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ARIL DIHIDROPIRIDINONA Y PIPERIDINONA COMO INHIBIDORES DE MONOACILGLICEROL ACILTRANSFERASA (MGAT2)
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
TURDI, HUJI,HANGELAND, JON J.,CHENG, DONG,AHMAD, SALEEM,MENG, WEI,BRIGANCE, ROBERT PAUL,ZHAO, GUOHUA,LAWRENCE, R. MICHAEL,DEVASTHALE, PRATIK
申请号:
PE0008532014
公开号:
PE13072014A1
申请日:
2012.11.30
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to dihidropiridinona and piperidinona aryl derivative compounds of formula (i) where X and y are a simple link or double r1 is - with (c4-c8 alkyl (alkyl) - conhch2co C2 C8), among others, R2 is alkyl (c1-c4), cycloalkyl (C3 - C4 haloalquilo) or (c1-c4) R3 is h, F, CL, CN, among others R4 And R5 are each h, F, cl or alkyl (c1-c4) R6 h, Halo, CN, NO2, among others, R11, R12, R13,R14 and R15 are each h, Halo, alkoxy (c1-c4), haloalquilo (c1-c4), among others R16 is H or alkyl (c1-c4).Preferred compounds are: (S) - 3 - (1h-tetrazol-5-yl) - 4 - (p-tolyl) - 6 - (4 - (4,4,4-trifluorobutoxy) phenyl) - 6 - (trifluoromethyl) - 5,6-dihydropyridin-2 (1H) - One (S) - N - (4-methoxyphenyl) - 2 - oxo - 4 - (p-tolyl) - 6 - (4 - (4,4,4-trifluorobutoxy) phenyl) - 6 - (trifluoromethyl) - 1,2,5,6 - tetrahidropiridin - 3 - carboxamide among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of monoacilglicerol acyltransferase (mgat2) being useful in the treatment of diabetes, insulin resistance, nephropathySE REFIERE A COMPUESTOS DERIVADOS DE ARIL DIHIDROPIRIDINONA Y PIPERIDINONA DE FORMULA (I) DONDE x E y SON UN ENLACE SIMPLE O DOBLE R1 ES -CONH(ALQUILO C4-C8), -CONHCH2CO-ALQUILO(C2-C8), ENTRE OTROS R2 ES ALQUILO(C1-C4), CICLOALQUILO(C3-C4) O HALOALQUILO(C1-C4) R3 ES H, F, Cl, CN, ENTRE OTROS R4 Y R5 SON CADA UNO H, F, Cl O ALQUILO(C1-C4) R6 ES H, HALO, CN, NO2, ENTRE OTROS R11, R12, R13, R14 Y R15 SON CADA UNO H, HALO, ALCOXI(C1-C4), HALOALQUILO(C1-C4), ENTRE OTROS R16 ES H O ALQUILO(C1-C4). SON COMPUESTOS PREFERIDOS: (S)-3-(1H-TETRAZOL-5-IL)-4-(p-TOLIL)-6-(4-(4,4,4-TRIFLUOROBUTOXI)FENIL)-6-(TRIFLUOROMETIL)-5,6-DIHIDROPIRIDIN-2(1H)-ONA (S)-N-(4-METOXIFENIL)-2-OXO-4-(p-TOLIL)-6-(4-(4,4,4-TRIFLUOROBUTOXI)FENIL)-6-(TRIFLUOROMETIL)-1,2,5,6-TETRAHIDROPIRIDIN-3-CARBOXAMIDA ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE MONOACILGLICEROL ACILTRANSFERASA (MGAT2) SIENDO UTILES EN EL TRATAMIENTO DE
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