Abstract: The present disclosure relates generally to certain compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of a Retroviridae infection, including an HIV infection.

Abstract: The present invention relates to water treatment. In one embodiment there is provided a method of treating an aqueous system to inhibit growth of one or more micro-organisms therein and/or to reduce the number of live micro-organisms therein. The method comprises adding treatment agents to said aqueous system and wherein said treatment agents comprise: (a) a phosphonium compound; and (b) an oxazolidine compound.

Abstract: Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.

Abstract: Provided are biocidal compositions comprising: a hydroxymethyl-substituted phosphorus compound and an isothiazolinone compound selected from 1,2-benzisothiazolin-3-one, 2-methyl-1,2-benzisothiazolin-3-one, and mixtures thereof. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.

Abstract: The invention relates to a method for the prevention and removal of H2S and/or other sulfhydryl compounds and iron sulfide deposits from gas and/or liquid streams in industrial process systems. Formulations comprising aldehydes, aldehyde donors, and/or aldehyde stabilizers, excluding triazines, in combination with the reaction product of an amino acid and a hydroxymethylphosphine or hydroxymethylphos-phonium salt, and optionally a quaternary ammonium compound and/or one or more N-hydrogen compounds such as 5,5-dialkylhydantoin or amines, are rapidly and sustainedly scavenging H2S originating from process and/or microbial sources. The formulations possess high capacities for H2S removal and are relatively pH-insensitive.

Abstract: A stabilized composition is disclosed which contains at least two biocides, particularly at least two non-oxidizing biocides. In one embodiment, the composition contains a phosphonium sulfate compound combined with a dialkyl dimethyl quaternary amine compound. In order to stabilize the composition, an alkyl trimethyl ammonium compound is added to the composition. In one embodiment, the stabilizing agent produces a single phase composition. With the aid of the stabilizing agent, the single phase concentrated compositions can be produced that can later be diluted for use. In one embodiment, the composition may be used to treat aqueous systems in industrial applications.

Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

Abstract: A biocidal composition comprising tributyl tetradecyl phosphonium chloride and tetrakis(hydroxymethyl)phosphonium sulfate at a weight ratio of 2:1 to 1:10, and its use for the control of microorganisms in aqueous and water-containing systems.

Abstract: Provided are biocidal compositions comprising: a hydroxymethyl-substituted phosphorus compound and 2-(decylthio)ethanamine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.

Abstract: Systems and methods for controlling microbial growth and/or activity in a gas field fluid or oil field fluid are provided, comprising: a) adding a first biocide component to the gas field fluid or oil field fluid in an amount effective to control microbial growth and/or activity; and b) after a delay, adding a second biocide component to the gas field fluid or oil field fluid.

Abstract: Described herein are methods of inhibiting or reversing the progression of presbyopia in an eye by administering a ?L-crystallin electrostatic interaction inhibitor. Presbyopia is caused by aggregation of the soluble crystalline lens proteins called the crystallins, particularly ?L-crystallin. It has been found that the aggregation of ?L-crystallin is an electrostatic phenomenon and that electrostatic interaction inhibitors can be employed to prevent the formation of ?L-crystallin aggregates as well as to deaggregate already formed aggregates.

Abstract: The disclosure provides compounds and methods to treat a microbial or a bacterial pathogenesis, and demonstrates that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.

Abstract: The present invention relates to purified 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt thereof, and a method for preparing such compound. The compound has at least 90% (w/w) purity. The present invention is also directed to a pharmaceutical composition comprises the purified compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation, inflammatory-related disorders, or pain, by administering 3-methanesulfonylpropionitrile or a pharmaceutically acceptable salt or solvate thereof to a subject in need thereof.

Abstract: This invention relates to a process for the co-encapsulation of biocidally active ingredients in a clay mineral, the process comprising the step of bringing the clay mineral into contact with a biocidally active nitrogen compound that contains at least one hydrocarbon group with 6 to 20 carbon atoms, and at the same time or subsequently with at least one biocidally active compound selected from the group consisting of 2-n-octyl-4-isothiazoline-3-one, 3-iodopropenylbutyl-carbamate and tetrahis(hydroxymethyl)phosphonium sulfate. And the use of such encapsulated product in water based paints, coatings and varnishes.

Abstract: Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents. In addition compositions and methods for mitigating or preventing a novel form of chemotherapy-induced peripheral neuropathy are disclosed and claimed.

Abstract: Compositions and methods for inhibiting sulfide biogeneration from biofilms are described, as well as methods for preparing the compositions. The compositions comprise anthrahydroquinone and a biocide. The compositions may also include anthraquinone.

Abstract: The current invention relates to a process for stabilising a phosphorus-containing compound aqueous composition, comprising the step of adding to said composition an efficient arsenic stabilizing amount of a compound selected from the group consisting of ammonia, ammonium salt, organic amino acid, peptide and polypeptide; application of the stabilized composition for treating an aqueous system optionally containing or in contact with metal sulphide scale, which method comprises adding to said system, separately or together, an efficient anti-scale amount of a stabilized aqueous composition or for treating a water system to kill or inhibit the growth of micro organisms comprising applying thereto or forming in situ an efficient inhibiting amount of the stabilized aqueous composition.

Abstract: The present invention provides methods and formulations for reducing or inhibiting increase in the concentration of microbes in a water-based fluid. The methods and formulations of the present invention use an oxazolidine compound and a hydroxymethyl-substituted phosphorus compound selected from the group consisting of tetrakis(hydroxymethyl)phosphonium salts, C1-C3 alkyl- and alkenyltris(hydroxymethyl)phosphonium salts and tris(hydroxymethyl)phosphine. The methods and formulations of the present invention can be useful in treating water contaminated with aerobic or anaerobic bacteria in oilfield, natural gas field, and other industrial applications.

Abstract: The disclosure provides compounds and methods to treat bacterial pathogenesis, and demonstrates that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.

Abstract: The present invention relates to compositions containing signal transduction modulator compounds, to methods for treating or preventing inflammation, or promoting healthy joints, using the compounds and to kits for the same.

Abstract: In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.

Abstract: The present invention concerns the use of oxygen antagonists and other active compounds for inducing stasis or pre-stasis in cells, tissues, and/or organs in vivo or in an organism overall, in addition to enhancing their survivability. It includes compositions, methods, articles of manufacture and apparatuses for enhancing survivability and for achieving stasis or pre-stasis in any of these biological materials, so as to preserve and/or protect them. In specific embodiments, there are also therapeutic methods and apparatuses for organ transplantation, hyperthermia, wound healing, hemorrhagic shock, cardioplegia for bypass surgery, neurodegeneration, hypothermia, and cancer using the active compounds described.

Abstract: The present invention concerns the use of oxygen antagonists and other active compounds for inducing stasis or pre-stasis in cells, tissues, and/or organs in vivo or in an organism overall, in addition to enhancing their survivability. It includes compositions, methods, articles of manufacture and apparatuses for enhancing survivability and for achieving stasis or pre-stasis in any of these biological materials, so as to preserve and/or protect them. In specific embodiments, there are also therapeutic methods and apparatuses for organ transplantation, hyperthermia, wound healing, hemorrhagic shock, cardioplegia for bypass surgery, neurodegeneration, hypothermia, and cancer using the active compounds described.

Abstract: Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.

Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. (I) [wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or branched alkylene group. B ring and C ring are selected from benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle. D is —(CH2)(n+1)—, —(CH2)-O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— (wherein: D ring is connected with the carbon atom composing C ring.) E is selected from oxygen atom or sulfur atom. P is phosphine atom. R1˜R7 (wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle. R1, R2 and R3 are not hydrogen atom if B ring is benzene ring.) may be the same or different and are substituents. R8 and R9 are may be the same or different and are substituents. R10 is alkyl group. n and m are 0-10. o is 0-2.

Abstract: This invention relates to a method of treating a patient suffering from ionizing radiation exposure, or of treating a patient about to undergo ionizing radiation therapy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents as inhibitors of phosphodiesterase 5 cardiovascular disorders

Abstract: Methods and compositions are provided for preventing, reducing and reversing ischemic neuronal damage related to congenital and acquired ophthalmologic conditions such as macular degeneration, retinitis pigmentosa, optic neuritis, neuroretinitis, Lebers congenital amaurosis, Stargardts disease, Parkinson's disease, diabetic retinopathy, idiopathic senile vision loss, uveitis, edema and ocular surgery. An amount of an acetylcholine esterase inhibitor containing composition is administered to the eye of a mammal, either topically or via a controlled-release drug delivery system.

Abstract: Methods and compositions for altering the viability of cells, particularly cancers in animals and humans are disclosed. The compositions of the present invention are formed from a set of components comprising one or more of the following: a dithiocarbonyl, preferably dithiocarbamate, compound; a divalent metal ion; a modulator of cellular glutathione levels; and an inhibitor of the phosphorylation of choline. The compositions described herein induce a relatively selective and rapid effect on the viability of cancer cells by inducing a mixture of apoptotic and necrotic cell death, with the dominant pathway being apoptosis. Particularly preferred active compositions comprise all four components, although combinations of fewer components can be fully effective in certain tumors.

Abstract: The invention relates to novel compounds of genera formula (I), with inhibitory properties for the type B botulism toxin activity, the methods for preparation thereof and corresponding pharmaceutical compositions. The invention further relates to corresponding pharmaceutical compositions.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain active compounds that together have unexpectedly good insecticidal and acaricidal properties.

Abstract: Compounds are described which modulate the tzrosine kinase activity of p56lck and signal transduction pathways in which this enzyme is involved. The invention also relates to compounds which have immunomodulatory activity, e.g., which have immunosuppressant or immunostimulatory activity, and/or which have an antineoplastic effect. The invention further relates to compositions comprising these compounds, and methods of using them.

Abstract: The invention provides methods of inhibiting cerebral amyloid angiopathy. The invention further provides methods of treating a disease state characterized by cerebral amyloid angiopathy in a subject with an A&bgr;40 inhibitor having the structure: Q-[—SO3−X+]n or Q-[—OSO3−X+]n wherein Q is a carrier group; X+ is a cationic group; and n is one.

Abstract: The invention relates to an insecticidal and miticidal composition which contains as active ingredients chlorfenapyr in combination with one or more organophosphoric acid ester-type compounds and to a method for controlling insecticidal or miticidal pests which have acquired resistance to commercial insecticidal and miticidal agents.

Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.

Abstract: This invention relates to a method of treating patients afflicted with atherosclerosis or to prevent the development of atherosclerosis in patients assessed to be high risk of developing the disease. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: An oxidizing species is described herein as a reaction product through an in situ preparation combining a protonizable phosphorus or sulfur compound, and a halide source at controlled proportions in an aqueous, non-aqueous, gel, aerosol, solid-phase or powdered media. The oxidizing species can be used to reduce microbial and viral populations on a surface or object or in a body or stream of water. The invention thus finds applications as a bleach, sanitizer, oxidant, or in any other application in which an oxidizing agent can be beneficially used alone or in a formulation.

Abstract: This invention relates to a method of treating patients afflicted with osteoporosis. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: Formulations and methods for reducing the unwanted toxicity and complications associated with treatments for diabetes mellitus. The formulations include co-formulations of an anti-diabetic agent and a toxicity reducing agent of the formula described in the specification. The methods include administration of effective amounts of the anti-diabetic agent and the toxicity reducing agent to safely treat the diabetic patient.

Abstract: A series of substituted sulfonamide derivatives have been prepared and may be used to treat antiviral infections, especially infections caused by orthopoxviruses.

Abstract: The present invention relates to acetylenic aryl sulfonamide thiols which act as inhibitors of TNF-&agr; converting enzyme (TACE). The compounds of the present invention are useful in disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: The present invention relates to a method of treating angiogenesis in tumor conditions in a mammal suffering therefrom which comprises administering to a mammal in need thereof an effective amount of a cyclic compound selected from the group consisting of cyclopentane, cyclohexane, cycloheptane, monosaccharide, disaccharide, trisaccharide, tetrasaccharide, piperidine, tetrahydrothiopyran, 5-oxotetrahydrothiopyran, 5,5-dioxotetrahydrothiopyran, tetrahydroselenopyran, tetrahydrofuran, pyrrolidine, tetrahydrothiophene, 5-oxotetrahydrothiophene, 5,5-dioxotetrahydrothiophene, tetrahydroselenophene, benzene, cumene, mesitylene, naphthalene and phenanthrene, in which said cyclic compound is substituted by at least three vicinal phosphorus containing radicals of the formula: 1

Abstract: There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1′ pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.

Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.

Abstract: This invention relates to a method of treating patients suffering from the inflammatory bowel disorders. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: Isophosphoramide mustard analogs useful for treating cancer are provided.

Abstract: This invention relates to a method of treating patients afflicted with acute renal failure. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: This invention relates to a method of treating patients afflicted with diabetic neuropathy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.

Abstract: To reduce the toxic effect of carboplatin, particularly myelosuppression and emesis, a dithioether having the formula R.sub.1 -(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.m --R.sub.2 (I) wherein:each of R.sub.1 and R.sub.2 individually is SO.sub.3 H or PO.sub.3 H.sub.2 ; andeach of m and n is individually 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, preferably disodium 2,2'-dithiobis(ethane sulfonate) (dimesna), is administered in combination with carboplatin to a patient, at substantially the same time or sequentially, whereby the dithioether and the carboplatin become co-present in the blood of the patient. Compositions comprising carboplatin and the dithioether are included in the invention.