TULLY, DAVID C.,RUCKER, PAUL VINCENT,ALPER, PHILLIP B.,MUTNICK, DANIEL,CHIANELLI, DONATELLA
申请号：
PE0014562013
公开号：
PE02072014A1
申请日:
2011.11.30
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Oxazole derivatives relates to compounds of formula (i) where z is cicloalquileno phenylene (C5, C7 or monociclico bicyclic heteroaryl) or from 5 to 10 members optionally substituted by Halogen, alkoxyl (C1 - C6), ciclopropilo, among others r1 is piridilo, phenyl Bicyclo [3.1.0] hexanilo, Spiro [2,3] hexanilo, among others R2 is alkyl (C1 - C3), haloalquilo (C1 - C3) or ciclopropilo R3 is hidroxialquilo (C1 - C6), conr4r5, among others, where tetrazolilo, R4 and R5 are each H or alkyl (C1 - C6). Preferred compounds are: 2 - [3 - ({5 - 2-cyclopropyl-1 - 3 - [2 - (trifluoromethoxy) phenyl] - 1.2 - oxazole il} - 4 - methoxy) - 8 - azabiciclo [3.2.1] octan-3-yl - 8 - yl] - 4 - 6 - 5 - fluoro - 1.3 - carboxylate 2 - [(1R, 5S) - 3 - ({5 - 2-cyclopropyl-1 - 3 - [2 - (trifluoromethoxy) phenyl] - 1.2 - oxazole il} - 4 - methoxy) - 8 - azabiciclo [3.2.1] octan-3-yl - 8 - yl] - 4 - 6 - 5 - fluoro - 1.3 - carboxylate among others. It also relates to a Pharmaceutical composition.These compounds are modulators of the activity of the fernesoides x receptor (FXR) being useful in the treatment of cholestasis, primary biliary cirrhosis, gallstonesSE REFIERE A COMPUESTOS DERIVADOS DE OXAZOL DE FORMULA (I) DONDE Z ES FENILENO, CICLOALQUILENO(C5-C7) O HETEROARILO MONOCICLICO O BICICLICO DE 5 A 10 MIEMBROS OPCIONALMENTE SUSTITUIDO CON HALOGENO, ALCOXILO(C1-C6), CICLOPROPILO, ENTRE OTROS R1 ES FENILO, PIRIDILO, BICICLO[3.1.0]HEXANILO, ESPIRO[2,3]HEXANILO, ENTRE OTROS R2 ES ALQUILO(C1-C3), HALOALQUILO(C1-C3) O CICLOPROPILO R3 ES HIDROXIALQUILO(C1-C6), CONR4R5, TETRAZOLILO, ENTRE OTROS, EN DONDE R4 Y R5 SON CADA UNO H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: 2-[3-({5-CICLOPROPIL-3-[2-(TRIFLUOROMETOXI)FENIL]-1,2-OXAZOL-4-IL}METOXI)-8-AZABICICLO[3.2.1]OCTAN-8-IL]-4-FLUORO-1,3-BENZOTIAZOL-6-CARBOXILATO DE METILO 2-[(1R,5S)-3-({5-CICLOPROPIL-3-[2-(TRIFLUOROMETOXI)FENIL]-1,2-OXAZOL-4-IL}METOXI)-8-AZABICICLO[3.2.1]OCTAN-8-IL]-4-FLUORO-1,3-BENZOTIAZOL-6-CARBOXILATO DE METILO ENTRE OTROS. TAMBI
