Abstract: The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.

Abstract: A method is provided for cultivating soybean or corn. Also provided is a method for controlling insect pests in a field of soybean or corn. By these methods, insect pests in the fields of soybean or corn can be controlled. Therefore, a good yield of corn or soybean can been obtained.

Abstract: The present invention provides stable, ready-to-use injectable pharmaceutical compositions, comprising the combination of neostigmine, glycopyrrolate, a stabilizing amount of one or more aminopolycarboxylic acids, and a pharmaceutically acceptable liquid vehicle. Other aspects of the invention relate to methods for making such compositions and methods of using such compositions for reversing the effects of non-depolarizing neuromuscular blocking agents. Preferably, the composition comprises neostigmine methylsulfate, glycopyrronium bromide, ethylenediaminetetraacetic acid (EDTA) and a pharmaceutically acceptable liquid vehicle, and is provided in a pre-filled, ready-to-use sealed container, such as a pre-filled syringe, suitable for intravenous administration.

Abstract: Substituted heteropentadieno-pyrrolopyrimidine ribonucleosides of general formula I, where R is selected from the group comprising furan-2-yl, furan-3-yl, benzofuran-2-yl, methylsulfanyl, methoxy, amino, dimethylamino, methyl or chloro, and pharmaceutically acceptable salt thereof, their optical isomers and mixtures of such optical isomers.

Abstract: The present invention provides stable, ready-to-use injectable pharmaceutical compositions, comprising the combination of neostigmine, glycopyrrolate, a stabilizing amount of one or more aminopolycarboxylic acids, and a pharmaceutically acceptable liquid vehicle. Other aspects of the invention relate to methods for making such compositions and methods of using such compositions for reversing the effects of non-depolarizing neuromuscular blocking agents. Preferably, the composition comprises neostigmine methylsulfate, glycopyrronium bromide, ethylenediaminetetraacetic acid (EDTA) and a pharmaceutically acceptable liquid vehicle, and is provided in a pre-filled, ready-to-use sealed container, such as a pre-filled syringe, suitable for intravenous administration.

Abstract: Described herein are compositions and methods for the treatment of meibomian gland dysfunction. Said compositions and methods comprise keratolytic agents, such as salicylic acid, selenium disulfide, or the like. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from meibomian gland dysfunction.

Abstract: The present invention regards a novel administration form and a novel administration regime useful in the treatment and prevention of a bacterial lung infection in patient in need thereof, in particular by providing a composition useful for aerosolization of a highly concentrated solution of aminoglycosides such as Tobramycin.

Abstract: In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof. Additionally, methods of treating and preventing bacterial infections using the aminoglycoside derivatives are also provided.

Abstract: Compositions having a drug-loaded microparticle and bone cement and methods of making such compositions are disclosed. Also disclosed are methods of employing such compositions for the treatment of injected joint spaces and bone disease.

Abstract: Biodegradable polymer-coated surgical meshes formed into pouches are described for use with cardiac rhythm management devices (CRMs) and other implantable medical devices. Such meshes are formed into a receptacle, e.g., a pouch or other covering, capable of encasing, surrounding and/or holding the cardiac rhythm management device or other implantable medical device for the purpose of securing it in position, inhibiting or reducing bacterial growth, providing pain relief and/or inhibiting scarring or fibrosis on or around the CRM or other implantable medical device. Preferred embodiments include surgical mesh pouches coated with one or more biodegradable polymers that can act as a stiffening agent by coating the filaments or fibers of the mesh to temporarily immobilize the contact points of those filaments or fibers and/or by increasing the stiffness of the mesh by at least 1.1 times its original stiffness.

Abstract: The invention provides compositions comprising a plurality of polymer layers for preventing or inhibiting microbial infections. Specifically, the invention provides a combination of a cationic polymer layer that resists adhesion of a microbe to its surface and an anionic polymer layer that releases a cationic anti-microbial agent in response to a change in pH or electrostatic balance.

Abstract: Described are agrochemical compositions, comprising (a) esters and/or amides of pyroglutamic acid, and (b) biocides. The compositions are clear and exhibit an improved stability even when stored at temperatures between 5° and 40° C. over a longer period.

Abstract: An antibiotic composition for the treatment of bacterial infections, especially in the respiratory tract is provided. The antibiotic composition may include a mixture of gentamicin as active pharmaceutical ingredient (API), and a micronized poloxamer composition as excipient. Micronized poloxamer composition may be produced by mixing poloxamer 188 and poloxamer 407 in a suitable apparatus where a low-frequency acoustic field may be applied to facilitate mixing. Antibiotic composition may be obtained in powder form, or in solution, and may be administered by inhalation or irrigation. In other embodiments, a topical formulation of the antibiotic inhalation or irrigation composition may be produced. In some embodiments, other suitable poloxamers, or sugar alcohols may be employed as excipients. Due to the synergistic effect of micronized poloxamer composition, antibiotic composition may provide improved solubility and bioavailability of gentamicin, thus decreasing side effects and time of treatment.

Abstract: The invention relates to anionic conjugates of glycosylated bacterial metabolites that may be used to mimic the structure and/or activity of the anionic bioactive molecules known as glycosaminoglycans (GAGs). The invention also relates to processes for the preparation of the conjugates. Such conjugates are useful in the prophylaxis and/or treatment of disease conditions and in particular chronic disease conditions such as inflammatory (including allergic) diseases, metastatic cancers and infection by pathogenic agents including bacteria, viruses or parasites.

Abstract: This disclosure relates generally to aminoglycoside derivatives of Formula (I) as described herein. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating bacterial infections by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Provided are methods for treating a NAD comprising administering to a patient suffering from a NAD an inhibitor of NMD and a nonsense suppressor, whereby degradation of NMD susceptible mRNA is decreased and translation termination at a misplaced nonsense codon is blocked.

Abstract: Products and methods are provided for the restoring the endogenous expression of theta-defensins, such as retrocyclin-1, in mamallian cells. The present invention also includes products and methods for inhibiting sexually transmitted virus entry, e.g., HIV-1 virus entry, into a mammalian cell via, for example, administering to a subject an amount of a read-through mediating agent sufficient to induce exogenous expression of an amount of retrocyclin nonapeptides in the mammalian cell.

Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.

Abstract: Compounds useful for the treatment of giardiasis are described.

Abstract: The present invention relates to a method for preparation of heparin silver, to use of heparin silver in manufacture of medicine for treating burns and/or scalds, to a method of using heparin silver to treat burns and/or scalds, and to a topical preparation containing heparin silver for treating burns and/or scalds. The heparin silver product prepared according to the method of the present invention has a high purity and less impurity. The animal test proved that the medicine made by using heparin silver exhibited effects of accelerating wound healing and reducing scar formation.

Abstract: This invention concerns compounds with the formula: in which: R1?OH or NH2; OR2, OR3, OR4 and OR5 are alcohol, ether, ester, carbonate, carbamate, sulphonate or sulphamate groups; and if R5?H if R2?R3?R4, then R2, R3 and R4?H; if R2?H, then R3?H and R4?H; if R3?H, then R2?H and R4?H; if R4?H, then R2?H and R3?H; if R5?H if R2=H, then R3?H and R4?H; if R3?H, then R2?H and R4?H; if R4?H, then R2?H and R3?H, their use as antibiotic agents and the process for synthesizing them.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 or R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Q1 and Q2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: This invention relates to a compound of Formula 1A: or a pharmaceutically acceptable salt thereof; wherein R1 to R4, R7, R9 to R12 and Y are as defined herein. The invention further relates to pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof; and method of using same for reducing or reversing bacterial resistance to at least one aminoglycoside antibiotic.

Abstract: Provided herein are systems for treating a subject with a pulmonary infection, for example, a nontuberculous mycobacterial pulmonary infection, a Burkholderia pulmonary infection, a pulmonary infection associated with bronchiectasis, or a Pseudomonas pulmonary infection. The system includes a pharmaceutical formulation comprising a liposomal aminoglycoside dispersion, and the lipid component of the liposomes consist essentially of electrically neutral lipids. The system also includes a nebulizer which generates an aerosol of the pharmaceutical formulation at a rate greater than about 0.53 gram per minute. The aerosol is delivered to the subject via inhalation for the treatment of the pulmonary infection.

Abstract: The present invention regards a novel administration form and a novel administration regime useful in the treatment and prevention of a bacterial lung infection in patient in need thereof, in particular by providing a composition useful for aerosolization of a highly concentrated solution of aminoglycosides such as Tobramycin.

Abstract: A combination therapy for treating a bacterial biofilm comprises a therapeutically effective amount of an antibiotic comprising an aminoglycoside or tetracycline, or a combination of two or more thereof, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm. A method of treating a bacterial biofilm comprising Pseudomonas aeruginosa comprises contacting the bacterial biofilm with a combination therapy comprising a therapeutically effective amount of an antibiotic, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm. A method of treating a bacterial biofilm comprising Pseudomonas aeruginosa in a patient comprises administering to the patient a combination therapy comprising a therapeutically effective amount of an antibiotic, and a cationic porphyrin in an amount effective for enhancing the effectiveness of the antibiotic in treating the bacterial biofilm.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I) or (II): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2, R3, R11 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention provides compounds and compositions that enhance the innate immune system. The present invention comprises methods of preventing, treating or ameliorating an infectious disease comprising administering said compounds to a subject. The invention also comprises methods of formulation and administration of said compounds.

Abstract: Biodegradable polymeric microparticle compositions containing one or more active agents, especially those useful for treating or preventing one or more diseases or disorders of the eye, and methods of making and using thereof, are described. In a preferred embodiment, the microparticle compositions contain one or more active agents useful for managing elevated intraocular pressure (IOP) in the eye. Relatively hydrophilic, and preferably carboxylated, polymeric materials such as PLGA are used for a drug such as timolol maleate, which is relatively water soluble, to increase drug loading. Higher molecular weight polymers, as well as the ratio of LA (which has a longer degradation time, up to one to two years) to GA (which has a short degradation time, as short as a few days to a week), are used to provide release over a longer period of time.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R11 and R12 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q5, R1, R2, R3, Z1 and Z2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention relates to a novel pharmacological treatment of bacterial infectious diseases in humans. Specifically the invention relates to the use of apramycin of formula (I) or apramycin derivatives to treat bacterial infectious diseases in humans. It is demonstrated that apramycin surprisingly does not have the expected high level of toxicity observed with related aminoglycoside antibiotics but actually is even significantly less toxic than compounds already used in human medicine such as gentamicin.

Abstract: In some aspects, the present invention provides aminoglycoside derivatives thereof that exhibit antibacterial activity. In some aspects, the aminoglycoside derivatives comprise compounds consisting of (a) an ammoglycoside group and (b) at least one hydrophobic carbamate and alkoxy group to the primary or secondary hydroxy position of the aminolvcoside group and salts thereof.

Abstract: Described are agrochemical compositions, comprising (a) esters and/or amides of pyroglutamic acid, and (b) biocides. The compositions are clear and exhibit an improved stability even when stored at temperatures between 5° and 40° C. over a longer period.

Abstract: A pharmaceutical composition containing at least one ?-lactam antibiotic, at least one ion-chelating agent, at least one buffer component, and at least one aminoglycoside antibiotic.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Z1, Z2, Z3, Z4, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention discloses polypeptides with antibacterial properties and use said polypeptides and/or polynucleotides encoding said polypeptides in the preparation of medicament for the treatment of infectious diseases. The inventors also provide vectors encoding and adapted for expression of the polypeptides and polynucleotides of the invention. The vectors may be used in the preparation of a medicament for the treatment of bacterial infections. Further, the vector of the invention may be used to reduce the load of bacteria in food and/or feed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Q1 and Q2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Methods for treating a bacterial infection in a mammal in need thereof, and compositions related thereto, are disclosed, the methods comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound and a second antibacterial agent.

Abstract: The invention relates to a new pharmaceutical composition, a method of treatment of infection and also a process to prepare the composition. The infectious complications are important causes of morbidity and mortality. Hospital acquired pneumonia (HAP) remains the most severe nosocomial infection in intensive care units. Beta-lactams alone are always considered inadequate when P. aeruginosa and/or methicillin-resistant S. aureus are implicated as pathogens or copathognes. The present invention provides the desired empirical therapy for control of all bacterial infections. The invention provides antibiotic combination products for delivering at least two different antibiotics, through parenteral dosage form comprising protein-synthesis-inhibiting antibiotic which is amikacin or its sulphate salt and non-protein-synthesis-inhibiting antibiotic which is cefepime or its hydrochloride salt. The invention provides a total solution, against multiresistant P. aeruginosa, or Acinetobacter spp.

Abstract: The invention provides a tobramycin formulation for delivery by aerosolization in the form of additive-free, isotonic solution whose pH has been optimised to ensure adequate shelf-life at room temperature. Said formulation can be advantageously used for the treatment and prophylaxis of acute and chronic endobronchial infections, in particular those caused by the bacterium Pseudomonas aeruginosa associated to lung diseases such as cystic fibrosis.

Abstract: An aminocarboxylic acid chelating agent, preferably EDTA, or a salt thereof has been found to be useful for inhibiting particulate formation in piperacillin/tazobactam parenteral combinations. The composition may also contain a buffer, preferably citrate, and optionally an aminoglycoside. The product may be in the form of a frozen composition that can be thawed for use. The product may also be in the form of a cryodesiccated powder that can be reconstituted by addition of an aqueous vehicle to reform a solution.