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：
PE2018001330
公开号：
PE20181378A1
申请日:
2012.09.20
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
It refers to bicyclic compounds derived from dihydroquinoline-2-one of formula I in which R1, R2, R3, R4, R5, R8, R9, R10 are H, alkyl, haloalkyl, cycloalkyl, halocycloalkyl； R6, R7, R12 are H, halogen, alkyl, haloalkyl, cycloalkyl, among others； A1 is N or CR13； A2 is NR14, among others； A3 is N or CR17； n is zero, 1 or 2. These compounds are useful for therapy or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism, among others. Among the preferred compounds we have the following: (rac) -N- [4- (1-methyl-2-oxo-1,2,3,4-tetrahydro-quinolin-6-yl) -5,6,7,8 -tetrahydro-isoquinolin-8-yl) propionamide；(RAC) - N - [4 - (1-methyl-2-oxo-1, 2, 3, 4-tetrahydroquinol-6-il) - 5, 6, 7, 8-tetrahydroisotope-8-il) ethane； and so on.Se refiere compuestos biciclicos derivados de dihidroquinolina-2-ona de formula I en los que R1, R2, R3, R4, R5, R8, R9, R10 son H, alquilo, haloalquilo, cicloalquilo, halocicloalquilo； R6, R7, R12, son H, halogeno, alquilo, haloalquilo, cicloalquilo, entre otros； A1 es N o CR13； A2 es NR14, entre otros； A3 es N o CR17； n es cero, 1 o 2. Dichos compuestos son utiles para terapia o profilaxis de enfermedad renal cronica, fallo cardiaco congestivo, hipertension, aldosteronismo primario, entre otros. Entre los compuestos preferidos tenemos los siguientes: (rac)-N-[4-(1-metil-2-oxo-1,2,3,4-tetrahidro-quinolin-6-il)-5,6,7,8-tetrahidro-isoquinolin-8-il)propionamida； (rac)-N-[4-(1-metil-2-oxo-1,2,3,4-tetrahidroquinolin-6-il)-5,6,7,8-tetrahidroisoquinolin-8-il)etanosulfonamida； entre otros.
