359 results about "Carbapenem" patented technology

The present invention relates to a compound represented by formula (1) or a salt thereof:wherein R represents a group that is easily removable upon hydrolysis in vivo. This compound is usable in the production of prodrug-type carbapenem antibacterial agents for oral administration. The use of this compound in the process of production of the antibacterial agents can realize enhanced production efficiency and reduced production cost.

The invention relates to a method for synthesizing 1 beta methyl carbapenem antibiotic, comprising the following steps of: (1) adding an organic solvent, water, pivaloyloxymethyl ester, organic base and a catalyst to a reactor, introducing hydrogen, and then reacting for above 15 minutes, wherein the pressure of the hydrogen is controlled in 10.0 MPa, and the reaction temperature is controlled below 70 DEG C; (2) monitoring by using a HPLC (High Performance Liquid Chromatography), removing the hydrogen after finishing reaction, and filtering and recovering the catalyst (palladium charcoal or platinum charcoal); and (3) cooling a filtrate, adding a crystallizing solvent, stirring and devitrifying for above 10 minutes, and then filtering to obtain a corresponding target compound. The method has convenient operation, and a reaction liquid can be directly added to the solvent for crystallization without purification.

The invention relates to a gene chip for high-flux detection of pathogens and application thereof. The gene comprises (1) a combination of 174 oligonucleotide probes of pathogen variety specific genes, toxin genes and drug-resistant genes; and (2) a probe array, which is formed by curing the oligonucleotide probes on a carrier material by arm molecules. The gene chip comprises 174 gene probes, namely 32 pathogen variety specific gene probes of the following 8 pathogens of Burkholderia mallei, Burkholderia pseudomallei, Brucella, salmonella, Yersinia pestis, Bacillus anthracis, comma bacillus and the like, 25 toxin gene probe of the following 7 toxins of diphtheria toxin, Shiga toxin, staphylococcus enterotoxin, choleratoxin and the like, and 117 drug-resistant gene probes of 17 drug-resistant genes of extended-spectrum beta-lactamase, cephalosporinase, carbapenemase, integrase gene, common gene engineering carrier drug-resistant gene and the like. The gene chip can be used to detect multiple pathogen variety specific genes, toxin genes and drug-resistant genes.

The invention provides a structural general formula (shown in the description) of a fluorescent probe for carbapenem type antibiotic bacteria. In the structural general formula, X represents carbon atoms or sulfur atoms; when the X represents CH, R1 represents methyl and can be of the configuration S or R, or the X represents CH2 or S; Y represents oxygen atoms, sulfur atoms or linkers on a fluorophorearomatic nucleus and comprises 4-hydroxymethylbenzyl or 4-hydroxyl or sulfydrylbenzyl or carbamate linkers. The synthesis method of the fluorescent probe comprises the following steps that 1, a compound 2 is prepared; 2, intermediates 3 and 4 are prepared; 3, a compound 5 is prepared; 4, a compound 6 is prepared; 5, a compound 7 is prepared; 6, a compound 8 is prepared; 7, a compound 9 is prepared; 8, a compound 10 is prepared;9, a compound CPC-1, namely a fluorescent probe compound is prepared. The fluorescent probe can be applied to detection of carbapenemases and drug-resistant bacteria containing the carbapenemases and has the important significance on antibiotic abandoning or few antibiotics adopted in medical treatment.

Provided herein are cell-free systems for generating carbapenems, e.g., a compound of the Formula (I):or salts thereof; wherein , R1, R2, R3, R4, R5, and R6 are defined herein. Also provided are pharmaceutical compositions comprising a compound generated by the inventive cell-free system, and use of these compounds and compositions for the treatment of bacterial infections.

An isolated strain of Enterococcus faecalis GALT deposited under number C E C T 7121 of the group of lactic bacteria is disclosed, which is capable of surviving and colonizing the gastrointestinal tract of humans and / or animals and showing beneficial probiotic activity for the health of humans and animals. The strain E. faecalis GALT and / or a culture supernatant and / or metabolites thereof shows no in vitro multiresistance to antibiotics of common use in human clinics as glycopeptides, such as vancomycin, teicoplanine; carbapenemes, such as impipenem, meropenem; and ampicillin. The strain E. faecalis GALT contains no red blood cell-destroying hemolysins of human, ovine and equine origin; and it does not produce any gelatinase, DNase and decarboxylases. The strain E. faecalis GALT is useful for the preparation of a composition intended for the treatment and / or prophylaxis of disorders associated with colonization by pathogenic microorganisms of the gastrointestinal tract; for use as a regulator of the immune response in human and animals, as well as for the preparation of a composition. The invention is also directed to methods and uses of the strain E. faecalis GALT.

The present invention provides carbapenem hydrochloride trihydrate crystals, which are chemically stable, easily purified and useful as antimicrobial agents, a process for producing them, and a powdery charged preparation for injection containing them. That is, it provides carbapenem hydrochloride trihydrate crystals having a powdery X-ray diffraction pattern containing lattice distances (d) of 9.0, 4.1 and 2.8 Å, a process for producing them, and a powdery charged preparation for injection containing them.

This invention provides Cephem compounds having the formula:or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof, a pharmaceutical composition thereof, and a method for treating a bacterial infectious disease with the compound, the ester, the protected compound, the salt, or the solvate thereof, wherein the symbols in the formula are defined in the specification. The compounds exhibit potent antimicrobial spectrum against a variety of bacteria including Gram negative bacteria and / or Gram positive bacteria, preferably beta-lactamase producing Gram negative bacteria, more preferably, multi-drug resistant microbials, in particular, Class B type metallo-beta-lactamase producing Gram negative bacteria, and still preferably extended-spectrum beta-lactamase (ESBL) producing bacteria. The compounds most preferably do not exhibit cross-resistance against known Cephem drugs or Carbapenem drugs.

Compositions and methods for the rapid and sensitive detection of a carbapenemase in a sample is provided. The compositions include novel primer and probe compositions for use in detecting the presence of this enzyme in a sample, particularly using PCR methods. These primers and probe sets can be used in amplification methods (such as PCR, particularly quantitative PCR) and packaged into kits for use in amplification methods for the purpose of detecting carbapenemase in a test sample, particularly a patient sample, particularly a direct sample. Thus, in one embodiment, the present invention provides for novel oligonucleotide primers set forth in SEQ ID NOs:1, 2, 4, 5, 7, 8, 14, 15, 17, 18, and 20, and the novel oligonucleotide probe sequences set forth in SEQ ID NOs:3, 6, 9, 16, and 19. These sequences can be used in a method of detecting carbapenemase in a sample.

The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of 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. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

The invention relates to a rapid identification method for carbapenem drug susceptibility, based on a Raman spectra technology. According to the method, a portable Raman detector is adopted, pathogenic bacteria to be detected is irradiated through laser, different types of nanostructures are taken as detection substrates, and scattered spectrum, the frequency of which is different from the frequency of incident light, is analyzed, so that information, such as molecular vibration, of a sample to be detected is obtained, corresponding molecular structure analysis is performed, obtained spectroscopic data of carbapenem drug sensitive bacteria and drug-resistance bacteria is analyzed through a chemometrics method, so that drug-resistance bacteria and sensitive bacteria are distinguished, and the method becomes an ultrasensitive pathogenic bacteria rapid detection tool. Compared with the clinically traditional drug sensitivity pathogenic microorganism detection method, the detection technology has the advantages that the quantity of samples is less, the detection time is short, the sensitivity is high, the detection time of clinical samples is shortened, and particularly as for detection samples with complex chemical and biochemical components, the detection efficiency is improved on the basis that the detection quality is guaranteed.

An isolated strain of Enterococcus faecalis GALT deposited under number CECT 7121 of the group of lactic bacteria is disclosed, which is capable of surviving and colonizing the gastrointestinal tract of humans and / or animals and showing beneficial probiotic activity for the health of humans and animals. The strain E. faecalis GALT and / or a culture supernatant and / or metabolites thereof shows no in vitro multiresistance to antibiotics of common use in human clinics as glycopeptides, such as vancomycin, teicoplanine; carbapenemes, such as impipenem, meropenem; and ampicillin. The strain E. faecalis GALT contains no red blood cell-destroying hemolysins of human, ovine and equine origin; and it does not produce any gelatinase, DNase and decarboxylases.The strain E. faecalis GALT is useful for the preparation of a composition intended for the treatment and / or prophylaxis of disorders associated with colonization by pathogenic microorganisms of the gastrointestinal tract; for use as a regulator of the immune response in human and animals, as well as for the preparation of a composition.The invention is also directed to methods and uses of the strain E. faecalis GALT.

The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum β-lactamase inhibitor.

A compound or its pharmaceutically acceptable salt represented by the following formula:The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing β-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as β-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.