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INHIBIDOR DE CETP DE OXAZOLIDINONA BICICLICO FUSIONADO
专利权人:
MERCK SHARP AND DOHME CORP.
发明人:
SHAO, PENGCHENG PATRICK,YE, FENG,VACHAL, PETR,SHA, DEYOU,KATIPALLY, REVATHI REDDY,LIU, JIAN,SUN, WANYING
申请号:
PE0006162014
公开号:
PE12302014A1
申请日:
2012.10.25
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to oxazolidinone compounds FUSED bicyclic Derivatives of formula (i) wherein R1 is H, alkyl, halogen (C1 - C5), among others X is 0 OR 1 The Dashed Lines represent a double Bond or CR2 is optional D1 D2 or D3 Cr3 is n n or CR4, where R2, R3 and R4 are each h, alq Uilo (C1 - C5), or alkyl (C1 - C5), alquenilo (C2 - C5), among others R5 is alkyl (C1 - C5), alquinilo (C2 - C5)Halogen, among others A1 is phenyl cycloalkyl (C3, C8), among others A2 is phenyl, among others is 0 to 3.Preferred compounds are: 3 - [2 - [(1R, 5S, 7aS) - 1 - [3,5-bis (trifluoromethyl) phenyl] - 3 - oxotetrahidro - 1H pyrrolo [1,2-c] [1,3] oxazole - 5} - il - 6 - methoxy - 4 - (trifluoromethyl) biphenyl il] - 3 - Methyl propanoate acid, 3 - [2 - [(1R, 5S, 7aS) - 1 - [3,5-bis (trifluoromethyl) phenyl] - 3 - oxotetrahidro - 1H pyrrolo [1,2-c] [1,3] oxazole - 5 - I L} - 6 - methoxy - 4 - (trifluoromethyl) biphenyl - 3 - il] propanoic acid among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of the cholesterol ester transfer protein (CETP) being useful in the treatment of dyslipidemia, atherosclerosisSE REFIERE A COMPUESTOS DERIVADOS DE OXAZOLIDINONA BICICLICO FUSIONADO DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C5), HALOGENO, ENTRE OTROS x ES 0 O 1 LAS LINEAS DISCONTINUAS REPRESENTAN UN DOBLE ENLACE OPCIONAL D1 ES N O CR2 D2 ES N O CR3 D3 ES N O CR4, EN DONDE R2, R3 Y R4 SON CADA UNO H, ALQUILO(C1-C5), O-ALQUILO(C1-C5), ALQUENILO(C2-C5), ENTRE OTROS R5 ES ALQUILO(C1-C5), ALQUINILO(C2-C5), HALOGENO, ENTRE OTROS A1 ES FENILO, CICLOALQUILO(C3-C8), ENTRE OTROS A2 ES FENILO, ENTRE OTROS a ES DE 0 A 3. SON COMPUESTOS PREFERIDOS: 3-[2-{(1R,5S,7aS)-1-[3,5-BIS(TRIFLUOROMETIL)FENIL]-3-OXOTETRAHIDRO-1H-PIRROLO[1,2-c][1,3]OXAZOL-5-IL}-6-METOXI-4-(TRIFLUOROMETIL)BIFENIL-3-IL]PROPANOATO DE METILO ACIDO 3-[2-{(1R,5S,7aS)-1-[3,5-BIS(TRIFLUOROMETIL)FENIL]-3-OXOTETRAHIDRO-1H-PIRROLO[1,2-c][1,3]OXAZOL-5-IL}-6-METOXI-4-(TRIFLUOROMETIL)BIFENIL-3-IL]PROPANOICO ENTRE OTROS. T
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