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METALLO-β-LACTAMASE INHIBITORS
专利权人:
MEJDZI SEJKA KAJSJA; LTD.
发明人:
TIKAUTI Ken (JP),ТИКАУТИ Кен (JP),IDA Mizujo (JP),ИДА Мизуйо (JP),ABE Takao (JP),АБЕ Такао (JP),KhIRAJVA Jukiko (JP),ХИРАЙВА Юкико (JP),MORINAKA Akikhiro (JP),МОРИНАКА Акихиро (JP),KUDO Tosiaki (JP),К,TIKAUTI KEN,IDA MIZUJO,ABE TAKAO,KHIRAJVA JUKIKO,MORINAKA AKIKHIRO,KUDO TOSIAKI,КУДО Тосиаки (JP)
申请号:
RU2008115512/04
公开号:
RU0002462450C2
申请日:
2006.09.22
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: maleic acid derivatives having general formulahave metallo-β-lactamase inhibiting activities. It is possible to recover anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of general formula (I) with β-lactam antibiotics. The metallo-β-lactamase inhibitor is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 denotes C2-6-alkyl; C3-7-cycloalkyl, where said cycle can be substituted with a hydroxyl group or can be condensed with an aryl; hydroxymethyl; - C1-3-alkylene phenyl, where said phenyl group can be substituted with a hydroxyl group, C1-6-alkyl group, hydroxymethyl group, a -COOM group, where M denotes a hydrogen atom or a pharmaceutically acceptable cation, a -CO-NR22R23 group, where R22 and R23, which can be identical or different, denote a hydrogen atom or C1-6-alkyl, wherein the alkyl can additionally be substituted with an aminocarbonyl, or R22 and R23, together with a nitrogen atom with which they are bonded, can form a five- or six-member saturated heterocyclic ring containing 1-2 oxygen or nitrogen atoms, and the heterocycle can be substituted with a hydroxyl group or a C1-6-alkanoyloxy group, a -O-R24 group, where R24 denotes C1-6-alkyl, wherein the alkyl is optionally substituted with an aminocarbonyl, an amine group, a guanidine group or a five- or six-member saturated heterocycle, having 1-2 nitrogen atoms, -COOM, where M denotes a hydrogen atom, C1-6-alkyl or a pharmaceutically acceptable cation, or a five- or six-member unsaturated heterocycle, having 1-2 nitrogen atoms; - C0-1 alkylene heterocycle, where said heterocycle is a five- or six-member saturated or unsaturated heterocycle containing one nitrogen or oxygen atom and can be substituted with a hydroxyl group; - O-C1-6-alkyl; or - S-C1-6-alkyl, R2 denotes C1-6-alkyl, C3-7-cycloalkyl, where said cycle can be substituted with a hydroxyl group or can be condensed wi
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