Abstract: The disclosure provides a method of producing a pharmaceutical composition. The method comprises (a) dissolving an active pharmaceutical ingredient (API) in a liquid vehicle to form a liquid medicament; (b) contacting the liquid medicament with a pharmaceutical carrier; (c) contacting the composition comprising the liquid medicament and pharmaceutical carrier with a pharmaceutical coating material to form a liqui-mass composition; and (d) pelletising the liqui-mass composition to form the pharmaceutical composition.

Abstract: A dry pharmaceutical composition is provided that is suitable for respiratory tract delivery of levodopa and DDI for treatment of Parkinson's disease or Parkinson syndrome. The dry pharmaceutical composition comprises levodopa, a dopa decarboxylase inhibitor (DDI) and at least one excipient. A unit dosage form of the dry pharmaceutical composition and a method of treating a patient with Parkinson's disease or Parkinson syndrome by administering the dry pharmaceutical composition are also provided.

Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.

Abstract: The invention relates to an oral polymeric pharmaceutical dosage form which comprises a thermoresponsive eutectic composition which is solid at or about room temperature and fluid at or about body temperature, the eutectic composition mixed together with a crosslinking agent and an active pharmaceutical ingredient (API) to form an API loaded region; and a porous polymeric composition at least partially surrounding the API loaded region to protect the API when the dosage form is in a stomach of the human or animal body, the porous polymeric composition allowing the ingress of water to contact the crosslinking agent thereby facilitating the crosslinking agent to cause crosslinking of the porous polymeric composition, which crosslinked porous polymeric composition allows controlled egress of API via egress of fluid thermoresponsive eutectic composition at the intestine. In a preferred embodiment, the dosage form further comprises a coating there around.

Abstract: Methods for improving the ability of a population of biological agents to compete and survive in a field setting are provided. By improving the population of biological agents, the modified population of agents is able to grow, compete with other microbial strains and fungi, and provide protection for plants from pathogens. In particular, modified biological agents and modified populations of such agents that are herbicide tolerant or resistant are selected or engineered. In this manner, the protection from disease-causing agents is enhanced. Such modified populations of biological agents can be added to soils to prevent fungal pathogens and the diseases they cause promoting plant growth. Therefore, the present invention is useful for enhancing the competitiveness of modified biological agents particularly over other microbial agents which are not herbicide resistant.

Abstract: The present invention relates to processes for preparing the compounds of general formula I, wherein the groups R1 and R3 are defined according to claim 1. Furthermore this inventions relates to intermediates obtained in these processes.

Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer, stereoisomer or deuterated analogue thereof, wherein X, R, R1, R2, R3, R4, M1, M2, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

Abstract: A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.

Abstract: The present invention relates to chemical total synthesis methods of six novel protein tyrosine phosphatase-1B (PTP1B) inhibitors and application of the inhibitors in the preparation of medicaments for treating type 2 diabetes mellitus (T2DM). The PTP1B inhibitors use one or more of the six compounds represented by the structural formulae 1, 2, 3, 4, 5 and 6, as active components. The compounds can enhance the sensitivity of an insulin receptor by inhibiting the activity of PTP1B, thereby having a favorable therapeutic effect on insulin-resistant T2DM.

Abstract: The present invention provides novel aspirin derivatives useful for preventing and/or treating cancer. The novel compounds of this invention may be particularly useful for the prevention and/or treatment of cancers affecting the gastrointestinal system, such as colorectal cancer.

Abstract: The present invention relates to chemical total synthesis methods of six novel protein tyrosine phosphatase-1B (PTP1B) inhibitors and application of the inhibitors in the preparation of medicaments for treating type 2 diabetes mellitus (T2DM). The PTP1B inhibitors use one or more of the six compounds represented by the structural formulae 1, 2, 3, 4, 5 and 6, as active components. The compounds can enhance the sensitivity of an insulin receptor by inhibiting the activity of PTP1B, thereby having a favorable therapeutic effect on insulin-resistant T2DM.

Abstract: This invention provides compounds having a structure of Formula (I). Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.

Abstract: The present invention relates to a use of a graft copolymer obtainable by free-radical polymerization of a monomer mixture comprising N-vinyllactam, vinyl ester, and a polyether for increasing the activity of a pesticide. The invention also relates to a composition comprising a pesticide and a graft copolymer obtainable by free-radical polymerization of a monomer mixture comprising i) 30 to 80% by weight of N-vinylpyrrolidone, N-vinylcaprolactam or mixtures thereof, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether. It further relates to a method for preparing said composition by mixing the pesticide and the graft copolymer and to a method for controlling phytopathogenic fungi and/or undesired plant growth and/or undesired attack by insects or mites and/or for regulating the growth of plants.

Abstract: The present invention provides novel 2,6-diisopropyl phenol2,6-diisopropyl phenol analogs and sterile, stable pharmaceutical compositions of 2,6-diisopropyl phenol 2,6-diisopropyl phenol and analogs thereof useful as an antioxidant in the treatment of ischemic injury including stroke and other cerebral injury. 2,6-diisopropyl phenol or its analogs are administered in a dosage effective to produce blood levels and brain levels of the drug that can prevent free radical damage associated with ischemic injury.

Abstract: A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.

Abstract: The present invention provides therapeutic agents for a cancer resistant to a protease inhibitor which comprises, as an active ingredient, a benzoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom or the like; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof as a heat shock protein 90 (Hsp90) family protein inhibitor, and the like.

Abstract: Fenofibric acid formulations comprising 105 mg of fenofibric acid are described as well as methods of use thereof. Dosage forms include, for example, immediate-release dosage forms.

Abstract: Disclosed is 1) a method for greatly increasing the solubility of useful actives in siloxane matrix-forming preparations, and 2) the associated preparations, themselves. Volatilizing coagents are utilized to give novel gels containing heretofore siloxane-insoluble additives.

Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.

Abstract: In one embodiment, a personal-care composition in the form of a water-in-oil emulsion comprises at least about 10% of a non-polar silicone oil; from about 0.1% to about 10% of a first oil-soluble solid sunscreen; and from about 0.1% to about 10% of a second oil-soluble solid sunscreen. The weight ratio of the first sunscreen to the second sunscreen may be from about 0.8 to about 2.0, or from about 1.0 to about 1.5. The first sunscreen may be oxybenzone. The second sunscreen may be avobenzone. The composition may further comprise a skin-care active selected from the group consisting of a vitamin B3 compound, a sugar amine, a peptide, a hexamidine compound, and combinations thereof. In another embodiment, the invention relates to a method for improving the solubility of a second oil-soluble solid sunscreen in the oil phase of a water-in oil emulsion.

Abstract: The present invention relates to compositions which, in sprayable or form, are suitable as wound sealants for woody plants. The invention also relates to a method of protecting woody plants from infection with phytopathogenic fungi, in particular ESCA infection, using such wound sealants. These compositions comprise: a) a water-insoluble sealing agent in dissolved or dispersed form, which is selected among film-forming water-insoluble polymers, waxes and their mixtures; b) at least one plant protectant, c) at least one volatile diluent, in particular an aqueous diluent, and, if appropriate, d) at least one nonionic surface-active substance in an amount of from 10 to 100% by weight, in particular 10 to 80% by weight, based on the sealing agent.

Abstract: Fenofibric acid formulations comprising 105 mg of fenofibric acid are described as well as methods of use thereof. Dosage forms include, for example, immediate-release dosage forms.

Abstract: Fenofibric acid formulations comprising 105 mg of fenofibric acid are described as well as methods of use thereof. Dosage forms include, for example, immediate-release dosage forms.

Abstract: The present invention provides a pharmaceutical composition comprising a combination of an Hsp 90 family protein inhibitor and at least one compound, the said pharmaceutical composition wherein the Hsp 90 family protein inhibitor is a benozoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl, or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like], or a prodrug thereof; or a pharmaceutically acceptable salt thereof, and the like.

Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.

Abstract: The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.

Abstract: Fenofibric acid formulations comprising 105 mg of fenofibric acid are described as well as methods of use thereof. Dosage forms include, for example, immediate-release dosage forms.

Abstract: The invention provides para substituted dialkylphenol derivatives of propofol. The invention further provides pharmaceutical compositions comprising such analogs, methods for preparing such analogs, and methods of using such analogs to induce general anesthesia, sedation, and/or hypnotic or sleep effects in a patient.

Abstract: Compounds and methods useful in the control, treatment, and prevention of fungal activity, of the following formula: where R1-3 are independently H, alkyl, methyl, acyl, halogen, phenyl, R4 is H, alkyl, methyl, acyl, alkoxy, halogen, phenyl provided that when R3 is methyl and R4 is H, R1 and R2 are not both H; and stereoisomers, analogs, and pharmaceutically acceptable salts thereof.

Abstract: A reagent and related method for use in passivating a biomaterial surface, the reagent including a latent reactive group and a bifunctional aliphatic acid (e.g., fatty acid), in combination with a spacer group linking the latent reactive group to the aliphatic acid in a manner that preserves the desired function of each group. Once bound to the surface, via the latent reactive group, the reagent presents the aliphatic acid to the physiological environment, in vivo, in a manner (e.g., concentration and orientation) sufficient to hold and orient albumin.

Abstract: A method for attenuating free radical formation resulting from a bodily insult includes the step of administering bicarbonate to the body of a subject. The bicarbonate is administered at a dosage of at least 1.5 mEq/kg of body weight within a 24-hour period.

Abstract: The use of a pharmaceutical formulation in treating coronary arteriosclerosis and a two-component pharmaceutical formulation. The pharmaceutical formulation contains peroxidic species or reaction products resulting from oxidation of an alkene, such as geraniol, by an oxygen-containing oxidizing agent, such as ozone; a penetrating solvent, such as dimithyl sulfoxide; a dye containing a chelated metal, such as hematoporphyrin; and an aromatic redox compound, such as benzoquinone.

Abstract: The benzophenone derivative of combretastatin A-1, designated “hydroxyphenstatin”, was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted to a sodium phosphate prodrug by dibenzyl phosphite phosphorylation and subsequent benzyl cleavage: Hydroxyphenstatin and the prodrugs thereof were found to be a potent inhibitor of tubulin polymerization and to demonstrate surprisingly effective antineoplastic activity against a series of human cancer cells and murine P388 lymphocytic leukemia cells.

Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which comprises a

Abstract: Fungicidal mixtures, comprising

Abstract: A fungicidal composition comprises an acceptable carrier and/or surface active agent and a synergistically effective amount of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; and at least one compound of formula II in which Ar and R8 have the meaning given. The composition is useful in a method of controlling the growth of phytopathogenic fungi at a locus. The method comprises applying synergistically effective amounts of (a) and (b) to the locus.

Abstract: The invention relates to a method of combating phytopathogenic diseases on crop plants which comprises applying to the crop plants or the locus thereof being infested with said phytopathogenic disease an effective amount of a combination of a) a benzophenone of formula I  wherein R1 is methoxy or methyl, R2 is C1-C4alkoxy or 2-halogenbenzyloxy, R3 is C1-C4alkoxy, R4 is C1-C4alkyl, halogen or trifluoromethyl, and R5 is hydrogen, halogen, C1-C4alkoxy, trifluoromethyl or nitro; in association with b) a compound selected from the group comprising compounds of formulae II, III, IV, V, VI, VII, VIII, IX, X and XI as described herein.

Abstract: The benzophenone derivative of combretastatin A-1, designated “hydroxyphenstatin”, was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted to a sodium phosphate prodrug by dibenzyl phosphite phosphorylation and subsequent benzyl cleavage: Hydroxyphenstatin and the prodrugs thereof were found to be a potent inhibitor of tubulin polymerization and to demonstrate surprisingly effective anti neoplastic activity against a series of human cancer cells and murine P388 lymphocytic leukemia cells.

Abstract: The invention comprises a method of combating phytopathogenic diseases on crop plants which comprises applying to the crop plants or the locus thereof being infested with said phytopathogenic disease an effective amount of a combination of

Abstract: The invention relates to method for the enhancement of the activity and/or systemicity of fungicidal compositions containing at least one benzoylbenzene of formula I wherein R1 through R7, m and n are as defined in claim 1, with the aid of one or more adjuvants selected from the group consisting of (a) alkylpolyglycosides, alkenyl succinic acid derivatives, dialkyl sulfosuccinates, polyvinylpyrrolidones, perfluoroalkyl acids derivatives, perfluoro(C3-20)alkyl esters of carboxylic acids, and mixtures thereof; (b) alkoxylated alcohols, amines or acids; (c) water-immiscible polar aprotic solvents; and to the use of such a composition as a fungicide.

Abstract: The invention relates to method for the enhancement of the activity and/or systemicity of fungicidal compositions containing at least one benzoylbenzene of formula I wherein R1 through R7, m and n are as defined in claim 1, with the aid of one or more adjuvants selected from the group consisting of (a) alkylpolyglycosides, alkenyl succinic acid derivatives, dialkyl sulfosuccinates, polyvinylpyrrolidones, perfluoroalkyl acids derivatives, perfluoro(C3-20)alkyl esters of carboxylic acids, and mixtures thereof; (b) alkoxylated alcohols, amines or acids; (c) water-immiscible polar aprotic solvents; and to the use of such a composition as a fungicide.

Abstract: The invention relates to a stable emulsifiable concentrate (EC) for crop protection active compounds which comprises (a) one or more crop protection active compounds, (b) 150 to 500 g/l of one or more adjuvants, (c) optionally one or more organic, non-polar solvents, (d) an emulsifying surfactant system forming an oil in water emulsion when the formulation is added to water, which essentially consists of one or more non-ionic surfactants, and one or more anionic surfactants, (e) a water-miscible polar aprotic solvent or one or more dimethyl dicarboxylates, and (f) optionally an antifoam agent, and to the use of such a suspension as a pesticide.

Abstract: A reagent and related method for use in passivating a biomaterial surface, the reagent including a latent reactive group and a bifunctional aliphatic acid (e.g., fatty acid), in combination with a spacer group linking the latent reactive group to the aliphatic acid in a manner that preserves the desired function of each group. Once bound to the surface, via the latent reactive group, the reagent presents the aliphatic acid to the physiological environment, in vivo, in a manner (e.g., concentration and orientation) sufficient to hold and orient albumin.

Abstract: This invention discloses an orally administered pharmaceutical composition for the treatment of elevated levels of cholesterol and related conditions comprising a statin and fenofibrate in the form of microparticles of solid fenofibrate that are stabilized by phospholipid as a surface active substance, wherein a therapeutically effective amount of the composition provides the statin and a quantity of fenofibrate to a fasted human patient that is greater than 80% of the quantity of fenofibrate provided by the same amount of the composition when administered to the same patient who has been fed a high fat meal.

Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which comprises a

Abstract: Fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of (a) at least one azolopyrimidine of formula I  in which R1, R2, L1, L2 and L3 have the meaning given in claim 1; and (b) at least one fungicidal active ingredient selected from benomyl, carboxin, captan, chlorothalonil, copper oxychloride, cyprodinil, dimethomorph, dithianon, dodine, famoxadone, fenhexamid, fenpiclonil, fenpropimorph, fluazinam, mancozeb, metalaxyl, pyrimethanil, quinoxifen, sulfur, triforine, vinclozolin, a fungicidal triazole derivative, and a synthetic strobilurine derivative. The invention also provides a method of controlling the growth of phytopathogenic fungi at a locus by applying synergistically effective amounts of at least one azolopyrimidine of formula I and at least one fungicidal active ingredient (b) to the locus.

Abstract: The invention relates to a novel fungicidal composition comprising a fungicidally acceptable carrier and/or surface active agent together with, and synergistically effective amounts of (a) at least one benzophenone of formula I  wherein R1, R2, R3, R4, R5, R6, R7, m and n have the meaning given; at least one fungicidal active ingredient selected from the following groups (A), (B), (C), (D) and (E): (A) an ergosterol biosynthesis inhibitor; (B) a strobilurine derivative, (C) a melanin biosynthesis inhibitor; (D) a compound selected from the group consisting of acibenzolar, benomyl, captan, carboxin, chlorothalonil, copper, cyprodinil, dinocap, dithianon, dimethomorph, dodine, ethirimol, famoxadone, fenpiclonil, fluazinam, mancozeb, metalaxyl, pyrifenox, sulfur, vinclozolin and (E) an azolopyrimidine of formula II  in which R8, R9, R10, R11, A, L and p have the meaning given; and to a method of controlling the growth of phytopathogenic fungi at a locus which

Abstract: A method of combating phytopathogenic diseases on crop plants includes applying to the crop plants or the locus thereof being infested with a phytopathogenic disease an effective amount of a combination of a) (E,E)-&agr;-(methoxyimino)-2-[[[[1-[3 (trifluoromethyl)phenyl]ethylidene]amino]oxy]methyl]-benzeneacetic acid methyl ester of formula I  in association with b) a benzophenone of formula II  wherein R1 is hydrogen, halogen, C1-5alkyl or CF3; R2 is halogen, C1-5alkyl or CF3; R3 is C1-5alkyl or optionally substituted benzyl; and R4 is C1-5alkyl.

Abstract: A method of combating phytopathogenic diseases on crop plants includes applying to the crop plants or the locus thereof being infested with a phytopathogenic disease an effective amount of a combination of a) (E,E)-&agr;-(methoxyimino)-2-[[[[1-[3(trifluoromethyl)phenyl]ethylidene]amino]oxy]methyl]-benzeneacetic acid methyl ester of formula I  in association with b) a benzophenone of formula II  wherein R1 is hydrogen, halogen, C1-4 alkoxy or NO2; and R2 is C1-6 alkyl or optionally substituted benzyl.