MASCITTI, VINCENT,DENINNO, MICHAEL PAUL,FUTATSUGI, KENTARO,KUNG, DANIEL WEI-SHUNG,LEFKER, BRUCE ALLEN,MUNCHHOF, MICHAEL JOHN,ROBINSON, JR., RALPH PELTON,MCCLURE, KIM FRANCIS
申请号：
PE0020282011
公开号：
PE03992012A1
申请日:
2010.05.27
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a piperidinil - pyrazole derivative Compound of formula (i), where X is a group consisting of (a) or (b) and \/ or (NR5 R5, CH) Z is C (o) - O - R6 or pyrimidine substituted c1-c4 alkyl, halogen, CF3, among others, M is 1, 2 or 3 n is 0, 1 or 2 r1 is H, c1-c4 alkyl, cycloalkyl C3 C6. 2a is H, F, c1-c4 alkyl R2B is H or F R3 is Oh, halogeno, cyano, c1-c4 alkyl,Among others, R5 is H or c1-c4 alkyl R4 is c1-c4 alkyl or cycloalkyl optionally replaced with C3 C6 Methyl or Ethyl.Preferred compounds are: {4 - [4 - (4 - carbamoyl - 3 - fluorofenoxi) methyl] - 5 - cyano - 1H pyrazol-1-yl) piperidin - carboxylate metilciclopropilo 1 - 1, 4 - (4 - [(2 - 4 - carbamoyl - fluorofenoxi) methyl] - 5 - cyano - 1H - pyrazol-1-yl) piperidin - carboxylate metilciclopropilo 1 - 1, 4 - (5 - cyano - 4 - [4 - (1H - (pyrazol-1-yl) phenoxy] methyl 1h} - (pyrazol-1-yl) piperidin - carboxylate isopropyl 1, among others.It also relates to a Pharmaceutical composition. These compounds modulate the activity of GPR119 G Protein coupled receptor, and are useful in the treatment of diabetes mellitus Type I and II, hyperlipidemia, coronary heart disease, ischemic stroke, among othersREFERIDA A UN COMPUESTO DERIVADO DE PIPERIDINIL-PIRAZOL DE FORMULA (I), DONDE X ES UN COMPUESTO DEL GRUPO (a) O (b) Y ES O, CH(R5) O NR5 Z ES C(O)-O-R6 O PIRIMIDINA SUSTITUIDA CON ALQUILO C1-C4, CF3, HALOGENO, ENTRE OTROS m ES 1, 2 O 3 n ES 0, 1 O 2 R1 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C6 R2a ES H, F, ALQUILO C1-C4 R2b ES H O F R3 ES OH, HALOGENO, CIANO, ALQUILO C1-C4, ENTRE OTROS R5 ES H O ALQUILO C1-C4 R6 ES ALQUILO C1-C4 O CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO CON METILO O ETILO. SON COMPUESTOS PREFERIDOS: 4-{4-[(4-CARBAMOIL-3-FLUOROFENOXI)METIL]-5-CIANO-1H-PIRAZOL-1-IL}PIPERIDIN-1-CARBOXILATO DE 1-METILCICLOPROPILO, 4-{4-[(4-CARBAMOIL-2-FLUOROFENOXI)METIL]-5-CIANO-1H-PIRAZOL-1-IL}PIPERIDIN-1-CARBOXILATO DE 1-METILCICLOPROPILO, 4-(5-CIANO-4-{[4-(1H-PIRAZOL-1-IL)FENOXI]METIL}-1H-PIRAZOL-1-IL)PIPERI
