C07D477/14

METHOD AND DEVICE FOR THE DETECTION OF CARBAPENEMASES AND CARBAPENEMASE PRODUCERS
20200248226 · 2020-08-06 ·

The invention refers to a method and a device for the phenotypic detection of carbapenemases and carbapenemase producers by adding a substrate of general formula A-(L)-M.sub.1-(X)Z, where M.sub.1 is a carbapenem backbone, A or Z is a quencher, the other one of the two, Z or A, is a fluorophore, L is an optional linker, X is an optional leaving group for linking Z to the carbapenem backbone, and Z is an optional leaving group, to a sample suspected of containing such carbapenemase producers and/or carbapenenmases. The invention further refers to a method for the phenotypic detection of resistant bacteria, in particular 3MRGN or 4MRGN, by releasing the enzymes of a bacterial culture into a lysate during lysis and then subjecting the lysate, as the sample to be analyzed, to an aforementioned method in order to phenotypically detect the presence of resistance-conferring carbapenemases.

METHOD AND DEVICE FOR THE DETECTION OF CARBAPENEMASES AND CARBAPENEMASE PRODUCERS
20200248226 · 2020-08-06 ·

The invention refers to a method and a device for the phenotypic detection of carbapenemases and carbapenemase producers by adding a substrate of general formula A-(L)-M.sub.1-(X)Z, where M.sub.1 is a carbapenem backbone, A or Z is a quencher, the other one of the two, Z or A, is a fluorophore, L is an optional linker, X is an optional leaving group for linking Z to the carbapenem backbone, and Z is an optional leaving group, to a sample suspected of containing such carbapenemase producers and/or carbapenenmases. The invention further refers to a method for the phenotypic detection of resistant bacteria, in particular 3MRGN or 4MRGN, by releasing the enzymes of a bacterial culture into a lysate during lysis and then subjecting the lysate, as the sample to be analyzed, to an aforementioned method in order to phenotypically detect the presence of resistance-conferring carbapenemases.

Carbapenem Compounds and Compositions for the Treatment of Bacterial Infections

The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

Carbapenem Compounds and Compositions for the Treatment of Bacterial Infections

The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

Methods of generating beta-lactamase resistant carbapenem compounds
10519161 · 2019-12-31 · ·

The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1-C1 di-substituted carbapenem compounds, C5 substituted carbapenem compounds, C6-C6 di-substituted carbapenem compounds and combinations thereof.

FLUOROGENIC ASSAY FOR RAPID SCREENING OF BACTERIAL BETA-LACTAMASE ACTIVITY
20240240226 · 2024-07-18 ·

A dual-caged fluorogenic resorufin probe (CDA) has been developed that is stable under physiological condition with low background but becomes highly fluorescent upon ?-lactamase/esterase activation and further oxidation. The probes of the disclosure are advantageous for initial screening of broad-spectrum ?-lactam antibiotics resistance and carbapenem resistant pathogens at diagnosis. After a two-step filtration, the assay of the disclosure can report 10.sup.3 c.f.u./mL cephalosporin- and carbapenem-resistant bacteria in urine within 2 hours at room temperature.

FLUOROGENIC ASSAY FOR RAPID SCREENING OF BACTERIAL BETA-LACTAMASE ACTIVITY
20240240226 · 2024-07-18 ·

A dual-caged fluorogenic resorufin probe (CDA) has been developed that is stable under physiological condition with low background but becomes highly fluorescent upon ?-lactamase/esterase activation and further oxidation. The probes of the disclosure are advantageous for initial screening of broad-spectrum ?-lactam antibiotics resistance and carbapenem resistant pathogens at diagnosis. After a two-step filtration, the assay of the disclosure can report 10.sup.3 c.f.u./mL cephalosporin- and carbapenem-resistant bacteria in urine within 2 hours at room temperature.

BIOLUMINOGENIC ASSAY FOR DRUG-RESISTANCE BACTERIA DETECTION
20240229098 · 2024-07-11 ·

Caged luciferin-based probes become a luciferase substrate emitting bioluminescence upon ?-lactamase/esterase activation. The inclusion of a cephalosporin moiety renders the probe capable of being used for the detection of a wide-range of ?-lactamases and ?-lactamase-expressing bacteria. Embodiments of a rapid high-throughput assay for the identification of ?-lactamase-expressing bacteria is made possible by the use of such probes. In some embodiments the cephalosporin is substituted by a carbapenem moiety to generate carbapenem-caged luciferin carbapenem-cleavable probes capable of being used for the detection of a wide-range of carbapenem-expressing bacteria. Accordingly embodiments of a rapid high-throughput assay for the identification of carbapenem-expressing bacteria is made possible by the use of these probes.

Fluorescent carbapenems
09969737 · 2018-05-15 · ·

Chromogenic or fluorescent carbapenems according to formula I, wherein Ar is a mono or disubstituted carbocyclic aromatic group or an optionally mono or disubstituted heterocyclic aromatic group, are useful compounds for the detection of bacterial carbapenemase. ##STR00001##

Fluorescent carbapenems
09969737 · 2018-05-15 · ·

Chromogenic or fluorescent carbapenems according to formula I, wherein Ar is a mono or disubstituted carbocyclic aromatic group or an optionally mono or disubstituted heterocyclic aromatic group, are useful compounds for the detection of bacterial carbapenemase. ##STR00001##