COPPOLA, GARY MARK,IWAKI, YUKI,KARKI, RAJESHRI GANESH,KAWANAMI, TOSHIO,KSANDER, GARY MICHAEL,MOGI, MUNETO,SUN, ROBERT
申请号：
PE0020042011
公开号：
PE03302012A1
申请日:
2010.05.26
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Amino propionicos relates to compounds of formula (i) wherein R1 is H, alkyl (C1 - C7), hydroxyl, alkoxyl (C1 - C7), among others, R2 is alkyl, halogen (C1 - C7), NO2, CN, alcanoilo (C1 - C7) amino -, among others R3 is a - C (o) x1 A1 or A2 - R4, wherein R4 is aryl, heteroaryl (C6 C10), among others X and X1 are Each Oh, o-alkyl (C1 - C7), NHS (OR) 2 - benzyl, among others A1 is a Link, alquileno (C1 - C7)PHENYL, among others A2 is a link or alquileno (C1 - C7) R5 is H, halogen, alkoxyl, hydroxyl, (C1 - C7), among others B1 is - C (o) NH - or - NHC (OR) - n is 0 to 5.Preferred compounds are: acid (R) - 3 - (Diphenyl - 4 - il - methyl) - 4 - (2 - amino - and carboxy ethyl) - 4 - oxo acid, butanoic acid, 3 - (R) - biphenyl - il - 4 - methyl - N - Carboxy - methyl - (succinamico Acid (R) - 4 - Diphenyl - 4 - il - 3 - [(1h tetrazole - 5 - carbonyl) - amino] - butyric acid among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of neutral Endopeptidase (NEP) being useful in the treatment of hypertension, Heart Failure, nephrotic syndrome, glomerulonephritisSE REFIERE A COMPUESTOS AMINO-PROPIONICOS DE FORMULA (I) DONDE R1 ES H, ALQUILO(C1-C7), HIDROXILO, ALCOXILO(C1-C7), ENTRE OTROS R2 ES ALQUILO(C1-C7), HALOGENO, NO2, CN, ALCANOILO(C1-C7)-AMINO, ENTRE OTROS R3 ES A1-C(O)X1 O A2-R4, EN DONDE R4 ES ARILO(C6-C10), HETEROARILO, ENTRE OTROS X Y X1 SON CADA UNO OH, O-ALQUILO(C1-C7), NHS(O)2-BENCILO, ENTRE OTROS A1 ES UN ENLACE, ALQUILENO(C1-C7), FENILO, ENTRE OTROS A2 ES UN ENLACE O ALQUILENO(C1-C7) R5 ES H, HALOGENO, HIDROXILO, ALCOXILO(C1-C7), ENTRE OTROS B1 ES -C(O)NH- O -NHC(O)- n ES DE 0 A 5. SON COMPUESTOS PREFERIDOS: ACIDO (R)-3-(BIFENIL-4-IL-METIL)-4-(2-CARBOXI-ETIL-AMINO)-4-OXO-BUTANOICO ACIDO (R)-3-BIFENIL-4-IL-METIL-N-CARBOXI-METIL-SUCCINAMICO ACIDO (R)-4-BIFENIL-4-IL-3-[(1H-TETRAZOL-5-CARBONIL)-AMINO]-BUTIRICO ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENDOPEPTIDASA N
