COPPOLA, GARY MARK,IWAKI, YUKI,KARKI, RAJESHRI GANESH,KAWANAMI, TOSHIO,KSANDER, GARY MICHAEL,MOGI, MUNETO,SUN, ROBERT
申请号:
PE0020112011
公开号:
PE09352012A1
申请日:
2010.05.26
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Refers to a compound of formula I, wherein R1 is alkyl C1 - C7 C1 - C7 R2 is alkyl, cycloalkyl NO2, CN, halogen, C3 - C7, among others R3 is A1c (or x1), A2 - R4, R4 C6 C10 is aryl, heteroaryl substituted bicyclic monociclico or 1 0 more oh, alkyl C - C7, among others R5 is H, halogen, Oh, alcox ILO C1 - C7, halogen, alkyl of C1 - C7 X and X1 are each Oh - (alkyl, or C1 - C7)NHS (OR) 2 - (alkyl C1 - C7), among others A1 is link, alquileno c1-c4 linear or ramificadocicloalquilo C3 - C7, heteroaryl phenyl, among others A2 is link, alquileno c1-c4 linear or branched, among others n is 0 - 5.Preferred compounds are: acid (2R, 4S) - Diphenyl - 4 - 5 - il - 4 - (3 - Carboxy - methyl - 3 - metilureido) - 2-methyl pentanoic acid acid - (5 - (1S, 3R) - Diphenyl - 1 - methyl - 4 - il - ethoxy - 3 - carbonyl - Butyl - carbamoyl) - 1H pyrazole carboxylic acid - 3 - among others.These compounds are inhibitors of neutral Endopeptidase useful in the treatment of various Disorders such as diabetic nephropathy, hypertension, Cardiac fibrosis, among othersREFERIDA A UN COMPUESTO DE FORMULA I, DONDE R1 ES ALQUILO C1-C7 R2 ES ALQUILO C1-C7, NO2, CN, HALOGENO, CICLOALQUILO C3-C7, ENTRE OTROS R3 ES A1C(O)X1, A2-R4 R4 ES ARILO C6-C10, HETEROARILO MONOCICLICO O BICICLICO SUSTITUIDO POR 1 0 MAS OH, ALQUILO C-C7, ENTRE OTROS R5 ES H, HALOGENO, OH, ALCOXILO C1-C7, HALOGENO, ALQUILO C1-C7 X y X1 SON CADA UNO OH, O-(ALQUILO C1-C7), NHS(O)2-(ALQUILO C1-C7), ENTRE OTROS A1 ES ENLACE, ALQUILENO C1-C4 LINEAL O RAMIFICADOCICLOALQUILO C3-C7, HETEROARILO, FENILO, ENTRE OTROS A2 ES ENLACE, ALQUILENO C1-C4 LINEAL O RAMIFICADO, ENTRE OTROS n ES 0-5. SON COMPUESTOS PREFERIDOS: ACIDO (2R,4S)-5-BIFENIL-4-IL-4-(3-CARBOXI-METIL-3-METILUREIDO)-2-METIL-PENTANOICO ACIDO-5-((1S,3R)-1-BIFENIL-4-IL-METIL-3-ETOXI-CARBONIL-BUTIL-CARBAMOIL)-1H-PIRAZOL-3-CARBOXILICO ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE ENDOPEPTIDASA NEUTRA UTILES EN LE TRATAMIENTO DE DIVERSOS TRASTORNOS TALES COMO HIPERTENSION, NEFROPATIA