AEBI, JOHANNES,AMREIN, KURT,FANTASIA, SERENA MARIA,HORNSPERGER, BENOIT,KUHN, BERND,LIU, YONGFU,MAERKI, HANS P.,MAYWEG, ALEXANDER V.,MOHR, PETER,SCALONE, MICHELANGELO,TAN, XUEFEI,ZHOU, MINGWEI
申请号：
PE0003932014
公开号：
PE10422014A1
申请日:
2012.09.20
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Refers to bicyclic Derivatives of compounds dihidroquinolina - 2 - one of formula (i) wherein R1, R2, R3, R4, R6, R8, R9, R10 and R11 are each h, alkyl, cycloalkyl or halocicloalquilo haloalquilo, R6, R7 and R12 are each h, halogen, alkyl, cycloalkyl, among others, A1 is n or cr13, where r 13 IS h, alkyl, halogen, among others A2 is nr14, among others, where R14 is - S (o) 2r18,- S (o) C (o) - 2or18, R18, among others, where is alquilcicloalquilo R18, cycloalkyl, triazolilalquilo, among others A3 is n or cr17 R17, where is H, halogen, haloalquilo, among others n is 0 to 2.Preferred compounds are: (R) - N - (4 - (1 - methyl - 2 - oxo - 1,2,3,4 - tetrahidroquinolin IL - 6 - - - tetrahidroisoquinolin 5,6,7,8) - 8 - il) propionamide (S) - N - (4 - (1 - methyl - 2 - oxo - 1,2,3,4 - tetrahidroquinolin - 6 - il) - minutebug - tetrahidroisoquinolin - 8 - il) etanosulfonamida among others. It also relates to a preparation method and a Pharmaceutical composition.These compounds are inhibitors of the aldosterone synthase CYP11B2 and CYP11B1 being useful in the treatment of diabetic nephropathy, renal fibrosis, congestive heart failureSE REFIERE A COMPUESTOS DERIVADOS BICICLICOS DE DIHIDROQUINOLINA-2-ONA DE FORMULA (I) DONDE R1, R2, R3, R4, R5, R8, R9, R10 Y R11 SON CADA UNO H, ALQUILO, HALOALQUILO, CICLOALQUILO O HALOCICLOALQUILO R6, R7 Y R12 SON CADA UNO H, HALOGENO, ALQUILO, CICLOALQUILO, ENTRE OTROS A1 ES N O CR13, DONDE R13 ES H, HALOGENO, ALQUILO, ENTRE OTROS A2 ES NR14, ENTRE OTROS, EN DONDE R14 ES -S(O)2R18, -S(O)2OR18, -C(O)R18, ENTRE OTROS, DONDE R18 ES CICLOALQUILO, ALQUILCICLOALQUILO, TRIAZOLILALQUILO, ENTRE OTROS A3 ES N O CR17, EN DONDE R17 ES H, HALOGENO, HALOALQUILO, ENTRE OTROS n ES DE 0 A 2. SON COMPUESTOS PREFERIDOS: (R)-N-(4-(1-METIL-2-OXO-1,2,3,4-TETRAHIDROQUINOLIN-6-IL)-5,6,7,8-TETRAHIDROISOQUINOLIN-8-IL)PROPIONAMIDA (S)-N-(4-(1-METIL-2-OXO-1,2,3,4-TETRAHIDROQUINOLIN-6-IL)-5,6,7,8-TETRAHIDROISOQUINOLIN-8-IL)ETANOSULFONAMIDA ENTRE OTROS. TAMBIEN SE REFIERE
