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Substituted aminobutyric derivatives as neprilysin inhibitors
专利权人:
Novartis AG
发明人:
COPPOLA, Gary Mark,IWAKI, Yuki,KARKI, Rajeshri Ganesh,KAWANAMI, Toshio,KSANDER, Gary Michael,MOGI, Muneto,SUN, Robert
申请号:
ES10726924
公开号:
ES2582395T3
申请日:
2010.05.26
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of the formula (I '): ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: R 1 is C 1-7 alkyl; for each occurrence, R2 is independently C1-7 alkyl, NO2, CN, halo, C3-7 cycloalkyl, hydroxy, C1-7 alkoxy, C1-7 haloalkyl, NRbRc, C6-10 aryl, heteroaryl or heterocyclyl; wherein Rb and Rc for each occurrence, are independently H or C1-7 alkyl; R3 is A2-R4; R4 is C6-10 aryl or a heteroaryl, which may be monocyclic or bicyclic and which may be optionally substituted with one or more substituents independently selected from hydroxy, hydroxyC 1-7 alkyl, NRbRc, nitro, C1-7 alkoxy, halo, C1-7 alkyl, halo- C1-7 alkyl, C2-7 alkenyl, C6-10 aryl, heteroaryl, -C (O) C1-7 alkyl, -NHS (O) 2-C1-7 alkyl, - SO2 C1-alkyl 7 and benzyl; R5 is H, halo, hydroxy, C1-7 alkoxy, C1-7 alkyl or halo- C1-7 alkyl; and X is OH, -O-C1-7 alkyl, -NRbRc, -NHS (O) 2-C1-7 alkyl, -NHS (O) 2-benzyl or -O-C6-10 aryl; wherein alkyl is optionally substituted with one or more substituents independently selected from the group consisting of aryl, heteroaryl, heterocyclyl, -C (O) NH2, -C (O) NH- C1-6 alkyl, and C (O) N (alkyl C1-6) 2; A2 is a linear or branched C1-7 alkylene bond or bond which is optionally substituted with one or more substituents independently selected from the group consisting of halo, C1-7 alkoxy, hydroxy, O-acetate and C3-7 cycloalkyl; and n is 0, 1, 2, 3, 4 or 5; wherein each heteroaryl is a monocyclic or bicyclic aromatic ring comprising 5-10 atoms of the ring selected from carbon atoms and 1 to 5 heteroatoms, and each heterocyclyl is a saturated or partially saturated but non-aromatic monocyclic structural unit comprising 4- 7 ring atoms selected from carbon atoms and 1-5 heteroatoms, wherein each heteroatom of a heteroaryl or a heterocyclyl is independently selected from O, N and S.Un compuesto de la fórmula (I'):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: R1 es alquilo C1-7; para cada aparición, R2 es independientemente alquilo C1-7, N
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