Abstract: The present invention relates to the novel use of Propineb for the physiological curative treatment under zinc deficiency. In addition to the physiological curative effect Propineb treatment results in higher yields even under conditions without zinc deficiency.

Abstract: The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.

Abstract: Disclosed are aspartic protease inhibitors represented by the following Formula: wherein R1, R2, R3, R4, R5, R6, R7a, R7b and n are as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods for treating an aspartic protease mediated disorder using the same.

Abstract: Agents that stimulate nuclear translocation of Nrf2 protein and the subsequent increases in gene products that detoxify and eliminate cytotoxic metabolites are provided in a method for treating glaucomatous retinopathy or optic neuropathy. The structurally diverse agents that act on the Nrf2/ARE pathway induce the expression of enzymes and proteins that possess chemically versatile cytoprotective properties and are a defense against toxic metabolites and xenobiotics. Agents include certain electrophiles and oxidants such as a Michael Addition acceptor, diphenol, thiocarbamate, quinone, 1,2-dithiole-3-thione, butylated hydroxyanisole, flavonoid, an isothiocyanate, 3,5-di-tert-butyl-4-hydroxytoluene, ethoxyquin, a coumarin, combinations thereof, or a pharmacologically active derivative or analog thereof.

Abstract: A crystalline form of a ?-aminobutyric acid analog, and methods of preparing same, are provided.

Abstract: The present application describes therapy with angiogenesis antagonists such as anti-VEGF antibodies. In particular, the application describes the use of such angiogenesis antagonists to treat end-stage liver disease and end-stage liver disease complications. The present application also describes the use of such angiogenesis antagonists to treat disorders of altered venous proliferation such hemorrhoids and varicose veins.

Abstract: This invention is directed to methods for controlling the duration of the depolarization and repolarization of the cardiac ventricle and therefore the QT interval, in therapeutically useful ways in a subject, comprising administering to the subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II), or a pharmaceutically acceptable salt or ester thereof: wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl, wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano.

Abstract: There are provided methods for controlling microbial or bioflim growth, comprising mixing a hypochlorite oxidant and at least one nitrogen-containing compound or salt thereof selected from a particular group of nitrogen-containing compounds and salts to form a biocide, and applying the biocide. Apparatus for practicing the methods are also provided.

Abstract: The invention relates to methods, compositions, and uses of those compositions for making medicaments, for potentiating the beneficial effects of inhibitors of COX-1, COX-2, and 5-LOX, and reducing adverse effects, by also administering inhibitors of soluble epoxide hydrolase (“sEH”), with or without also administering one or more cis-epoxyeicosantrienoic acids. The invention further relates to the use of inhibitors of sEH as analgesics and to methods and compositions of epoxides of eicosapentaenoic acid and docosahexaenoic acid, optionally with an inhibitor of sEH, to reduce pain or inflammation or both.

Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.

Abstract: The present invention provides methods and compositions for reducing pigmentation.

Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.

Abstract: A method of controlling (e.g., influencing or affecting) connexin 43 expression in a subject may include administering to the subject an effective amount of a pharmaceutically acceptable formulation. In some embodiments, controlling connexin 43 expression in a subject may effectively treat cardiac arrhythmia and/or cancerous and pre-cancerous cells in a subject. The pharmaceutically acceptable formulation may include a synthetic analog or derivative of a carotenoid. The subject may be administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include an acyclic alkene including at least one substituent and/or a cyclic ring including at least one substituent. In some embodiments, a carotenoid analog or derivative may include at least one substituent.

Abstract: An antimicrobial composition of 3-iodo-2-propynylbutyl carbamate (IPBC) and 1,3-butylene glycol (BG) as solvent, in a defined weight ratio, preferably 9-11% IPBC and 89-91% BG, and personal care formulations including the composition in an amount of about 0.1-0.2% therein, at a pH of 4-9, is described.

Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.

Abstract: Methods of reducing food intake and glucose production in a mammal, or restoring hepatic autoregulation are provided. The methods involve increasing long-chain fatty acyl-Co-A (LC-CoA) levels in the hypothalamus, or stimulating efferent fibers in the hepatic branch of the vagus nerve. Also provided are methods of increasing food intake and glucose production in a mammal. The methods involve decreasing long-chain fatty acyl-Co-A (LC-CoA) levels in the hypothalamus of the mammal.

Abstract: Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.

Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.

Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixt

Abstract: Compounds of formula wherein R1 and R1? are hydrogen or deuterium, R2, R3 and R4 are hydrogen or deuterium, R5 is the residue of an amino acid, X is S or N-ALK, is piperidinyl or tetrahydropyridinyl, ALK is (C1-4)alkyl, and R6 is hydrogen, hydroxy or (C2-12)acyloxy, and their use as antimicrobials.

Abstract: Compositions have been discovered that are suitable for forming a stable dispersion. The compositions comprise an agriculturally active compound and a multivalent metal oligomeric or polymeric compound having a molecular weight of from about 150 to about 15,000 Daltons.

Abstract: Mammalian hair growth is reduced by topically applying a composition including a heat shock protein inhibitor.

Abstract: Acyloxyalkyl carbamate prodrugs of ?-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of ?-amino acids and methods of using acyloxyalkyl carbamate prodrugs of ?-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of ?-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

Abstract: Provided are methods of reducing cell death, attenuating a burst of reactive oxygen species, reducing cytotoxicity, reducing intracellular oxidant stress due species in a population of cells following hypoxia by reoxygenating the cells in the presence of a reversible electron transport chain inhibitor or under hypercarbic conditions. Also provided is a method to determine the effectiveness of a reversible electron transport chain inhibitor for reducing cell death in a population of cells.

Abstract: The invention provides reagents and methods for conjugating a polymer specifically to the ?-amine of a polypeptide. The invention provides monofunctional, bifunctional, and multifunctional PEGs and related polymers having a terminal thioester moiety capable of specifically conjugating to the ?-amine of a polypeptide having a cytokine or histidine residue at the N-terminus. The invention provides reactive thioester-terminated PEG polymers that have suitable reactivity with an N-terminal cysteine or histidine residue of a polypeptide to produce an amide bond between the PEG molecule and the polypeptide.

Abstract: The present invention generally relates to the field of treating oxidative stress disorders by administering a pharmaceutically effective amount of a compound that elevates the intracellular levels of glutathone or intracelluar levels of at least one Phase II detoxification enzyme in animal tissue. The present invention also relates to the field of protecting a subject from oxidative stress disorders by administering a pharmaceutically effective amount of a compound that elevates the intracellular levels of glutathone or intracelluar levels of at least one Phase II detoxification enzyme in the subject. The present invention also relates to a pharmaceutical composition useful for the treatment of oxidative stress disorders.

Abstract: A medicament for preventive and/or therapeutic treatment of a bowel diseases such as inflammatory bowel diseases including Crohn's disease, which comprises as an active ingredient a retinoid such as, for example, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid.

Abstract: Substantially homogeneous topical preparations for cosmetic, veterinary, and pharmaceutical use comprise at least one active ingredient solubilized in a novel composition base. The composition base comprises solubilized allantoin at a level of at least 0.5% and urea at a level of at least 10% in an aqueous vehicle.

Abstract: The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.

Abstract: The invention relates to aqueous insecticidal compositions embodied in the form of an aqueous polymer fine particle dispersion containing at least one type of organic insecticidal active substance whose water solubility is equal to or less than 5 g/l at 25° C./1013 mbar and a polymer particle average size, determined by dynamic light scattering, is equal to or less than 300 nm, wherein the polymer particles containing at least one insecticidal active substance exhibit a cationic surface charge and the aqueous dispersion of active substance containing polymer particles is obtained by radical aqueous emulsion polymerisation of an ethylenically unsaturated monomer composition M, in which said ethelenycally unsaturated monomer M contains at least one type of insecticidal active substance in a dissolved form. The use of the inventive aqueous insecticidal compositions for protecting lignocellulose-containing materials, in particular wood, against infest pest attacks is also disclosed.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):

Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2–10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5–10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4–20% of at least one inorganic solid carrier; and d) 3–20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and

Abstract: Pleuromutilin compounds of the formula: are of use in anti-bacterial therapy.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: The present invention relates to thiourea compounds and the pharmaceutical compositions containing the same, and particularly, to novel thiourea compounds as an antagonist against vanilloid receptor (VR) and the pharmaceutical compositions thereof. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: Segmented water soluble polymers, containing a higher molecular weight segment linked to a lower molecular weight segment, are described. In one embodiment, the polymer segments are poly(ethylene glycol) segments. The segmented polymers are functionalized and are useful for conjugation to various moieties such as pharmacologically active substances. Also described are conjugates of such polymers and methods of their preparation.

Abstract: Compositions including an aromatic compound for inhibiting the production of exoproteins by Gram positive bacteria are disclosed. The aromatic inhibitory compounds of the present invention have the general formula: wherein R1 is selected from the group consisting of H, —OR5, —R6C(O)H, —R6OH, —R6COOH, —OR6OH, —OR6COOH, —C(O)NH2, and NH2 and salts thereof; R5 is a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety; R6 is a divalent saturated or unsaturated aliphatic hydrocarbyl moiety; R7 is a trivalent saturated or unsaturated aliphatic hydrocarbyl moiety; R8 is a monovalent substituted or unsubstituted saturated or unsaturated aliphatic hydrocarbyl moiety which may or may not be interrupted with hetero atoms; R2, R3, and R4 are independently selected from the group consisting of H, OH, COOH, and —C(O)R9; R9 is hydrogen or a monovalent saturated or unsaturated aliphatic hydrocarbyl moiety.

Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compoundsd and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1–R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.

Abstract: The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (“BBB”) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.

Abstract: An aqueous composition suitable for applying fungicides to plant propagation materials is provided, comprising water and a blend of the following components, by weight: a) 2-10% of a surface-active agent comprising a1) at least one anionic surfactant; b) 0.5-10% of at least one polymer selected from water-dispersible polymers and water-soluble film-forming polymers; c) 4-20% of at least one inorganic solid carrier; and d) 3-20% of at least one antifreeze agent. In one embodiment, the composition comprises a fungicidally effective amount of at least one fungicidally active compound. The inventive composition is storage stable, ready-to-apply (RTA), ecologically and toxicologically favorable and has good fungicidal efficacy.

Abstract: The present invention relates to novel compounds which make it possible to transfer nucleic acids into cells. These novel compounds are lipid derivatives of polythiourea. They are useful for the in vitro, ex vivo or in vivo transfection of nucleic acids into various cell types.

Abstract: A hydrochloride salt of ferrous bisglycinate having the formula Fe(C2H4NO2.HCl)2, which is highly soluble in water, making the compound beneficial as a dietary supplement. One form of the commercial product of the compound has the ferrous bisglycinate hydrochloride dissolved in water.

Abstract: A stable complex of calcium and aspartic acid having the formula CaCOOCH2CHNH2COO, which is highly soluble both in water, making the compound beneficial as a dietary supplement for calcium. One form of the commercial product of the compound has the calcium monoaspartate dissolved in water.

Abstract: A method for supplementing magnesium in an animal by administering a stable complex of magnesium and aspartic acid having the formula MgCOOCH2CIINII2COO, which is highly soluble in water, to the animal. One form of the commercial product of the compound has the magnesium monoaspartate dissolved in water. Another form has the magnesium monoaspartate added to a food.

Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine polymitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.