AKHTAR, NADIM,BRADBURY, ROBERT HUGH,BUTTAR, DAVID,CURRIE, GORDON STUART,DE SAVI, CHRISTOPHER,YAVARI, NEDA,NORMAN, RICHARD ALBERT,OSBORNE, MATTHEW,RABOW, ALFRED ARTHUR,REDFEARN, HEATHER MARIE,WILLIAMS,
申请号：
PE0024292015
公开号：
PE08742016A1
申请日:
2014.05.27
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
Relates to compounds of formula (i) or its Salts where R1, R2, R3, R4 and R5 are as defined in the description.Preferred compounds are: acid (e) - 3 - (3,5 - difluoro - 4 - ((1R, 3R) - 2 - (fluoro - 2-methylpropyl) - 3 - methyl - 2,3,4,9 - tetrahydro - 1H indole pirido [3,4-b] - 1 - il) phenyl Acrylic acid) (e) - 3 - (4 - ((1R, 3R) - 2 - (fluoro - 2-methylpropyl) - 3 - methyl - 2,3,4,9 - tetrahydro - 1H indole pirido [3,4-b] - 1 - il) phenyl) acrylic among others. It also relates to a process for Preparation thereof and a Pharmaceutical composition.These compounds reduce expression of the estrogen receptor (ER alpha or ER1) selectively (Serd) to be useful for the treatment of cancerSE REFIERE A COMPUESTOS DE FORMULA (I) O A SUS SALES DONDE R1, R2, R3, R4 Y R5 SON TAL COMO SE DEFINEN EN LA DESCRIPCION. SON COMPUESTOS PREFERIDOS: ACIDO (E)-3-(3,5-DIFLUORO-4-((1R,3R)-2-(2-FLUORO-2-METILPROPIL)-3-METIL-2,3,4,9-TETRAHIDRO-1H-PIRIDO[3,4-b]INDOL-1-IL)FENIL)ACRILICO ACIDO (E)-3-(4-((1R,3R)-2-(2-FLUORO-2-METILPROPIL)-3-METIL-2,3,4,9-TETRAHIDRO-1H-PIRIDO[3,4-b]INDOL-1-IL)FENIL)ACRILICO ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA SU PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS REDUCEN LA EXPRESION DEL RECEPTOR ESTROGENICO (ER1 O ER ALFA) DE FORMA SELECTIVA (SERD) SIENDO UTILES PARA EL TRATAMIENTO DEL CANCER
