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Carbamoylmethoxyacetic acid derivatives substituted as novel NEP inhibitors
专利权人:
Novartis AG
发明人:
Iwaki, Yuki,Kawanami, Toshio,Ksander, Gary Michael,Mogi, Muneto
申请号:
ES14155848
公开号:
ES2598961T3
申请日:
2010.11.18
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of the formula (I '): ** Formula ** in which: X1 is OH, -O-C1-7 alkyl, -NRaRb, C1-7-NHS (O) 2 alkyl or benzyl -NHS ( O) 2-, in which Ra and Rb for each event are independently H or C1-7 alkyl; R1 is H, C1-6 alkyl or C6-10 aryl-C1-6 alkyl, wherein alkyl is optionally substituted with benzyloxy, hydroxy or C1-6 alkoxy; for each event, R2 is independently C1-6 alkoxy, hydroxy, halogen, C1-6 alkyl, cyano or trifluoromethyl; A2 is O; R4 is H or C1-6 alkyl; A1 is a C1-3 alkylene bond or chain; R3 is a 5- or 6-membered heteroaryl, C6-10 aryl or C3-7 cycloalkyl, wherein each heteroaryl, aryl or cycloalkyl is optionally substituted with one or more groups independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, C1-6 alkoxy, hydroxy, CO2H and C1-6CO2 alkyl; R6 for each event is independently halogen, hydroxy, C1-7 alkoxy, 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 membered heterocyclyl or a 5 to 6 membered heteroaryl, each of which is optionally substituted with one or more independently selected groups from the group consisting of C1-6 alkyl, halogen, halo C1-6 alkyl, C1-6 alkoxy, hydroxy, CO2H and C1-6 CO2 alkyl; and m is 0 or an integer from 1 to 5; s is 0 or an integer from 1 to 4; or a pharmaceutically acceptable salt thereof.Un compuesto de la fórmula (I'):**Fórmula** en la que: X1 es OH, alquilo -O-C1-7, -NRaRb, alquilo-C1-7-NHS(O)2 o bencilo -NHS(O)2-, en la que Ra y Rb para cada evento son independientemente H o alquilo C1-7; R1 es H, alquilo C1-6 o arilo C6-10-alquilo-C1-6, en la que alquilo es sustituido opcionalmente con benciloxi, hidroxi o alcoxi C1-6; para cada evento, R2 es independientemente alcoxi C1-6, hidroxi, halógeno, alquilo C1-6, ciano o trifluorometilo; A2 es O; R4 es H o alquilo C1-6; A1 es un enlace o cadena de alquileno C1-3; R3 es un heteroarilo de 5 o 6 miembros, arilo C6-10 o cicloalquilo C3-7, en la que cada heteroarilo, ar
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