DU, Zhimin,DORNAN, David,GUERRERO, Juan A.,KAPLAN, Joshua A.,KNOX, John E.,NADUTHAMBI, Devan,PHILLIPS, Barton W.,STINSON, Susanna Y.,VENKATARAMANI, Chandrasekar,WANG, Peiyuan,WATKINS, William J.
申请号：
PE0011142018
公开号：
PE10732018A1
申请日:
2016.12.15
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
Relates to compounds of formula (i) where n is 0 to 3 R is Halogen, Oxo, CN, NO2, c1-c6 alkyl.Among others, the cycloalkyl ring is C3 C5 - C8 C8 or cicloalquenilo x1 or x2 is CR1 and CR2 is n n n is X3 X4 or Cr3, CR4 is o n r1 is H, Halo, NS,Among others, R2 and R4 are each H or Halo Halo R3 is H, alkyl, C1 - C6, among others R5 is H, alkyl hydroxyl, C1 - C6, among others.Preferred compounds are: N - (4 - (3 - cyano - 4 - (pyrrolidin-1-yl) phenyl) pyridin-2-yl) ciclopropanocarboxamida n - (4 - (3 - cyano - 4 - ((Tetrahydro - 2H - piran - 4-yl) oxy) pyrimidine phenyl) - 4 - ciclopropanocarboxamida, il)Among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of the kinase 1 (Tank binding kinase TBK1) and \/ or i-kappa B being useful in the treatment of non small cell lung cancer, acute myeloid leukemiaSE REFIERE A COMPUESTOS DE FORMULA (I) DONDE n ES DE 0 A 3 R ES HALOGENO, OXO, CN, NO2, ALQUILO C1-C6, ENTRE OTROS EL ANILLO A ES CICLOALQUILO C3-C8 O CICLOALQUENILO C5-C8 X1 ES CR1 O N X2 ES CR2 O N X3 ES CR3 O N X4 ES CR4 O N R1 ES H, HALO, CN, ENTRE OTROS R2 Y R4 SON CADA UNO H O HALO R3 ES H, HALO, ALQUILO C1-C6, ENTRE OTROS R5 ES H, HIDROXILO, ALQUILO C1-C6, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(4-(3-CIANO-4-(PIRROLIDIN-1-IL)FENIL)PIRIDIN-2-IL)CICLOPROPANOCARBOXAMIDA N-(6-(3-CIANO-4-((TETRAHIDRO-2H-PIRAN-4-IL)OXI)FENIL)PIRIMIDIN-4-IL)CICLOPROPANOCARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA QUINASA 1 DE UNION A TANK (TBK1) Y/O LA QUINASA I-KAPPA-B SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE PULMON DE CELULAS NO PEQUENAS, LEUCEMIA MIELOIDE AGUDA
