Abstract: Benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase for inhibiting the growth of cancer cells.

Abstract: Novel cyclic ether vitamin D3 compounds having a cyclic ether side chain are disclosed. These compounds were first identified as metabolites of 3-epi vitamin D3 produced via a tissue-specific metabolic pathway which catalyzes the formation of a cyclic ether structure. Also disclosed are 1?(OH) 3-epi vitamin D3 compounds, which are produced via the epimerization of a 3-?-hydroxyl group of 1?(OH) vitamin D3 precursor in vivo. The vitamin D3 compounds of the present invention can be used as substitutes for natural and synthetic vitamin D3 compounds.

Abstract: A topical composition and method for the reduction of scar tissue and/or improving the appearance of scar tissue after it has formed. The topical composition includes one or more flavonoids formulated in a pharmaceutically acceptable topical carrier. The method includes the step of topically applying a composition including one or more flavonoids formulated in a pharmaceutically acceptable topical carrier to scar tissue to reduce the amount of, or improve the appearance of the scar tissue. The topical compositions and methods of the present invention reduce scar tissue after it has formed as well as improving the appearance of the remaining scar tissue.

Abstract: Pyran derivatives of general formula (I) wherein Y is a 5-, 6- or 7-membered ring, preferably a 5-membered ring, methyl or ethyl mono- or polysubstituted, and optionally unsaturated, and R1, R2, R3, R4 are, each independently, a hydrogen atom or a linear or branched C1-5 alkyl or C2-5 alkenyl group, and X is present or absent; when X is present, R5, R6, R7, R8, R9 are all present, and X is a hydrogen atom or an OZ group, wherein Z is a hydrogen atom or a R10 group or a C(O)R10 group; when X is absent, a double bond involving the carbon atom at the 4 position is present and R7, R8 and R9 are present, and one of R5 or R6 is present and the other one is absent, or R5, R6, and R7 are present, and one of R8 or R9 is present and the other one is absent, or R7 is a ?C(R11)(R12) group and R5, R6, R8, R9 are present; and when they are present, each of R5-R12 group is, independently, a hydrogen atom or a linear or branched C1-5 alkyl or C2-5 alkenyl group; and use of at least one pyran derivative of formula (I)

Abstract: Embodiments of the present invention include compositions and pharmaceutical compositions comprising citrulline and Hmg-CoA reductase inhibitors. Further embodiments relate to the use of such composition treat subjects and stimulating nitric oxide synthase.

Abstract: Use of an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with another antihypertensive, a cholesterol lowering agent, a diuretic or aspirin, in the manufacture of a medicament for the prevention of cardiovascular events; a method of preventing cardiovascular events comprising administering to a patient in need of such prevention an effective amount of an inhibitor of the renin angiotensin system or a pharmaceutically acceptable derivative thereof, optionally together with another antihypertensive, a cholesterol lowering agent, a diuretic or aspirin; and a combination product containing an an inhibitor of the renin-angiotensin system or a pharmaceutically acceptable derivative thereof and a cholesterol lowering agent.

Abstract: Novel compounds of the formula I in which R, X and n are as defined herein, are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.

Abstract: The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, for use in the treatment or prophylaxis of condition mediated by an androgen receptor.

Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

Abstract: The present invention discloses a process for preparing a nitrile compound, a carboxylic acid compound or a carboxylic acid ester compound represented by the formula (2): wherein R represents a cyano group, a carboxyl group or an ester group, R1 and R2 each represent a group which does not participate in the reaction, which may have a substituent, and R1 and R2 may be combined to each other to form a ring, which comprises subjecting an acetic acid compound represented by the formula (1): wherein R, R1 and R2 have the same meanings as defined above, to decarboxylation in the presence of a metal catalyst.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: A method of making a red pigmented composition is disclosed which includes (a) preparing an aqueous extract of Garcinia indica fruit comprising at least one red colorant; (b) treating the extract with a cation exchange resin so that one or more red colorant associates with the resin; (c) eluting the red colorant from the resin with an eluting solution containing one or more alcohol such as methanol, ethanol and isopropanol and one or more acid such as hydrochloric acid, citric acid, acetic acid, tartaric acid and hydroxy citric acid to yield a red-colored eluate; (d) collecting and concentrating the eluate to provide a concentrate; and (e) adding an antioxidant agent and/or placing the concentrate in an aseptic container in a non-oxidizing atmosphere. A combination comprising the resulting stabilized Garcinia extract in aseptic packaging in a non-oxidizing atmosphere is also disclosed, along with methods of use.

Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups ?wherein A, B, D, G, X, Y and Z have the meaning given in the description, several processes and intermediate products for their preparation and their use as pest control agents and herbicides.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.

Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.

Abstract: A method for preventing or for treating anxiety in a patient in need thereof comprising administering wogonin to the patient in an effective dose that does not cause sedative or myorelaxant side effects. Methods for extracting wogonin from the roots of Scutelleria baicalensis Georgi are also described.

Abstract: A compound of the formula where R1 is H, C1–C4 alkyl and OH; R2 in is H, C1–C4 alkyl and OH; R3 is H and C1–C4 alkyl; R4 is H and C1–C4 alkyl; n is an integer between 0 and 2 inclusive; R5 is a nullity, NHR7C(O)—, C6H4—, C6H4—O—; R7 is C2–C6 alkyl; and R6 is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine, blood brain barrier (BBB) peptide, membrane translocating peptide, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, transferrin, glucosylamine, amino saccharin, saccharin ester, lactylamine, leucine, tryptophan, amino glutamate and amino cholines.

Abstract: Benzocycloheptenes of formula (I), in which R1, R2 and Y have the meanings that indicated herein, exhibit selective estrogenic activity on bones and are suitable for the production of pharmaceutical agents, especially for prophylaxis and therapy of osteoporosis:

Abstract: A method of treating plant and animal systems and inanimate surfaces for the purposes of controlling plant pests, introducing pesticides and nutrients into plants, mitigating frost damage to plants, increasing crop yields, controlling certain plant diseases, controlling arthropod, bacterial, fungal, mycoplasma, rickettsia, and viral pests of animals and humans, and disinfecting inanimate surfaces. The method utilizes the unique multi-directional dispersion property of the tannate complex of picro ammonium formate and the tannate complex of picro cupric ammonium formate, in aqueous solution, combined with a minor amount of a surfactant sufficient to prevent formation of ammonium picrate, to penetrate plant and animal systems and inanimate surfaces and travelling multidirectionally therein. The method is carried out by introducing a small but effective amount of the tannate complex to the plant or animal system or inanimate surface.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, Streptomyces, Actinomadura, Micromonospora, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.

Abstract: A preparation process is provided for preparing a novel flavonoid compound having a high level of antioxidative action. The flavonoid compound is obtained by subjecting hesperidin to microbial fermentation treatment with Aspergillus saitoi.

Abstract: We describe the use of bicyclic carbohydrates for the treatment of hepatitis C virus infections. Different bicyclic carbohydrates were tested in vitro against DNA-viruses, retro-viruses and Flaviviridae sp., an important family of human and animal RNA pathogens. Significant activity was observed against the bovine viral diarrhea virus (BVDV). As pestiviruses, such as BVDV, share many similarities with hepatitis C virus (HCV), the bicyclic carbohydrates in general and the preferred bicyclic carbohydrates more specifically are expected to be a treatment for hepatitis C viral infections.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.

Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.

Abstract: The topical administration of statins for the treatment of bone disorders is disclosed.

Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: Administered anticraving compositions are disclosed for treating patients addicted to alcohol comprising an effective amount of at least one alpha-pyrone compound formulated into a physiologically acceptable carrier medium. Additionally, a method of oral administration of the anticraving compounds is disclosed where an effective amount of at least one alpha-pyrone compound is formulated into a wine, beer or distilled spirit where the alcohol has been removed and replaced by one or more kavapyrones.

Abstract: The present invention generally relates to compounds and compositions useful for the modulation of ligase activity. The invention further relates to Compounds of the Invention, compositions thereof, and methods for treating or preventing cancer, a neoplastic disorder, acute or chronic renal failure, an inflammatory disorder, an immune disorder, a cardiovascular disease, an effect of aging or an infectious disease comprising administering an effective amount of a Compound of the Invention. The invention further relates to the use of a Compound of the Invention as a preservative of a cell, blood, tissue or an organ or as an agent to modulate stem cells.

Abstract: The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica.

Abstract: CETP Inhibitors have improved solubility and bioavailability in a lipophilic vehicle comprising a digestible oil, a lipophilic solvent, or a surfactant. Preferred such compositions are self-emulsifying or self-microemulsifying, and comprise 1. a CETP inhibitor; 2. a cosolvent; 3. a surfactant having an HLB of 1 to 8; 4. a surfactant having an HLB of over 8 to 20; and 5. optionally, a digestible oil.

Abstract: Compounds expressed by the following general formula (1), [wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1), (1-2), (1-3), (1-4) and (1-5)]. The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.

Abstract: An dermatological agent for external use is disclosed which contains a chromanol glycoside represented by the following general formula (1) (wherein R1, R2, R3, and R4 which may be the same or different, each represent a hydrogen atom or a lower alkyl group, R5 represents a hydrogen atom, a lower alkyl group, or a lower acyl group, X represents a monosaccharic residue or an oligosaccharic residue optionally having the hydrogen atom of the hydroxyl group in the saccharic residue substituted with a lower alkyl group or a lower acyl group, n represents an integer in the range of 0-6, and m represents an integer in the range of 1-6). This is a novel dermatological agent for external use which excels in stability and percutaneous absorbency, manifests an effective action safely at a small application rate, and effectively prevents and cures the dermopathy.

Abstract: An antibiotic SF2487 substance having the formula (I) or a salt thereof possesses an antimalarial activity against the proliferation of malarial parasites and is therefore useful as an antimalarial drug.

Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.

Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.

Abstract: Co-therapy for the treatment of neurological dysfunctions comprising administration of one or more fructopyranose sulfamates and erythropoietin.

Abstract: This invention features the use of the spirolaxine of formula (I) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the Type 2 insulin-resistant diabetes. This invention also features a pharmaceutical composition in which the spirolaxine of formula (I) acts as active principle in association with the all-trans retinoic acid of formula (II) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the acute malignant haemopathies.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical.

Abstract: The present invention describes the identification and purification of 7-hydroxychromes that exhibit potent antioxidant activity. In one embodiment the present invention includes a method for providing an antioxidant to a host in need thereof, comprising administering an effective amount of a 7-hydroxychrome or a mixture of 7-hydroxychromones. The present invention includes methods that are effective in inhibiting free radical and oxidation caused damage through the simultaneous suppression of free radical generation and the suppression of the production of reactive oxygen species (ROS). The present invention also includes methods for preventing and treating ROS mediated diseases and conditions and diseases and conditions associated with other oxidative processes.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

Abstract: Hydrates of the compound of formula (I) and crystalline forms thereof have excellent storage stability and are useful medicaments.

Abstract: Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.

Abstract: A composition for accelerating the disposal of ethanol from bodily fluid. Certain additives can accelerate the metabolic oxidation of ethanol, and others in addition act as catalysts or “pseudo” enzymes for the oxidation. Additives include the oxidant Nicotinamide Adenine Dinucleotide and a variety of other additives such as transition metal ions and complexes thereof which favor the oxidation reaction. The compositions described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: The present invention relates to novel compositions based on hydrated lipidic lamellar phases or liposomal compositions, prepared by combining different lipid molecules, synthetic and/or from natural sources, said compositions comprising at least one of a) labd-13-ene-8?, 15-diol and/or derivatives thereof; b) labd-14-ene-8, 13-diol or derivatives thereof; c) 3?-hydroxy-labd-14-ene-8, 13-epoxy and/or derivatives thereof, d) a plant extract containing the aforementioned labdanes or derivatives thereof. The compositions of the invention exhibit cytotoxicity against cancerous cells and are utilized for the treatment of tumors and leukemias.