Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: With the subject invention, a method is provided for preparing a filter membrane including the steps of dispersing a liquid which is generally hydrophobic into the pores of a porous membrane, and applying a solution containing lipids onto at least a first surface of the porous membrane containing the liquid. Advantageously, the subject invention allows for filter membranes to be prepared which can be stored for periods of time without degradation in performance. The subject invention may have applicability in various contexts, but is well-suited for preparing filter membranes for permeability screening, particularly Parallel Artificial Membrane Permeability Assay (PAMPA).

Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).

Abstract: The present invention relates to compounds of formula I and to compounds of formula II wherein the substituents have various meanings. These compounds are useful as beta lactamase inhibitors.

Abstract: The invention describes a composition for combating beta-lactamase-mediated antibiotic resistance using beta-lactamase inhibitor useful for injection, capable of pharmaceutical application. The invention relates to pharmaceutical composition containing ceftriaxone (normally as ceftriaxone sodium) and sulbactam (normally as sulbactam sodium). Such compositions are found to be useful for intramuscular or intravenous administration as antibiotics for hospitalized patients with serious infections. Specifically, this invention relates to a pharmaceutical composition further including an aminocarboxylic acid chelating agent, for example, ethylenediaminetetraacetic acid (EDTA), or a pharmaceutically acceptable salt thereof. The pharmaceutical compositions of this invention have been found normally to enhance resistance to particulate formation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use.

Abstract: The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.

Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.

Abstract: New monobactam antibiotics compounds which contain an 3-amino-azetidin-2-one ring and are active against gram-negative bacteria, wherein the compounds include the compound 2-(2-amino-thiazol-4-yl)-2-[(Z)-(1H,4H-1,5-dihydroxy-4-oxo-pyridin-2-yl)methoxyimino]-N-[3(S)-1-oxysulfonyl-2,2-dimethyl-4-oxo-azetidin-3-yl]acetamide.

Abstract: Disclosed is a method of treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject. SIBO-caused conditions include irritable bowel syndrome, fibromyalgia, chronic pelvic pain syndrome, chronic fatigue syndrome, depression, impaired mentation, impaired memory, halitosis, tinnitus, sugar craving, autism, attention deficit/hyperactivity disorder, drug sensitivity, an autoimmune disease, and Crohn's disease. Also disclosed are a method of screening for the abnormally likely presence of SIBO in a human subject and a method of detecting SIBO in a human subject. A method of determining the relative severity of SIBO or a SIBO-caused condition in a human subject, in whom small intestinal bacterial overgrowth (SIBO) has been detected, is also disclosed.

Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.

Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.

Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).

Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.

Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a

Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.

Abstract: Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as ?-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ?-lactamases. These compounds restore/potentiate the activities of ?-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ?-lactamases.

Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

Abstract: Methods of sepsis in a sample from a patient are provided. Methods of detecting changes in expression of one or more RNAs associated with sepsis are also provided. Compositions and kits are also provided.

Abstract: This invention describes a novel composition of matter describing a complex comprising leaf protein and a lipophilic substance(s), along with the method of producing it. Delivery of lipid-soluble materials into the body is challenging because they are generally highly insoluble in water and very subject to oxidative degradation. The inventors have found that leaf protein—the water-soluble proteins derived from plant leaves—can efficiently form a complex with lipophilic materials. This leaf protein—lipid-soluble material complex is an effective carrier of lipophilic substances. As such, the leaf protein—lipid-soluble material complex disclosed herein can be used for the delivery of lipophilic vitamins, fatty acids, caretenoids, lipophilic drugs, and other lipophilic materials. This complex can be used to deliver lipophiles in foods, nutritional and dietary supplements, topical compositions and in pharmaceutical products.

Abstract: The invention describes a composition for combating beta-lactamase-mediated antibiotic resistance using beta-lactamase inhibitor useful for injection, capable of pharmaceutical application. The invention relates to pharmaceutical composition containing ceftriaxone (normally as ceftriaxone sodium) and sulbactam (normally as sulbactam sodium). Such compositions are found to be useful for intramuscular or intravenous administration as antibiotics for hospitalized patients with serious infections. Specifically, this invention relates to a pharmaceutical composition further including an aminocarboxylic acid chelating agent, for example, ethylenediaminetetraacetic acid (EDTA), or a pharmaceutically acceptable salt thereof. The pharmaceutical compositions of this invention have been found normally to enhance resistance to particulate formation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use.

Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.

Abstract: The present invention provides for silk fibroin-based compositions comprising one or more antibiotic agents for prevention or treatment of microbial contamination, methods of making antibiotic-containing silk scaffold, methods of stabilizing antibiotics in silk scaffolds, and methods for preventing or treating microbial contamination using the antibiotic-containing compositions. Various methods may be used to embed the antibiotic(s) into the silk fibroin-based compositions. The antibiotic-containing compositions of the invention are particular useful for stabilizing antibiotics, preventing bacterial infections, and for medical implants, tissue engineering, drug delivery systems, or other pharmaceutical or medical applications.

Abstract: The invention generally relates to compositions and methods for preventing sternal wound infections, such as mediastinitis. In certain embodiments, the invention provides an antimicrobial composition including at least one bioresorbable polymer, such as a tyrosine-derived polyesteramide, and at least one antimicrobial agent, in which the composition is adapted to be topically applied to an esophageal perforation in a subject or a median sternotomy incision site in the subject, and in which the at least one antimicrobial agent is present in an amount effective to inhibit development of mediastinitis in the subject.

Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.

Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: This invention relates to a fulvic acid and antibiotic combination for use in the treatment of various diseases and conditions. The invention further relates to the use of the combination for the treatment of various diseases and conditions, including bacterial infection. In particular, the bacteria are antibiotic resistant bacteria.

Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.

Abstract: Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.

Abstract: A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).

Abstract: This invention discloses and claims methods for inhibiting bacterial ?-lactamases and treating bacterial infections by inhibiting bacterial ?-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a ?-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a ?-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.

Abstract: Inhibitors of the enzyme beta-lactamase are provided. The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.

Abstract: Particular aspects provide compositions and methods for treating or preventing bacterial infection or at least one symptom related to bacterial infection, and the like in a subject in need thereof by administering a therapeutic composition comprising at least one electrokinetically generated fluid (including gas-enriched electrokinetically generated fluids) as disclosed herein, the electrokinetically altered aqueous fluid suitable to alter cellular membrane structure or function sufficient to provide for modulation of intracellular signal transduction, wherein treating bacterial infection or at least one symptom related to bacterial infection is thereby afforded. In particular embodiments, the fluids are gas-enriched fluids or therapeutic compositions and methods, and include oxygen-enriched water optionally in combination with other therapeutic agents. Other embodiments include particular routes of administration or formulations for the gas-enriched therapeutic compositions.

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

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

Abstract: A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such deposition more safe, efficacious, controllable and predictable. The method of the invention is especially useful for enhancement of deposition of immunosuppressive agents in the lung(s) of transplant patients, improved tolerance of the drugs by reducing cough, and improving pulmonary drug deposition.

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: The present invention relates to the use of benzoic acid and/or its sodium salt in combination with saccharide(s) as active components in the manufacture of a vaginal composition for modulating vaginal flora and vaginal acidity, thereby maintaining the pH value of vaginal secretion within a range from 3.5 to 4.5; and the present invention further relates to a vaginal composition and a method for modulating and maintaining normal vaginal flora and vaginal acidity.

Abstract: The invention relates to prodrugs of sulopenem of formula (I): wherein R1 is —(C2-C8)alkyl, or a solvate or hydrate thereof. The invention also relates to the preparation, formulation, and use of the prodrugs of sulopenem to treat a disorder such as an infection in a patient in need thereof.

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: Prodrugs of 6-?-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.

Abstract: The present invention provides a compound of formula 1, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

Abstract: Compounds of formula I: 1

Abstract: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond tha

Abstract: Compound of formula I: 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 &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-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.

Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin to treat bacterial infection. In particular, this compound is a potent drug for the treatment of Mycobacteria infection.

Abstract: The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for anti-MRSA activity replaces the non-releaseable liphophilic side-chains found in 2-aryl and 2-benzothiazolylthio carbapenem compounds. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.