Abstract: Provided is a long-acting method for preventing or treating glucose metabolism disorders that includes administering a beta-lactam compound or a pharmaceutically acceptable salt thereof to a subject in need thereof. The method for preventing or treating glucose metabolism disorders has a long-acting effect that lasts more than two days even after medication has been stopped.

Abstract: The present disclosure relates to a pharmaceutical composition comprising: (a) ?-lactam antibiotics and (b) a metallo-?-lactamases (MBLs) inhibitor. The inhibitor relates to Bi(III) compounds or the pharmaceutically acceptable salts thereof. The present patent also provides methods of making Bi(III) compounds or the pharmaceutically acceptable salts thereof. Also provided is a method for treating MBLs-producing bacterial infection using a metal replacement mechanism.

Abstract: The present disclosure relates to a pharmaceutical composition comprising: (a) ?-lactam antibiotics and (b) a metallo-?-lactamases (MBLs) inhibitor. The inhibitor relates to Bi(III) compounds or the pharmaceutically acceptable salts thereof. The present patent also provides methods of making Bi(III) compounds or the pharmaceutically acceptable salts thereof. Also provided is a method for treating MBLs-producing bacterial infection using a metal replacement mechanism.

Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.

Abstract: There is provided inter alia a method of treating microbial infection comprising administering to a subject in need thereof a therapeutically effective amount of: (a) 4-(4-ethyl-5-fluoro-2-hydroxyphenoxy)-3-fluorobenzamide; and (b) an antibacterial agent selected from the group consisting of carbapenems, aminoglycosides, polymixins, glycylcyclines, rifampifin and sulbactam.

Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

Abstract: The present invention relates to the crystalline form of carbapenems derivative or hydrate thereof and the preparation methods thereof. Specifically, the present invention relates to the crystalline form of carbapenem derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid as represented by formula (I) or hydrate thereof, characterized in that the X-ray powder diffraction pattern thereof using Cu-Ka radiation represented as 2? has characteristic peaks at 18.9±0.2, 19.4±0.2, 21.0±0.2, 21.7±0.2, and 23.4±0.2, the preparation methods thereof, and the use thereof in the preparation of medicament for treating and/or preventing infectious diseases, as well as a pharmaceutical composition comprising such compound and one or more pharmaceutical carriers and/or diluents.

Abstract: The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which are useful for intravenous and intramuscular administration.

Abstract: Provided herein are methods and computer-implemented systems for using computer simulations to predict likelihood of a cell population associated with a pathophysiological condition acquiring resistance to a therapeutic agent, to screen for therapeutic agents effective to suppress acquisition of resistance within a cell population and to treat the pathophysiological conditions associated therewith. The computer simulation comprises at least an input/out system and a mathematical model, including operably linked equations, parameter values and constant values, of growth response over a period of time of a cell population in contact with an therapeutic agent. Also provide is a method for determining a best-fit mathematical model of adaptation of a microbial population to a therapeutic agent over time and using the model to simulate microbial population behavior to a therapeutic agent.

Abstract: Provided is a crystalline form E of ertapenem sodium. Further provided is a method for preparing a crystalline form E of ertapenem sodium, characterized by using an aqueous ertapenem sodium solution at a low concentration as a raw material. The crystalline form E can be easily filtered and dried, the properties in the drying process are stable, and the purity of the crystal is high and can be up to 98.5% or higher.

Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to the use of inhibitors of FtsZ, an ancestral tubulin of prokaryotes, to restore susceptibility to ?-lactam antibiotics, including carbapenems and cephalosporins, particularly in methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphyloccus epidermis (MRSE), and other coagulase negative staphylococci (MRCNS).

Abstract: There is proposed herein a process for production of composite antimicrobial preparations for parenteral administration, featuring a higher therapeutic efficiency in case of grave infection and inflammatory diseases. The proposed compositions include active agents being betalactam antibiotics and finely dispersed nanostructured silica dioxide with a weight ratio from 10:1 to 75:1 respectively. The silica dioxide particles are antibiotic molecules delivery agents into the phagocytes, which allows increasing the antimicrobial preparations concentration at inflammation areas and considerably decrease microorganisms antibiotic resistance. The mentioned production process includes mixing betalactam antibiotic with finely dispersed nanostructured silica dioxide.

Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.

Abstract: The present invention relates to the crystalline form of carbapenems derivative or hydrate thereof and the preparation methods thereof. Specifically, the present invention relates to the crystalline form of carbapenem derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-(4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid as represented by formula (I) or hydrate thereof, characterized in that the X-ray powder diffraction pattern thereof using Cu-Ka radiation represented as 2? has characteristic peaks at 18.9±0.2, 19.4±0.2, 21.0±0.2, 21.7±0.2, and 23.4±0.2, the preparation methods thereof, and the use thereof in the preparation of medicament for treating and/or preventing infectious diseases, as well as a pharmaceutical composition comprising such compound and one or more pharmaceutical carriers and/or diluents.

Abstract: Pharmaceutical compositions containing a carbapenem of the structural formula I and epicillin are strongly bactericidal against MRSA and MRSE. Equivalently, compositions of conventional carbapenem antibiotics and epicillin are highly synergistic in eradicating said bacteria.

Abstract: The present invention relates to a crystalline form of carbapenems derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid_as represented by formula (I) or hydrate thereof and the preparation methods thereof, wherein said method comprise: dissolving the compound as represented by formula (I) by an aqueous solution of N,N?-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), and then adding a poor solvent dropwise to this solution, filtering and drying to obtain a crystal. Another method comprises: formulating the compound as represented by formula (I) as an aqueous suspension; after adjusting pH until complete dissolution, adding a mixed solvent of organic solvent/water with a certain volume ratio; adjusting pH to 5.4-7.0, cooling to low temperature, filtering and drying to obtain a crystal.

Abstract: The present invention includes novel carbapenem derivatives having structural formula (I) or (II): wherein R1, R2, R3, R4 are described in the specification. The present invention also provides pharmaceutical compositions comprising the novel carbapenem derivatives and the use of the novel carbapenem derivatives for treating infectious diseases.

Abstract: Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about ?50° C. to about ?10° C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (?50 to ?10° C.), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject.

Abstract: The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which are useful for intravenous and intramuscular administration.

Abstract: The present application describes deuterium-enriched meropenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The peptidoglycan layer is a vital component of the bacterial cell wall, which comprises 4?3 and 3?3 transpeptide cross-linkages, the formation of which are catalyzed by D,D- and L,D-transpeptidases, respectively. Methods for the treatment of bacterial infections with agents that inhibit L,D-transpeptidases, either alone or in combination with D,D-transpeptidase inhibitors, are provided herein. Also provided are methods for the treatment of chronic stage tuberculosis with agents that inhibit enzyme with L,D-transpeptidase activity.

Abstract: A new metallo-?-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of ?-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-?-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of ?-lactam antibiotics against metallo-?-lactamase producing bacteria by combining the compound of the general formula (I) with ?-lactam antibiotics.

Abstract: Compounds useful as antimicrobials are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are derivatives having a carbapenem core, and are useful for treating a microorganism infection.

Abstract: The present invention relates to a process for preparing a carbapenem antibiotic composition. The present invention further relates to a carbapenem antibiotic composition substantially free of degradation impurities. The present invention further relates to a polymorphic form of ertapenem mono sodium designated as Form D and its preparation.

Abstract: A pharmaceutical composition comprising carbapenem and Aztreonam each in the dosage range of about 0.25 g to 0.75 g and pharmaceutically acceptable excipients for the prevention and treatment of infections caused by Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumoniae or MRSA (Methicillin Resistant Staphylococcus aureus).

Abstract: The present invention includes novel carbapenem derivatives having structural formula (I) or (II): wherein R1, R2, R3, R4 are described in the specification. The present invention also provides pharmaceutical compositions comprising the novel carbapenem derivatives and the use of the novel carbapenem derivatives for treating infectious diseases.

Abstract: In an embodiment of the invention, a method of enhancing the efficacy of an anti-infective therapeutic agent against an obligate or facultative intracellular parasite in a host is provided. The method comprises administering to the host an effective amount of a bifunctional compound of less than about 5000 Daltons comprising the therapeutic or an active derivative, fragment or analog thereof and a protein binding moiety. The protein binding moiety binds to at least one intracellular protein. The bifunctional compound has a higher intracellular concentration as compared to the therapeutic itself in order to enhance the efficacy of the anti-infective therapeutic against the obligate or facultative intracellular parasite.

Abstract: The present invention relates to novel carbapenem derivatives and belongs to pharmaceutical field. Specifically, the present invention relates to the compounds as represented by formulae (1) and (2), pharmaceutically acceptable salts, hydrolysable esters, isomers and intermediates thereof, wherein R1, R2, R3, R4 are described as in the description. The present invention also relates to the processes for the preparation of these compounds, to the pharmaceutical compositions comprising these compounds, and to their use for the manufacture of a medicament for the treatment and/or prevention of infectious diseases.

Abstract: Pharmaceutical compositions containing a carbapenem of the structural formula I and epicillin are strongly bactericidal against MRSA and MRSE. Equivalently, compositions of conventional carbapenem antibiotics and epicillin are highly synergistic in eradicating said bacteria.

Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.

Abstract: 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 ?-lactamase inhibitor.

Abstract: A method for treating individuals affected with latent tuberculosis comprising a step of administering an effective amount of one or more carbapenem compounds to the said individuals.

Abstract: A 1-methylcarbapenem compound ethanolate of the formula (I-1) in the crystalline form that shows main peaks at interplanar spacings d=7.60, 6.69, 6.33, 6.14, 5.15, 4.58 and 4.48 in the X-ray powder diffraction pattern obtained with Cu K? irradiation and a 1-methylcarbapenem compound tetrahydrate of the formula (I-2) in the crystalline form that shows main peaks at interplanar spacings d=11.68, 8.79, 7.53, 6.57, 5.58, 5.37, 3.99 and 3.09 in the X-ray powder diffraction pattern obtained with Cu K? irradiation These compounds are useful for treating or preventing bacterial infections.

Abstract: The present application describes deuterium-enriched meropenem, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A surfactant can be added, safely and effectively, to a drug solution containing any antimicrobial agent, such as an antibiotic like tobramycin, that is suitable for administration to the lungs via inhalation. Thus, when an aerosolized drug solution includes surfactant, Marangoni flows cause the drug particles, once deposited in the lungs, to spread over a wider surface area, thereby ensuring greater antimicrobial efficacy. A solution that contains, for example, an antibiotic and tyloxapol or another surfactant providing a similar surface tension to the composition is optimally delivered by the functional combination of a breath-actuated nebulizer and a high-flow compressor.

Abstract: An antimicrobial combination medicament for injection comprising a ?-lactam compound represented by the formula [1], wherein R1 is lower alkyl or the like, R2 is H or lower alkyl group, X is O, S or NH; m and n are 0 to 4, provided that the sum of m and n is 0 to 4; Y1 is halogen or the like; and Y2 is hydrogen, optionally substituted lower alkyl group or the like; and carbapenems such as meropenem.

Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.

Abstract: Among crystalline forms of compound (I), a 1-methylcarbapenem compound represented by the formula (I) in a crystalline form that shows main peaks in the X-ray powder diffraction pattern obtained with copper K? irradiation.

Abstract: The present invention relates to carbapenems and provides a compound of the formula (I): or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen or C1-4alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4-alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4-alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N—C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n— wherein n is zero, one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to —NR3—. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

Abstract: This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I-1), (I-2) or (I-3) The crystalline forms of the 1-methylcarbapenem derivative exhibit excellent antibiotic activity against various bacterial strains and sufficient stability for practical use.

Abstract: This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I) or of pharmaceutically acceptable salts thereof. The crystalline forms of the 1-methylcarbapenem derivative exhibit excellent antibiotic activity against various bacterial strains and sufficient stability for practical use.

Abstract: A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: 1

Abstract: This invention relates to a method of inhibiting growth of Bacillus anthracis, Bacillus cereus and/or Bacillus thuringiensis bacterial strains in a mammal comprising administration to a patient in need thereof a therapeutically effective amount of a carbapenem compound. In particular, this invention relates to a method of inhibiting growth of Bacillus anthracis, Bacillus cereus and/or Bacillus thuringiensis bacterial strains in a mammal using compounds having the structural formula (I) or a pharmaceutically acceptable salt, enantiomer, diastereomer or in vivo hydrolysable ester or mixture thereof. This invention further relates to the use of carbapenem compounds of formula I in the treatment of anthrax and other conditions which are related to an anthrax infection.

Abstract: A carbapenem compound represented by the formula (I′): 1

Abstract: The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula I: 1

Abstract: This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I) or of pharmaceutically acceptable salts thereof.

Abstract: This invention provides crystalline forms of a 1-methylcarbapenem derivative of formula (I) or of pharmaceutically acceptable salts thereof.

Abstract: A process for the preparation of a carbapenem antibacterial compound of the following formula (4) having a 1-alkylpyrrolidine structure or a salt thereof, a useful synthetic intermediate of the following formula (1) or a salt thereof, and a process for the preparation thereof: 1