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Novel glutaminyl cyclase inhibitors
专利权人:
PROBIODRUG AG
发明人:
THORMANN, MICHAEL,ALMSTETTER, MICHAEL,TREML, ANDREAS,HEISER, ULRICH,BUCHHOLZ, MIRKO
申请号:
ES07822341
公开号:
ES2481442T3
申请日:
2007.11.08
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula (I) ** Formula ** in which R 1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or 3-imidazol-1-yl-propyl; R2 represents alkyl, which may be optionally substituted with one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, -C (O) O-alkyl and -C (O) OH; carbocyclyl, which may be optionally substituted with one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C (O) O-alkyl and -C (O) OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; - alkyl carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl; heteroaryl; heterocyclyl; or R2 together with R4 can form a carbocyclyl group optionally substituted with one or more alkyl groups; R3 represents alkyl, which may be optionally substituted with one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, -C (O) OH and -C (O) O-alkyl; carbocyclyl, which may be optionally substituted with one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, -C (O) OH and -C (O) O-alkyl; alkenyl; -alkyl-aryl; -alkyl (aryl) 2, -alkyl (heteroaryl) 2, - alkyl (aryl) (heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl whose heterocyclyl group may be optionally substituted with one or more groups selected from alkyl, hydroxyl and oxo; -alkyl-carbocyclyl; -aryl-heteroaryl; - heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl; -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-Oalkyl-aryl; -C-alkyl (O) -NH-alkyl-aryl; -C-alkyl (O) -NH-alkyl-heteroaryl; -C-alkyl (O) -NH-alkyl-heterocyclyl; - alkyl-C (O) - (N-piperidinyl) or -alkyl-C (O) - (N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be condensed with optionally substituted phenyl; R4 represents H or alkyl; wherein said aryl, heteroaryl and imidazol-1-yl groups may be optionally substituted with one or more groups selected from
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