Abstract: The present invention concerns tablet formulations of fosfomycin trometamol, methods of manufacturing and using thereof. More specifically, it relates to an oral pharmaceutical composition in tablet form comprising or consisting of: a. fosfomycin trometamol; b. a low moisture diluent selected from the group consisting of anhydrous calcium hydrogen phosphate, anhydrous microcrystalline cellulose and combinations thereof; c. optionally, a lubricant; and d. optionally, other pharmaceutically acceptable excipients.

Abstract: The present invention relates to dressings such as bandages improved extensibility. The present invention further relates to dressings comprising an absorbent body and backing layer having improved extensibility.

Abstract: Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, L1, L2, G1, G2 and G3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

Abstract: A method of degrading bilirubin in skin is provided. The method involves identifying a target portion of skin where a reduction in bilirubin level is desired, and applying a vitamin B3-containing, low-pH composition to the target portion of skin during a treatment period. The composition contains an effective amount of a vitamin B3 compound, has a pH of less than 5.0, and reduces bilirubin level in the target portion of skin during the treatment period. The amount of vitamin B3 compound and the pH of the composition may be selected to provide a synergistic reduction in bilirubin level, as compared to the reduction in bilirubin level provided by the same composition at a neutral pH.

Abstract: The invention discloses novel endocrine treatment phytochemicals which affect androgenic status. The method for treatment of 5-alpha-reductase responsive diseases using four novel 5-alpha-reductase inhibitor compounds; leucoanthocyanidin, glabrene, glabridin, and alpha-terpineol is disclosed. Glabridin does not interfere with normal testosterone to androgen receptor binding.

Abstract: It is an object of the present invention to provide a novel therapeutic agent for demyelinating disease which has an action to suppress demyelination of nerve axons. According to the present invention, a therapeutic agent for demyelinating disease which comprises cyclic phosphatidic acids, carba-cyclic phosphatidic acids, thia-cyclic phosphatidic acids, or a salt thereof is provided.

Abstract: Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, L1, L2, G1, G2 and G3 are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.

Abstract: Oral care compositions comprising: (a) a peroxide complex comprising a peroxide component and an N-vinyl heterocyclic polymer (e.g., poly-N-vinyl polylactam, or poly-N-vinyl-polyimide); (b) a whitening agent (e.g., hydrogen peroxide); and (c) an orally acceptable carrier. In one embodiment, the carrier comprises a film forming material. Methods are also provided for making an oral care composition comprising: (a) mixing a whitening agent, silicone adhesive and carrier fluid to form a homogenous mixture; (b) adding a peroxide complex to said homogenous mixture, wherein said complex comprises hydrogen peroxide and an N-vinyl heterocyclic polymer; and (c) mixing under vacuum.

Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

Abstract: An improved method for identifying the size, shape and duration of drug exposure necessary to improve drug treatment in a subject with a bacterial infection. In addition, an improved method for identification of new dosing strategies which optimize the probability of positive treatment outcomes in subjects using resistance inhibitory concentration (RIC), wherein the subject has a bacterial infection caused by a bacterium with a propensity for heteroresistance. Further, an improved method for decreasing the potential for on-therapy drug resistance by determining a patient's RIC prior to administration of fosfomycin treatment, wherein RIC is utilized to differentiate the parameter which is best related to the driver or index of fosfomycin efficacy for the resistant subpopulation present and the required inhibitory concentration of those mutants.

Abstract: The present invention provides compositions comprising fosfomycin or a pharmaceutically acceptable salt, solvate or prodrug thereof (e.g., fosfomycin disodium) alone or in combination with an antibacterial agent. The present invention provides methods of treating bacterial infections, which include administering an effective amount of fosfomycin or a pharmaceutically acceptable salt, solvate or a prodrug thereof (e.g., fosfomycin disodium) alone or in combination with an antibacterial agent.

Abstract: Disclosed are primers, probes, and single nucleotide polymorphisms (SNP) specific to a distinct subclones of the E. coli sequence type 131 (ST131). Also disclosed are methods and assay kits useful in detecting the presence of the distinct subtype of E. coli and methods of treating a subject suffering from an infection from a subclone of ST131.

Abstract: Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.

Abstract: The main object of the present invention relates to a novel crystalline form of Fosemprenavir Calcium designated as Form A. Another object of the present invention relates to a process for the preparation of Crystalline Form A of Fosemprenavir Calcium. Yet another object of the present invention relates to crystalline Forma A of Fosemprenavir Calcium characterized by a PXRD diffraction having reflections at about 3.1±0.2, 4.4±0.2, 5.0±0.2, 6.3±0.2, 7.4±0.2, 8.0±0.2, 2?.

Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass median aerodynamic diameter predominantly between 1 to 5?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

Abstract: An ascorbic acid derivative composition of a first aspect according to the present invention consists of a salt of a compound (1) represented by a general formula (1) shown below; and a salt of a compound (2) represented by a general formula (2) shown below, wherein a ratio of the salt of the compound (2) with respect to a total amount of the salt of the compound (1) and the salt of the compound (2) is from 0.1 to 10% by mass, wherein R1 represents a linear or branched alkyl group of 6 to 20 carbon atoms, R2 represents a linear or branched alkyl group of 6 to 20 carbon atoms, and R1 and R2 are the same or are different from each other.

Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

Abstract: Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium.

Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

Abstract: The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 a linker; R3 is a spacer group; R4 is hydrogen, alkyl, aryl, or heterocyclic; or R4 and R1, or R4 and R3, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl.

Abstract: An object of the present invention is to provide a W/O/W emulsion having temporal stability, which comprises a water soluble active component in an inner aqueous phase, and a method for producing the same. This invention makes it possible to provide a W/O/W emulsion having temporal stability by incorporating a water soluble active component in an inner aqueous phase, a solid oil component and a silicone surfactant in an oil phase, and a water soluble polymer in an outer aqueous phase.

Abstract: A topical composition and its use for the prophylaxis and the treatment of defects connected to inflammatory dermopathies. Particularly, a topical composition including at least an alum, 18-?-glycyrrhetic acid and/or one derivative thereof, and vitamin A and/or one derivative thereof, and the use of such composition for the prophylaxis and the treatment of inflammatory dermopathies, preferably of the seborrhoeic dermatitis and of those affections in which the presence of an excess of sebum occurs.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: A process for delivering and/or removing metal from a biological system by loading a titanate sorbent with a biometal either before introduction into the system for delivery to a site within the system or after introduction into the system for delivery to a site where there is an excess accumulation of metal and thereafter the sorbent is loaded at the site with the excess metal and is removed from the system.

Abstract: Provided are a method for detecting respiratory infection associated with bacterial infection, a method for selecting patients with respiratory infection to receive an antibiotic, and a method for determining the timing for ending administration of an antibiotic to a patient with respiratory infection receiving the antibiotic, wherein said methods are characterized in that they are able to appropriately select patients with respiratory infection to whom the antibiotic is to be administered, to adjust the administration period of the antibiotic, and to treat respiratory infection associated with bacterial infection, and in that a measured value of sCD14-ST in urine is used as an indication.

Abstract: The present invention relates to novel aromatic thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: Methods of determining a subject's ototoxicity risk from administration of a pharmacotherapeutic compound having an ototoxicity risk, methods of administering a pharmacotherapeutic compound having an ototoxicity risk and oligonucleotides, peptide nucleic acids, arrays, and addressable collections for performing embodiments of the methods are provided herein.

Abstract: The present invention relates to allene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.

Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.

Abstract: A product comprising at least one given antibiotic and a calixarene for use as medicament.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: There is described a composition comprising a therapeutically active imidazole, and derivatives thereof, and an agent active on a bacterial cell surface selected from the group consisting of one or more of colistin, nisin, D-cycloserine, fosfomycin, fosfomycin trometamol, fosfomycin disodium and polymixin B, and derivatives thereof.

Abstract: A personal care composition is disclosed comprising a di-amido gellant, wherein the di-amido gellant has a formula: wherein R1 and R2 are aminofunctional end-groups which may be the same or different, and L is a linking moiety of molecular weight from 14 to 500 g/mol. The personal care composition may take a variety of forms such as a leave-on composition or an emulsion and/or may comprise one or more actives or agents.

Abstract: The present invention relates to a solid fosfomycin pharmaceutical composition stable in front the coloration, suitable for diabetics and not entailing gastrointestinal problems. The pharmaceutical composition of this invention comprises fosfomycin trometamol, glycine, and optionally other excipients as sucralose, silice dioxide, polyvinylpyrrolidone and flavor; and is substantially free from sugars and sugar alcohols as sucrose, fructose, glucose, xylitol, mannitol, sorbitol or mixtures thereof.

Abstract: Methods are disclosed for treating glaucoma by treating a novel target. Methods for treating glaucoma by restoring the filtration capabilities of the endothelial lining of Schlemm's canal are provided. A method for identifying compounds capable of restoring the filtration capability of the juxtacanalicular meshwork is also provided.

Abstract: Hypoxia activated prodrugs, such as, e.g., TH-281, TH-302, and TH-308, are useful for the treatment of various blood cancers, such as acute leukemias, chronic leukemias, MDS, MF, and multiple myeloma.

Abstract: Methods are disclosed for treating glaucoma by treating a novel target. Methods for treating glaucoma by restoring the filtration capabilities of the endothelial lining of Schlemm's canal are provided. A method for identifying compounds capable of restoring the filtration capability of the juxtacanalicular meshwork is also provided.

Abstract: A skin external preparation containing an ascorbic acid-2-phosphate derivative is characterized in that only a sodium ascorbic acid-2-phosphate-6-palmitate is formulated as the ascorbic acid-2-phosphate derivative, and the skin preparation further includes at least one betaine-type amphoteric surfactant selected from the group consisting of compounds represented by the following general formula (1) or (2) (wherein R1 represents a linear or branched alkyl group of 6 to 30 carbon atoms, and R2 represents a linear or branched alkyl group of 8 to 30 carbon atoms).

Abstract: Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.

Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: Methods and compositions for detection of drug resistant pathogens and treatment against infections thereof are provided. Methods for detection of oseltamivir-resistant influenza viruses by competitive binding assays utilizing non-oseltamivir influenza virus neuraminidase inhibitors and oseltamivir carboxylate are provided. Influenza virus neuraminidase inhibitors coupled to sensors and useful for employment in the methods of the invention are disclosed. Novel phosphonate compounds active as neuraminidase inhibitors against wild-type and oseltamivir-resistant influenza strains of H1N1, H5N1 and H3N2 viruses are disclosed. An enantioselective synthetic route to preparation of these phosphonate compounds via sialic acid is provided.

Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.

Abstract: There is proposed herein a process for production of composite antimicrobial and vulnerary preparations for external administration, featuring a higher therapeutic efficiency in case of skin and soft tissues infections treatment. The proposed compositions include an active agent being fosfomycin and finely dispersed nanostructured silica dioxide, with a weight ratio of (25-75 mass. %):(75-25 mass. %) respectively. The mentioned production process includes mixing fosfomycin with finely dispersed nanostructured silica dioxide. The process is distinct in that the mixture of aforementioned substances with the mentioned weight ratio is exposed to mechanical processing by blow impact and abrasive actions until a portion of the fine powder fraction with particles smaller than 5 micrometers, contained in the mixture, increases to at least 40%.

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 an active agent being fosfomycin and finely dispersed nanostructured silica dioxide, with a weight ratio from 10:1 to 75:1 respectively. The mentioned production process includes mixing fosfomycin with finely dispersed nanostructured silica dioxide. Its main difference is that the mixture of aforementioned substances with the mentioned weight ratio is exposed to mechanical processing by blow impact and abrasive actions until a portion of the fine powder fraction with particles smaller than 5 micrometers, contained in the mixture, increases to at least 25%. The so obtained mixture is used for injection preparations.

Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.