Abstract: The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production, and are useful as an agent for the prophylaxis and/or treatment of diseases such as, cardiac disease, autoimmune disease, inflammatory disease, central nervous system disease, infectious disease, sepsis, and septic shock.

Abstract: Diagnosing or treating a human ear includes transporting a conjugated nanoparticle or a magnetically responsive nanoparticle into a human's middle or inner ear. Otologic nanophoresis includes electrically, magnetically or electromagnetically driving a nanoparticle through a membrane of the ear, including a tympanic membrane, a round window membrane, an oval window membrane, or a circulatory membrane. An otologic diagnostic device includes a nanoparticle conjugated with a material selected from the group consisting of lipids, proteins, growth factors, growth hormones, antioxidants, free radical scavengers, steroid preparations, and metabolically active substances; an otologic therapeutic device includes the same categories of substances and chemotherapeutic drugs. Another otologic composition includes a nanoparticle conjugated with a substance perceptible to magnetic resonance imaging.

Abstract: Compounds of the formula (I): in which R1, R2, R3, R?3 and R4 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, the pharmaceutical compositions comprising them, and the processes for the preparation of these compounds.

Abstract: The present invention provides compounds having estrogenic activity selected from the group consisting of RRR-?-tocopherol, hydro-Q9 chromene, coenzyme Q9, cycloartane, 1-Feruloyl glycerol, ?-tocopherol-9, and analogues thereof. The compounds of the present invention activate ER? and ER?, and express high estrogenic activity.

Abstract: The invention relates to substituted para-trifluoromethyl phenyl ether compounds and its preparation and use thereof especially. The substituted para-trifluoromethyl phenyl ether compounds of the invention having general formula (I): The substitutes see Description. The compounds of present invention have broad-spectrum activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete, and it may also provide good control efficacy at very low dosage because of the high activity. The compounds of the invention have good insecticidal activity and have good activity against many pests, especially for Carmine spider mite. The compounds are fit for synthetical control against many kinds of pests.

Abstract: The use is described of merocyanine derivatives of formula (1), wherein R1 and R2 are each independently of the other hydrogen; C1-C22alkyl; cyclo-C3C8alkyl; or unsubstituted or C1-C5alkyl- or C1-C5alkoxy-substituted C6-C20aryl; orl; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is uninterrupted or, interrupted by —O— or by —NH—; R3 is a cyano group; —COOR5; —CONHR5; —COR5; or —SO2R5; R4 is a cyano group; —COOR6; —CONHR6; —COR6; or —SO2R6; R5 and R6 are each independently of the other C1-C22alkyl; or unsubstituted or C1-C5alkyl substituted C6-C20aryl; or R3 and R4 together or R5 and R6 together form in a 5- to 7-membered, monocyclic, carbocyclic or heterocyclic ring; Z1, and Z2 are each independently of the other a —(CH2)n— group which is uninterrupted or interrupted by —O—, —S—, or by —NR7—, and/or is unsubstituted or substituted by C1-C5alkyl; R7 is (ClC5alkyl; 1 is from 1 to 4; m is from 1 to 7; n is from 1 to 4; when n=2, R1, R5 or R6 is a bivalent alkyl group; or R1

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: The invention relates to methods of treating metabolic syndrome, or the specific disorders associated with metabolic syndrome, comprising the administration of norfluoxetine enriched for the (R) or (S) enantiomer conjointly with niacin, fenofibrate, a H1 antagonist or inverse agonist, or a H3 agonist or partial agonist.

Abstract: This invention is directed to the crystalline potassium salt of a lipoxin A4 analog of Formula (I): processes for preparing the crystalline potassium salts, methods for using them to treat disease-states characterized by inflammation, and pharmaceutical compositions comprising such crystalline potassium salts.

Abstract: Dermatological/cosmetic compositions suited for preventing or treating cell differentiation and/or proliferation and/or keratinization disorders, including preventing or treating common acne, comprise, in a physiologically acceptable medium, (i) at least one dispersed retinoid, (ii) dispersed benzoyl peroxide, in free or encapsulated form, and (iii) at least one pH-independent gelling agent, said dermatological/cosmetic composition having physical stability without loss of viscosity over time at a temperature ranging from 4° C. to 40° C., said dermatological/cosmetic composition having a stable flow threshold over time as measured by viscosity measurements for rheograms which measure a shear stress ? for a given rate gradient ? and which measure a rate gradient ? for a given shear stress ?, the yield value (?0) being extrapolated visually or by calculation.

Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.

Abstract: Methods of treating skin diseases such as plaque psoriasis and inverse psoriasis include topical application of one or a combination of caffeic acid phenethyl ester, caffeic acid benzyl ester, and analogs thereof as an active agent. A pharmaceutical composition containing the active agent may further include a cell differentiating agent such as a retinoid, and/or vitamin D or analogs thereof. The method enables treatment of a lesion with active agent dosages of ten percent by weight, for example.

Abstract: This invention relates to combination therapy for the treatment of lower urinary tract symptoms (LUTS) associated with or without benign prostatic hyperplasia (BPH). The combination therapy comprises of tailored 1 adrenoceptor antagonist, which is selective for 1a over 1b subtype but non-selective for 1a over 1d subtype, in combination with muscarinic receptor antagonist, preferably bladder selective antagonist and optionally included 5-reductase inhibitor for relief of LUTS in a mammal with or without BPH.

Abstract: Novel derivatives of fumagalone have the general formula (I): and are useful angiogenes is inhibitors; these can be formulated into pharmaceutical compositions suited for human or veterinary medicine, or can be formulated into cosmetic compositions.

Abstract: Compounds, compositions and methods that are useful for the treatment of metabolic disorders, inflammatory diseases and cancer are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in lipid metabolism, inflammation and cell proliferation. The subject compounds are linked biaryl compounds.

Abstract: The invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention more specifically relates to new uses of compounds that inhibit the prenylation of proteins, in particular the geranylgeranyl and/or farnesyl modifications of proteins, for treating neurodegeneration involving oxidative stress and, more particularly, Parkinson's disease. The invention also relates to corresponding methods of treatment, and can be used in human subjects for preventive or curative treatment, either alone is or in combination with other active agents or treatments.

Abstract: The present invention is related to an antifungal composition for inhibition of wood decay caused by wood rot fungi. The invention further comprises a method for inhibition of wood decay with gallates.

Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-?v?3 are inhibited by an inhibitor compound of formula: wherein G1 and G2 are each independently —NH—C(O)—O—(CH2)v—(C6H4)—X3 ; Y1 and Y2 are each independently —OH or C1-C4 alkoxy; X1 and X2 are each independently halo or C1-C4 alkoxy; X3 is fluoro, nitro, C1-C4 alkyl, C1-C4 alkoxy, or C1-C4 perfluoroalkyl; Z is —C?C—, —C6H4—, cis-CH?CH—, trans-CH?CH—, cis-CH2—CH?CH—CH2—, trans-CH2—CH?CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1,3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each 1; t is an integer having a value of 0 or 1; p and r are each 2, and v is 1; with the proviso that when A is H, t is 0, and when A is a covalent bond, t is 1.

Abstract: Disclosed is a raw material for cosmetic preparations having excellent gloss imparting properties and oxidation stability. Also disclosed is a cosmetic preparation having excellent gloss and feeling of use. The raw material for cosmetic preparations contains an ester compound of (A) benzoic acid, (B) an alcohol selected from the group consisting of neopentyl glycol, dineopentyl glycol, trineopentyl glycol, trimethylolpropane, ditrimethylolpropane, tritrimethylolpropane, dipentaerythritol and tripentaerythritol, and (C) a fatty acid having 3-28 carbon atoms and/or a hydroxycarboxylic acid having 3-28 carbon atoms. The cosmetic preparation contains this raw material for cosmetic preparations.

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

Abstract: Substituted phenol derivatives of Formula (I) are useful as antiproliferative agents including, for example, anticancer agents, and as radioprotective and chemoprotective agents.

Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils and/or their constituents, plant essential oils and/or their constituents in admixture with known active pesticidal compounds or plant essential oils and/or their constituents in admixture with other compounds not previously used as active ingredients in pesticidal formulations, such as, for example, so called signal transduction modulators. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.

Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.

Abstract: The present invention relates, in general, to the treatment of estrogen-dependent diseases and disorders and, in particular, to a method of treating estrogen-dependent cancers, particularly breast cancer, with antiestrogens.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

Abstract: The present invention relates to a preparation for stimulating or enhancing an immune system comprising one or more agents that stimulate T-lymphocytes in vivo. Such a preparation can be sued in the prophylaxis and/or treatment of a medical condition. The invention further relates to a preparation for use in a pharmaceutical or food product and to a preparation for medical use.

Abstract: An external preparation characterized by comprising, as selected from gallic acid derivatives of the following formula (I), wherein R1 represents a hydrogen atom, an alkali metal, an alkaline earth metal, an ammonium salt, or an alkyl or alkenyl group having from 1 to 18 carbon atoms and R2, R3, and R4 independently represent a hydrogen atom, an hydroxyl group, an alkoxy group having from 1 to 18 carbon atoms, a polyoxyethylene group, a polyoxypropylene group, or a residue of a monosaccharide, a disaccharide, or an oligosaccharide; 90 wt % or over of one or more gallic acid derivatives (A) wherein two of R2, R3, and R4 in the formula (I) independently represent a residue of a monosaccharide, disaccharide, or oligosaccharide and from 0.001 wt % to less than 10 wt % of one or more gallic acid derivatives (B) wherein one of R2, R3, and R4 represents a residue of a monosaccharide, disaccharide, or oligosaccharide, each based on the total content of the gallic acid derivatives.

Abstract: The present invention provides new amyloidogenesis inhibiting compounds of formula (I): in which R1 is a —NRaRb group, where Ra and Rb, independently, are a hydrogen atom or a C1-C6 alkyl group; —ORC group, where RC is a hydrogen atom or a C1-C6 alkyl group; a glycosyl; a C1-C6 polyhydroxyalkyl; or a —NH—CH(Rd)—COORe group, where Rd is a side chain of one of the 20 natural alpha-amino acids in either of their two enantiomerically pure forms L or D, and Re is a hydrogen atom or a C1-C6 alkyl group; and R2 is a hydrogen atom, a C1-C6 alkyl group, a glycosyl; a C1-C6 polyhydroxyalkyl; —C(?O)—Rf group, where Rf is a C1-C6 alkyl group; or a —CH2—COO—Rg group, where Rg is a hydrogen atom or a C1-C6 alkyl group; and pharmaceutically acceptable salts thereof, which are useful in the treatment of neurodegenerative diseases, among others.

Abstract: The present invention provides a novel crystalline form of n-butyl[4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2?-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhibits excellent inhibitory activities against activated blood coagulation factor X, and is useful for the treatment or prevention of a tromboembolic disease.

Abstract: This invention relates to compounds that alter PPAR activity. The invention also relates to pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing dyslipidemia, hypercholesterolemia, obesity, hyperglycemia, atherosclerosis, hypertriglyceridemia and hyperinsulinemia in a mammal. The present invention also relates to methods for making the disclosed compounds.

Abstract: A method of treating a non-human dermatological disorder, wherein the method comprises topically administering to a non-human dermatological disorder a therapeutically effective amount of a topical composition containing: (1) an active component comprising at least one salicylate derivative; and (2) at least one pharmaceutically acceptable solubilizer.

Abstract: Prodrugs of propofol, methods of making prodrugs of propofol, pharmaceutical compositions of prodrugs of propofol and methods of using prodrugs of propofol and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting are disclosed herein.

Abstract: The invention provides substituted phenol compounds and pharmaceutical compositions containing substituted phenol compounds which are useful for inducing or maintaining anesthesia or sedation in a mammal. This invention also provides methods for inducing or maintaining anesthesia or sedation in a mammal using substituted phenol compounds.

Abstract: The present invention provides ethyl (?)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxy]acetate hydrochloride, crystalline forms thereof and pharmaceutical compositions containing them, which have excellent ?3-adrenoceptor stimulating effects, therapeutic effects on pollakiuria or urinary incontinence and storage stabilities and are useful as a medicament.

Abstract: According to the invention, there is provided a novel 3,4-dihydroxyhydrocinnamic acid derivative, designated DHH105, having blood glucose lowering effects in vivo as a result of the enhancement of glucose transport mediated by the increase of insulin receptor signaling. This invention thus relates to a 3,4-dihydroxyhydrocinnamic acid derivative useful as an anti-diabetic agent, represented by the following formula I: or pharmaceutically acceptable salts thereof, to a method for preparing the compound, and to a composition for treating diabetes comprising the same as an active ingredient.

Abstract: The invention relates to compounds of the formula I in which the radicals are defined as specified, and also to their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: This patent discloses a substituted fullerenes, compositions comprising the same, and their use as antioxidants. The substituted fullerenes comprise a fullerene core (Cn) and at least one of: (i) from 1 to 6 (>CX1X2) groups bonded to the fullerene core; (ii) from 1 to 18 —X3 groups bonded to the fullerene core; (iii) from 1 to 6 —X4— groups bonded to the fullerene core; or (iv) from 1 to 6 dendrons bonded to the fullerene core.

Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: Angiogenesis, tumor growth, and metalloproteinase 2 (MMP2) interaction with integrin-?v?3 are inhibited by an inhibitor compound of formula (I): wherein G1 and G2 are each independently NH—C(O)—O—R1, —NH—C(O)—O—(CH2)v—(C6H4)—X3, —NH—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—NH—(CH2)v—(C6H4)—X3, —O—C(O)—O—(CH2)v—(C6H4)—X3, or NH—C(O)—CH2—(C6H4)—X3; Y1 and Y2 are each independently OH, C1–C4 alkyl, C1–C4 hydroxyalkyl, C1–C4 alkoxy, phenyl, benzyl, or NH2; R1 is C1–C4 alkyl; X1 and X2 are each independently halo or C1–C4 alkoxy; X3 is halo, nitro, C1–C4 alkyl, C1–C4 alkoxy, or C1–C4 perfluoroalkyl; Z is —C?C—, —C6H4—, cis-CH?CH—, trans CH?CH—, cis-CH2—CH?CH—CH2—, trans —CH2—CH?CH—CH2—, 1,4-naphthyl, cis-1,3-cyclohexyl, trans-1, 3-cyclohexyl, cis-1,4-cyclohexyl, or trans-1,4-cyclohexyl; A is H or a covalent bond; m and n are each independently an integer having a value of 0 or 1; t is an integer having a value of 0 or 1; and p, r, and v are each independently an integer having a value of 1 or 2; with provisos that when A

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

Abstract: Alkoxylated esters of dicarboxylic or tricarboxylic acids have an anti-irritating activity measured as a reduction in intracellular leakage of sodium fluorescein of 15% or more at 1:50 dilution or 40% or more at 1:100 dilution from a test composition containing 5% of the alkoxylated ester. These alkoxylated esters are useful in cosmetic and personal care products, especially in products such as baby shampoos, hand dishwashing liquids and bubble bath preparations. A method of reducing irritation provides for application of an irritant with the alkoxylated esters to the subject in a personal care or cosmetic product.

Abstract: The present invention concerns esters of R-enantiomers of a non-steroidal anti-inflammatory drug, which is substantially free from the S-enantiomer. The compounds of the invention may be used in treating a disease or illness in a mammal. To this end, a composition comprising a compound mentioned above, or a pharmaceutically acceptable salt thereof where salt formation occurs, is administered to the mammal in an amount sufficient to elicit a chemopreventative effect or a chemoprotective effect or a therapeutic effect or a prophylactic effect.

Abstract: A NF-?B inhibitor represented by the following formula (I) is provided: ?

Abstract: The present invention relates to in situ compositions of mono- or diester dicarboxylates, methods employing these in situ compositions, and methods of making these in situ compositions. More particularly, the invention relates to mono- or diester dicarboxylate antimicrobial compositions that can reduce the population of microbes on various surfaces such as facilities, containers, or equipment found in food, beverage, or pharmaceutical processing, or in food, beverage, or pharmaceutical industries, at temperatures between about ?70° C. to about 100° C.

Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.

Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

Abstract: The invention relates to novel stilbene compounds having the general formula (I): as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological, rheumatic, respiratory, cardiovascular and ophthalmic conditions and cosmetic compositions and methods of use thereof.

Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.

Abstract: Disclosed are novel compounds of formula (I) wherein A1, A2, Ar, R5, R6, R8, M, Q, Y, Z, k, m and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). Such conditions include diabetes and obesity.