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Derivatives of hydroxy - 17 - 17 - pentafluoroetil estra - 4 - 9 (10) - dien - 11 - aryl as progesterone antagonists and processes for their Preparation
专利权人:
BAYER INTELLECTUAL PROPERTY GMBH
发明人:
BONE, Wilhelm,ROTGERI, Andrea,SCHWEDE, Wolfgang,KLAR, Ulrich,MOLLER, Carsten
申请号:
PE0022082016
公开号:
PE00842017A1
申请日:
2010.07.07
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
The present Invention relates to Derivatives of hydroxy - 17 - 17 pentafluoroetil estra - 4.9 - (10) - dien - 11 - aryl of formula (i), their stereoisomers, salts, solvates of salts, solvates,Wherein: R1 is a radical and a phenyl Ring or mono - or alkylated with and and SR2, S (OR) among others R3, R2 is H, alkyl of C1 - C6, among others R3 is C1 - C6 alkyl or aryl X is o,Nro7 or nnhso2r7 R7 is H, alkyl or aryl C1 - C10.Preferred compounds are: (11? 17?) - 17 - hydroxy - 11 - [4 - (methylsulfanyl) phenyl] - 17 - (pentafluoroetil) estra - 4.9 - dien - 3-one (11? 17?) - 11 - [4 - (etilsulfanil) phenyl] - 17 - 17 - (Hydroxy pentafluoroetil estra - 4)9 - dien - 3-one among others. These compounds have antagonistic Action of progesterone being useful in the Treatment or prevention of uterine fibroids, endometriosis, among othersLa presente invencion se refiere a derivados de 17-hidroxi-17-pentafluoroetil-estra-4,9(10)-dien-11-arilo de formula (I), sus estereoisomeros, sales, solvatos, solvatos de las sales, en donde: R1 es un radical Y o un anillo fenilo mono- o disustituido con Y Y es SR2, S(O)R3, entre otros R2 es H, alquilo C1-C6, entre otros R3 es alquilo C1-C6 o arilo X es O, NRO7 o NNHSO2R7 R7 es H, alquilo C1-C10 o arilo. Son compuestos preferidos: (11?, 17?)-17-hidroxi-11-[4-(metilsulfanil)fenil]-17-(pentafluoroetil)estra-4,9-dien-3-ona (11?, 17?)-11-[4-(etilsulfanil)fenil]-17-hidroxi-17-(pentafluoroetil)estra-4,9-dien-3-ona entre otros. Estos compuestos tienen accion antagonista de progesterona siendo utiles en el tratamiento o prevencion de fibroides uterinos, endometriosis, entre otros
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