BURDACK, CHRISTOPH,KALINSKI, CEDRIC,ROSS, GUENTHER,WEBER, LUTZ,KHAZAK, VLADIMIR
申请号：
PE0006242011
公开号：
PE09312011A1
申请日:
2009.09.15
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a compound pyrrolidin-2-one Derivatives of formula (i), where V is c = o, s or CH2 = C X is s or CH2, NH, among others and is co, COO, CH2O, ch2co, among others n is an integer from 0 to 3 R1, R2, R3, R4, R5, R7 and R8 is H, alkyl alquenilo C1 - C2 - C20 and C20, among others.Preferred compounds are: cis-2 - (6 - Chloro - 1 - methyl - 1H indole - 3 - yl) - 1 - [(4-chlorophenyl) methyl] - 3 - [(4-methylphenyl) sulfanyl] - 5 - oxo - N - (2 - pyridin - ylmethyl) - pyrrolidin-3-yl 3 - carboxamide, cis-2 - (6 - Chloro - 1 - methyl - 1H indole - 3 - yl) - 1 - [(4-chlorophenyl) methyl] - 3 - [(4-methylphenyl) sulfanyl] - 5 - oxo - N - (tiofen - 2 - methyl - 3 - pyrrolidin-3-yl) CA Rboxamida,Cis - 2 - (6 - Chloro - 1 - methyl - 1H indole - 3 - yl) - 1 - (4-chlorophenyl) - 3 - [(4-methylphenyl) sulfanyl] - 5 - (N - oxo - pyridin - 2 - methyl - 3 - carboxamide pyrrolidin-3-yl), among others. It also relates to a Pharmaceutical composition. These compounds are ligands Binding to the Hdm2 Protein Inducing Apoptosis and inhibition of proliferation and are useful in the treatment of cancerREFERIDA A UN COMPUESTO DERIVADO DE PIRROLIDIN-2-ONA DE FORMULA (I), DONDE V ES C=O, C=S O CH2 X ES S, O, CH2, NH, ENTRE OTROS Y ES CO, COO, CH2O, CH2CO, ENTRE OTROS n ES UN ENTERO DE 0 A 3 R1, R2, R3, R4, R5, R7 Y R8 SON H, ALQUILO C1-C20, ALQUENILO C2-C20, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: CIS-2-(6-CLORO-1-METIL-1H-INDOL-3-IL)-1-[(4-CLOROFENIL)METIL]-3-[(4-METILFENIL)SULFANIL]-5-OXO-N-(PIRIDIN-2-ILMETIL)PIRROLIDIN-3-CARBOXAMIDA, CIS-2-(6-CLORO-1-METIL-1H-INDOL-3-IL)-1-[(4-CLOROFENIL)METIL]-3-[(4-METILFENIL)SULFANIL]-5-OXO-N-(TIOFEN-2-ILMETIL)PIRROLIDIN-3-CARBOXAMIDA, CIS-2-(6-CLORO-1-METIL-1H-INDOL-3-IL)-1-(4-CLOROFENIL)-3-[(4-METILFENIL)SULFANIL]-5-OXO-N-(PIRIDIN-2-ILMETIL)PIRROLIDIN-3-CARBOXAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON LIGANDOS DE UNION A LA PROTEINA HDM2 QUE INDUCEN LA APOPTOSIS Y LA INHIBICION DE LA PROLI
