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93 results about "Carbapenem Antibiotics" patented technology

Carbapenems are a subclass of antibiotics called beta-lactam antibiotics (antibiotics that have a chemical structure called a beta-lactam ring). Beta-lactam antibiotics also include cephalosporins, monobactams, and penicillins. Carbapenems are broad-spectrum antibiotics.

An improved process for the preparation of carbapenem antibiotic

InactiveUS20090312539A1Speed ​​up the processSimple, commercially viable, and industrially scalableOrganic chemistryBulk chemical productionHydrogenAntibiotic Y
The present invention provides a process for the preparation of the carbapenem antibiotic of formula (I) or its salt in amorphous form. Formula (I) wherein R represents hydrogen or COOM and M represents hydrogen or sodium.
Owner:ORCHID CHEM & PHARM LTD

Carbapenem antibiotic resistant bacterium fluorescent probe and synthesis method and application thereof

The invention discloses a carbapenem antibiotic resistant bacterium fluorescent probe. In a structural formula as shown in the specification, X refers to carbon atoms or sulfur atoms; when X is CH, R1 is methyl and can be R or S configuration, or X is CH2 or S; a dye is any one of boron-dipyrromethene, naphthalimides, coumarin, fluorescein or rhodamine. A synthesis method of the fluorescent probe includes steps: (1) preparation of a compound 3; (2) preparation of a compound 4; (3) preparation of a fluorescent probe CVB-1. The fluorescent probe can be made into test paper, kits or detection chips to be applied to detection of carbapenemases and carbapenem drug-resistant bacteria, detection or distinguishing of carbapenemases is realized by determining whether fluorescence intensity or color of the fluorescent probe changes or not, and accordingly pathogenic drug-resistant bacteria with expression of carbapenemases can be detected quickly, reasonable utilization of antibiotics in treatment or clinical application can be guided, and important significance to avoidance or low consumption of antibiotics is achieved.
Owner:EAST CHINA UNIV OF SCI & TECH

Primer, probe, method and kit for detecting KPC (Klebsiella Pneumoniae Carbapenemases) antibiotic gene

The invention relates to the technical field of molecular biology, and discloses a primer, a probe, a method and a kit for detecting a KPC (Klebsiella Pneumoniae Carbapenemases) antibiotic gene. Primers and fluorescent labeled probes are respectively designed aiming at a conservative region of a phoE gene, a KPC gene and an interior standard (int) gene by adopting a Taqman probe real-time fluorescence PCR (Polymerase Chain Reaction) method; the 5' ends of phoE gene probes and KPC gene probes are all labeled by a fluorescent report group FAM, and 3' ends are labeled by a fluorescent quenching group TAMRA; the 5' ends of int genes are labeled by a fluorescent report group JOE, and the 3' ends are labeled by a fluorescent quenching group BHQ1. After the primer and the probe are prepared into a PCR detection mixed solution, enzyme and sample nucleic acid are added, an FAM channel on a fluorescent PCR instrument is selected to amplify the phoE gene and the KPC gene, a JOE channel is selected to amplify the int gene, and detection on a target gene is realized through change of a fluorescent signal. The primer, the probe, the method and the kit, disclosed by the invention, have the characteristics of high accuracy, strong specificity ad high sensitivity, and KPN (Klebsiella Pneumoniae) and KPC in sputum and a throat swab sample can be rapidly and accurately detected.
Owner:宁波基内生物技术有限公司 +1

Preparation and application of DNA (deoxyribonucleic acid) chip for carbapenem antibiotic drug-resistant gene detection

The invention relates to preparation and application of a DNA (deoxyribonucleic acid) chip for carbapenem antibiotic drug-resistant gene detection. The preparation method comprises the following steps: preparing nine carbapenem drug-resistant gene specific primers, preparing nine carbapenem antibiotic drug-resistant gene specific probes, preparing an oligonucleotide chip, establishing a multiplex PCR (polymerase chain reaction) system, and establishing a hybrid system. The gene chip can simultaneously detect nine common carbapenem drug-resistant genes, including KPC, NDM-1, OXA-23, OXA-48, OXA-51, IMP, VIM, SIM and DIM. The DNA chip has the advantages of high speed, high accuracy, high flux and high specificity, and can provide a new detection means for drug-resistant gene confirmation and molecular epidemiological survey of carbapenem antibiotic drug-resistant phenotypes.
Owner:INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA

Intermediate of carbapenem antibiotics and process for the preparation thereof

There is disclosed an azetidinone compound of the formula (I): wherein R is hydrogen, or a hydroxy protecting group, R1 and R2 are each independently alkyl of 1-15 carbon atoms, benzyl or cyclized together with the carbon atom to which they are attached to form a 5 or 6-membered cyclic hydrocarbon or a heterocyclic radical having one or two hetero ring atoms, said hetero ring atoms being selected from the group consisting of O and S; R3 is lower alkyl or —COO(lower alkyl) R4 is phenyl, or phenyl substituted with halogen, lower alkoxy or nitro which is useful as a synthetic intermediate to the 1′β-methylcarbapenem-type antibacterial agent.
Owner:DONG WHA PHARM CO LTD +1

Prepn of carbapenum type antibiotic Faropenum sodium

The present invention provides Faropenum sodium preparing process, and the preparation process has short reaction path, no use of strong stimulating substance sulfhydryl compound and chlorosulfoxide, mild reaction condition, no need of purifying intermediate product and simple operation and is suitable for industrial production.
Owner:SHANGHAI NEW ASIA PHARMA

LAMP primer combination for detecting seven types of drug-resistant genes resisting carbapenem antibiotics and application of LAMP primer combination

The invention discloses an LAMP primer combination for detecting seven types of drug-resistant genes resisting carbapenem antibiotics and application of the LAMP primer combination. The invention first provides a primer combination consisting of 42 types of DNA molecules as shown in sequences 1-42. The primer combinations can be applied to detect whether a to-be-tested bacterium or sample contains a drug-resistant gene OXA-23 and / or a drug-resistant gene OXA-24 and / or a drug-resistant gene OXA-58 and / or a drug-resistant gene OXA-66 and / or a drug-resistant gene KPC-2 and / or a drug-resistant gene IMP-4 and / or a drug-resistant gene VIM-2. The primer combination provided by the invention is identified to be used for detecting the seven types of drug-resistant genes resisting carbapenem antibiotics, has high specificity and high sensitivity, and can implement simple, convenient, quick and accurate detection. The LAMP primer combination provided by the invention has a significant promotion value.
Owner:CAPITALBIO CORP

Detection method for antibiotic resistance genes

The invention provides a detection method for antibiotic resistance genes. The method can simultaneously detect the presence or level of multiple antibiotic resistance genes (such as KPC and other genes capable of causing bacterial drug resistance to carbapenem antibiotics, CTX-M and other genes capable of causing drug resistance to beta-lactam antibiotics, AAC and other genes capable of causing drug resistance to cephalosporin antibiotics, and drug resistance genes capable of causing bacterial drug resistance to other types of antibiotics) in nucleic acid molecules in samples. A probe set anda kit including the probe set of one or more kinds are also provided. The probe set and kit can be used for implementing the method. In addition, the kit is also provided; the kit can simultaneouslydetect the presence or level of the multiple antibiotic resistance genes (such as KPC and other genes capable of causing bacterial drug resistance to carbapenem antibiotics, CTX-M and other genes capable of causing drug resistance to beta-lactam antibiotics, AAC and other genes capable of causing drug resistance to cephalosporin antibiotics and the drug resistance genes capable of causing bacterial drug resistance to other types of antibiotics) in the nucleic acid molecules in the samples in a round of reaction.
Owner:XIAMEN UNIV

Synthetic method for penem and carbapenem antibiotic type key intermediate 4AA

The invention relates to a synthetic method for a penem and carbapenem antibiotic type key intermediate 4AA, belonging to the technical field of medicine. The method comprises the following steps of: reacting L-threonine with sodium nitrite-hydrochloric acid to generate a diazo compound; performing an internal nucleophilic substitution reaction on the diazo compound under the action of sodium hydroxide; acidifying to obtain epoxy sodium butanoate; acidifying to obtain epoxy butyrate; reacting the epoxy butyrate with p-methoxyanilinoethyl acetate to obtain a condensation product; generating a quaternary ring compound from the condensation product under the actions of hexamethyldisilazane and lithium amide; and performing hydroxy protection, hydrolysis, oxidative decarboxylation and ozonization deprotection on the ring compound to obtain 4AA. The process has the advantages of readily-available raw material, mild reaction conditions, short reaction time, low pollution, high yield and the like, and is suitable for industrial production.
Owner:CHINA THREE GORGES UNIV

Culture medium and preparation method for selective separation culture extensively drug-resistant pseudomonas aeruginosa

The invention discloses a culture medium and a preparation method for selective separation culture extensively drug-resistant pseudomonas aeruginosa. Culture supernatant fluid and an antibiotic combination for pseudomonas aeruginosa in a logarithmic phase are added into an NAC basal culture medium. The culture supernatant fluid contains quorum sensing substances secreted by pseudomonas aeruginosa, the quorum sensing substances can accelerate growth of bacteria and promote secretion of aeruginosa pigments, and the detection time is greatly shortened. The antibiotic combination comprises carbapenems antibiotics, aminoglycoside antibiotics and quinolone antibiotics, the additive amount of the carbapenems antibiotics is 0.016 g / L, the additive amount of the aminoglycoside antibiotics is 0.016 g / L, and the additive amount of the quinolone antibiotics is 0.016 g / L, the antibiotic combination can specifically inhibit growth of sensitive pseudomonas aeruginosa strains and growth of single-drug resistant pseudomonas aeruginosa strains, the purpose of selective separation culture of extensively drug-resistant pseudomonas aeruginosa is achieved, and specificity and sensitivity are high. Moreover, the culture medium can be stored for a long time and can be effectively applied to quick detection of extensively drug-resistant pseudomonas aeruginosa in clinical samples.
Owner:广东和信健康科技有限公司

Bactericidal Anti-mrsa active pharmaceutical composition containing carbapenems

InactiveUS20100173887A1Antibacterial agentsBiocideBacteroidesBacteria aspects
Pharmaceutical compositions containing a carbapenem of the structural formula Iand epicillin are strongly bactericidal against MRSA and MRSE. Equivalently, compositions of conventional carbapenem antibiotics and epicillin are highly synergistic in eradicating said bacteria.
Owner:PFAENDLER HANS RUDOLF

Lactobacillus casei and composition thereof

The invention discloses lactobacillus casei and a composition thereof and belongs to the technical field of microbial applications. The lactobacillus casei provided by the invention has a collection number of CGMCC No.4520 and is collected in the China General Microbiological Culture Collection Center in Beijing on 29 in December in 2010. The lactobacillus casei provided by the invention has a synergistic growth effect with bifidobacterium animalis, enterococcus faecalis and bacillus cereus, has tolerance on glycopeptides, monocyclic ring beta-lactam and carbapenem antibiotics and sulfonamide and is applied to foods, medicines and / or health products.
Owner:HANGZHOU GRAND BIOLOGIC PHARMA INC

Antibiotic combination containing Avibactam and application of antibiotic combination

The invention belongs to the technical field of medicines, relates to an antibiotic combination containing Avibactam and an application of the antibiotic combination, provides an application of Avibactam or pharmaceutically acceptable salt and carbapenems antibiotics to preparation of medicines for treating or preventing bacterial infection, particularly an application of the Avibactam to preparation of medicines for treating infection caused by escherichia coli, pseudomonas aeruginosa, klebsiella pneumoniae, baumanii and enterobacter aerogenes so as to solve the problem of drug resistance of the carbapenems antibiotics.
Owner:CHIA TAI TIANQING PHARMA GRP CO LTD

Preparation of carbapenem antibiotic side chain

The invention discloses a method for preparing side chains of carbapenems antibiotics, comprising the following steps: A) L-hydroxyproline (ii) reacts with 4-nitrobenzyl chloroformate and then is separated and crystallized to obtain a compound (iii); B) the compound (iii) reacts with diphenylphosphinyl chloride to obtain a compound (iv); the compound (iv) reacts with methanesulfonyl chloride to obtain a compound (v); the compound (v) reacts with sodium sulfide nonahydrate and is heated to 15-35 DEG C to react for 0.5-6h to obtain a compound (vii); C) the compound (vii) reacts with dimethyl amine hydrochloride and then is separated and crystallized to obtain a compound (i). The method simplifies the operation, ensures easy industrial production, reduces the production cost and leads the products to be easily purified; therefore, the obtained products have high purity and yield.
Owner:ZHEJIANG HISOAR CHUANNAN PHARMA +1

Carbapenem antibiotic containing sulfhydryl piperidine

The invention pertains to the technical field of medicine and particularly relates to carbon-substituted penem antibiotic which contains sulfhydryl piperidine and is shown as general formula (I), and pharmaceutically acceptable salts, easily hydrolysable ester and isomers of the antibiotic; wherein, R<1>, R<2>, R<3>, R<4>, R<5>, R<6> and R<7> are defined as the specification. The invention also relates to a preparation method of the compounds, medicine composition containing the compounds as well as application of the compounds to the preparation of medicines treating and / or preventing infectious diseases.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD

Method for preparing meropenem using zinc powder

The present invention relates to an improved method for synthesizing meropenem trihydrate [(1R,5S,6S)-2-[((2′S,4′S)-2′-dimethylaminocarbozyl)pyrrolidin-4′-ylthio]-6-[(R)-1-hydroxyethyl]-1-methylcarbapen-2-em-3-carboxylic acid, trihydrate], which is a novel carbapenem antibiotic.
Owner:DAEWOONG BIO +1

Metal beta-lactamase inhibitor open chain pyridine carboxylic acid derivative and preparation method thereof

ActiveCN106496110AMIC (minimum bactericidal concentration) value decreasedPromote research and developmentAntibacterial agentsOrganic active ingredientsCytotoxicityMeropenem
Belonging to the field of medicinal chemistry, the invention discloses a metal beta-lactamase inhibitor open chain pyridine carboxylic acid derivative and a preparation method thereof. The compound has the following structure shown as the specification. The derivative can restore the sensitivity of metal beta-lactamase enterobacteriaceae bacteria to carbapenem antibiotics. In vitro antibacterial experiment results prove that the derivative can reduce the MIC value of carbapenem resistant Escherichia coli (producing NDM-1 type metal beta-lactamase) to meropenem by about 40960 times maximumly. In vitro red blood cell toxicity experiments also prove that the compound has very small red blood cell toxicity. Therefore, the compound is expected to be used as a candidate drug of novel metal beta-lactamase inhibitor.
Owner:ZHENGZHOU UNIV

Meropenem palladium-carbon catalyst preparation method and catalyst prepared through same

The invention belongs to the field of chemical catalyst preparation and particularly discloses a meropenem palladium-carbon catalyst preparation method. The palladium-carbon catalyst is obtained by dipping palladium hydroxide solution on an activated carbon carrier and restoring through a reducing agent. The preparation method comprises the steps: 1) utilizing a palladium-contained compound to prepare palladium hydroxide; 2) preparing palladium hydroxide solution; 3) throwing activated carbon into the palladium hydroxide solution to prepare dipping slurry; 4) performing chemical reduction reaction on the dipping slurry. The invention further discloses meropenem palladium-carbon catalyst prepared through the method. The palladium-carbon catalyst disclosed by the invention has a simple preparation technological process and strong selective pertinence; furthermore, preparation raw materials are simple and easy to obtain, and a reaction product is green and environment-friendly; the palladium-carbon catalyst is mainly applied to preparation of meropenem in carbapenems antibiotics and also has other wide application in the field of medical treatment.
Owner:JIANGXI HANS PRECIOUS METALS CO LTD +1

Metal [beta]-lactamase inhibitor cyclo-amidodithioformate derivative and preparation method of same

The invention belongs to the field of medical chemistry and discloses a metal [beta]-lactamase inhibitor cyclo-amidodithioformate derivative and a preparation method of the same. The compound is represented as the structural formulas 1, 2 or 3 as follows, wherein R is sodium, a methyl group, an n-hexyl group, an n-decyl group or an n-dodecyl group. The inhibitor is combined with a carbapenem antibiotic (e.g. meropenem) to achieve the inhibition activity of metal [beta]-lactamase, so that the sensitivity to the carbapenem antibiotic of a bacterial strain having drug resistance against the carbapenem is recovered. The inhibitor has significant effects on a bacterial strain producing NDM-1 enzyme and having drug resistance against the carbapenem. A red blood cell haemolytic test and a cytotoxicity test prove that the compound is low in toxicity. The series of the compounds is hopeful to serve as a potential candidate medicine of the metal [beta]-lactamase inhibitor.
Owner:ZHENGZHOU UNIV

Antibacterial composition and uses thereof

The present invention relates to the technical field of medicine, specifically to a composition, which contains a compound (a), a pharmaceutically acceptable salt, an ester, a solvate or a stereoisomer thereof, and at least a carbapenem antibiotic or a derivative thereof, wherein the compound (a) has a structure represented by a formula (I) defined in the specification. The invention further relates to uses of the composition in preparation of drugs for prevention and / or treatment of infectious diseases caused by bacteria, wherein preferably the bacteria have drug resistance caused by beta-lactamase.
Owner:SHANDONG XUANZHU PHARMA TECH CO LTD

Acid addition salts of synthetic intermediates for carbapenem antibiotics and processes for preparing the same

The present invention provides a process for preparing an acid addition salt of a synthetic intermediate for carbapenem antibiotics and a novel acid addition salt of a synthetic intermediate for carbapenem antibiotics obtained from the process. The present invention also provides a process for preparing a carbapenem antibiotic using the acid addition salt. According to the process of the present invention, an acid addition salt of a synthetic intermediate for carbapenem antibiotics can be prepared in a high yield and high purity, without conducting column chromatography. Thus, the process of the present invention can be applied to mass production with an industrial scale. Furthermore, since the acid addition salts have solid forms, they are easy to handle and keep in a manufacturing site.
Owner:KUKJE PHARMA IND CO LTD

Preparation method for synthesizing key intermediate 4-BMA of 1beta-methyl carbapenem antibiotic bicyclic nucleus

The invention relates to a preparation method for synthesizing a key intermediate 4-BMA of 1beta-methyl carbapenem antibiotic bicyclic nucleus and belongs to the technical field of synthesis of carbapenem antibiotics. The method disclosed by the invention comprises the following steps: taking an aqueous solution of tetrahydrofuran as a solvent, taking indium as a catalyst, taking (3R,4R)4-carbethoxy-3-[(R)-((tert-butyldimethylsilyl)oxy)ethyl]-2-2-azetidinone (IV) as a raw material, and carrying out a reaction with alpha-bromo-acrylamide XV with large inductive groups so as to produce a compound XIV; not separating the reaction solution of the compound XIV, and performing oxidation-hydrolysis, thereby obtaining the target product VI. The method disclosed by the invention is stable in process, short in reaction route, simple and convenient in operation, mild in reaction conditions, high in product purity, few in three wastes, low in cost, high in yield and suitable for large-scale industrial production.
Owner:YIYUAN XINQUAN CHEM

Method for manufacturing (3S,4R)-4-[(R)-1'-formylethyl]azetidin-2-one derivatives

A method for manufacturing (3S,4R)-4-[(R)-1'-formylethyl]azetidin-2-one derivatives represented by formula (3) wherein R1 represents a hydrogen atom or a protective group, through asymmetric hydroformylation of 4-vinylazetidin-2-one represented by formula (1) wherein R1 has the same meaning as described above; in the presence of a rhodium complex and a (2S,4S)-diphosphine compound represented by formula (2) wherein R2 represents a phenyl group which may be substituted with 1-5 substituent(s) selected from a lower alkyl group, a lower alkoxy group, and a halogen atom.By use of both an inexpensive optically active diphosphine compound and a rhodium complex as catalysts, intermediate compounds important for carbapenem antibiotics can be manufactured with high selectivity and efficiency.
Owner:TAKASAGO INTERNATIONAL CORPORATION

Primer, probe, method and kit for detecting carbapenem antibiotic resisting gene of baumanii

The invention relates to the technical field of molecular biology, and discloses a primer, probe, method and kit for detecting a carbapenem antibiotic resisting gene of baumanii. A Taqman probe real-time fluorescence PCR method is adopted, and the primer and the fluorescence labeling probe are designed aiming at OXA51 and OXA23 nucleic acid conserved domains respectively. After the primer and the probe are prepared into PCR detecting mixed liquid, enzymes and sample nucleic acid are added, an FAM channel on a PCR instrument is selected for amplification, and the target gene is detected through changes of fluorescence signals. The primer, probe, method and kit have the advantages of being high in accuracy, specificity and sensitivity, and baumanii and CRAB in a clinical sample can be fast and accurately detected.
Owner:宁波基内生物技术有限公司 +1

Synthesis method of carbapenem antibiotic parent nucleus MAP

The invention discloses a synthesis method of carbapenem antibiotic parent nucleus MAP. Compared with the prior art, the method redesigns an MAP synthesis route, enhances the synthesis efficiency, has the advantages of lower reaction raw material price, low reaction conditions and lower three wastes, lowers the energy consumption and cost, and satisfies the environment-friendly requirement.
Owner:SUZHOU KAKEA BIOCHEM SCI & TECH LTD

Method for preparing ring-opening impurity of carbapenems

The invention relates to a method for preparing a ring-opening impurity of carbapenems. The ring-opening impurity is of a structure represented by formula I. In the formula I, R represents a meropenem side chain, an ertapenem side chain or a doripenem side chain. The method includes the following steps: (1) adding carbapenems into an alkaline solution, stirring and reacting for 1-4 hours; (2) adjusting the pH to 6.0-9.0; (3) freeze-drying the materials to obtain the ring-opening impurity of carbapenems. The method provided by the invention is simple to operate and short in reaction time; the product has the purity of 95% or above and can be directly used as a reference substance for quantitative and qualitative research on the ring-opening impurity of carbapenem products, so that the product quality can be effectively controlled. The formula I is shown in the description.
Owner:山东安弘制药有限公司

Crystal of intermediate of tebipenem pivoxil and preparation method thereof

The invention relates to a crystal of an intermediate of carbapenem antibiotic tebipenem pivoxil and a preparation method thereof. The crystal type of the intermediate comprises a type A crystal of the intermediate of tebipenem pivoxil and a type B crystal of the intermediate of tebipenem pivoxil, wherein in a powder X-ray diffraction pattern, the type A crystal has main peaks when the diffraction angle 2(theta) is 5.90, 8.02, 14.93, 19.30, 22.65, 22.10, 24.16, 26.50 and 26.98; the type B crystal has main peaks when the diffraction angle 2(theta) is 6.76, 8.25, 15.13, 16.35, 17.47, 21.02, 22.31, 31.31 and 32.77. The preparation method of the crystal form mainly comprises a preparation method of the type A crystal of the intermediate and a method for preparing the type B crystal through crystal transformation of the type A crystal.
Owner:SHANDONG MINGREN FURUIDA PHARMA +1
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