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Composed of 4 - amino - 2 - /, Pharmaceutical composition containing Said composition, Process for Preparation and use
专利权人:
GLAXOSMITHKLINE LLC
发明人:
申请号:
ARP120100455
公开号:
AR085163A1
申请日:
2012.02.10
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
We describe 4 - amino - 2 - butenamidas having pharmacological activity, Pharmaceutical compositions containing them, and Methods for the treatment of diseases mediated by the Enzyme cathepsin V.Claim 1: a compound according to formula (1) or a pharmaceutically acceptable Salt thereof, where: Each of R1 and R2 are independently selected from the group consisting of hydrogen, alkyl alquenilo C2 C1 - 8 - 8 - 8 alquinilo C2, C3, C5 cicloalquenilo cycloalkyl - 8 - 8 - 10 heterocicloalquilo cicloalquil bicicloalquilo C6 C3, C1 - alkyl - 8 6Cicloalquenil alkyl C1 - C5 - 8 - 6 - 6, heterocicloalquil C1 alkyl aryl, heteroaryl, aryl, alkyl heteroarilalquilo C1 and C1 - 6 - 6 - 8; where any Rent C1, C2 or C2 alquinilo alquenilo - 8 - 8 is optionally substituted by one to three times, independently, by CF3, ciano - CO2, c1-4 alkyl, - With c1-4 alkyl, alkyl - c1-4 alkyl c1-4 alkyl C1 - SO2 -, - 4, - so2nh c1-4 alkyl,- so2n - alkyl c1-4 alkyl c1-4 alkyl, amino, C1 - 4amino (c1-4 alkyl) (c1-4 alkyl) amino, hydroxyl or alkoxy c1-4; and where any Group cicloalquenilo bicicloalquilo cycloalkyl, optionally replaced, or heterocicloalquilo is one to three times, independently. By c1-4 alkyl, halo C1-4 alkyl, cyano -, CO2 - c1-4 alkyl, alkyl - with c1-4 alkyl, with c1-4 alkyl c1-4,- SO2 - c1-4 alkyl, alkyl - so2nh c1-4 alkyl - - so2n c1-4 alkyl c1-4 alkyl, amino, amino (c1-4 alkyl, c1-4) (c1-4 alkyl) amino, hydroxyl, c1-4 alkoxy alkyl, aryl or aryl - C1 4, where the rest of the aryl aryl - aryl or alkyl, optionally substituted C1 - 4 is one to three times, which Ntemente, halogen, - CF3, c1-4 alkyl,Hydroxyl or alkoxy c1-4; and where any group or aryl heteroaryl is optionally substituted one to three times, independently by Halogen, alkyl, cycloalkyl C1 - C3 - 6, 6, cicloalquenilo haloalquilo C1 - C5 - 6, 6 -, cyano -, CO2 - with c1-4 alkyl, alkyl - C1 4 - alkyl c1-4 alkyl C1-4 alkyl C1 - SO2 -, - 4, - so2nh c1-4 alkyl, - - so2n c1-4 alkyl c1-4 alkyl, amino,C1-4 alkyl amino (c1-4 alkyl (
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