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DERIVADOS DEL ACIDO CARBAMOIL-METIL-AMINO-ACETICO SUSTITUIDO COMO INHIBIDORES DE NEP NOVEDOSOS
专利权人:
NOVARTIS AG
发明人:
IWAKI, YUKI,KAWANAMI, TOSHIO,KSANDER, GARY MICHAEL,MOGI, MUNETO
申请号:
PE0006612012
公开号:
PE13112012A1
申请日:
2010.11.18
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
Referring to a compound derived from acid methyl Carbamoyl amino acid of formula (i), where X1 is Oh, o-alkyl C1 - C7, NHS (OR) 2 - alkyl C1 - C7, among others r1 is H, c1-c6 alkyl, aryl alkyl C1 - C6 C10 C6, among others R2 is C1 - C6 Oh alkoxyl, alkyl, halogen, C1 - C6, among others A2 is o or nr 5 R4 and R5 are H or c1-c6 alkyl A1 is a link or alquileno C1 - C3 C6 C10 R3 is aryl,Heteroaryl of 5 or 6 members, among others Oh, R6 is Halogen, halogen, alkoxyl C1 - C7, among others M is an integer from 0 to 5 s is an integer from 0 to 4.Preferred compounds are: acid tert butyl ester (S) - 2 - [(S) - 2 - (2 , 5 - Dichloro biphenyl - 4-yl) - 1 - (1h tetrazole - 5 - ilcarbamoil amino) ethyl] - propionic acid ethyl ester, (S - 3 - (Benzyloxy) - 2 - [(S) - 2 - (2 - chloro biphenyl - 4-yl) - 1 - (1h-tetrazol-5-yl - carbamoyl amino) ethyl] - propionic acid, Tert Butyl ester ( (S) - 2 - [(R) - 2 - (2 , 5 - Dichloro biphenyl - 4-yl) - 1 - (1h-tetrazol-5-yl - carbamoyl amino) ethyl] - propionic acid,Among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of neutral Endopeptidase (NEP) and are useful in the treatment of hypertension, congestive heart failure, nephrotic syndrome, renal fibrosis, among othersREFERIDA A UN COMPUESTO DERIVADO DE ACIDO CARBAMOIL-METIL-AMINO-ACETICO DE FORMULA (I), DONDE X1 ES OH, O-ALQUILO C1-C7, NHS(O)2-ALQUILO C1-C7, ENTRE OTROS R1 ES H, ALQUILO C1-C6, ARILO C6-C10-ALQUILO C1-C6, ENTRE OTROS R2 ES ALCOXILO C1-C6, OH, HALOGENO, ALQUILO C1-C6, ENTRE OTROS A2 ES O O NR5 R4 Y R5 SON H O ALQUILO C1-C6 A1 ES UN ENLACE O ALQUILENO C1-C3 R3 ES ARILO C6-C10, HETEROARILO DE 5 O 6 MIEMBROS, ENTRE OTROS R6 ES HALOGENO, OH, ALCOXILO C1-C7, HALOGENO, ENTRE OTROS m ES UN ENTERO DE 0 A 5 s ES UN ENTERO DE 0 A 4. SON COMPUESTOS PREFERIDOS: TERBUTIL-ESTER DEL ACIDO (S)-2-[(S)-2-(2,5-DICLORO-BIFENIL-4-IL)-1-(1H-TETRAZOL-5-ILCARBAMOIL)-ETIL-AMINO]-PROPIONICO, ETIL-ESTER DEL ACIDO (S)-3-BENCILOXI-2-[(S)-2-(3-CLORO-BIFENIL-4-IL)-1-
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