Abstract: The present invention aims to provide a means by which a cured product to be obtained has a low dielectric loss tangent and higher heat resistance. Specifically, provided are an active ester compound represented by chemical formula (1): (where in chemical formula (1), Ar1 is a substituted or unsubstituted first aromatic ring group, and each Ar2 is independently a substituted or unsubstituted second aromatic ring group, in which at least one of Ar1 and Ar2 has an unsaturated bond-containing substituent, and n is an integer of 2 or 3), a curable composition containing the active ester compound, and a cured product thereof.

Abstract: A method of screening for a plant defense activator, which enhances an immune response of a plant, from at least one candidate substance includes: contacting a plant cell in which a jasmonic acid-dependent defense pathway and a salicylic acid-dependent defense pathway of a plant defense system are capable of working independently from each other, with a candidate substance; contacting the plant cell with a trigger material that induces an immune response; and assaying the plant cell after contacting with the trigger material based on an index representing an immune response, to select a target substance that enhances an immune response of the plant. A method of enhancing an immune response of a plant includes use of a specific compound, and a plant immune response enhancer includes the specific compound.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.

Abstract: An object of the present invention is to provide an auxin biosynthesis inhibitor superior to L-AOPP. The object can be attained by a compound represented by general formula (I): wherein, R1 to R5 and X are the same as defined in the specification or a salt or solvate thereof.

Abstract: Pro-apoptotic compounds having a tripartite structure: A-L-B are disclosed. In these compounds A is an IBM mimetic moiety; L is a linker and B is a moiety that binds to a protein on the outer mitochondrial membrane. The compounds are useful for inducing cell apoptosis and therefore treating cancer.

Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.

Abstract: The present invention relates to a process for obtaining cinatrins C1 and C3 and derivatives thereof which comprises the hydroxylation of a compound of formula (III).

Abstract: Described are a method and a composition for preventing and/or treating a disease related to mitochondrial dysfunction by inhibiting the fatty acid oxidation of one or more cells of an organism. Particularly, the fatty acid oxidation is inhibited by inhibiting the expression and/or activity of the enzyme Camitin-Palmitoyl-Transferase-1 (CPT-1) by means of an arylalkyl- or arlyoxyalkyl-substitued oxirane carboxylic acid or pharmaceutically acceptable salts and derivatives of the arylalkyl-substituted oxirane carboxylic acid.

Abstract: Carnitin-Palmitoyl-Transferase-1 (CPT-1) inhibitor for use in treating and/or preventing disorders caused by delipidation of neural tissue.

Abstract: Compounds of formula (I): are disclosed. In these compounds Y is —CH(OH)—, —CH(NHR6)—, —C(=0)-, —CH?CHCO— or—formula (II)—and R1 and R2 are hydrogen, OH, alkyl, alkoxy, benzyloxy and aryl, and, when Y is —CH(OH)—, additionally alkenyl or alkynyl. Processes for the production of these compounds are also disclosed.

Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.

Abstract: Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.

Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm×1.

Abstract: [Problems] To provide a modulator for signaling of TLR [Means for solving the problems] A medicament containing cathepsin inhibitor such as monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate as a active ingredient is used as a modulator for signaling of TLR, a therapeutic agent for treating diseases associated with TLR signaling, a therapeutic agent for treating diseases associated with induction of Th17 cells, a therapeutic agent for treating diseases associated with production of IL-6, IL-12, IL-17, or IL-23, or a therapeutic agent for treating systemic lupus erythematosus, lupus nephritis, crohn's disease, psoriasis, or acute disseminated encephalomyelitis.

Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.

Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.

Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm?1.

Abstract: The present descriptive report refers to a patent of invention of primary PVC plasticizers composed of epoxidized ethyl and/or isoamyl esters of vegetable oil fatty acids and to the compounds of PVC plasticized with epoxidized bioesters, belonging to the technical field of polymer additives, developed from renewable sources such as vegetable oils and sugar cane, to reduce the cost and improve the properties of PVC compounds. The epoxidized bioesters are suitable to be added to at least one PVC resin and are obtained from a transesterification reaction of at least one type of vegetable oil with ethanol or isoamylic alcohol and subsequent epoxidation, presenting oxirane index equal to or less than 8.

Abstract: A polymerizable actinic radiation curable composition comprising a photo-acid generating compound and an epoxy compound represented by Formula (1): wherein X represents a divalent group selected form the group consisting of —O—, —S—, —SO—, —SO2—, —CBr2—, —C(CBr3)2—, and —C(CF3)2—; R1 to R18 each independently represent a hydrogen atom, a halogen atom, a hydrocarbon group having 1-8 carbon atoms, provided that the hydrocarbon group may contain an oxygen atom or a halogen atom, or a substituted or unsubstituted alkoxy group having 1-8 carbon atoms.

Abstract: The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.

Abstract: The invention relates to processes for preparing oxiranecarboxylic acids and derivatives thereof, in particular to processes which proceed under stereochemical control of the reaction steps, to the oxiranecarboxylic acids prepared according to the invention and derivatives thereof and to their use in pharmaceutical compositions, in particular for treating hyperlipaemia.

Abstract: The present invention relates to a novel and efficient chemoenzymatic process of preparation of optically active trans alkyl phenylglycidates. The invention particularly discloses a novel process for the chemoenzymatic synthesis of two enantiomers of trans alkyl phenylglycidate i.e.

Abstract: Optically active fluorine-containing compounds of the formula (1): or of formula (2): are used for producing optically active 3,3,3-trfluoro-2-hydroxy-2-methylpropionic acids.

Abstract: An optically active epoxypropionate derivative of the following formula (1): wherein symbol * represents optically active carbon. Also disclosed is an optically active epoxypropionate derivative of the following formula (2): wherein symbol * represents optically active carbon.

Abstract: A process for the conversion of aldehydes to esters, specifically acrolein or methacrolein to methyl acrylate or methyl methacrylate, respectively. Essentially in the absence of water, an aldehyde is contacted with an oxidizing agent to form an intermediate and then the intermediate is contacted with a diol or an alcohol to form an ester or diester. Preferably, the oxidizing agent is also a chlorinating agent. Specifically, acrolein or methacrolein is contacted with an oxidizing/chlorinating agent, such as t-butyl hypochlorite, and the chlorinated compound is contacted with an alcohol, such as methanol, to form methyl acrylate or methyl methacrylate, respectively. Generally, the order of addition is for the oxidizing agent to be added to the aldehyde, specifically for t-butyl hypochlorite to be added to acrolein or methacrolein, and for the diol or alcohol to be added to the intermediate, specifically for the methanol to be added to the reaction product of acrolein or methacrolein and t-butyl hypochlorite.

Abstract: An ester compound of formula (1) is provided. R1 is H or methyl, R2 is tertiary C4-20 alkyl, and k=0 or 1. A resist composition comprising as the base resin a polymer resulting from the ester compound is sensitive to high-energy radiation, has excellent sensitivity, resolution, etching resistance and substrate adhesion, and is suited for micropatterning using electron beams or deep-UV.

Abstract: The present invention relates to novel epoxides having the formulas 1

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.

Abstract: An ester compound of formula (1) is provided.

Abstract: The present invention relates to macromonomer compounds having the formula (I) where R1 is hydrogen, halogen, and optionally substituted alkyl, aryl, alkylaryl or arylalkyl radical; R2 and R3, which can be similar or different, are hydrogen, halogen, alkyl, aryl, alkylaryl, arylalkyl or alkoxy radical; R4 is an optionally substituted alkyl, aryl, alkylaryl or arylalkyl radical, or —XR5, with R5 being hydrogen, and optionally substituted alkyl, aryl, alkylaryl or aryalkyl; X is oxygen or sulphur; A corresponds to a unit issued from at least one ethylenically unsaturated monomer; and n is comprised between 1 and 10000. The invention also relates to dienic compounds having the formula (II): H2C═CR1—CH═CH—C(R2)(R3)—X2—R6 wherein R1 R2, R3 and X have the same meaning as above and R6 represents R5 or a group —COR7 or —COOR7 with R7 being alkyl, aryl, alkylaryl or arylalkyl.

Abstract: A process for preparing an optically-enriched chiral epoxide of formula I wherein R1, R2 and R3 are each independently selected from H, R, R—CO— and R—O—CO—, each R independently being substantially a hydrocarbon group of up to 20 carbon atoms, and X is an alkyl or cycloalkyl group of up to 10 carbon atoms, provided that —CO—X is not enolisable, which comprises the asymmetric epoxidation of a corresponding prochiral alkene of formula II R1R2C═CR3—CO—X  (II) by reaction with an oxidant in the presence of a chiral catalyst. Many optically-enriched epoxides (I) are novel.

Abstract: A process for the preparation of I: in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: is described.

Abstract: The present invention is related to compounds, compositions and methods of treating viral infections. Compounds of the present invention have the following general formula: ##STR1## wherein R is selected from --CH.sub.2 OH, --CO.sub.2 R.sup.2, --CONR.sup.3 R.sup.4, or COR.sup.5, wherein R.sup.2 is hydrogen or a lower alkyl group, R.sup.3 and R.sup.4 are each independently hydrogen or a lower alkyl group, R.sup.5 is an amino acid residue bound via a terminal nitrogen or peptide having at least two amino acid residues; and wherein R.sup.1 is C.sub.5 -C.sub.13 alkyl, aryl, aralkyl, aralkyl(lower alkyl)ether, or C.sub.5 -C.sub.13 alkyl(lower alkyl)ether.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: Cryptophycin compounds possessing a .beta.-epoxy moiety may be made with high stereoselectivity at various steps in the overall synthetic process. This invention also provides novel intermediates useful in preparing Cryptophycin compounds.

Abstract: The invention relates to a process for preparing an optically active trans-compound having formula (1), in which R represents a phenyl group, whether or not substituted, preferably p-methoxyphenyl, and A is derived from an optically active compound, in which an aldehyde having formula (2), in which R is as defined above, is, in the presence of a base, brought into contact with an optically active acetyl compound having formula (3), in which X represents a leaving group and in which A is derived from an amino alcohol, preferably a .beta.-amino alcohol having a rigid structure.Particularly good results were obtained when use was made of a compound having formula (3), in which A is derived from an amino indanol compound having formula (4), in which R.sub.1 and R.sub.2 represent a (hetero)alkyl or (hetero)aryl group, whether or not substituted, having 1-10 C atoms, or R.sub.1 and R.sub.2 constitute an aromatic or aliphatic ring together with the N atom to which they are bound, in particular in which R.sub.

Abstract: This invention relates to a novel oxirane carboxylic acid derivative and thereof manufacturing method. Based on thereof mechanism to inhibit the CPT I, oxirane carboxylic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and less side effects.

Abstract: (Het)aryloxy-, -thio- and -aminocrotonates of the formula I ##STR1## where the substituents have the following meanings: U is oxygen, sulfur or amino;V is oxygen, sulfur, amino or alkylamino;X, Y and Z independently of one another are .dbd.N-- or .dbd.CR.sup.3 --;R.sup.1 and R.sup.2 independently of one another are alkyl;R.sup.3 is hydrogen, cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio and haloalkylthio; andR.sup.4 is an organic radical which is bonded to the skeleton directly or via an oxy, mercapto, amino, carboxyl or carbonylamino group,process for their preparation, and their use.

Abstract: A process for the preparation of organic compounds through C--C bond forming reaction which comprises reacting a diene with a dienophile in the presence of solid acid based on either yttrium, scandium or lanthanum supported on metal oxide supports such as oxides of zirconium or tin or titanium or iron oxide modified by sulphation as catalysts for a period ranging from 5 to 48 hours and recovering the reaction products from the reaction mixture by filtration and removal of the solvent by evaporation followed by column chromatography.

Abstract: An epoxysuccinic acid derivative having the following formula: ##STR1## ?wherein R.sup.1 is hydrogen, alkyl, aryl, or aralkyl; each of R.sup.2 and R.sup.3 independently is aryl, aralkyl or alkyl; X is --O-- or --NR.sup.4 --; and R.sup.4 is hydrogen, alkyl, or aralkyl! is useful for prevention and treatment of bone diseases such as osteoporosis, malignant hypercalcemia and Paget's syndrome, and further useful for treatment of osteoarthritis and rheumatoid arthritis which are accompanied by abnormal enhancement of cathepsin L activity, and furthermore useful as a medicine for treating diseases in which cathepsin B and L participate, such as muscular dystrophy and muscular atrophy.

Abstract: The invention relates to phenyl propane derivatives of the general formulae: ##STR1## or their mixtures, in which R.sub.1 and R.sub.2 are a branched or straight-chained alkyl residue of the general formula C.sub.n H.sub.2n+1 with n=1-18, for use as a therapeutic agent.

Abstract: A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediates include C13 deoxy taxoids; C13 enone substituted taxoids; and C1-C2 cyclo carbonate esters of taxoids.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sub.1 stands for an optionally esterified or amidated carboxyl group, X stands for an optionally substituted divalent hydrocarbon residue, R.sub.2 stands for hydrogen or an optionally substituted hydrocarbon residue, R.sub.3 stands for an alkyl group which is substituted with a group bonded through O or S(O).sub.n wherein n is 0, 1 or 2, with a proviso that when the partial structural formula: --NH--X--CO-- is leucine residue, R.sub.3 is not 3-hydroxy-3-methylbutyl group nor 4-hydroxy-3-methylbutyl group, or a salt thereof, which is useful as prophylactic and therapeutic agents of bone diseases and as inhibitory agents of thiol protease.

Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula (I) ##STR1## wherein R.sub.1 stands for H or an optionally substituted hydrocarbon group; R.sub.2 and R.sub.3 independently stand for H, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic group; Z stands for a carbon chain containing a double bond or --Z'--C(OH)-- (Z' stands for a bond or a straight-chain or branched alkylene chain); the symbol .........

Abstract: Novel (cyclo)aliphatic epoxy compounds that contain at least one acrylate group in the molecule and at least one cycloaliphatic epoxy group can be used for the production of coating formulations, adhesives, photoresists or in stereolithography. As they contain a cohesive homogeneous network, the three-dimensional objects produced have very good green strength and very good strength properties.

Abstract: Chlorine-substituted olefins I ##STR1## (R.sup.1 =organic radical; R.sup.2 =--CN, --CO--R.sup.3, --CO--S--R.sup.3, --CO--O--R.sup.3 --CO--N(R.sup.4,R.sup.5); R.sup.3 =organic radical; R.sup.4, R.sup.5 =H, organic radical)are prepared by reacting oxiranes II ##STR2## in the presence of a carboxamide (IIIa) or of a lactam (IIIb) in liquid phase with a chlorinating agent (IV). The products I are important intermediates for dyes, drugs and crop protection agents.

Abstract: A compound of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may optionally be esterified or amidated; R.sup.2 represents a cyclic group which may optionally be substituted or a polar group; n is an integer of 0 to 6; R.sup.3 represents hydrogen or a hydrocarbon residue which may optionally be substituted; R.sup.4 represents (1) a hydrocarbon residue which is substituted by an optionally protected amino group or (2) an alkenyl group; or R.sup.3 and R.sup.4 may be combined with the adjacent nitrogen atom to form a heterocyclic group containing at least two hetero atoms, or a salt thereof.The compound or a salt thereof of the present invention inhibits thiol proteases such as cathepsin L and B and serves well as a prophylactic/therapeutic agent for bone diseases such as osteoporosis.