QIN, DONGHUI,JOSHI, HEMANT,TANGIRALA, RAGHURAM,CHRISTENSEN IV, SIEGFRIED BENJAMIN
申请号：
PE0025202013
公开号：
PE06182014A1
申请日:
2012.05.18
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Relates to compounds of formula (i) wherein R1 is alkyl (C1 - C6) (C3 - C7), cycloalkyl, aryl, among others R2 is H, alkyl, alkoxy (C1 - C3), CN, among others R4 is CH2COOH, COOH, Ester or amide R5 is H, hydroxyl or oxo R7 is H or alkyl (C1 - C3) X is c or N and is n or Cr3, where R3 is H, alkyl (C 1 - C6), halogen, among others M is 0 to 3 n is 0 OR 1.Preferred compounds are: {1 - acid - 2 - oxo - (6 - [4 - [4 - (trifluoromethyl) phenyl] carbamoyl) amino) phenyl] - 1,2,3,4 - tetrahidroisoquinolin - il - 2} acetic acid 2 - [6 - (4 - [(3-methylphenyl) Carbamoyl] amino} phenyl) - 1 - 2 - oxo - 1,2,3,4 - tetrahidroisoquinolin - il] acetic acid {1 - 2 - oxo - (6 - [4 - [4 - (trifluoromethoxy) phenyl] carbamo Il} - amino) phenyl] - 1,2,3,4 - tetrahidroisoquinolin - il - 2} acetic acid among others.It also relates to a Pharmaceutical composition. These compounds are inhibitors of acyl coenzyme A diacylglycerol acyltransferase (DGAT) 1 1 to be useful in the treatment of hyperlipoproteinemia, obesity, dyslipidemiaSE REFIERE A COMPUESTOS DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C6), CICLOALQUILO(C3-C7), ARILO, ENTRE OTROS R2 ES H, ALQUILO(C1-C3), ALCOXI, CN, ENTRE OTROS R4 ES CH2COOH, COOH, ESTER O AMIDA R5 ES H, HIDROXILO U OXO R7 ES H O ALQUILO(C1-C3) X ES C O N Y ES N O CR3, EN DONDE R3 ES H, ALQUILO(C1-C6), HALOGENO, ENTRE OTROS m ES DE 0 A 3 n ES 0 O 1. SON COMPUESTOS PREFERIDOS: ACIDO 2-{1-OXO-6-[4-({[4-(TRIFLUOROMETIL)FENIL]CARBAMOIL}AMINO)FENIL]-1,2,3,4-TETRAHIDROISOQUINOLIN-2-IL}ACETICO ACIDO 2-[6-(4-{[(3-METILFENIL)CARBAMOIL]AMINO}FENIL)-1-OXO-1,2,3,4-TETRAHIDROISOQUINOLIN-2-IL]ACETICO ACIDO 2-{1-OXO-6-[4-({[4-(TRIFLUOROMETOXI)FENIL]CARBAMOIL}-AMINO)FENIL]-1,2,3,4-TETRAHIDROISOQUINOLIN-2-IL}ACETICO ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE ACIL COENZIMA A DIACILGLICEROL ACILTRANSFERASA 1 (DGAT-1) SIENDO UTILES EN EL TRATAMIENTO DE OBESIDAD, HIPERLIPOPROTEINEMIA, DISLIPIDEMIA
