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Title:
ベータ-ラクタマーゼの新規阻害剤
Document Type and Number:
Japanese Patent JP5562634
Kind Code:
B2
Abstract:
This invention provides novel beta-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of beta-lactamases and synergize the antibacterial effects of beta-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the beta-lactam antibiotics as a result of the presence of the beta-lactamases.

Inventors:
Frank Dinino
Hammond, Milton El
Kevin, Dixtra
Kim, songkon
Tan, Chang
Young, Catherine
Jeffrey Donald, Hermes
Chen, Helen
Laepel, Stephan
Manion, michael
Gaudette, Frederick
Bysburg, Arkadi
Rahl, Jubilee
Georgo Papadakou, Nafsika
Nancy Zed
Application Number:
JP2009512059A
Publication Date:
July 30, 2014
Filing Date:
May 21, 2007
Export Citation:
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Assignee:
Methyl Gene Incorporated
International Classes:
C07F9/6539; A61K31/67; A61K31/675; A61P31/04; A61P43/00; C07F9/6541; C07F9/6553; C07F9/6558; C07F9/6561
Domestic Patent References:
JP2002520418A
JP2002509934A
JP2002503643A
JP49087633A
JP2003503505A
JP2009538302A
Foreign References:
WO2004048393A2
Other References:
LI,N. et al.,Structure-activity studies of the inhibition of serine β-lactamases by phosphonate monoesters,Bioorganic & Medicinal Chemistry,1997年,Vol.5, No.9,p.1783-1788
DRYJANSKI,M. and PRATT,R.F.,Inactivation of the enterobacter cloacae P99 β-lactamase by a fluorescent phosphonate: Direct detection of ligand binding at the second site,Biochemistry,1995年,Vol.34,p.3569-3575
Attorney, Agent or Firm:
Fukami patent office