JUNG, MICHAEL E.,YOO, DONGWON,SAWYERS, CHARLES L.,TRAN, CHRIS
申请号：
PE0006382012
公开号：
PE14702012A1
申请日:
2008.10.24
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula (i) where diarilhidantoina: R1 and R2 together comprise 2 to 8 Carbon Atoms and are independently an alkyl group or alkyl group C1 C1 - 8 8 - hydroxy substituted with a sustiuyente selected, Bromine, Fluorine, Chlorine, among others and R3 is H Formilo R4 is H, F, CL, BR and I, R11 and R12 are independently H or Methyl.Preferred compounds are: 4 - (3 - (4 - (3 - cianopropil) phenyl) - 4.4 - dimethyl - 5 - 2 - oxo - tioxo Co. - 1 - il) - 2 - (trifluoromethyl) benzonitrile 4 - 8 - oxo - (5 - (4 - (phenyl oxobutil) 6) - - - - tioxo 5.7 diazaspiro [3.4] octan-3-yl - 7 - yl) - 2 - (trifluoromethyl) benzonitrile 4 - (4 - (7 - (4 - cyano - 3 - (trifluoromethyl) phenyl) - 2 - oxo - tioxo - 5.7 - Day 6 Zaspiro [3.4] oct - an - 5 - yl) - 2-fluorophenyl) - 2,2-dimethyl - N - metibutanamida among others.In addition to such a Pharmaceutical composition. This Compound is an androgen receptor antagonist to be useful in the treatment of Hormone Refractory Prostate CancerSE REFIERE A UN COMPUESTO DERIVADO DE DIARILHIDANTOINA DE FORMULA (I) DONDE: R1 Y R2 JUNTOS COMPRENDEN DE 2-8 ATOMOS DE CARBONO Y SON INDEPENDIENTEMENTE UN GRUPO ALQUILO C1-8 O UN GRUPO ALQUILO C1-8 SUSTITUIDO CON UN SUSTIUYENTE SELECCIONADO DE HIDROXI, BROMO, FLUORO, CLORO, ENTRE OTROS R3 ES H Y FORMILO R4 ES H, F, Cl, Br Y I. R11 Y R12 SON INDEPENDIENTEMENTE H Y METILO. SON COMPUESTOS PREFERIDOS: 4-(3-(4-(3-CIANOPROPIL)FENIL)-4,4-DIMETIL-5-OXO-2-TIOXO-IMIDAZOLIN-1-IL)-2-(TRIFLUOROMETIL)BENZONITRILO 4-(8-OXO-5-(4-(4-OXOBUTIL)FENIL)-6-TIOXO-5,7-DIAZASPIRO[3.4]OCTAN-7-IL)-2-(TRIFLUOROMETIL)BENZONITRILO 4-(4-(7-(4-CIANO-3-(TRIFLUOROMETIL)FENIL)-8-OXO-6-TIOXO-5,7-DIAZASPIRO[3.4]OCT-AN-5-IL)-2-FLUOROFENIL)-2,2-DIMETIL-N-METIBUTANAMIDA ENTRE OTROS. REFERIDA ADEMAS A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES UN ANTAGONISTA DEL RECEPTOR DE ANDROGENO SIENDO UTIL EN EL TRATAMIENTO DE CANCER DE PROSTATA REFRACTARIO A LA HORMONA
