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:
PE0013302018
公开号:
PE13782018A1
申请日:
2012.09.20
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
Bicyclic compounds refers dihidroquinolina - 2 - One Derivatives of formula I in which R1, R2, R3, R4, R6, R8, R9, R10 is H, alkyl, cycloalkyl, halocicloalquilo haloalquilo, R6, R7, R12,Are h, halogen, alkyl, cycloalkyl, haloalquilo, among others A1 or A2 is cr13 nr14, among others or cr17 A3 is n n is 0, 1 or 2.These compounds are useful for the prophylaxis or Therapy of Chronic Kidney Disease, congestive heart failure, hypertension, Primary Aldosteronism, among others.The preferred compounds are the following: (RAC) - N - [4 - (1 - methyl - 2 - oxo - 1,2,3,4 tetrahydro - quinolin-1 - 6 - yl) - 5,6,7,8-tetrahydro - isoquinolin - 8 - il) propionamide (RAC) - N - [4 - (1 - methyl - 2 oxo - 1,2,3,Tetrahidroquinolin IL - 4 - 6 - 8 tetrahidroisoquinolin 5,6,7,8) - - - - il) etanosulfonamida among others.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.