
代理人:
摘要：
Refers to [1,8] naftiridina derivative compounds of formula (i) wherein W1, W2, W3, W4 and W5 are each N or Cr3, where R3 is H, Oy, NYY, among others and it is H OR, where a is (C1 - C10 alkyl or cycloalkyl (C3) - C8) Z is c = C, c = N, o, S, CH, among others r1 is aryl or heteroaryl (C5 - C10) R2 is H NO2, CN, Cho, among others R5 is H, a, Oy, NYY or heterocycle P and q are each of 0 to 3.Preferred compounds are: 2 - (2 - Chloro - 5 - fluoro - phenyl) - 4 - (1h pyrrolo [2,3-c] pyridin-3-yl) - [1,8] naftiridina 2 - (2 - Chloro - 5 - fluoro - phenyl) - 4 - isoquinolin IL - [- 5 - 1.8] naftiridina 2 - (2-fluoro-5 - trifluoromethyl phenyl) - 4 - (1h pyrrolo [2,3-c] pyridin-3-yl) - [1,8] naftiridina among others. It also relates to a preparation method and a Pharmaceutical composition.These compounds are inhibitors of Protein using ATP as TAK1, PDK1, MINK1, HER4, among others, being useful in the treatment of cancer, sarcoma, gliomaSE REFIERE A COMPUESTOS DERIVADOS DE [1,8]NAFTIRIDINA DE FORMULA (I) DONDE W1, W2, W3, W4 Y W5 SON CADA UNO N O CR3, EN DONDE R3 ES H, OY, NYY, ENTRE OTROS Y ES H O A, DONDE A ES ALQUILO(C1-C10) O CICLOALQUILO(C3-C8) Z ES C=C, C=N, O, S, CH, ENTRE OTROS R1 ES ARILO(C5-C10) O HETEROARILO R2 ES H, NO2, CN, CHO, ENTRE OTROS R5 ES H, A, OY, NYY O HETEROCICLO p Y q SON CADA UNO DE 0 A 3. SON COMPUESTOS PREFERIDOS: 2-(5-CLORO-2-FLUORO-FENIL)-4-(1H-PIRROLO[2,3-c]PIRIDIN-3-IL)-[1,8]NAFTIRIDINA 2-(5-CLORO-2-FLUORO-FENIL)-4-ISOQUINOLIN-5-IL-[1,8]NAFTIRIDINA 2-(2-FLUORO-5-TRIFLUOROMETIL-FENIL)-4-(1H-PIRROLO[2,3-c]PIRIDIN-3-IL)-[1,8]NAFTIRIDINA ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE PROTEINAS CONSUMIDORAS DE ATP TAL COMO TAK1, PDK1, MINK1, HER4, ENTRE OTROS, SIENDO UTILES EN EL TRATAMIENTO DE CANCER, SARCOMA, GLIOMA
