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:
PE2014000393
公开号:
PE20141042A1
申请日:
2012.09.20
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
REFERS TO FORMULA (I) DIHYDROKINOLINE-2-ONA BICYCLE DERIVATIVE COMPOUNDS WHERE R1, R2, R3, R4, R5, R8, R9, R10, AND R11 ARE EACH ONE, ALKYL, HALOALKYL, CYLLOALKYL, OR HALOCHYL, HALOCHYCLE R6, R7 AND R12 ARE EACH H, HALOGEN, ALKYL, CYCLOALKYL, AMONG OTHERS; A1 IS N OR CR13, WHERE R13 IS H, HALOGEN, ALKYL, AMONG OTHERS; A2 IS NR14, AMONG OTHERS, WHERE R14 IS -S (O) 2R18, -S (O) 2OR18, -C (O) R18, AMONG OTHERS, WHERE R18 IS CYCLLOALKYL, ALKYLCLOALKYL, AMONG OTHERS; A3 IS N O CR17, WHERE R17 IS H, HALOGEN, HALOALKYL, AMONG OTHERS;N is 0 to 2. The most popular compounds are: (R) n - (4 - (1-methyl-2-oxo-1,2,3,4-tetrahydroquinol-6-il) - 5,6,7,8-tetrahydroisotope-8-il) acrylamide; (s) - N - (4 - (1-methyl-2-oxo-1,2,3,4-tetrahydroquinol-6-il) - 5,6,8-tetrahydrocyanamide; others. He also mentioned a preparatory process and a pharmaceutical composer. These compounds are aldehydes that inhibit the exchange rate of cell 11b2 or CYP11B1 and are useful in the treatment of diabetic nefroptia, renal fibrosis and congestive heart failure.SE 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 A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBID