QU, JUNYA,RIVERO, RALPH A.,SANCHEZ, ROBERT,TEDESCO, ROSANNA
申请号:
PE0007872013
公开号:
PE01922014A1
申请日:
2011.09.23
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Relates to benzimidazole derivatives as PI3 Kinase Inhibitors of formula I, where R1 is H, c1-c6 alkyl, alkoxy, among others R2 is H, NHRA, alkoxy, among others R3 is aryl, heteroaryl among others R4 is H or ra, where ra is C1 - C3 alkyl R5 is C1 - C6 alkyl and N is 0 - 2.It also refers to a compound of formula (i) (c) wherein R6, R7 and R8 is C1 - C3 alkyl, halogen, CF3, among others. Preferred compounds are: 2 - (1 - methyl - ethyl) - 6 - (4-morpholinyl) - 1 - (1-naphthalenyl - methyl) - 1H benzimidazole - 4 - ol, 2 - ethyl - 6 - (4-morpholinyl) - 1 - (1-naphthalenyl - methyl) - 1H benzimidazole - 4 - ol, 1 - (2,3 - Dichloro phenyl) - methyl - 2 - (1 - methyl - ethyl) - 6 - (4-morpholinyl) - 1H benzimidazole - 4 - ol, among others.In addition to such a Pharmaceutical composition. These compounds are useful in the treatment of cancer.SE REFIERE A DERIVADOS DE BENCIMIDAZOL COMO INHIBIDORES DE CINASA PI3 DE FORMULA I, DONDE: R1 ES H, ALQUILO C1-C6, ALCOXI, ENTRE OTROS R2 ES H, -NHRa, ALCOXI, ENTRE OTROS R3 ES ARILO, HETEROARILO ENTRE OTROS R4 ES H O Ra, DONDE Ra ES ALQUILO C1-C3 R5 ES ALQUILO C1-C6 Y n ES 0-2. TAMBIEN HACE REFERENCIA A UN COMPUESTO DE FORMULA (I)(C) DONDE R6, R7 Y R8 SON ALQUILO C1-C3, HALOGENO, CF3, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(1-METIL-ETIL)-6-(4-MORFOLINIL)-1-(1-NAFTALENIL-METIL)-1H-BENCIMIDAZOL-4-OL, 2-ETIL-6-(4-MORFOLINIL)-1-(1-NAFTALENIL-METIL)-1H-BENCIMIDAZOL-4-OL, 1- (2,3-DICLORO-FENIL)-METIL -2-(1-METIL-ETIL)-6-(4-MORFOLINIL)-1H-BENCIMIDAZOL-4-OL, ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE CANCER.