Abstract: The invention relates to the use of a derivative compound of 1,3-benzodioxole of formula (I) wherein R is a linear or branched (C4-C10)alkyl substituent as a synergistic compound of insecticidal active ingredients insecticidal compositions comprising at least one compound of Formula (I) and at least one insecticidal active ingredient are also described.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

Abstract: The present invention relates to the use of lignan compounds for treating or preventing an inflammatory disease. More particularly, it relates to a method for preventing or treating an inflammatory disease, comprising administering to a subject in need thereof an effective amount of macelignan represented by Chemical Formula I or a pharmaceutically acceptable salt thereof. The lignan compound has the effect of inhibiting inflammatory reactions by inhibiting the production or expression of inflammation mediators NO, iNOS, PGE2, COX-2 and TNF-? and by treating or preventing inflammatory disease in vivo. Accordingly, the lignan compound or a Myristica fragrans extract will be highly useful for the treatment or prevention of an inflammatory disease.

Abstract: A polyacetylenes and application thereof. The polyacetylenes is isolated from an extract of the sporophores of Antrodia Cinnamomea and has a function of inhibiting the production of nitric oxide. Therefore, the polyacetylenes can be used for preparing a pharmaceutical composition for anti-inflammation. The present invention also teaches the representative metabolites of the sporophores of Antrodia Cinnamomea, which can be used to evaluate the quality thereof.

Abstract: Disclosed are a method for preparing an n-hexane extract of the fruiting body of Antrodia cinnamomea (AC), wherein the fruiting body of AC is sequentially extracted with the ethanol solution and the n-hexane solution to obtain the n-hexane extract containing at least one benzenoid compound. The amounts of 4,7-dimethoxy-5-(3-methylbut-3-en-1-ynyl)-6-methyl-1,3-benzodioxole, 4,7-dimethoxy-5-methyl-1,3-benzodioxole, antrocamphine A and the combination thereof in the at least one benzenoid compound are determined using chromatography, NMR and HPLC. In addition, the present invention is applicable on detecting the amounts of benzenoid compounds in the AC healthcare food/drug or the fruiting body of AC, and thus owns the industrial values.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

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.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of specific ruthenium catalysts, or pre-catalysts, in hydrogenation processes for the reduction of ketones and/or aldehydes into the corresponding alcohol respectively. Said catalysts are ruthenium complexes comprising a tetradentate ligand (L4) coordinating the ruthenium with: —two nitrogen atoms, each in the form of a primary or secondary amine (i.e. a NH2 or NH group) or N-alkyl imine functional groups (i.e. a C?N group), and —two sulfur atoms, each in the form of thioether functional groups.

Abstract: The invention relates to hydroxytyrosol ethers derived from fatty alcohols and phenolic compounds of olive oil and the salts, solvates and hydrates thereof, which have an affinity for type 1 cannabinoid receptors (CB1) and which can: prevent the oxidation of low-density lipoprotein (LDL); and modulate the actions regulated by said receptor, such as inducing satiety, controlling intake and reducing body fat.

Abstract: Microwave irradiation is used to synthesize graphene and metallic nanocatalysts supported on graphene either by solid or solution phase. In solid phase methods, no solvents or additional reducing agents are required so the methods are “environmentally friendly” and economical, and the graphene and nanocatalysts are substantially free of residual contaminants. Recyclable, high efficiency Pd nanocatylysts are prepared by these methods.

Abstract: The present invention provides a method for preparing sesamin and sesamolin. The method includes the steps of passing a mixed solution of an oil containing sesamin and sesamolin and an aliphatic hydrocarbon solvent through a silica gel column, washing the silica gel column with an aliphatic hydrocarbon solvent, and eluting the sesamin and sesamolin adsorbed by the silica gel column with an eluent selected from the group consisting of methanol, ethanol, acetone and ethyl acetate. The method of the present invention allows a simple and convenient operation, and has excellent purifying effects and high recovery rates. Thus, the method of the present invention has substantial applicability in related industries.

Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

Abstract: Derivatives of dillapiol, sesamol and related monolignans having the following general formula: These compounds have synergistic properties, inhibit cytochrome P450 enzymes such as human CYP3A4, and can be used as pesticide synergists or pharmaco-enhancers. Accordingly, methods for increasing the efficacy and/or bioavailability of a pharmaceutically active agent and for increasing the potency of a pesticide are described, as are synergistic pesticidal and pharmaceutical compositions.

Abstract: An object of the present invention is to provide a high-purity aromatic methyl alcohol compound having reduced a bis(arylmethyl)ether compound as a side product mixed thereinto and a high-purity aromatic methyl alcohol composition having excellent preservation stability and methods for producing them. The object of the present invention is achieved by a method for producing a high-purity aromatic methyl alcohol compound, which comprises obtaining a high-purity aromatic methyl alcohol compound in high yield from an aromatic methyl alcohol-containing crude product by subjecting the crude product to distillation in the presence of an anti-decomposition agent. Further, the object for the preservation stability is achieved by producing a high-purity aromatic methyl alcohol composition using the obtained high-purity aromatic methyl alcohol compound.

Abstract: The present invention relates to a novel use of lignan compounds, which are isolated and purified from nutmeg or the aril of nutmeg for anti-wrinkle, and more particularly, the present invention relates to a novel use for anti-wrinkle of an extract of the nutmeg or an extract of the aril of the nutmeg, fragrin A, austobailignan 7, licarin E, and macelignan. The extracts and lignan compounds of the present invention have activities in suppressing collagen degradation enzyme-1 (MMP-1, matrix metalloprotei-nase-1) and formation of new collagen (type-1 procollagen), thereby having effect on inhibitng wrinkle caused by photoaging. Accordingly, the extracts and lignan compounds of the present invention may be useful for preventing or treating wrinkle caused by photoaging.

Abstract: Compositions for use in lubricating thin film storage media are provided, as well as storage media formed using the compositions, the compositions including one or more central cores having a cyclic group, and a plurality of arms extending from the central cores, wherein each arm comprises phenol or piperonyl. Methods of preparing the compositions are also provided. Methods of preparing storage media that incorporate the compositions therein are further provided.

Abstract: The present invention relates to [1] a method for keeping a quality of 2-methyl-3-(3,4-methylenedioxyphenyl)propanal useful as a perfume, which comprises incorporating from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene in the 2-methyl-3-(3,4-methylenedioxyphenyl)propanal; [2] a process for producing 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene; and [3] 2-methyl-3-(3,4-methylenedioxyphenyl)propanal having a content range from 50 to 3000 ppm of 1-acetyl-3,4-methylenedioxybenzene.

Abstract: A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity.

Abstract: The present invention relates to new 3,4-methylenedioxyphenyl inhibitors of GABA aminotransferase activity and/or GABA reuptake transporter activity, pharmaceutical compositions thereof, and methods of use thereof.

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: The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and 13C in place of normally abundant 12C. These compounds are selective PDE5 inhibitors and possess advantageous biopharmaceutical and pharmacokinetic properties. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to PDE5 inhibition, alone and in combination with additional agents.

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

Abstract: The present invention provides a method for preparing sesamin and sesamolin. The method includes the steps of passing a mixed solution of an oil containing sesamin and sesamolin and an aliphatic hydrocarbon solvent through a silica gel column, washing the silica gel column with an aliphatic hydrocarbon solvent, and eluting the sesamin and sesamolin adsorbed by the silica gel column with an eluent selected from the group consisting of methanol, ethanol, acetone and ethyl acetate. The method of the present invention allows a simple and convenient operation, and has excellent purifying effects and high recovery rates. Thus, the method of the present invention has substantial applicability in related industries.

Abstract: The invention relates to a process for the preparation of stiripentol particles having a defined particle size distribution.

Abstract: A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.

Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

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.

Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optiona

Abstract: The present invention relates to a novel process for the preparation of compounds of formula (I) wherein X, Q, R1 and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents. The invention further relates to novel intermediates useful in the preparation of the therapeutic agents.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.

Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.

Abstract: Perfluoropolyethers obtained by oxidation of perfluorodioxoles of formula (I) 1

Abstract: 2-Chloro-1,1,1-trialkoxyethane of formula (II): 1

Abstract: A process for preparing 3,4-methylenedioxymandelic acid by reacting 1,2-methylenedioxybenzene with glyoxylic acid in the presence of a strong acid and of at least one substance selected from the group consisting of an aprotic organic solvent and 100 to 1200 ml of an organic acid per kg of 1,2-methylenedioxybenzene.

Abstract: The present invention discloses a process for the synthesis of reverse hydroxamate matrix metalloproteinase (MMP) inhibitors.

Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.

Abstract: The present invention regards a three-step process for the synthesis of 5-(&agr;-hydroxyalkyl) benzo[1,3]dioxols. The process comprises: (i) the reaction of pyrocatechin (1,2-dihydroxybenzene) with a dihalo or di-alkoxyalkane, with the formation of a benzo[1,3]dioxol derivative; (ii) 5-selective catalytic acylation of the benzo[1,3]dioxol, with formation of a 5-alkanoylbenzo[1,3]dioxol and its subsequent (iii) reduction to 5-(&agr;-hydroxyalkyl) benzo[1,3]dioxol. Also described are new benzodioxols obtainable using the above-mentioned process. The process of the invention is industrially simple and has low environmental impact; it allows to obtain in high yields derivatives of considerable interest, in particular for the perfumery industry, and in the sector of insecticides.

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The invention relates to compounds of general formula (I), their optically active isomers and salts wherein Ar=alycylic, aromatic or one or more heteroatom containing heterocyclic moiety, optionally substituted by one or more alkoxy-, methylenedioxy-, alkyl-, halogen-, haloalkyl-,or nitro- group and/or condensed with a benzene ring. Ar—(CR1R2)m—(YR3R4)n—X—(CR5R6)o—(CR7R8)p—C≡C—E  (I) The compounds of general formula (I) according to the invention can be applied as active ingredients of pesticides, preferably arthropodicide compositions, and as synergists of other arthropodicideactive ingredients.

Abstract: This document describes a novel and practically excellent process for the preparation of optically active compounds, such as optically active alcohols or amines which are useful for various applications, for example, as synthetic intermediates of pharmaceuticals, liquid crystal materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compounds as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound.

Abstract: A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentanopyridine derivatives. The most preferred compounds prepared by this invention are (+)(1S,2R,3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylen edioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S,2R,3S)-3-(2-carboxymethoxy-4-methoxyphenyl)-1-(3,4-methylenedioxyph eyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Abstract: The invention relates to a class of enantiomerically pure intermediates represented by Formula I, where X is F, Cl, Br, or I, and a novel enantioselective bioreductive process using yeast to form these intermediates, which are useful in the synthesis of endothelin antagonists, and the like.

Abstract: This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;R.sup.2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R.sup.3 is halogen;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl;R.sup.5 is carboxy or an acid isostere;X is oxygen or sulphur; andn is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.

Abstract: The present invention provides to cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-?5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl!heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma.

Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.