AEBI, JOHANNES,AMREIN, KURT,CHEN, WENMING,HORNSPERGER, BENOIT,KUHN, BERND,MAERKI, HANS P.,LIU, YONGFU,MAYWEG, ALEXANDER V.,MOHR, PETER,TAN, XUEFEI,WANG, ZHANGUO,ZHOU, MINGWEI
申请号:
PE2014000766
公开号:
PE20141283A1
申请日:
2012.11.27
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
It refers to bicycle derivatives in dihydroisocyano-1-ona (I) preparation process, wherein R1, R2, R3 and R4 are h, tar, cyclopentadiene, alcohole, etc.; A1 is CR8 or N; A5 is Cr6 or N, wherein R5, R6, R7 and R8 are each halogen, CN, halogen, hydroxyl, etc.; A2 is CR9 or N, wherein R9 is h, halogen, lalco, lallo, etc. Others; A3 is n, etc.; A4 is cr11 or N, R11 is h; n is 0 or 1. The most popular compounds are: 6-chloro-2-pyridine-3-il-3, 4-dihydro-2h-isoquinlin-1-ona; 5 - (6-chloro-1-oxo-3, 4-dihydro-1h-isoquinlin-2-il) - nicotine nitro;There are others He also mentioned an acquisition process and a drug synthesis. These compounds inhibit estraldehyde and are useful in the treatment of chronic kidney disease, congestive heart failure, hypertension and aldehyde poisoning.SE REFIERE A DERIVADOS BICICLICOS DE DIHIDROISOQUINOLIN-1-ONA DE FORMULA (I) DONDE R1, R2, R3 Y R4 SON CADA UNO H, ALQUILO, CICLOALQUILO, ALCOXIALQUILO, ENTRE OTROS; A1 ES CR8 O N; A5 ES CR6 O N, EN DONDE R5, R6, R7 Y R8 SON CADA UNO HALOGENO, CN, HALOALQUILO, HIDROXI, ENTRE OTROS; A2 ES CR9 O N, EN DONDE R9 ES H, HALOGENO, CN, ARILALQUILO, ENTRE OTROS; A3 ES N, ENTRE OTROS; A4 ES CR11 O N, EN DONDE R11 ES H; n ES 0 O 1. SON COMPUESTOS PREFERIDOS: 6-CLORO-2-PIRIDIN-3-IL-3,4-DIHIDRO-2H-ISOQUINOLIN-1-ONA; 5-(6-CLORO-1-OXO-3,4-DIHIDRO-1H-ISOQUINOLIN-2-IL)-NICOTINO-NITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO DE OBTENCION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ALDOSTERONA SINTASA SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES RENALES CRONICAS, FALLO CARDIACO CONGESTIVO, HIPERTENSION, ALDOSTERONISMO