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Nitrovinyl diamine derivatives as glutaminyl cyclase inhibitors
专利权人:
PROBIODRUG AG
发明人:
BUCHHOLZ, MIRKO,HEISER, ULRICH,HAMANN, ANTJE
申请号:
ES08736360
公开号:
ES2468551T3
申请日:
2008.04.18
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
U compound of formula (I) ** Formula ** or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof: 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; C1-6 alkyl-C6-12 aryl; -C 1-6 alkyl-C5-12 heteroaryl; -phenyl condensed to C3-12 carbocyclyl or -phenyl condensed to C3-12 heterocyclyl; 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 aforementioned phenyl, C6-12 aryl and heteroaryl C5-12 groups may be optionally 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 alkenyl-C3 alkynyl -6-oxy-, -C (O) C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, nitro, halogen, cyano, hydroxyl, -C (O) OH, -NH2, -N C1-4alkyl , -N (C1-4 alkyl) (C1-4 alkyl), -C (O) N (C1-4 alkyl) (C1-4 alkyl), - C (O) NH2, -C (O) NH (alkyl C 1-4), -C (O) C 1-6 alkyl, -C 1-4 alkyl and -C 3-6 cycloalkyl; or R1 represents phenyl substituted with phenyl, or phenyl substituted with an optionally substituted 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 alkyl -4, halogen and C1-4 alkoxy; or R1 represents benzyloxy-substituted phenyl in which any of the 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 in which Y represents a C2-5 alkylene chain, which may be optionally substituted with one or two methyl groups or may be optionally su
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