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351 results about "Beta-lactam" patented technology

A beta-lactam (β-lactam) ring is a four-membered lactam. (A lactam is a cyclic amide.) It is named as such because the nitrogen atom is attached to the β-carbon atom relative to the carbonyl. The simplest β-lactam possible is 2-azetidinone.

Poly-beta-peptides from functionalized beta-lactam monomers and antibacterial compositions containing same

Disclosed is a method of making β-polypeptides. The method includes polymerizing β-lactam-containing monomers in the presence of a base initiator and a co-initiator which is not a metal-containing molecule to yield the product β-polypeptides. Specifically disclosed are methods wherein the base initiator is potassium t-butoxide, lithium bis(trimethylsilyl)amide (LiN(TMS)2), potassium bis(trimethyl-silyl)amide, and sodium ethoxide, and the reaction is carried out in a solvent such as chloroform, dichloromethane, dimethylsulfoxide, or tetrahydrofuran.
Owner:WISCONSIN ALUMNI RES FOUND

Combinations of substituted azetidinones and CB1 antagonists

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one selective CB1 antagonist; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity, metabolic syndrome and lowering plasma levels of sterols or 5α-stanols.
Owner:SCHERING CORP

Beta-lactam antibiotic-containing tablet and production thereof

This invention provides beta-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a beta-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and / or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.
Owner:ASTELLAS PHARMA INC

Components and preparation method of beta-lactam injection

The invention discloses the components and preparation method of beta-lactam injection. The beta-lactam injection comprises 5 to 20 percent of beta-lactam antibiotics, 0.05 to 5 percent of suspending agent, 0.005 to 0.3 percent of antioxygen, 0.1 to 0.2 percent of nonionic surfactant and the balance of vegetable oil or grease for injection. The injection can be used for preventing and curing animal bacterial infectious diseases and can be injected hypodermically or in muscle and be applied through breast for a few times. The preparation method provided by the invention comprises: firstly, making the antibiotics and the antioxygen into micro powder and making the suspending agent into fine powder; secondly, adding the vegetable oil or grease for injection, which is sterilized at high temperature, into the fine powder of the suspending agent, heating the mixture, uniformly mixing the mixture and keeping the mixture in a sterile environment to cool the mixture to room temperature for later use; and finally, transferring the prepared oil or grease added with the suspending agent to a colloid mill, adding medicament micro powder, the antioxygen and the non-ionic surfactant with stirring, and performing uniform mixing and sterilization to obtain the beta-lactam injection.
Owner:LUOYANG HUIZHONG ANIMAL MEDICINE

Method of attaching drug compounds to non-reactive polymer surfaces

Polymers are disclosed that are chemically modified to retard bacterial growth. Such modified polymers (e.g. ePTFE and polypropylene) are produced by first creating acid groups on the polymer surface through reactions with an anhydride. The acid groups are then linked to polyethylene glycol (PEG) through esterification or other reactions such as amidation. Preferably, at least two different molecular weight PEG species are employed. The antimicrobial surface is completed by linking antibiotics (e.g. β-lactam antibiotics) to the PEG extensions. One preferred embodiment of such a modified polymer is produced using ePTFE, maleic anhydride (MA), and penicillin (PEN) to yield PEN-PEG-MA-ePTFE, which inhibits gram-positive bacteria. The PEG spacer is critical for PEN function in this context, since PEN-ePTFE is ineffective against bacterial growth. Another preferred embodiment incorporates ampicillin (AMP) and a heterobifunctional PEG, HOOC—(CH2—CH2—O)n—NH2, to yield AMP-PEG-MA-ePTFE. This latter example inhibits both gram-negative and gram-positive bacteria.
Owner:SOUTHERN MISSISSIPPI THE UNIV OF

Modified beta-lactamase and method for its preparation

The invention relates to targeted post translational modifi-cation of metallo-beta-lactamase by truncation and inser-tion of a dipeptide at the amino terminal end to reduce amino terminal heterogeneity in a recombinant DNA pro-duction system. A protein K-T-E-ΔBL is expressed, and modified by host proteases to E-ΔBL. Appropriate nucleotide molecules, vectors and hosts are also de-scribed. E-ΔBL is useful in a pharmaceutical composition for treating antibiotic induced adverse effects in the intes-tine of patients treated with beta-lactam antibiotics.
Owner:SYNTHETIC BIOLOGICS INC

Method for simultaneously detecting multi-kind pesticide residues in bee products

InactiveCN101358953ASolve the problem of matrix effectFast wayComponent separationRetention timePhosphate
The present invention relates to a method of simultaneously detecting a plurality of agro-veterinary drug residues in bee products. The extracted liquid trichloroacetic acid or perchloric acid and the extracted liquid acetate, phosphate or borate solution are added into a sample; the pH value is controlled between 4.5 and 9.0; the mixed solution is centrifuged, the filtrate is added into a solid phase extraction column to be extracted, the extraction column is eluted and dried, the column is washed by oxalic acid-methanol solution, the volume of the eluent is defined by the aqueous solution of methanol, the eluent is added into liquid chromatography-tandem mass spectrometry to be analyzed and tested, the acquired chromatographic peak is contrasted with the known standard chromatographic peak of the drug, and according to the retention time and the abundance of the mass spectrum ions, the specific name of the detected drug is determined. The method only requires one pre-treatment of the sample, and thus can simultaneously extract 11 classes and more than 60 kinds of veterinary drug residues, such as sulfonamides, quinolones, macrolides, lincomycins, nitroimidazoles, beta-lactams, tetracyclines, chloromycetins, trinethoprims, chlordimeform, triadimenol and the like, the efficiency of analysis is high, and the detection cost is greatly reduced.
Owner:中华人民共和国江苏出入境检验检疫局

Stable pharmaceutical compositions of aminoglycoside antibiotics, ion-chelating agents, and buffers

A pharmaceutical composition comprising: at least one aminoglycoside antibiotic and (a) at least one ion chelating agent used for inhibiting particulate formation, or (b) at least one buffer, or (c) at least one ion chelating agents and at least one buffer simultaneously. The composition for use in controlling microbial infection can be formulated into a solution, or combined with at least one beta-lactam antibiotic, or combined with at least one of beta-lactam antibiotic and at least one beta-lactamase inhibitor into a solution in a container.
Owner:ZHANG HESHENG

Modified beta-lactamase and method for its preparation

The invention relates to targeted post translational modification of metallo-beta-lactamase by truncation and insertion of a dipeptide at the amino terminal end to reduce amino terminal heterogeneity in a recombinant DNA production system. A protein K-T-E-ΔBL is expressed, and modified by host proteases to E-ΔBL. Appropriate nucleotide molecules, vectors and hosts are also described. E-ΔBL is useful in a pharmaceutical composition for treating antibiotic induced adverse effects in the intestine of patients treated with beta-lactam antibiotics.
Owner:SYNTHETIC BIOLOGICS INC

Process for preparing taxoids from baccatin derivatives using lewis acid catalyst

ActiveUS20120149925A1Organic chemistryTaxoidLewis acid catalysis
The present invention relates to a process of preparing a taxoid (X) by reacting a protected baccatin derivative (B) with a β-lactam (C) in the presence of one or more Lewis acids and a base agent. The present invention also relates to a process of preparing the protected baccatin derivative (B) from a baccatin derivative (A) comprising a protection reaction catalyzed by one or more Lewis acids with an optional base agent.
Owner:YUNG SHIN PHARMACEUTICALS INDUSTRIAL CO LTD

Pharmaceutical compositions

A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I):In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of beta lactam antibiotics against many beta-lactamase producing bacteria.
Owner:SMITHKLINE BECKMAN CORP

Stabilized preparations of beta-lactam antibiotic

Stabilized preparations which contain a beta-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
Owner:TAKEDA SCHERING PLOUGH ANIMAL HEALTH

Purified clavulanic acid and salts thereof

A new antibacterially active agent has been isolated from Streptomyces clavuligerus. This new compound which is designated clavulanic acid has the formula (I): In addition to being a broad spectrum antibiotic of medium potency, clavulanic acid and its salts and esters have the ability to enhance the effectiveness of beta -lactam antibiotics against many beta -lactamase producing bacteria.
Owner:SMITHKLINE BECKMAN CORP

Chphalosporin-derived mercaptans as inhibitors of serine and metallo-beta-lactamases

Compounds of formula I: See Formula I in Figures Section 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-β-lactamase enzymes, for enhancing the activity of β-lactam antibiotics, and for treating β-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.
Owner:BUYNAK JOHN D +1

Ezetimible intermediate and synthetic method of ezetimible

The invention provides an intermediate for synthesizing ezetimibe and a preparation process thereof, and also provides a method for synthesizing the ezetimibe by the intermediate. The synthesizing method has short route, and comprises the following concrete steps: a compound I and substituted 1, 3-propanediol react to generate a compound II; the compound II and pivalyl chloride react to generate a compound III; the compound III and a compound A react to generate a compound IV; the compound IV and a compound V react to generate a compound VI under the condition of a titanium compound catalyst; the compound VI is re-ringed to generate a compound VII with beta-lactam; the compound VII is hydrolyzed to produce a compound VIII; and the compound VII is reduced to a compound IX ezetimibe by a borane chiral reducing agent. The synthesization has short route and mild reaction condition; and the produced intermediate and final product has high yield and high purity.
Owner:ENANTIOTECH CORP

Antibiotic polymers

Polymers (i.e. polyesters, polyamides, polythioesters, polyanhydrides, or a mixture thereof) which degrade hydrolytically to provide a combination of a beta-lactam antibiotic (e.g., amoxicillin) and a beta-lactamase inhibitor (e.g., clavulanic acid) (or a pharmaceutically acceptable salt thereof) are provided. Methods of producing these polymers, intermediates useful for preparing these polymers, and methods of using these polymers to deliver a combination of a beta-lactam antibiotic and a beta-lactamase inhibitor (or a pharmaceutically acceptable salt thereof) to a host are also provided.
Owner:RUTGERS THE STATE UNIV

Process for The Preparation of Beta-Lactam Antibiotic

The present invention relates to a process for the preparation of Meropenem of formula (I) in sterile form and also provides an improved process for the preparation of compound of formula (V), which is an important intermediate in the synthesis of Meropenem.
Owner:ORCHID CHEM & PHARM LTD

Stable pharmaceutical composition comprising beta-lactam antibiotic and ion-chelating agent

A pharmaceutical composition comprising: at least one β-lactam antibiotic and at least one ion-chelating agent; wherein when said pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic.
Owner:ZHANG HESHENG

Lactam nucleic acids

Novel beta -lactam monomers bearing various functional groups are prepared. The novel beta -lactam monomers can be joined into oligomeric compounds such as via preferred phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and / or groups that participate in hydrogen bonding. The oligomeric compounds are useful as diagnostic and research reagents.
Owner:IONIS PHARMA INC

Compositions and methods for treatment of staphylococcal infection while suppressing formation of antibiotic-resistant strains

Co-administration of a lysostaphin or other anti-staphylococcal agent which cleaves cross-links of peptidoglycans of staphylococci cell walls such as lysostaphin and an antibiotic effective against staphylococci due to antibiotic activity mediated by cell-wall activity is effective against staphylococcal infection, even staphylococci that may be resistant to one or other of lysostaphin or the cell-wall active antibiotic. Co-administration simultaneously suppresses the generation of antibiotic-resistant mutant strains. Effective cell-wall active antibiotics include β-lactams and glycopeptides.
Owner:NUTRITION 21 INC

Stable pharmaceutical composition comprising beta-lactam antibiotic and buffer

InactiveUS20090156518A1Prevent first-time-treatment failureEffective treatment regimenAntibacterial agentsBiocideMedicineAntibiotic Y
A pharmaceutical composition, comprising: at least one β-lactam antibiotic and at least one buffer component; wherein when the pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic mixed with the β-lactam antibiotic and the buffer component.
Owner:ZHANG HESHENG

Compositions and methods for antibiotic potentiation and drug discovery

The present invention provides methods for identifying target genes whose partial or complete functional inactivation potentiates the activity of an antibiotic agent, e.g., a quinolone antibiotic. The invention further provides methods for identifying agents that modulate expression of target genes or that modulate activity of expression products of target genes. Agents identified according to various methods of the invention potentiate the activity of antibiotics such as quinolones, aminoglycosides, peptide antibiotics and β-lactams. Also provided are agents that suppress and / or retard resistance to antibiotics. The inventive methods provide potentiating agents and compositions comprising potentiating agents and antibiotics. Such agents and compositions can be used for inhibiting growth or survival of a microbial cell or of treating a subject suffering from or susceptible to a microbial infection.
Owner:TRUSTEES OF BOSTON UNIV

Beta-lactamase inhibitor and process for preparing the same

A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I):wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O═, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.
Owner:MEIJI SEIKA KAISHA LTD

Amidine substituted beta - lactam compounds, their preparation and use as antibacterial agents

The present invention relates to novel beta-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel beta-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.
Owner:AICURIS GMBH & CO KG

Cefprozil medicinal composition

The invention relates to a cefprozil medicinal composition, in particular to a medicinal composition containing cefprozil and cellulose derivatives, which is prepared by a dry granulation method. The cefprozil and the cellulose derivatives are uniformly mixed, and the mixture is pressed into plates under the pressure of 0.1 to 25MPa so as to form tight combination; and then, according to requirements, the plates are prepared into tablets, powder, granules or capsules. The medicinal composition can further contain other conventional auxiliary materials; the obtained plates are ground, mixed with a diluent, a disintegrating agent, a lubricating agent, an adhesive and / or other auxiliary materials; and the mixture is prepared into tablets, powder, granules, suspension or capsules according to requirements. The dry granulation process is adopted; and after the cefprozil and the cellulose derivatives are tightly combined through proper pressure, the beta-lactam ring of the cefprozil is effectively prevented from ring-opening degradation, the stability of the medicinal composition is improved, and the effectiveness and safety of clinical medication are further guaranteed.
Owner:SINOPHARM SHANTOU JINSHI PHARMA CO LTD

Preparation method of tazobactam sodium

The invention relates to a preparation method of a beta-lactam inhibitor, namely tazobactam sodium. The preparation method comprises the following steps: dissolving tazobactan acid in 6-15 DEG C of cooling water, mixing with a salt forming agent solution under the condition of controlling the temperature, stirring to ensure that the solution is clear, and lyophilizing to obtain tazobactam sodium powder. The tazobactam sodium prepared by the method has high purity; and the entire technological operation is convenient, the cost is low and the production efficiency and yield are increased.
Owner:海南美好西林生物制药有限公司
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