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Thiourea derivatives as glutaminyl cyclase inhibitors
专利权人:
PROBIODRUG AG
发明人:
BUCHHOLZ, MIRKO,NIESTROJ, ANDRÉ J.,HEISER, ULRICH,SOMMER, ROBERT
申请号:
ES08736364
公开号:
ES2533484T3
申请日:
2008.04.18
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compound of formula (I) ** Formula ** or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: R1 represents C1-12 alkyl; C2-12 alkenyl, in which the double bond is not adjacent to nitrogen; C3-12 carbocyclyl; -C 1-6 alkyl-C3-12 carbocyclyl; C3-12 heterocyclyl; -C 1-6 alkyl-C 3-12 heterocyclyl; C6-12 aryl; C5-12 heteroaryl; -C 1-6 alkyl-C6-12 aryl; -C1-6 alkyl- (C6-12 aryl) 2; -C 1-6 alkyl-C5-12 heteroaryl; -C3-12 carbocyclyl condensed phenyl, -C1-6 alkyl- (C3-12 carbocyclyl condensed phenyl), -C3-12 heterocyclyl or phenyl-C1-6- alkyl (C3-12 heterocyclyl-fused phenyl); wherein any of the C3-12 carbocyclyl and C3-12 heterocyclyl groups mentioned above may be optionally substituted with one or more groups selected from methyl and oxo; and wherein any of the above-mentioned phenyl, C6-12 aryl and heteroaryl groups may optionally be substituted with one or more substituents selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1- haloalkyl 6, -C 1-6 thioalkyl, -SO 2 -C 1-4 alkyl, C 1-6 alkoxy, -O-C 3-8 cycloalkyl, C 3-8 cycloalkyl, -SO 2 -C 3-8 cycloalkyl, C 3-6 alkenyloxy, alkyloxy C3-6-, -C (O) -C 1-6 alkyl, C 1-6 alkoxy-C 1-6 alkyl-, nitro, halogen, cyano, hydroxyl, -C (O) OH, -NH2, -NH-C1-alkyl -4, -N (C1-4 alkyl) (C1-4 alkyl), -C (O) N (C1-4 alkyl) (C1-4 alkyl), -C (O) NH2, -C (O) NH (C1-4 alkyl), -C (O) O-C1-6 alkyl, -SO-C1-4 alkyl and -SO-C3-6 cycloalkyl; or R1 represents phenyl substituted with phenyl, or phenyl substituted with a monocyclic C5-12 heteroaryl group in which any of the aforementioned monocyclic C5-12 heteroaryl groups may be optionally substituted with one or more groups selected from C1-4 alkyl , halogen and C1-4 alkoxy; or R1 represents benzyloxy-substituted phenyl in which any of the aforementioned phenyl or benzyloxy groups may be optionally substituted on the ring with one or more groups selected from C1-4 alkyl, halogen and C1-4 alkoxy; and A represents ** Formula ** in
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