Abstract: Disclosed herein are a coumarin-based derivative compound, a preparation method thereof, and a fluorescent composition containing the same.

Abstract: The invention relates to a novel polypeptide vitamin K epoxide recycling polypeptide (VKORC1) as a target for coumarin and its derivatives. The invention further provides methods for identifying coumarin derivatives, and also claims VKORC1 polypeptides and VKORC1 nucleic acids containing a sequence abnormality associated with a VKORC1 associated deficiency such as warfarin resistance, wherein the VKORC1 polypeptides and VKORC1 nucleic acids can be used for diagnosing these deficiencies. Moreover, the invention relates to methods for identifying coumarin derivatives usable in pest control of rodents.

Abstract: The invention relates to a method for carrying out an oxidation reaction for producing a product by heating a reaction medium containing a reactant and oxygen or an oxygen carrier in a reactor, wherein the reaction medium is brought into contact with a solid heating medium which may be heated by electromagnetic induction, which is surrounded by the reaction medium. The heating medium is heated by electromagnetic induction using an inductor, wherein an oxidation reaction is carried out on the first reactant to give a product and the product is separated from the heating medium. The inductor preferably generates an alternating field with a frequency in the range 1 to 100 kHz, preferably in the range 10 to 80 kHz and in particular up to 50 kHz.

Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.

Abstract: The present invention provides a composition including a polar organic extract of Eurycoma longifolia and a fraction derived from the polar organic extract, said composition comprising of quassinoids, coumarins, their glycosides, analogues and derivatives, which exhibits bioactivity of increasing spermatozoa production and spermatozoa quality in terms of morphology and motility, as well as increasing testosterone synthesis and release from cells of males. The extraction method of E. longifolia plant to produce the polar organic extract, and the subsequent purification to produce the fraction of polar organic extract containing the quassinoids, coumarins, their glycosides, analogues and derivatives, and uses for manufacturing a preparation for infertility treatment are also provided. The fraction of polar organic extract containing the quassinoids, coumarins, their glycosides, analogues and derivatives is formulated for medical applications via several routes of administration.

Abstract: A liquid crystal compound is to be obtained that has stability to heat, light and so forth, a high clearing point, a suitable optical anisotropy, a large negative dielectric anisotropy, and excellent compatibility with other liquid crystal compounds. A liquid crystal composition containing the compound is also to be obtained that has a low viscosity, a suitable optical anisotropy, a suitable negative dielectric anisotropy, a low threshold voltage, a high maximum temperature of a nematic phase (phase transition temperature from a nematic phase to an isotropic phase), and a low minimum temperature of a nematic phase. A compound having a hydrocoumarin skeleton is synthesized, and a liquid crystal composition containing the compound is produced.

Abstract: The present invention relates to novel coumarin derivatives, their carboxamides, pharmaceutical compositions containing them and their uses as drugs for kidney protection, treating drugs of hypertension, cardio-cerebrovascular diseases, non-insulin dependent diabetes, tumor, pre-cancerous lesion, and edemas.

Abstract: The invention relates to a method for carrying out an oxidation reaction for producing a product by heating a reaction medium containing a reactant and oxygen or an oxygen carrier in a reactor, wherein the reaction medium is brought into contact with a solid heating medium which may be heated by electromagnetic induction, which is surrounded by the reaction medium. The heating medium is heated by electromagnetic induction using an inductor, wherein an oxidation reaction is carried out on the first reactant to give a product and the product is separated from the heating medium. The inductor preferably generates an alternating field with a frequency in the range 1 to 100 kHz, preferably in the range 10 to 80 kHz and in particular up to 50 kHz.

Abstract: The present invention is directed to coumarin derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.

Abstract: Disclosed is the use of pyranopyranone derivatives of formula wherein R1, R2, R3, R4 and R5 independently of one another are hydrogen; C1-C30alkyl, C2-C30alkenyl, or C3-C12cycloalkyl, which may be substituted by one or more E and/or interrupted by one or more D; C6-C20aryl, which may be substituted by one or more G; C4-C20heteroaryl, which may be substituted by one or more G, C2-C18alkenyl, C2-C18alkynyl, C7-C25aralkyl, or —CO—R6; —SiR8R9R10; or R4 and R5 together form a five or six membered ring; or R3 and R4 together form a five or six membered ring; D is —CO—; —COO—; —S—; —SO—; —SO2—; —O—; —NR7—; —SiR8R9—; —POR10—; —CR12?CR13—; or —C?C—; and E is —OR6; —SR6; —NR14R15; —NR14COR15; —COR6; —COOR6; —CONR14R15; —CN; halogen; or OSO3R11; SO3R11; SO2R11; PO3(R11)2; OPO3(R11)2; G is E; C1-C18alkyl, which is optionally interrupted by D; C1-C18 perfluoroalkyl; C1-C18alkoxy, which is optionally substituted by E and/or interrupted by D; wherein R6 is H; C6-C18aryl which is optionally substituted by OH, C1-C30alky

Abstract: A liquid crystal compound is to be obtained that has stability to heat, light and so forth, a high clearing point, a suitable optical anisotropy, a large negative dielectric anisotropy, and excellent compatibility with other liquid crystal compounds. A liquid crystal composition containing the compound is also to be obtained that has a low viscosity, a suitable optical anisotropy, a suitable negative dielectric anisotropy, a low threshold voltage, a high maximum temperature of a nematic phase (phase transition temperature from a nematic phase to an isotropic phase), and a low minimum temperature of a nematic phase. A compound having a hydrocoumarin skeleton is synthesized, and a liquid crystal composition containing the compound is produced.

Abstract: 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

Abstract: The present invention relates to an esterification catalyst composition that includes a zirconium compound and a method for producing an ester compound, which includes the steps of esterifying alcohol and carboxylic acid compounds by using the same, and it may be applied to a mass synthesis process.

Abstract: Novel compounds are provided, which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Y, wherein Y is a chemical structure as shown in FIG. 1. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.

Abstract: There are provided novel fluorescent agents, such as pyrazoline compounds represented by formula (I): (wherein R1, R2 and R3 are as defined in the specification), having an ethynyl group in the molecule, which have high absorptivity in the ultraviolet-visible short wavelength range (for example, 350 nm-420 nm).

Abstract: The invention provides coumarin compounds, in particular glycosidic coumarin compounds, useful in the treatment of dermatophyte fungal infections.

Abstract: The present invention provides a method for improving the bioavailability of a renin inhibitor, preferably, of a ?-amino-?-hydroxy-?-aryl-alkanoic acid derivative, which method comprises co-administering to a mammal, especially a human, in need of such treatment, a combination of a renin inhibitor, or a pharmaceutically acceptable salt thereof, and an MDR1 inhibitor selected from a non-pharmacologically active compound.

Abstract: The invention relates to the use of sirtuin inhibitors for reducing TNF-alpha production by cells and organisms. The invention also concerns prophylactic and therapeutic applications of sirtuin inhibitors in TNF-alpha mediated pathologies, such as various inflammatory and autoimmune disorders.

Abstract: Present invention refers to substituted cumarines that are capable to emit fluorescent light when illuminated by wave lengths within ultraviolet range. Present invention also refers to process of production of said substituted cumarines, well as provides compositions containing said substituted cumarines, especially compositions containing said cumarines and volatile solvents and/or adjuvants. Said compositions can be used in objects of great value for its owner, in view of facilitating the identification of such objects.

Abstract: The present invention is directed to novel coumarin derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to ion channels such as potassium channels.

Abstract: The present invention relates in part to nettle extracts that are useful for treating or preventing seasonal allergies, allergic rhinitis, and other inflammatory conditions.

Abstract: A photosensitive compound has two or more structural units, in a molecule, represented by the following general formula (1): wherein R1 to R5 are selected from the group consisting of hydrogen atom, halogen atom, alkyl group, alkoxy group, acetoxy group, phenyl group, naphthyl group, and alkyl group in which a part or all of hydrogen atoms are substituted with fluorine atom; and X is a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group.

Abstract: The present invention is directed to molecules deriving from a 3-aryl-coumarine or 3-aryl-quinolin-2-one and having potent anti-proliferative and/or cytotoxic activity, especially against tumoral cells. The present invention also concerns the uses of these molecules in therapeutic application, for the treatment of different cancers. The invention also discloses the use of said compound for the manufacture of a medicament for treating cancer. The invention also concerns a process for inhibiting cell proliferation comprising contacting said cells with a compound of the invention.

Abstract: Novel mercaptan compounds, particularly those including a photolabile protecting group, are described as well as methods of using the compounds for the prevention and treatment of ocular damage and disease.

Abstract: This invention provides a method of detecting enzyme activity on a solid medium. The enzyme substrate has a chromogenic portion comprising a catechol residue, in which a derivitising moiety is linked to the aromatic ring of the catechol via a bond, and an enzyme cleavable group which is attached via an ester or ether linkage to the oxygen atom derived from a hydroxyl group of the catechol residue. If the enzyme substrate contacts an enzyme capable of cleaving the enzyme cleavable groups and the cleaved compound contacts a chelatable metal ion, a substantially non-diffusable coloured precipitate is formed.

Abstract: 3-Isochromanone is prepared by partially chlorinating o-tolylacetic acid with sulphuryl chloride or chlorine gas in an inert organic solvent in the presence of a free radical initiator. The 2-chloromethylphenylacetic acid first obtained is converted to 3-isochromanone by treatment with a base and separated from unreacted o-tolylacetic acid, which is in the form of a salt, by a phase separation technique. The separated o-tolylacetic acid salt is converted to o-tolylacetic acid by controlled acidification and the o-tolylacetic acid is extracted for re-use. The invention reduces the formation of unwanted, over-chlorinated by-products and leads to a more efficient process.

Abstract: The present invention provides a crosslinking agent which have photodegradable protective groups at two ends to crosslink double-stranded nucleic acid, a nucleic acid and a protein or a polypeptide, or proteins or polypeptides, in particular, double-stranded RNA; a method for crosslinking a double-stranded RNA or the like using the same; a method for regulating gene expression, which can control the expression of a target gene at an arbitrary timing and location; and a method for examining a gene function. According to the present invention, crosslinking between double-stranded nucleic acids between a nucleic acid and a protein or a polypeptide, or between proteins or polypeptides, in particular, between double-stranded RNA can be easily formed, and in addition, the crosslinking can also be easily removed, so that the expression of a target gene can be easily controlled at an arbitrary timing and location with high efficiency.

Abstract: A dihydrocoumarin ring-containing compound of the invention is represented by the following formula (1): wherein R represents hydrogen or an alkyl; A1 to A3 each represents 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z3 each represents a single bond, —(CH2)2—, —CH2O—, —OCH2—, —CF2O—, —OCF2—, —CH?CH—, —CF?CF—, —C?C—, —(CH2)4—, —O(CH2)2O—, —(CH2)2CF2O—, —(CH2)2OCF2—, —CF2O(CH2)2—, —OCF2(CH2)2—, —CH?CH—CH2O—, or —OCH2—CH?CH—; X represents hydrogen, fluorine, chlorine, —CN, —CF3, —CHF2, —CH2F, —OCF3, —OCHF2, or —OCH2F; G represents oxygen or sulfur; and n and m each represents 0, 1, or 2.

Abstract: Dihydrocoumarin produced technologically from coumarin by biotransformation is claimed together with related production variants that are carried out with the aid of isolated enzymes and/or microorganisms. Pure coumarin as well as coumarin isolated from a plant extract or coumarin-containing plant extracts can be used as starting materials. Selected strains of Saccharomyces, Arthrobacter, Pseudomonas, Bacillus, Basidiomycetes and Fusarium can be directly used for the biotransformation or can provide the enzymes required for the biotransformation. Preferred enzymes are coumarate and coumarin reductases. A production variant is additionally claimed which starts with coumarin and which, via o-coumaric acid or via intermediary dihydrocoumarin, leads to the subsequent melilotic acid which is subsequently dehydrated to dihydrocoumarin.

Abstract: A method of separating ZE-nepetalactone and EZ-nepetalactone from catnip oil involving mixing catnip oil dissolved in at least one water immiscible, non-halogenated organic solvent with at least one inorganic base dissolved in water to form a biphasic mixture, stirring the biphasic mixture to hydrolyze ZE-nepetalactone to form ZE-nepetalic acid, separating the aqueous phase containing ZE-nepetalic acid from the organic phase containing EZ-nepetalactone in the biphasic mixture, and optionally acidifying the aqueous phase to about pH 4.5 and adding at least one water immiscible, non-halogenated organic solvent to azeotropically lactonize the ZE-nepetalic acid in the presence of a catalytic amount of p-toluene sulfonic acid to form ZE-nepetalactone.

Abstract: 4-Substituted coumarin compounds having the general formula of where R is H, CHO, OCH3, X, NO2, an alkyl having C1-10, —OCH2O—, an aryl being mono- or poly-substituted with CN or COOCH3 with the aryl being a phenyl, naphthyl, or azaryl, or a coumarin group that is substituted with R1, R2, R3, R4, with R1, R2, R3, and R4 being H, an alkyl having C1-10, X, NO2, CN, OCH3, COOCH3 or OR5, R5 being H or an alkyl having C1-10, and X being a halogen.

Abstract: A process for the preparation of 6-methyl-4-(R)-phenyl-chroman-2-one and 6-methyl-4-(S)-phenyl-chroman-2-one, intermediates for the synthesis of tolterodine and its (S) enantiomer, by reaction of 6-methyl-coumarin with phenylboronic acids, esters and derivatives thereof, in the presence of chiral catalysts.

Abstract: A process for the preparation of 3-isochromanone which comprises contacting an o-xylene-?,??-dihalide with carbon monoxide, in the presence of a catalyst and a hindered amine base in a liquid medium comprising water and a tertiary alcohol.

Abstract: Novel coumarin derivatives comprising a coumarin moiety linked to a non-nucleosidic backbone moiety are disclosed. The resulting molecules are typically used as photoactivate crosslinking groups when incorporated into polynucleotides as replacements for one or more of the complementary nucleoside bases present in probes used in procedures involving nucleic acid hybridization reactions.

Abstract: The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Villiger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb): wherein R1, R2 and R3 are as defined above; d) converting the compou

Abstract: The present invention relates to cyclic compounds which are of the class of compounds of formula I wherein X and Y represent an oxygen atom and to processes for preparing such compounds. The compounds are useful in the treatment of dyslipidemia, atherosclerosis, and diabetes.

Abstract: Described are bicyclic lactones, both fused ring lactones defined according to the generic structure: and spiro lactones defined according to the generic structure: uses thereof in augmenting, enhancing or imparting aromas in or to perfume compositions, perfumed articles, colognes and perfumed polymers; processes for preparing such bicyclic lactones and intermediates therefor. In the structure: Z is one of the moieties: one of R1 or R3 is methyl and the other is hydrogen; and R4, R5, R6, R7, R8 and R9 are hydrogen or nonadjacent C1-C3 alkyl.

Abstract: Dihydrocoumarin is prepared by hydrogenating coumarin in the presence of a palladium catalyst.

Abstract: Dihydrocoumarin is prepared by hydrogenating coumarin in the presence of a palladium catalyst.

Abstract: (1) Methods for producing isochromanone compounds from o-xylene compounds as starting compounds through &agr;-halogeno-o-xylene derivatives, &agr;-cyano-o-xylene derivatives, and &agr;-halogeno-&agr;′-cyano-o-xylene derivatives, and (2) methods for producing isochromanone compounds from o-xylene compounds as starting compounds through &agr;,&agr;′-dihalogeno-o-xylene derivatives, &agr;,&agr;′-dihydroxy-o-xylene derivatives, &agr;-halogeno-&agr;′-hydroxy-o-xylene derivatives and &agr;-cyano-&agr;′-hydroxy-o-xylene derivatives, and methods for producing these intermediate compounds.

Abstract: The present invention is directed to novel methods for identifying small molecule ligands that are capable of binding with high affinity to a biological target molecule of interest. High affinity binding ligands identified by the described methods find use, for example, as small molecule lead compounds that may they themselves be, or may give rise to, novel therapeutic drugs. More specifically, the subject invention is directed to methods for identifying a ligand that binds to a target biological molecule of interest, wherein a population of small organic compounds are selected and then “pre-screened” to identify those that are capable of binding to the molecular target.

Abstract: Method for identifying a drug lead compound that inhibits binding of target bioogical molecules (TBM) by contacting TBM with members of a library of candidate cross-linked target binding fragments (CXBF), each CXBF having at least two candidate target bindig fragments (CTBF), which are inhibitors of binding, linked to a cross-linker, and selecting CXBF that inhibit the binding of the TBM to a greater extent than either of the individual CTBF linked to said cross-linker, wherein the library of CXBF is produced by: (a) screening a population of CTBF capable of being chemically cross-linked by a cross-linker to identify a subpopulation of the CTBF that inhibit binding of the TBM; and (b) chemically cross-linking members of the subpopulation of CTBF or structurally related analogs thereof with a cross-linker to provide a library of CXBF, wherein at least one linking group comprises an oxime ether linking group.

Abstract: The invention relates to a process for the enantioselective preparation of tolterodine and analogues and salts thereof comprises the steps of: a) enantioselectively reducing the carbonyl function in a compound of formula (II): wherein R1, R2 and R3 independently of each other are hydrogen, methyl, methoxy, hydroxy, hydroxymethyl, carbamoyl, sulphamoyl or halogen, to form an enantiomerically enriched compound of formula (IIIa) or (IIIb): wherein R1, R2 and R3 are as defined above; b) subjecting the compound of formula (IIIa) or (IIIb) to a sigmatropic rearrangement to form a corresponding enantiomerically enriched compound of formula (IVa) or (IVb): wherein R1, R2 and R3 are as defined above; c) subjecting the compound of formula (IVa) or (IVb) to a Baeyer-Virliger oxidation to form a corresponding enantiomerically enriched compound of the general formula (Va) or (Vb): wherein R1, R2 and R3 are as defined above; d) converting the compo

Abstract: The present invention relates to a process for the preparation of a 3-isochromanone of the formula (I) by reaction of an o-chloromethylphenylacetic acid of the formula (II) at a temperature of 100 to 250° C. in the presence or absence of an ionic halide, in the presence or absence of an organic solvent with and removal of hydrogen chloride, where in the formulae (I) and (II) the radicals R1, R2, R3 and R4 independently of one another are: a hydrogen or fluorine atom; an NC or F3C group; an alkyl alkoxy or acyloxy radical, each having 1 to 18 carbon atoms; or a C6-C18-aryloxy, aryl or heteroaryl radical, 1 to 3 atoms from the group consisting of O, N and/or S being present as heteroatoms; or in which at least two of the radicals R1, R2, R3 and R4 are linked to one another and form at least one aliphatic or aromatic ring having 5 to 18 carbon atoms.

Abstract: 3-Isochromanone is prepared by contacting an o-xylene-&agr;,&agr;′-dihalide with carbon monoxide in a two-phase liquid medium, in which one phase is aqueous and the other phase is water-immiscible, in the presence of a catalyst and a hindered amine base.

Abstract: The present invention provides a safer and more efficient process for producing [2-(arylsulfonyl)ethenyl]benzene derivatives of the formula (3): wherein R1, R2, R3 and R4 are the same or different and each independently represent a hydrogen, fluorine, or chlorine atom, a lower alkyl group, or the like, and two adjacent R3 and R4 may bond each other at their terminals to form a ring, which the process is characterized in that a 2-(arylsulfonyl)ethanol of formula (1): wherein R1 and R2 are as defined above, and an acid anhydride are reacted in the presence of a base, and the reaction liquid obtained is supplied to a reaction with an aromatic halide of formula (2): wherein X represents a chlorine, bromine, or iodine atom, and R3 and R4 are the same as defined above, in the presence of a palladium catalyst and a base.

Abstract: 3-Isochromanome is prepared by reacting an o-xylene-&agr;,&agr;′-dihalide with carbon monoxide and water in the presence of a metal catalyst such that the pH of the reaction is maintained between about 7 and 11.

Abstract: Methods for recovering isoflavones and derivatives thereof from soy molasses are disclosed. In a first embodiment, a method is disclosed in which isoflavones are recovered from soy molasses. In a second embodiment, a method is disclosed whereby isoflavone conjugates present in soy molasses are converted to isoflavone glucosides, and an isoflavone glucoside material is recovered from the soy molasses. In a third embodiment, a method is disclosed in which isoflavones are converted to their aglucone form, and an aglucone isoflavone material is recovered from soy molasses.

Abstract: The present invention relates to a process for preparing an isochroman-3-one of the formula (I) by reacting a 1,2-bishalomethylbenzene of the formula (II) ##STR1## in which X is chlorine, bromine or iodine with carbon monoxide and water at a CO pressure of from 0.1 to 50 MPa and a temperature of from 20 to 200.degree. C. in the presence or absence of an ionic halide, in the presence of a palladium catalyst and a dipolar aprotic solvent, where in the formulae (I) and (II) the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another denote:a hydrogen or fluorine atom;a HO.sub.2 CCH.dbd.CH--, NC-- or F.sub.3 C group;an alkyl, alkoxy or acyloxy radical having in each case 1 to 18 carbon atoms; or a C.sub.6 -C.sub.18 -aryloxy, aryl or heteroaryl radical, where the heteroatoms present are 1 to 3 atoms from the group O, N and/or S;a R.sup.5.sub.2 P(.dbd.O)--, R.sup.6 C(.dbd.O)--, R.sup.6 OC(.dbd.O)--, R.sup.6 OC(.dbd.O)CH.dbd.CH--, R.sup.7 C(.dbd.O)--, R.sup.7 OC(.dbd.O)CH.dbd.CH-- or R.sup.7.sub.

Abstract: 3-Isochromanone is prepared by reacting o-tolyacetic acid with sulphuryl chloride in the presence of a free radical initiator, e.g. AIBN, followed by ring closure of the 2-chloromethylphenylacetic acid so formed with a base, e.g. potassium bicarbonate.