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PIRAZOLOPIRROLIDINOS AS GAMMA SECRETASA INHIBITORS.
专利权人:
ELAN PHARMACEUTICALS INC.
发明人:
DRESSEN, DARREN,BOWERS, SIMEON,GAROFALO, ALBERT,HOM, ROY,MATTSON, MATTHEW
申请号:
ES08756023
公开号:
ES2373253T3
申请日:
2008.05.21
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
Compounds of formula Formula I, stereoisomers, tautomers, mixtures of stereoisomers and / or tautomers or their salts acceptable for pharmaceutical use, where A is a C1-C6 alkyl or aryl group, cycloalkyl, heteroaryl or C3-C6 heterocyclyl, where each ring can be substituted in a substitutable position with one or more halogens, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, hydroxyl, hydroxyalkyl, CN, aryloxy, arylalkyl, -SO2- (C1-C6 alkyl), - NR'R ", C1-C6 alkanoyl, C0-C3-C (O) OR 'alkyl, heteroaryl, heterocyclyl, aryl, arylalkyl or -SO2-NR'R" and where A is a C1-C6 alkyl, the C1-C6 alkyl group may be substituted in a position substitutable by one or more halogens, C2-C6 alkenyl, C2-C6 alkynyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C6 haloalkoxy, hydroxyl, hydroxyalkyl, CN, aryloxy, arylalkyloxy, -SO2- (C1-C6 alkyl), -NR'R ", C1-C6 alkanoyl, C0-C3-C alkyl (O) OR ', heter oaryl, heterocyclyl, aryl, arylalkyl or -SO2-NR'R ", R1, R1a, R2 and R2a are independently: hydrogen, alkyl, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloalkyl-C1-C6 alkyl, C1-C6 haloalkyl, aryl, aryl C1-C6 alkyl, heteroaryl, heterocyclyl, -C (O) OR ', -CONR'R ", C1-C4 haloalkoxyalkyl, C1- hydroxy alkyl C6, C1-C6 alkoxy, C2-C6 alkanoyl, C1-C6 aryloxy, C1-C6 alkyl heteroaryloxy, -C0-C6-OC alkyl (O) NR'R ", - C0-C6-NR'R alkyl", hydroxyl, CN or -C0-C6-OC (O) -heterocyclyl group, where each aryl, heteroaryl and heterocyclyl group may be substituted with one or more groups which can be independently halogen, C1-C6 alkyl, C1-C6 alkoxy, alkanoyl C1-C6, halo C1-C4 alkyl, halo C1-C4 alkoxy, -C (O) -NR'R ", -NR'R", hydroxyl, CN or -C (O) OR '; or R1 and R1a or R2 and R2a together with the carbon to which they are attached form the C3-C6 cycloalkyl group in which one of the carbons can be replaced by a heteroatom such as N, O or S and where said ring can be substituted by a C1-C6 alkyl; or R1 and R1a or R2 and R2a together wi
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