Abstract: This invention provides cross-linked glycopeptides—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to a method of treatment of bacterial infections including administering an effective amount of an oral time-dependent antibiotic to a human or warm blooded animal.

Abstract: Methods for treating perioral dermatitis are described herein. The method includes administering topically a composition containing an effective amount of a systemic or topical antibiotic and a corticosteroid. The concentration of the antibiotic is from about 0.01% to about 5% by weight of the composition and the concentration of the corticosteroid is from about 0.01% to about 5% by weight of the composition. The composition can contain one or more pharmaceutically acceptable excipients and/or carriers. The compositions can be formulated as a lotion, cream, gel, ointment, paste, powder, solution, suspension, spray, foam, or patch.

Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.

Abstract: Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60% of the antibiotic in about 30 minutes and not less than about 70% of the antibiotic after 8 hours when subjected to in vitro dissolution study or when tested in vivo. Further, the compositions of the present invention which when tested in a group of healthy humans provide a mean peak plasma concentration (Cmax) after at least about 0.5 hour of administration of the dosage form.

Abstract: A non-disintegrating, non-eroding, non-bioadhesive and non-swelling oral controlled release pharmaceutical composition and process for preparation of such compositions is provided which comprises at least one high dose water soluble active ingredient, at least one diluent, at least one binder, and a polymer system comprising of at least one release controlling polymer wherein the composition formulated into a suitable dosage form maintains its geometric shape even after the drug has diffused from the dosage form and provides the concentrations of active ingredient above effective levels for extended periods of time, optionally with other pharmaceutically acceptable excipients. The compositions preferably comprise antibiotic(s) as active ingredient, more preferably Amoxicillin or its pharmaceutically acceptable salts, hydrates, polymorphs, esters, and derivatives thereof, most preferably amoxicillin sodium, either alone or in combination with other antibiotic(s).

Abstract: The invention is intended for a treatment of severe infections using an injectable drug-delivery system comprising nanoparticles of a biodegradable polymer with incorporated antibacterial drug.

Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and intermediates useful for the synthesis of compounds of formula (I).

Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

Abstract: This invention is directed to graft materials comprising an extracellular matrix (ECM) and therapeutic agents. This invention is also directed to methods of using the graft materials for healing of damaged or diseased tissues on a patient's body.

Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.

Abstract: The invention relates to a pharmaceutical composition comprising at least one first active therapeutic substance selected among carveol, thymol, eugenol, borneol, carvacrol, alpha-ionone, beta-ionone, as well as isomers, derivatives and mixtures thereof, and comprising at least one second active therapeutic substance that is an antibiotic.

Abstract: Compositions and methods for identifying polyribonucleotides that binds with high affinity to a metallo-?-lactamase. The polyribonucleotides inhibit the activity of the metallo-?-lactamase.

Abstract: Cyclooxygenase (COX2) and inducible nitric oxide synthase (iNOS) are two major inflammatory mediators. Inducible NOS specifically binds to COX2 and S-nitrosylates it, enhancing COX2 catalytic activity. Selectively disrupting iNOS—COX2 binding prevents NO-mediated activation of COX2. The synergistic molecular interaction between two inflammatory systems permits assays for developing anti-inflammatory drugs.

Abstract: This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses.

Abstract: This invention provides cross-linked glycopeptide—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: The present invention is directed to a method of treating respiratory disorders by delivering an aerosol composition of an antibiotic drug to the lung alveoli.

Abstract: A method of treating an individual exhibiting at least one symptom of a mental disorder is provided which comprises administering to the individual an antimicrobial composition in an amount effective to inhibit or eliminate the at least one symptom of the disorder. This invention also pertains to a method of treating an individual exhibiting at least one symptom of a mental disorder by administering a probiotic mixture to replenish gastrointestinal microbes.

Abstract: An amino acid in solution is precipitated with concentrated hydrochloric acid and isolated as the dihydrochloride monohydrate. Said dihydrochloride is redissolved and reprecipitated by adding a solvent.

Abstract: Disclosed is a floating sustained release pharmaceutical dosage form including a drug that is adapted to release the drug over an extended period of time. The buoyant pharmaceutical dosage form provides extended gastric residence time of the formulation so that substantially all of the drug is released in the stomach over an extended period. The pharmaceutical dosage form is formulated with low molecular weight concentrated milk proteins to provide buoyancy to the dosage form which can float in gastric fluid for an extended period, including up to about 48 hours.

Abstract: A topical skin composition containing a dipeptide compound represented by formula (1) or a salt of the dipeptide: wherein R1 represents a hydrogen atom, an alkyl group, an alkanoyl group, or —CH(R6)COOR7 (wherein R6 represents a hydrogen atom or a lower alkyl group, and R7 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group); R2 represents a hydrogen atom or an alkyl group which may have a substituent; R3 represents a lower alkyl group or a phenyl group; R4 represents a hydrogen atom or a lower alkyl group, and may form a heterocyclic ring together with R5 and an adjacent nitrogen atom; R5 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, and may form the heterocyclic ring together with R4; X represents —COOR8 (wherein R8 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group) or —SO3H; and n is an integer of 0-4; and a pharmaceutically acceptable carrier

Abstract: A substantially taste masked liquid pharmaceutical composition containing a pharmaceutically effective amount of an unpleasant tasting drug dissolved or dispersed in an aqueous excipient base, said excipient base comprising polyvinyl pyrrolidone and/or copolyvidone, and high molecular weight polyethylene glycol.

Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.

Abstract: Use of organic compounds containing the —ONO2 function, or inorganic compound containing the —NO group or compositions comprising said compounds to reduce the toxicity caused by drugs to the gastrointestinal and/or renal apparatus, said compounds being characterized in that they are nitric oxide NO donors i.e., when they are put into contact in vitro with cells of the vasal endothelium or platelets.

Abstract: The present invention relates to a vaccine for the prevention of lactic acidosis in a vertebrate, said vaccine comprising at least one isolated microorganism, or fragment or fragments thereof, wherein said microorganism is capable of producing lactic acid within the gut of said vertebrate, and wherein said microorganism is selected from the group consisting of: Clostridium-like species, Prevotella-like species, Bacteroides-like species, Enterococcus-like species, Selenomonas species, non-dextran slime producing Streptococcus species and non-slime producing lactic acid bacterial isolates.

Abstract: A method for improving blood cholesterol and its conjugates levels in a mammal, which is based on the administration of steroidal plant hormone 24-epibrassinolide.

Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2?-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), wherein R1 and R2 are each independently hydrogen, (C1-C10)alkyl, (C2-C10)alkenyl, (C2-C10)alkenyl, (C3-C8)cycloalkyl, (C1-C10)alkoxy, (C1-C10)alkanoyl, (C1-C10)alkanoyloxy, (C1-C10)alkoxycarbonyl, aryl, heterocycle, halo, cyano, nitro, —COORe, —C(?O)NRfRg, —OC(?O)NRfRg, NRfRg, or —S(O)nRh; R3 is hydrogen, halo, aryl, heteroaryl, —S(O)nRh, or —CH?CHC(?O)NRmRp; R4 is hydrogen; A is thio, sulfinyl, or sulfonyl; and intermediates useful for the synthesis of compounds of formula (I).

Abstract: The invention provides pharmaceutical compositions comprising compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts. The pharmaceutical compositions are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal.

Abstract: This invention relates generally to the production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals. Advantageously, the inorganic used is calcium sulfate.

Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.

Abstract: Methods for Cystic Fibrosis disease assessment in an individual comprise detecting the presence or absence of outer membrane protein in a sample from an individual or the methods comprise detecting the presence or absence of outer membrane protein antibodies in a sample from an individual. Methods for treating anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease comprise detecting the presence of outer membrane protein in a sample from an individual; and selecting a therapy regimen for the individual based on the presence of OprF, wherein the anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease are treated by the therapy regimen or the methods comprise detecting the presence of outer membrane protein antibodies in a sample from an individual; and selecting a therapy regimen for the individual based on the presence of OprF antibodies; wherein the anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease are treated by the therapy regimen.

Abstract: A composite is disclosed having a controlled rate of dissolution. The composite includes (a) a first region that includes a first composition that includes calcium sulfate, the first region exhibiting a first rate of dissolution; and (b) a second region that includes a second composition that includes calcium sulfate, the second region exhibiting a second rate of dissolution, the first rate of dissolution being different from the second rate of dissolution.

Abstract: Embodiments of the invention generally provide pharmaceutical drug compositions, methods of preparing oral drug compositions, such as extended release dosage compositions, and methods for treating infection. More particularly, the invention relates to formulations containing a drug and a carrier material. In one aspect, the invention provides a pharmaceutical formulation including a therapeutically active agent, from about 0.1% to about 4.9% by weight of a pharmaceutically acceptable polymer, and from about 0.1% to about 30% by weight of a pharmaceutically acceptable acid, wherein the pharmaceutical composition have a zero order release profile of the therapeutically active agent. In another aspect, the invention provides methods for preparing and administering a pharmaceutical antibiotic composition in oral dosage form, such as a tablet.

Abstract: A fullerene-antibiotic conjugate including at least one antibiotic molecule per fullerene moiety. The fullerene may comprise C60 and the antibiotic may comprise vancomycin or may be selected from the group consisting of penicillins, cephalosporins, quinolones, fluoroquinolones, macrolides, lincosamines, carbepenems, conobactams, aminoglycosides, glycopeptides, tetracyclines, sulfonamides, rifampin, oxazolidonones, and streptogramins. The conjugate preferably includes at least two and more preferably at least three antibiotic molecules per C60 center. A method for making a fullerene(C60)-antibiotic conjugate, comprises: synthesizing a linker precursor (I); reacting the linker precursor (I) with C60 via a Bingel-reaction, to produce a fullerene-linker conjugate (II); hydrolyzing the fullerene-linker conjugate (II), resulting in a desired derivative of C60 (III); and reacting the derivative (III) with a desired antibiotic to produce a fullerene-antibiotic conjugate (IV).

Abstract: Administration of &bgr;-Lactam compounds, including &bgr;-lactam antibiotics and &bgr;-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.

Abstract: A pharmaceutical composition is provided comprising a vehicle that comprises (a) an amphipathic oil that is water dispersible and ethanol insoluble, (b) microcrystalline wax, and (c) a pharmaceutically acceptable non-aqueous carrier; and having an antibacterial substance in an antibacterially effective amount stably dispersed in the vehicle. The composition is suitable for administration by intramammary infusion to a milk producing animal for treatment and/or prevention of mastitis or other diseases of the udder, as well as for otic administration for treatment and/or prevention of an ear infection.

Abstract: A method is provided for treatment of an infective condition in a fluid-containing organ having a natural exterior orifice, such as the udder of a milk producing animal or an ear. The method comprises administering an antibacterial agent to the organ via the exterior orifice and administering in combination therapy with the antibacterial agent a second agent that is an anti-inflammatory agent, an analgesic and/or an antipyretic. The antibacterial agent and, optionally, the second agent, are administered as a pharmaceutical composition further comprising a vehicle that comprises an amphipathic oil that is water dispersible and ethanol insoluble, microcrystalline wax and a pharmaceutically acceptable non-aqueous carrier. Also provided is such a composition comprising the antibacterial agent and the second agent.

Abstract: The present invention is directed to sanitizing compositions or preparations comprising of a combination of an alcohol-based, volatile biocide and an additional low-concentration, non-volatile antimicrobial agent. In one embodiment of the present invention, the sanitizer preparation comprises a surface sanitizing composition or preparation comprised of at least: (1) a biocide comprising a volatile alcohol at a concentration of from greater than or equal to 30% to less than or equal to 70% w/w; and (2) one or more non-volatile antimicrobial agent that is soluble in said alcohol at a concentration of from greater than or equal to 0.001% to less than or equal to 0.1% w/w.

Abstract: The invention provides methods and compositions for treatment of bacterial infections. Methods of the invention include administration of dalbavancin for treatment of a bacterial infection, in particular a Gram-positive bacterial infection of skin and soft tissue. Dosing regimes include once weekly administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection.

Abstract: A device for releasing a therapeutic agent in the body space in the form of a prosthetic joint implant having a first portion such as a stemmed portion for contacting bone tissue in an intramedullary canal of a long bone. The implant has a second portion which extends into the body space such as a joint space. The joint component contains a reservoir filled with a bioabsorbable/resorbable polymer which includes a therapeutic agent. The reservoir is open or in contact with the joint space as the body fluid diffuses in and out of the polymeric device it carries the drug into the joint space.

Abstract: Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases.

Abstract: This invention relates to a method for coating a medical device comprising the steps of applying to at least a portion of the surface of said medical device, an antimicrobial coating layer and a non-pathogenic bacterial coating layer, wherein the antimicrobial and non-pathogenic bacterial coating layers inhibit the growth of pathogenic bacterial and fungal organisms. The non-pathogenic bacterium used in the bacterial coating layer is resistant to the antimicrobial agent. Furthermore, the non-pathogenic bacterium layer includes at least one of the following: viable whole cells, non-viable whole cells, or cellular structures or extracts. The antimicrobial agent and non-pathogenic bacterium are used to develop a kit comprising these compositions in one container or in separate containers. The kit is used to coat a catheter prior to implantation in a mammal.

Abstract: A method of treating an individual exhibiting at least one symptom of a mental disorder is provided which comprises administering to the individual an antimicrobial composition in an amount effective to inhibit or eliminate the at least one symptom of the disorder. This invention also pertains to a method of treating an individual exhibiting at least one symptom of a mental disorder by administering a probiotic mixture to replenish gastrointestinal microbes.

Abstract: The present invention provides methods and compositions useful for preventing bacteremia by decolonizing the intestinal tract of a patient. Although the present invention is useful for preventing bacteremia by any Gram-positive bacteria, it is particularly useful against antibiotic-resistant bacteria, such as vancomycin-resistant Enterococcus (VRE), methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide intermediary susceptible Staphylococcus aureus (GISA), and penicillin-resistant Streptococcus pneumoniae (PRSP). Decolonization therapy using the methods and compositions of this invention are also useful for preventing a Gram-negative bacteremia.

Abstract: Provided, among other things, is a method of treating or ameliorating pulmonary infection in a cystic fibrosis patient comprising pulmonary administration of an effective amount of a liposomal/complexed antiinfective to the patient, wherein the (i) administrated amount is 50% or less of the comparative free drug amount, or (ii) the dosing is once a day or less, or (iii) both.

Abstract: The present invention relates to novel Death Domain Containing Receptor-5 (DR5) proteins which are members of the tumor necrosis factor (TNF) receptor family, and have now been shown to bind TRAIL. In particular, isolated nucleic acid molecules are provided encoding the human DR5 proteins. DR5 polypeptides are also provided as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying antagonists and antagonists of DR5 activity.

Abstract: A composition comprising:

Abstract: Catacholate beta-lactam conjugates, methods for producing these compounds, and compositions containing these compounds useful as siderophores or for treatment of bacterial infections are provided.

Abstract: Biodegradable microspheres implanted, injected, or otherwise placed totally or partially within the body are capable of near-linear controlled release of an antibiotic for a predetermined period of time for the treatment and prevention of infections involving the body. The microspheres are formed of polylactic-co-glycolic acid (PLGA) and an effective amount of antibiotic sufficient to produce bactericidal levels in body tissues, and may or may not include polyethylene glycol (PEG). The microspheres exhibit near-linear delivery of the antibiotic for at least 4 weeks at levels exceeding the minimum inhibitory concentration (MIC) for organisms commonly found to be the cause of infections.