Abstract: The present invention relates to novel synthetic toll like receptor antagonist. The present invention in particular provides compounds, methods and compositions for specifically inhibiting immune stimulation involving TLR ligands, especially TLR-4. The compounds are potentially useful in treatment of inflammation, autoimmunity, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract: Resveratrol and/or pterostilbene are added to a chewable carrier, to enhance absorption of resveratrol and/or pterostilbene buccally or through the mucous membranes of the mouth. The composition containing the resveratrol and/or pterostilbene is designed to be retained in the mouth for at least 20 seconds and up to 20 minutes to ensure absorption of the resveratrol and/or pterostilbene through the mucous membranes of the mouth.

Abstract: The invention disclosed a total synthesis process of novel ethoxy combretastatins and their prodrugs. Combretastatins are chemically modified by ethoxy substituted on the 4?-position of their B aryl ring and are converted to be their soluble prodrugs of phosphate or their inner salt of phosphorylcholine by modifying the hydroxyl on the 3?-position of their B aryl ring. Similarly, 3?-amino combretastatin is 4?-ethoxy chemically modified and further side chain of amino acid can be introduced to the amino to form soluble prodrug of amino acidamide. The structure of the said compound is showed as formula (I). Ethoxy combretastatins possess potent tubulin polymerization inhibitory activity and can be used for the treatment of inhibiting tumor or neovascular.

Abstract: The invention provides a medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The invention also provides a method of treating a narrowing in a body passageway comprising placing an implantable medical device comprising a hydrophobic analog of a medicament known to inhibit cell proliferation and migration. The medicaments can be incorporated within or coated on the device. The invention further provides hydrophobic analogs of medicaments known to inhibit cell proliferation and migration.

Abstract: The present invention aims to provide a composition suitable for normalizing the blood pressure, which is useful as food, health food, supplement, nutritional supplement, food for specified health uses, food with nutrient function claims, pharmaceutical product, quasi-drug, feed or pet food. The present inventors have found that coenzyme Q has a superior effect for normalizing the blood pressure and completed the present invention. That is, the present invention provides a composition for normalizing the blood pressure, which contains reduced coenzyme Q as an active ingredient, and a composition for normalizing the blood pressure, which contains oxidized coenzyme Q as an active ingredient and improves hypotension.

Abstract: Methods and formulations for treating animal ectoparasites, effective against parasites such as fleas and ticks are provided. The methods comprise topically co-administering a non-mobile insect growth regulator, a mobile insect growth regulator, and an adulticide to the animal. Parasiticidal formulations for treating animal ectoparasites are also provided, which can be safe to use and avoids the many common deleterious side effects of conventional topical formulations. The topical formulations comprise a combination of two insect growth regulators and an additional insecticide. The topical formulation can be packaged together or packaged so that active components are stored separately prior to administering the topical insecticide formulation to the animal.

Abstract: Disclosed is a pharmaceutical composition for treating oxidative stress comprising a therapeutically effective amount of a substantially pure compound of pterostilbene and a physiologically acceptable carrier. Pterostilbene is administered in an amount between about 2.5 mg to about 10 mg per kilogram of subject body weight. Also disclosed is a method for increasing a working memory of a subject, the method comprising administrating an effective amount of a substantially pure compound of pterostilbene, wherein the working memory for a subject increase and the therapeutic effectiveness is about 10 mg of pterostilbene per kilogram of subject body weight.

Abstract: The present invention provides compounds represented by formula (1) shown below: (wherein R1, R2, R3, R4, and R5 are each individually selected from among a hydrogen atom, methyl group, acetyl group, hydroxyl group, and alkoxy group; and X represents an alkylene group or alkenylene group); and compounds represented by formula (2) shown below: (wherein R6, R7, R8, R9, and R10 are each individually selected from among a hydrogen atom, alkyl group, acetyl group, hydroxyl group, and alkoxy group; A represents an oxygen atom or NH, and m is 0 or 1; and Y represents an alkylene group or alkenylene group, and Z represents a hydrogen atom or hydroxyl group). The compounds of the present invention are useful for preventing or treating brain dysfunctions, motor dysfunctions, or urinary dysfunctions caused by the degeneration and/or loss of the central nervous system or peripheral nervous system cells.

Abstract: The present invention relates to new methoxylated aromatic compounds. It also relates to novel compositions comprising methoxylated aromatic compounds as well as to the use of these compositions as a medicament, in particular as a medicament for the treatment, co-treatment or prevention of inflammatory disorders.

Abstract: Combretastatin derivatives of formula (I), preparation and use thereof are disclosed, wherein: Rf is alkyl with 1-8 carbon atoms and 1-17 fluorine atoms, R is amino, substituted amino, hydroxyl, nitro, halo, alkyloxy, phosphate or amino acid side chain. Said derivatives have a capability to inhibit the polymerization of microtubules and are useful in treatment against tumor and neovascularization.

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, poly-cystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.

Abstract: The present invention relates to a process for preparing a ginger fraction, the fraction prepared by this process and the use thereof on its own or combined with drugs for inhibiting human cytochrome P450 (CYP) enzymes (particularly cytochrome P450 3A4, CYP3A4) for positively influencing the oral bioavailability and pharmacokinetics of active substances.

Abstract: The present invention relates to obovatol compound isolated from Magnolia obovata Thunb. for the prevention and treatment of anxiety disorders involved with CNS. The obovatol compound isolated from Magnolia obovata Thunb. have potent anti-anxiety activity, verified by an increased percentage of time on the open arms, an increased number of entries into, time spent on, the distal portion of the open arms, and a decreased activity of locomotor. Therefore it can be used as the therapeutics or health care food for treating and preventing anxiety disorders.

Abstract: Materials and methods for treating certain cancers are described, preferably cancers that result from the up-regulation of the RAF-MEK-ERK pathway, and more preferably chronic myelogenous leukemia, and which cancer is preferably resistant to the inhibition of the Bcr-Abl tyrosine kinase, imatinib.

Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

Abstract: The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)- type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal motility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.

Abstract: Methods and compounds for reversing pathological vasodilation of blood vessels, for example vasodilation caused by activation of CB1-like receptors, by administering to a subject a therapeutically effective amount of a compound sufficient to induce vasoconstriction, the compound comprising: wherein dashed lines independently represent either a single or a double bond, R1 is a lower alkyl, R2 is a lower alkyl, R3 is a lower alkyl or halogen, R4 is a lower alkyl or hydrogen, R5 is a lower alkyl or hydrogen, R6 is a hydrogen, lower alkyl or halogen, and R7 is a hydrogen, lower alkyl or halogen. The vasoconstrictor can be used for a variety of purposes, including hemostasis or the treatment of shock, for example vasodilatory shock syndromes such as septic shock.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.

Abstract: The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)-type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal motility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.

Abstract: The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)-type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal motility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.

Abstract: Disclosed are anti-viral compositions containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients), and a pharmaceutical carrier. Also disclosed are methods of treating lesionous symptoms of a viral infection involving applying an effective amount of the anti-viral composition to the lesions.

Abstract: Antimicrobial compounds, compositions containing the same, and methods of using of the same for reducing the presence of microorganisms on a substrate or in a fluid environment comprising an antimicrobial effective carrier and at least one antimicrobial compounds including non-halogenated phenoxy and/or benzyloxy substituted phenol compounds.

Abstract: The present invention is directed to 4-cyclopentyl resorcinol monohydrate, its Form I polymorph, formulations containing at least one of these compounds, and their use to lighten skin.

Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.

Abstract: Antimicrobial compounds, compositions containing the same, and methods of using of the same for reducing the presence of microorganisms on a substrate or in a fluid environment comprising an antimicrobial effective carrier and at least one antimicrobial compounds including non-halogenated phenoxy and/or benzyloxy substituted phenol compounds.

Abstract: An antimicrobial compound, composition containing such compound, and method of use of the same for reducing the presence of microorganism on a substrate or in a fluid environment comprising an antimicrobial effective carrier and one or more essential antimicrobial compounds including non-halogenated naphthol compounds.

Abstract: The invention relates to compositions and methods for use in treating skeletal system disorders in a vertebrate at risk for bone loss, and in treating conditions that are characterized by the need for bone growth, in treating fractures, and in treating cartilage disorders. More specifically, the invention concerns the use of inhibitors of microtubule assembly for enhancing bone growth.

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: The invention relates to pharmaceutical preparations containing a dibenzocyclooctane lignan derivative for prevention and treatment of neurodegenerative disease.

Abstract: Composition in the form of an aqueous solution, useful for disinfecting hard surfaces comprises: a) from 0.0005% to 20% by weight of peracetic acid, b) from 0.001% to 45% by weight of acetic acid, c) from 0.001% to 35% by weight of hydrogen peroxide, d) from 0.0001% to 2% by weight of at least one compound of formula (I) (R1)(R2)(R3)N→O  (I) e) if desired, up to 2.5% by weight of at least one nonionic surfactant, and wherein f) the weight ratio between the compound of formula (I) and the peracetic acid is less than or equal to 1, and in that g) the weight ratio between the nonionic surfactant and the peracetic acid is less than or equal to 0.2.

Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.

Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.

Abstract: Colchinol derivatives of formula wherein R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl, PO3H2; X is carbonyl (CO), thiocarbonyl (CS), methylene (CH2) or a group CHR4; R4 is OH, O-alkyl or NR8R9; R5 and R7 are each independently H, alkyl, halogen, hydroxy, alkoxy, nitro or amino; R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulphonyl, arylsulphonyl, aminosulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl or arylaminosulphonyl; and R9 is H, alkyl or cycloalkyl; and the pharmaceutically acceptable salts, solvates, and hydrates thereof have been found to be useful for treatment of diseases involving angiogenesis. Some of these compounds are novel. Particularly preferred are those compounds in which R6 is PO3H2.

Abstract: The application relates to the identification that cannabinoids, such as cannabidiol can be used to treat inflammatory diseases. Cannabinoids for use in treating inflammatory diseases, methods of treating inflammatory diseases and cannabinoids in combination with pharmaceutically acceptable carriers are claimed.

Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: The present invention is directed to retinyl ethers, derivatives and analogues and their use in inhibiting breast carcinogenesis or breast cancer cell growth.

Abstract: Conformationally rigid aryl prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising said prostaglandins.

Abstract: Composition in the form of an aqueous solution, useful for disinfecting hard surfaces comprises: a) from 0.0005% to 20% by weight of peracetic acid, b) from 0.001% to 45% by weight of acetic acid, c) from 0.001% to 35% by weight of hydrogen peroxide, d) from 0.0001% to 2% by weight of at least one compound of formula (I) (R1) (R2) (R3)N→O  (I) e) if desired, up to 2.5% by weight of at least one nonionic surfactant, and wherein f) the weight ratio between the compound of formula (I) and the peracetic acid is less than or equal to 1, and in that g) the weight ratio between the nonionic surfactant and the peracetic acid is less than or equal to 0.2.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds having the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## which are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders are provided. In particular, based on their RXR-agonist activity, these compounds may be used to treat noninsulin-dependent diabetes mellitus (NIDDM) and obesity.

Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: A pesticidal compound of formula I: ##STR1## in which formula: either R.sup.1 is hydrogen and R.sup.2 represents a cyclopropyl group or R.sup.1 and R.sup.2 each represent an alkyl group, which alkyl groups may be the same or different;Ar.sub.A represents an optionally substituted phenyl or naphthyl group;Ar.sub.B represents a phenoxy, phenyl, benzyl or benzoyl-substituted phenyl group which is optionally further substituted;the configuration of the groups Ar.sub.A --CR.sup.1 R.sup.2 and --CH.sub.2 Ar.sub.B about the double bond being mutually trans.Preferably Ar.sub.A is a substituted phenyl group; more preferably being substituted at the 4-(para) position by halogen, alkoxy or haloalkyl.Further provided is a process for the preparation of a pesticidal compound of formula I in which a compound comprising a moiety ##STR2## and a compound comprising a moiety Ar.sub.B -- are reacted together forming a link --CH.dbd.C(F)CH.sub.2 -- between ##STR3## and Ar.sub.B in the compound of formula I.

Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: This invention relates to certain 1,3,3-(trisubstituted)cyclohex-1-ene dimers and related compounds which are useful in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: (3-hydroxy-4-methoxybenzyl)-7-methylene-1-vinyl-2,3,3a,4,7,7a-hexahydroinde n-4-one of formula (I): ##STR1## and 3-(3-hydroxy-4-methoxybenzyl)-4-hydroxy-7-methyl-1-vinylindan of formula (II): ##STR2## as well as their stereoisomeric forms are disclosed. Also disclosed are a process for producing these compounds from the plant Ottelia alismoides and pharmaceutical compositions containing them. The novel compounds of formulas (I) and (II) have remarkable antitumor and antileukaemic properties.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.