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Carbamoylmethylamino acetic acid derivatives substituted as new NEP inhibitors
专利权人:
NOVARTIS AG
发明人:
IWAKI, YUKI,KAWANAMI, TOSHIO,KSANDER, GARY MICHAEL,MOGI, MUNETO
申请号:
ES10781884
公开号:
ES2481890T3
申请日:
2010.11.18
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of the formula (III): wherein: X1 is OH, -O-C1-7alkyl, -NRaRb, -NHS (O) 2-C1-7 alkyl or -NHS (O) 2-benzyl, wherein Ra and Rb for each occurrence are independently H or C1-7 alkyl; R1 is C1-6 alkyl or C6-10-aryl-C1-6 alkyl, wherein the alkyl is optionally substituted with benzyloxy, hydroxy or C1-6 alkoxy; for each occurrence, R2 is independently C1-6-alkoxy, hydroxy, halo, C1-6-alkyl, cyano or trifluoromethyl; R4 and R5 are independently H or C1-6 alkyl; A1 is a bond or a C1-3 alkylene chain; R3 is a 5- or 6- membered heteroaryl, C6-10-aryl or C3-7-cycloalkyl, wherein each heteroaryl, aryl or cycloalkyl are optionally substituted with one or more groups independently selected from the group consisting of C1-6 alkyl, halo, halo C1-6 alkyl, C1-6 alkoxy, hydroxy, CO2H and CO2C1-6 alkyl; R6 for each occurrence is independently halo, hydroxy, C1-C7 alkoxy, halo, C1-7 alkyl or halo-C1-7 alkyl; or R4, A1-R3, together with the nitrogen to which R4 and A1-R3 are attached, form a 4- to 7- member heterocyclyl or a 5- to 6- member heteroaryl, each of which is optionally substituted with one or more groups independently selected from the group consisting of C1-6 alkyl, halo, halo C1-6 alkyl, C1-6 alkoxy, hydroxy, CO2H and CO2C1-6 alkyl; and m is 0 or an integer from 1 to 5; s is 0 to an integer from 1 to 4; X2 is halo; and p is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt thereof.Un compuesto de la fórmula (III): en donde: X1 es OH, -O-C1-7alquilo, -NRaRb, -NHS(O)2-C1-7 alquilo o -NHS(O)2-bencilo, en donde Ra y Rb para cada ocurrencia son independientemente H o C1-7 alquilo; R1 es C1-6 alquilo o C6-10-arilo-C1-6 alquilo, en donde el alquilo es opcionalmente sustituido con benciloxi, hidroxi o C1- 6 alcoxi; para cada ocurrencia, R2 es independientemente C1-6-alcoxi, hidroxi, halo, C1-6-alquilo, ciano o trifluorometilo; R4 y R5 son independientemente H o C1-6 alquilo; A1 es un enlace o una cadena C1-3 alquileno; R3 es un heteroarilo de 5- o 6- miem
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