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Title:
セリンおよびメタロ-β-ラクタマーゼの阻害剤
Document Type and Number:
Japanese Patent JP2005525399
Kind Code:
A
Abstract:
Compounds of formula (I): wherein R1, R2, R3, R4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting simultaneously serine and metallo-beta-lactamase enzymes, for enhancing the activity of beta-lactam antibiotics, and for treating beta-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

Inventors:
John Di Binac
Chen Hanson
Application Number:
JP2003584061A
Publication Date:
August 25, 2005
Filing Date:
April 04, 2003
Export Citation:
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Assignee:
ALAMX,L.L.C.
International Classes:
A61K31/43; A61K31/431; A61P31/04; A61P43/00; C07D499/00; C07D499/04; C07D499/897; C07D501/14; C07D499/861; (IPC1-7): C07D499/86; A61K31/43; A61K31/431; A61P31/04; A61P43/00; C07D499/04; C07D499/861
Domestic Patent References:
JPS6143115A1986-03-01
JPS55129289A1980-10-06
JPH08505645A1996-06-18
JPS5340795A1978-04-13
JPS56123985A1981-09-29
JPS6431786A1989-02-02
Other References:
ADAM,S.: "Synthesis of methylene (R)-6-acetonylidene-3-methyl-7-oxo-4-thia-1- azabicyclo[3.2.0]hept-2-ene-carb", HETEROCYCLES, vol. 22, no. 7, JPN6009058534, 1984, pages 1509 - 12, XP009127357, ISSN: 0001464397, DOI: 10.3987/R-1984-07-1509
MAK,C.P. ET AL: "Chemical studies on the transformation of penicillins. I: Synthesis of cyclic disulfides and thiosu", HETEROCYCLES, vol. 27, no. 2, JPN6009058532, 1988, pages 331 - 7, ISSN: 0001464398
BITHA,PANAYOTA ET AL: "6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C β-lactamases I", BIOORGANIC & MADICINAL CHEMISTRY LETTERS, vol. 9, no. 7, JPN5004013908, 1999, pages 991 - 996, ISSN: 0001464399
BITHA,PANAYOTA ET AL: "6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C β-lactamases II", BIOORGANIC & MADICINAL CHEMISTRY LETTERS, vol. 9, no. 7, JPN5004013909, 1999, pages 997 - 1002, ISSN: 0001464400
Attorney, Agent or Firm:
Mitsuo Tanaka
Masaki Yano