Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.

Abstract: This invention relates to the control of plant pests, such as aphid and whitefly by treating plants with a compound which inhibits the plant pest's ability to overcome plant defence responses, such as piperonyl butoxide or propyl gallate, in combination with a compound which activates plant defence responses, such as cis-Jasmone or beta-amino butyric acid.

Abstract: A method by which the physiological activities of sesamin-class compounds can be efficiently exhibited and enhanced, as well as an effective compound that can be combined with the sesamin-class compounds to this end. By using sesamin-class compounds in combination with more than specified proportions of arachidonic acid class compounds, the physiological activities of the sesamin-class compounds, for example, their anti-fatigue action is synergistically enhanced to provide compositions that are safe in humans and non-human animals and which hence can be ingested continuously.

Abstract: Disclosed herein are an external composition for skin, which contains, as an active ingredient, manassantin B extracted from Saururus chinensis Baill, and the use thereof for skin whitening. More particularly, disclosed are an external composition for skin, which contains, as an active ingredient, manassantin B, which inhibits the transfer of melanosomes, thus providing a skin-whitening effect without influencing the melanin synthesis function of the melanocytes, ad well as the use thereof for skin whitening.

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 appropriately substituted chalcones, such as, for example, represented by the structural formula as shown herein below Wherein R1, R2 and R3 are selected from the group consisting of H, OH, O-alkyl, O-phenyl and O-substituted phenyl; B represents Ar—Z—O or RO; where Z is an alkane having up to 5 carbon atoms; R is substituted propanol amino, wherein substituted amino groups are selected from the group consisting of t-butyl, n-butyl, i-butyl, i-propyl, 4-phenyl piperazine-1-yl, 4-(2-methoxyphenyl)-piperazin-1-yl and 3,4-dimethoxy phenethyl; and Ar is thiazolidine-dione methylene phenoxy. The compounds prepared have been demonstrated to exhibit significant antidiabetic effect in various animal models indicating potential for further exploitation.

Abstract: A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-?) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient.

Abstract: The present invention relates to compositions that include a combination of one or more pesticides and one or more adjuvants.

Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.

Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

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.

Abstract: The present invention relates to a compound of the following formula (I): or a pharmaceutically acceptable salt thereof, for use in the prevention or treatment of peripheral neuropathies.

Abstract: There is provided a compound having an excellent controlling effect on arthropod pests represented by the formula (I-1): wherein Z represents an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; G represents a -A1-R1 group, etc.; X0 represents a -A2-R4 group, etc.; X represents a -A2-R4 group, etc.; X0 represents a -A3-R6 group, etc.; or X and X0 are optionally taken together to form a -A2-T0-A3- group; M1 represents a —R8 group, etc.; A1, A2 and A3 independently represent an oxygen atom, etc.; R1 and R8 independently represents an optionally substituted C1-C20 chain hydrocarbon group, etc.; R4 and R6 independently represent an optionally substituted C1-C6 chain hydrocarbon group, etc.; and T0 represents an optionally substituted C2-C6 alkanediyl group.

Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.

Abstract: Provided are essentially preservative-free personal care product compositions that comprise a combination of fragrance compounds that stabilises the personal care product against microorganisms. The combination comprises certain benzaldehyde or benzaldehyde derivative compounds combined with certain fragrant acids. The composition is free of classical preservatives including parabens or their derivatives. Further provided are methods of forming such compositions and products and the use of the combination of fragrance compounds in such compositions and products.

Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.

Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.

Abstract: A laundry additive such as a fabric dryer sheet formed of a flexible substrate contains an insecticidally effective amount of an insecticide, preferably a pyrethrum, in an amount between about 0.05 and about 10 grams per square foot. Alternatively, the insecticide may be included as a component in a rinse-cycle laundry additive. Such laundry additives are appropriate for use by institutions such as hotels, cruise ships, and nursing homes, hospitals, and shelters in the prevention and control of bed bugs.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.

Abstract: The present invention relates to a compound of the following formula (I): or a pharmaceutically acceptable salt thereof, for use in the prevention or treatment of autism spectrum disorders (ASD).

Abstract: The invention relates to a compound of the formula (I) in which: R1, R2 and R3 are independently a methoxy group optionally substituted by one or more fluorine atoms; R4 is a hydrogen atom; R5 and R6 are identical and each represent a hydrogen or fluorine atom; A is a cycle selected from the group including aryl and heteroaryl groups, wherein said groups can be substituted.

Abstract: Composition and methods of treating pain and reducing or reversing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and an endothelin antagonist as active agents to treat pain in mammals, including humans.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The present invention relates to a pharmaceutical composition for the prevention and treatment of cancer comprising daurinol as an active ingredient, more precisely a pharmaceutical composition for the prevention and treatment of cancer comprising daurinol isolated from the medicinal plant of Mongolia, Haplophyllum dauricum or Haplophyllum cappadocicum, as an active ingredient. Daurinol can selectively block the S phase of cancer cell cycle to disturb the cycle and induce apoptosis stepwise, resulting in anticancer effect. Therefore, daurinol of the present invention can be used as a positive control chemical in the research and development field of cancer biology especially for cancer therapy and prevention. Daurinol also can be a promising candidate for a novel cell cycle blocker and a novel apoptosis inducer which could be effectively used for the prevention and treatment of cancer in the end.

Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The invention relates to a novel class of inhibitors of arachidonic acid formation that can be useful for treating inflammatory conditions. Specifically, the invention relates to derivatives of sesamol that confer lower toxicity and increased circulatory lifetimes than pure sesamol.

Abstract: An O/W/O emulsion composition having at least one of lignan-class compounds dissolved in an internal oil phase is disclosed. This composition can be produced by a process comprising the steps of 1) dissolving at least one of lignan-class compounds in oil or fat to prepare a lignan-class compound dissolving liquid; 2) emulsifying the lignan-class compound dissolving liquid in a water phase to form an O/W emulsion; and 3) further emulsifying the O/W emulsion in an oil phase to prepare an O/W/O emulsion. This is a lignan-class compound containing composition that is enhanced in the amount of bodily absorption of lignan-class compounds.

Abstract: The present invention relates to agonists of the hTAS2R14 bitter taste receptor and its role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R14 bitter taste transduction or bitter taste response.

Abstract: Disclosed are a method for controlling the elution of a drug from a stent and a drug-eluting stent capable of reducing the restenosis rate after therapy. A coating composition for a drug-eluting stent comprising an endothelin receptor antagonist and a copolymer of 2-methacryloyloxyethyl phosphorylcholine and n-butyl methacrylate. The elution of the endothelin receptor antagonist from the coating composition can be controlled by varying the ratio of 2-methacryloyloxyethyl phosphorylcholine to n-butyl methacrylate in the copolymer.

Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.

Abstract: The present invention provides compounds of structural formula (I), which are agonists of formyl peptide receptor (FPR), particularly formyl peptide receptor like 1 (FPRL1). The present invention also provides the therapeutic use of the compounds of formula (I).

Abstract: Resistance-repellent and multidrug resistant retroviral protease inhibitors are provided. Pharmaceutical composition comprising such compounds, and methods of using such compounds to treat HIV infections in mammals, are also provided.

Abstract: Compounds of the formula: are described in which Z, Q, X, L, m and n assume the meanings stated in the description. The compounds (I) inhibit the production of TNF ? and may thus be useful in the treatment of inflammation and pathological conditions involving overproduction of said cytokine. They furthermore exhibit significant inhibitory activity on the proliferation of tumour cells and may thus be used for the treatment and/or prevention of tumorous, neurodegenerative or autoimmune disorders.

Abstract: A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g.

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, COPD.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of prostaglandins or prostaglandin analogs which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent prostaglandins or prostaglandin analogs after crossing the biological barrier and thus can render treatments for the conditions that the parent prostaglandins or prostaglandin analogs can. Additionally, the HPPs are capable of reaching areas that parent prostaglandins or prostaglandin analogs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: The present patent application is directed to novel fluoroethyl urea compounds and compositions and their therapeutic use in the treatment of pain and other conditions.

Abstract: An object of the invention is to provide compositions containing lignan-class compounds as dissolved at high concentrations. The compositions having lignan-class compounds such as sesamin and episesamin dissolved in solvent oils or fats that contain triglycerides of middle-chain fatty acids having 8-12 carbon atoms, preferably triglycerides of caprylic acid and/or capric acid and/or lauric acid can contain the lignan-class compounds stably at higher concentrations than when other solvents are used and, hence, have high enough value as foods and pharmaceuticals.

Abstract: A melanogenesis inhibitor characterized by containing at least one kind of piperonyl alcohol represented by the following general formula (1) wherein R is a straight chain or branched chain alkyl group having 3 to 18 carbon atoms, a straight chain or branched chain alkenyl group having 3 to 18 carbon atoms, or an optionally substituted alicyclic alkyl group. The melanogenesis inhibitor is superior in stability and safety and has a high melanogenesis-inhibiting effect; and a skin preparation containing the melanogenesis inhibitor is very stable, safe, and has a sufficient fair skin effect and a sufficient effect for curing skin dyspigmentation.

Abstract: The present invention relates to compounds of the formula (I); wherein R1 is H, CH3 or OCH3; R3=H, OH, CH3, OCH3, O-glucose or benzoyloxy; R4=H; R5=H or OH; R6=H or OCH3; R7=H, CH3, OCH3, cinnamoyloxy or (3,4,5-trimethoxy)-benzoyloxy; R8=H, OH, CH3 or OCH3; or R7 and R8 form together a group 0-CH2—O; R9=H or OCH3; R10=H or N-acetyl, N-methyl-2-aminoethyl; to their use as medicament for the treatment of non-autoimmune type 2 diabetes mellitus and/or syndrome X, to dietary and pharmaceutical compositions containing them and to a method for the treatment of non-autoimmune type 2 diabetes mellitus and/or syndrome X in animals including humans, said method comprising the step of administering an effective dose of a compound of the formula (I) to animals including humans which are in need thereof.

Abstract: An object of the present invention is to increase the rate at which lignan-class compounds are absorbed into the body, namely, to provide fast-acting lignan-class compounds. Provided is an oil-in-water emulsion which comprises a water phase and an oil phase comprising at least one kind of lignan-class compounds dissolved therein and being emulsified in the water phase, wherein the oil droplets which serve as a dispersion phase in the emulsion are made finer by high-speed agitation or other method so that their average particle size is 1000 nm or smaller, preferably 500 nm or smaller, and more preferably 300 nm or smaller, whereby the rate at which lignan-class compounds are absorbed into the body is improved to impart immediate action.

Abstract: The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I?) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group.

Abstract: A process for the production of a substance or composition for the therapeutic or prophylactic treatment of erectile dysfunction or the enhancement of libido in a male human or animal subject comprises the step of formulating the substance or composition from at least one of plant material and an extract of plant material of at least one plant species of the family Geraniaceae.

Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

Abstract: A method for treating skin, reducing oxidative damage to a skin cell, reducing lipoxygenase (LO) activity in a skin cell, reducing cyclooxygenase (COX) activity in a skin cell, reducing tumor necrosis factor alpha (TNF-?) in a skin cell, or reduction matrix metalloproteinase enzyme activity in a skin cell comprising contacting skin or a skin cell with an aromatic skin-active ingredient.

Abstract: The present invention relates to a method and composition for treating acne using lignan compounds represented by Formula 1. More particularly, the invention relates to an antibacterial composition against acne-causing bacteria, containing lignan compounds represented by Formula 1, as well as a method for treating acne using the same. The lignan compounds represented by Formula 1 are excellent not only in the antibacterial activity of, inhibiting the growth of acne-causing bacteria, but also in thermal stability. Accordingly, the lignan compounds may be useful as antibacterial agents against the acne-causing bacteria, and acne treatment agents.