Coppola, Gary Mark,Iwaki, Yuki,Karki, Rajeshri Ganesh,Kawanami, Toshio,Ksander, Gary Michael,Mogi, Muneto,Sun, Robert
申请号：
ES13151792
公开号：
ES2602826T3
申请日:
2010.05.26
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
Compound of formula I ': or a pharmaceutically acceptable salt thereof, wherein: R 1 is H, C 1-7 alkyl, hydroxyl, C 1-7 alkoxy, halogen, -SH, -S-C 1-7 alkyl or NRaRb； R2 for each occurrence, is independently C1-7 alkyl, halo, NO2, CN, C1-7 alkanoylamino, C3-7 cycloalkyl, hydroxyl, C1-7 alkoxy, C1-7 haloalkyl, -NRaRb, C6-10 aryl, heteroaryl or heterocyclyl； in which Ra and Rb for each occurrence are independently H or C1-7 alkyl； R3 is A1-C (O) X1； R5 is H, halo, hydroxyl, C1-7 alkoxy, halo, C1-7 alkyl or halo- C1-7 alkyl； and X and X1 are independently OH, -O-C1-7 alkyl, -NRaRb, -NHS (O) 2-C1-7 alkyl, -NHS (O) 2-benzyl or -O-C6-10 aryl； wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C6-10 aryl, heteroaryl, heterocyclyl, C (O) NH2, C (O) NH-C1-6 alkyl and C (O) N (C1-6 alkyl) 2； B1 is -C (O) NH- or -NHC (O) -； A1 is a link； or A1 is a phenyl or a heteroaryl； each of which is optionally substituted with one or more substituents independently selected from the group consisting of C1-7 alkyl, C3-7 cycloalkyl, halo- C1-7 alkyl, hydroxyl, C1-7 alkoxy, halo, -NRaRb, - OCH2CO2H and -OCH2C (O) NH2； or A1 is a C3-7 cycloalkyl； A1 is -C 1-4 alkylene-C 6-10 aryl, -C 1-4 alkylene-heteroaryl- or -C 1-4 alkylene-heterocyclyl-, in which A1 may be in any direction； and n is 0, 1, 2, 3, 4 or 5； wherein each heteroaryl is a monocyclic or bicyclic aromatic ring comprising 5-10 ring atoms selected from carbon atoms and from 1 to 5 heteroatoms, and each heterocyclyl is a saturated or partially saturated but non-aromatic monocyclic moiety 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.Compuesto de fórmula I': o una sal farmacéuticamente aceptable del mismo, en la que: R1 es H, alquilo C1-7, hidroxilo, alcoxilo C1-7, halógeno, -SH, -S-alquilo C1-7 o NRaRb； R2 para cada aparición, es inde
