Abstract: The present invention is directed to an aqueous pharmaceutical composition, particularly an aqueous ophthalmic composition, suitable as an injection, particularly an intravitreal injection. The composition includes a biologic therapeutic agent (e.g., an isolated monoclonal antibody that specifically binds to a C5 protein) that tends to raise the viscosity of the composition and a guanidine and/or guanidine derivative (e.g., L-arginine) that tends to lower the viscosity of the composition.

Abstract: A liposomal drug composition comprising: a dimeric or polymeric guanidine derivative or a pharmaceutically acceptable salt thereof as drug substance, and a lipid modified by polyethylene glycole (PEG). The drug composition have cytostatic and antimicrobial activity.

Abstract: Provided herein are methods and compositions for the treatment of motor neuron diseases including, for example, amyotrophic lateral sclerosis. Suitable therapeutic agents include, for example, agents that up-regulate the expression IGF-II or guanine deaminase in a cell.

Abstract: The present invention relates to stable salts of creatine imino sugar amides and an inorganic or organic acid endowed with enhanced nutritional and/or therapeutical efficacy in respect to their individual effects and to solid compositions containing such salts, particularly suited to oral and parenteral administration. Methods of preparation and use of these compositions are also provided.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.

Abstract: The use of polyhexamethylene guanidine hydrochloride as preservative for preventing and controlling citrus sour rot and its application are disclosed by the present invention. The citrus preservative calculated by 100% total mass fraction comprises 0.05%-0.5% polyhexamethylene guanidine hydrochloride, 0.05%-0.2% of one or more selected from the group consisting of a mixture of several of the following: 0.05%-0.2% imidazole fungicidebactericide, benzimidazole fungicidebactericide, pyrimethanil, fludioxonil and [or] azoxystrobin, and 0.02%-0.15% polyethenoxy ether emulsion or quaternary ammonium salt emulsion, and the rest is water. The citrus preservative can significantly inhibit the decay of citrus fruit such as Citrus microcarpa during storage, especially the incidence of sour rot. So the commercial value of citrus is obviously increased.

Abstract: Cycling of ApoE4 isoform is promoted in a person in need thereof by contacting the person with an effective amount of a pharmaceutically-acceptable modulator of intracellular ApoE4 transport vesicle pH.

Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.

Abstract: The invention provides to a family of aryl guanidine—based F1F0—ATPase inhibitors, e.g., mitochondrial F1F0—ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.

Abstract: Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Abstract: The present invention provides synergistic biocidal composition such as a synergistic detergent composition for use e.g. in disinfection and cleaning.

Abstract: The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrein, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.

Abstract: This invention provides a method of inactivating human noroviruses and other acid stable viruses. The method includes the step of contacting the virus with a virucidally-enhanced alcoholic composition that includes an alcohol, and an enhancer selected from cationic oligomers and polymers, chaotropic agents, and mixtures thereof.

Abstract: The present invention relates to compounds, intermediates used in the preparation of such compounds, processes for the preparation of such compounds of the formula VI and formula VII and such intermediates, pharmaceutical compositions comprising such compounds of the formula VI and such compounds of the formula VII, and the uses of such compounds of the formula VI and such compounds of the formula VII as antidiabetic, pre-antidiabetic, antiobesity and cardioprotective agents.

Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.

Abstract: The invention relates to medicine, in particular to sanitary and hygiene, more specifically to methods for producing a disinfecting agent for decontaminating different types of water, including drinking water. The inventive disinfecting agent producing method by dissolving quaternary ammonium compounds in water in the presence of an active additive in the form of guanidines, consists in preparing an aqueous 1-15% guanidine solution by permanently agitating it at a temperature ranging from 30 to 90° C., in cooling the solution accompanied with a precipitation control, when the precipitation process is over, in filtering the solution by using a filter whose cell size ranges from 10 to 1 mkm and in adding the quaternary ammonium compounds into the solution in such away that the concentration thereof in said solution is equal to 0.1-3%.

Abstract: Compounds produced by combining imino sugars and creatine are herein disclosed. The compounds being in the form of a creatine imino sugar amides and produced by the disclosed methods; protecting the guanidine group of creatine and then activating the protected creatine with DCC and reacting it with an imino sugar, followed by removal of the guanidine protecting groups. The resulting creatine imino sugar amides have enhanced stability in solution as compared to related esters. In addition, specific benefits are conferred by the imino sugar in addition to, and separate from, the creatine substituent. Methods of preparation and use of these compounds are also disclosed.

Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.

Abstract: Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

Abstract: Wallboard and facing paper that provides increased mold resistance at lower biocide loadings. The biocide is: (a) an n-alkyl isothiazolinone such as octylisothiazolinone (OIT), a monohalo and dihalo substituted n-alkylisothiazolinone such as chloromethylisothiazolinone (CMIT) or dichlorooctylisothiazolinone (DCOIT), 3-iodo-2-propynyl-butylcarbamate (IPBC), chlorothalonil, methylene-bis-thiocyanate, or mixtures of two or more thereof; or (b) carbendazim and a second biocide selected from 3-iodo-2-propynyl-butylcarbamate (IPBC), diiodomethyltolylsulfone (DIMTS), sodium pyrithione, octylisothiazolinone (OIT), dichlorooctylisothiazolinone (DCOIT), and chlorothalonil.

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: A class of topomimetic calixarene-based peptide mimetics is described. Calixarene-based peptide mimetics have various biological activities such as, for example, bactericidal activity, antiangiogenic activity, and/or antitumor activity. Methods of use and methods of designing calixarene-based peptide mimetics are described.

Abstract: The invention relates to the use of creatine, creatinine and/or derivatives thereof and/or their salts in an agent for hardening, strengthening, restructuring or increasing the shine, volume or combability of keratin fibers, particularly of human hair.

Abstract: The invention relates to a sterile wound dressing having a backing and a nonabsorbent elastomer wound contact layer, wherein the elastomer matrix is formed by a synthetic three-block elastomer, preferably a copolymer of polystyrene block and polyolefin block (SEPS, SEBS, SEEPS, etc.) or mixtures thereof, wherein the total polymer content is less than 3.2 wt %, in particular 3.0 wt % or less, preferably 2.6 wt % or less, and is plasticized by an apolar oil and/or petroleum jelly.

Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.

Abstract: The present invention relates to antibacterial and antifungal compositions having 3-isothiazolone and polyhexamethyleneguanidine phosphate. These new antiseptic compositions demonstrate a superior degree of effectiveness on a wide spectrum of pathogens. The present invention also relates to the use of these new antiseptic compositions to kill and/or restrain the growth of bacteria and fungi in a variety of applications.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (for example, SEQ ID NO:86).

Abstract: The invention concerns the use of guanabenz and its derivatives for making drugs for treating cystic fibrosis and diseases related to a protein addressing deficiency in the cells, said derivatives corresponding to formula (I), wherein: R?H or C1 and the phenyl group comprises two substituents, or a pharmaceutically acceptable salt of said derivatives.

Abstract: The present invention relates to a protein, ADAM10, ADAM10 nucleic acid sequences and ADAM10 proteins encoded by these sequences that are involved in infection by one or more pathogen such as a virus, a parasite, a bacteria or a fungus or are otherwise associated with the life cycle of a pathogen.

Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.

Abstract: Pancreatic islet dysfunction, in both type 1 and type 2 diabetes results, in part, from cytokine-mediated inflammation leading to iNOS generation and the death of pancreatic islets. The production of pro-inflammatory cytokines involved in the generation of iNOS is facilitated by the availability of the hypusine-containing translational factor eIF5A, necessary for the maturation of antigen-presenting cells. Treatment with agents capable of interfering with the mRNA translating iNOS or with agents that can interfere with the hypusination of eIF5A, prevents the death of islets, lowers blood glucose levels, avoids insulin resistance, and generally avoids the inflammatory response in islets associated with type 1 and type 2 diabetes.

Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.

Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.

Abstract: A method of treating or preventing an immune disorder, such as graft versus host disease, in a subject. The method includes the administering a SHIP1 inhibitor, such as 3?-aminocholestane, to a subject in need of treatment. Thus, SHIP1 inhibitors taught herein represent a novel class of small molecules that have the potential to enhance allogeneic transplantation, boost innate immunity and improve the treatment of hematologic malignancies.

Abstract: Compositions, methods and systems for treating disordered epithelial tissues, such as is caused by pathogens and/or by toxins produced thereby. The invention relates to the use of an anti-infective and/or antimicrobial active agent in a carrier, with vigorous agitation of the disordered epithelial tissue for topical treatment thereof under such conditions sufficient to achieve clinically discernable improvement of the disordered epithelial tissue. The preferred anti-infective and/or antimicrobial active agent comprises an organohalide, such as a quaternary ammonium halide compound, preferably benzalkonium chloride. The inventive compositions and methods may employ the use of an applicator adapted for use in promoting the penetration of the treatment composition and/or the vigorous agitation of the disordered tissue.

Abstract: The present invention is based on the discovery of a cell-based system to identify novel modulators of splicing or splicing dependent processes. The cell-based system of the present invention utilizes a fast and highly sensitive reporter, that responds to defects in the splicing machinery itself and is sensitive to changes in the signals that regulate splicing dependent processes such as those that modulate the EJC, splicing-dependent export, localization or translation efficiency. The present invention further uses the cell-based screen to identify several small molecules that modulate both constitutive and alternative splicing. Accordingly, the present invention includes general or alternative splicing inhibitors identified using the assay described herein. The present invention also provides methods of treating a subject having a condition associated with aberrant target RNA expression.

Abstract: A drug composition containing as a drug substance a polymeric guanidine derivative based on a diamine containing oxyalkylene chains between two amino groups, with the guanidine derivative representing a product of polycondensation between a guanidine acid addition salt and a diamine containing polyalkylene chains between two amino groups, as well as the pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to the use of at least one ether guanidine of the general formula (I) and/or of a salt or hydrate thereof, in which R1?—CH2—CH2—CH2—O—R3, where R3 is a linear or branched hydrocarbon radical having 6 to 22 carbon atoms, and R2?H or an optionally branched hydrocarbon radical which has 1 to 22 C atoms and which optionally comprises double bonds, for reducing the growth of microorganisms, and to cosmetic and pharmaceutical formulations comprising at least one ether guanidine of the general formulae (I).

Abstract: Disclosed are complexes of an antipneumocystic compound and an antimalarial compound, processes for their preparation, pharmaceutical compositions and methods of using said complexes or compositions for the treatment and/or prophylaxis of parasitic infections.

Abstract: The present invention relates to stabilized 123I-labelled radiopharmaceutical compositions having a stabilizer which comprises gentisic acid or a salt thereof with a biocompatible cation. Methods of preparation of the stabilized radioiodine compositions as well as the use of gentisic acid to stabilize 123I-labelled radiopharmaceutical at a specified radioactive concentration range are also described.

Abstract: The present invention relates to compounds, compositions, methods and/or kits for determining and/or predicting and/or diagnosing and/or treating restenosis in a patient.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Methods of using phenformin to treat certain types of cancers are described.

Abstract: Compositions, methods and systems for treating disordered epithelial tissues, such as is caused by pathogens and/or by toxins produced thereby. The invention relates to the use of an anti-infective and/or antimicrobial active agent in a carrier, with vigorous agitation of the disordered epithelial tissue for topical treatment thereof under such conditions sufficient to achieve clinically discernable improvement of the disordered epithelial tissue. The preferred anti-infective and/or antimicrobial active agent comprises an organohalide, such as a quaternary ammonium halide compound, preferably benzalkonium chloride. The inventive compositions and methods may employ the use of an applicator adapted for use in promoting the penetration of the treatment composition and/or the vigorous agitation of the disordered tissue.

Abstract: The invention relates to the use of endogenous metabolites to produce a metabolic profile of a disorder or disease in a subject, e.g. an autoimmune disease, in particular rheumatoid arthritis, and the analysis of such metabolic profiles in order to find disturbances in such profiles in a subject which are caused by or correlated with the said diseases or disorders. Such disturbances can be normalised by treatment of the subject with specified compounds, particularly N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine or an aminoguanidine.

Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.