HEIMBACH, DIRK,ROHRIG, SUSANNE,CANCHO GRANDE, YOLANDA,BENDER, ECKHARD,ZIMMERMANN, KATJA,BUCHMULLER, ANJA,GERDES, CHRISTOPH,GNOTH, MARK JEAN,GERICKE, KERSTEN MATTHIAS,JESKE, MARIO
申请号：
PE0020092011
公开号：
PE04022012A1
申请日:
2010.05.18
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a piperidine derivative Compound of formula (i), wherein R1 is trifluoromethyl, 1.1 - difluoroetilo, 2,2,2 - trifluoroetilo, among others R2 is hidroxiet - 2 - 1 - 2 - 1 - metoxiet ILO, ILO, ciclopropilo, among others R3 is oxidotiomorfolinilo or dioxidotiomorfolinilo.Preferred compounds are: {3 - [3 - (2-methoxyethyl) - 1,2,4 - Oxadiazoles - 5 - yl] - 5 - [4 - (trifluoromethoxy) phenyl] piperidin-1-yl} - (oxidotiomorfolin - 4-yl) methanone, {3 - (3 - 2-cyclopropyl-1 - 1,2,4 - Oxadiazoles - 5 - il) - 5 - [4 - (trifluoromethoxy) phenyl] piperidin-1-yl] - (1 - oxidotiomorfolin - 4-yl) methanone, {3 - [3 - (2-ethoxyethyl) - 1,2,4 - oxadiaz Ol - 5 - yl] - 5 - (4-ethyl-phenyl) piperidin-1-yl] - (1 - oxidotiomorfolin - 4-yl) methanone, among others.It also relates to a preparation method and a Pharmaceutical composition. These compounds are antagonists of protease activated receptors (par-1) and are useful in the treatment of cardiovascular thromboembolic disorders, tumor, among othersREFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINA DE FORMULA (I), DONDE R1 ES TRIFLUOROMETILO, 1,1-DIFLUOROETILO, 2,2,2-TRIFLUOROETILO, ENTRE OTROS R2 ES 2-HIDROXIET-1-ILO, 2-METOXIET-1-ILO, CICLOPROPILO, ENTRE OTROS R3 ES OXIDOTIOMORFOLINILO O DIOXIDOTIOMORFOLINILO. SON COMPUESTOS PREFERIDOS: {3-[3-(2-METOXIETIL)-1,2,4-OXADIAZOL-5-IL]-5-[4-(TRIFLUOROMETOXI)FENIL]PIPERIDIN-1-IL}-(OXIDOTIOMORFOLIN-4-IL)METANONA, {3-(3-CICLOPROPIL-1,2,4-OXADIAZOL-5-IL)-5-[4-(TRIFLUOROMETOXI)FENIL]PIPERIDIN-1-IL}-(1-OXIDOTIOMORFOLIN-4-IL)METANONA, {3-[3-(2-ETOXIETIL)-1,2,4-OXADIAZOL-5-IL]-5-(4-ETILFENIL)PIPERIDIN-1-IL}-(1-OXIDOTIOMORFOLIN-4-IL)METANONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DE LOS RECEPTORES ACTIVADOS POR PROTEASA (PAR-1) Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS CARDIOVASCULARES, TROMBOEMBOLICOS, TUMORALES, ENTRE OTROS
