AEBI, JOHANNES,AMREIN, KURT,HORNSPERGER, BENOIT,KNUST, HENNER,KUHN, BERND,LIU, YONGFU,MAERKI, HANS P.,MAYWEG, ALEXANDER V.,MOHR, PETER,TAN, XUEFEI,ZHOU, MINGWEI
申请号:
PE0003282014
公开号:
PE13722014A1
申请日:
2012.09.12
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to compounds derived from dihidroquinolina - 2 - one of formula (i) wherein R1, R2, R3, R4, R5 and R6 are each h, halogen, alkyl, cycloalkyl, haloalquilo, among others R3 and R4 can form a double Bond H or R8 R6, R8 is where - OM (cr9r10) - N - (cr11r12) (P - Q - nr15r16, between cr13r14) Where other, R9, R10, R11, R12, R13 and R14 are each h, halogen, alkyl,Among others, R15 is H, alkyl, alkoxyalkyl esters, among others R16 is H, alkyl, aryl, among others M is 0 OR 1 n, P and q are each from 0 to 2 it is CR20 A1 or A2 is cr21 or N n n is cr22 A3 or, where R20 R21, R22 and are each h, alkyl, cycloalkyl, among others.Preferred compounds are: [5 - (1 - methyl - 2 - oxo - 1,2,3,4 tetrahydro - quinolin-1 - 6 - il) pyridin-3-yl] - etanosulfonico acid amide [5 - (1 - methyl - 2 - oxo - 1,2,3,4 tetrahydro - quinolin-1 - 6 - il) - pyridin - ilcarbamoil] - 3 - methyl ester of acetic acid among others. It also relates to a production method and a Pharmaceutical composition.These compounds are inhibitors of the aldosterone synthase CYP11B2 and CYP11B1 being useful in the treatment of Chronic Kidney Disease, congestive heart failure, hypertensionSE REFIERE A COMPUESTOS DERIVADOS DE DIHIDROQUINOLINA-2-ONA DE FORMULA (I) DONDE R1, R2, R3, R4, R5 Y R7 SON CADA UNO H, HALOGENO, ALQUILO, HALOALQUILO, CICLOALQUILO, ENTRE OTROS R3 Y R4 PUEDEN FORMAN UN DOBLE ENLACE R6 ES H O R8, EN DONDE R8 ES -Om-(CR9R10)n-(CR11R12)p-(CR13R14)q-NR15R16, ENTRE OTROS, EN DONDE R9, R10, R11, R12, R13 Y R14 SON CADA UNO H, HALOGENO, ALQUILO, ENTRE OTROS R15 ES H, ALQUILO, ALCOXIALQUILO, ENTRE OTROS R16 ES H, ALQUILO, ARILO, ENTRE OTROS m ES 0 O 1 n, p Y q SON CADA UNO DE 0 A 2 A1 ES CR20 O N A2 ES CR21 O N A3 ES CR22 O N, EN DONDE R20, R21 Y R22 SON CADA UNO H, ALQUILO, CICLOALQUILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [5-(1-METIL-2-OXO-1,2,3,4-TETRAHIDRO-QUINOLIN-6-IL)-PIRIDIN-3-IL]-AMIDA DE ACIDO ETANOSULFONICO [5-(1-METIL-2-OXO-1,2,3,4-TETRAHIDRO-QUINOLIN-6-IL)-PIRIDIN-3-ILCARBAMOIL]-METIL