Abstract: Isotopically labeled alpha-keto acids and esters are disclosed herein. Also disclosed are methods of synthesizing isotopically labeled alpha-keto acids and esters.

Abstract: The invention relates to substituted 1,3-diphenylprop-2-en-1-one derivative compounds, pharmaceutical and/or cosmetic compositions containing same, and the applications thereof in therapeutics and cosmetics. The invention also relates to a method for preparing said derivatives.

Abstract: The present invention relates to C4-demethyl-epothilones or C4-bisnor-epothilones of Formula (I), their pharmaceutical use, pharmaceutical composition containing the same and methods for their preparation.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: A compound represented by formula I is used as a marker for organic products. wherein Ar1 and Ar2 each independently represent a substituted or unsubstituted phenylene group or a substituted or unsubstituted naphthylene group; R1 represents a straight or branched chain alkyl group having 1 to 22 carbon atoms; R2 represents a hydrogen atom or a group of the formula C(O)R4 where R4 is a hydrogen atom or a straight or branched chain alkyl group having 1 to 22 carbon atoms; and R3 represents a hydrogen atom, a straight or branched chain alkyl group having 1 to 12 carbon atoms, a straight or branched chain alkoxy group having 1 to 12 carbon atoms, a hydroxyl group, or a substituted or unsubstituted phenyl group or a substituted or unsubstituted naphthyl group; and Z represents a hydrogen atom or a group of atoms that combine with Ar2 or R3 to form a lactone ring.

Abstract: The invention relates to triazolopyrimidines of formula (I), in which the substituents are defined as follows: L1 represents cyano, S(?O)nA1 or C(?O)A2, wherein A1 stands for hydrogen, hydroxy, alkyl, alkylamino or dialkylamino; A2 stands for C1–C8 alkoxy, C1–C6 haloalkoxy or one of the groups named in A1; and n stands for 0, 1 or 2; L2, L3 represent hydrogen or halogen; L4, L5 represent hydrogen, halogen or alkyl; X represents halogen, cyano, alkyl, haloalkyl, alkoxy or haloalkoxy; R1 represents alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, alkadienyl, haloalkenyl, cycloalkenyl, alkynyl, haloalkynyl or cycloalkynyl, phenyl, naphthyl, or a five to ten-membered saturated, partially unsaturated or aromatic heterocyclus containing between one and four heteroatoms from the group containing O, N or S; R2 represents hydrogen or R1; R1 and R2 can form, together with the nitrogen atom to which they are bonded, a five or six-membered ring, which can be interrupted and/or substituted by an atom from the group

Abstract: Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).

Abstract: Palladum-phosphine complexes obtained by reacting a 5 compound of formula (1) below with a palladium compound: F(I) (wherein R1 is a hydrogen atom, an alkyl group, a cycloalkyl group or a phenyl group which may be substituted; R2 and R3 are each, the same or different, an alkyl group, a cycloalkyl group or a phenyl group which may be substituted; R4 and R5 are each, the same or different, a hydrogen atom, an alkyl group, a cycloalkyl group or a phenyl group which may be substituted; R6, R7, R8 and R9 are each, the same or different, an alkyl group, a cycloalkyl group, a phenyl group which may be substituted, an alkoxyl group, a dialkylamino group, a halogen atom, a phenyl group, a benzyl group, a naphthyl group or a halogenated alkyl group; R6 and R7, R8 and R9 may be combined to form, each, a fused ring, a trimethylene group, a tetramethylene group or a 20 methylenedioxy group; p, q, r and s are each an integer of 0 to 5; and p+q, and r+s are each in the range of 0 to 5.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: Disclosed are a method for producing fungicidal triazolopyrimidine compounds, agents containing said compounds, and the use thereof for controlling harmful fungi. Also disclosed are triazolopyrimidines of formula (I), in which the substituents have the following meaning: L1 represents alkyl; L2 represents halogen; L3represents hydrogen or halogen; X represents halogen, cyano, alkyl, alkoxy, or haloalkoxy; R1, R2 represent hydrogen, alkyl, haloalkyl, cycloalkyl, alkenyl, alkadienyl, alkinyl, or cycloalkinyl, phenyl, naphthyl, or a five-unit to ten-unit saturated, partially unsaturated, or aromatic heterocycle containing one to four heteroatoms from the group O, N, or S, R1 and R2 can also form a five-unit or six-unit ring along with the nitrogen atom to which they are linked. Said ring can be interrupted and/or substituted by an atom from the group O, N, and S while R1 and/or R2 can be substituted according to the description.

Abstract: The invention relates to new antibiotics designated Cyan-416A, Cyan 416B, Cyan-416C, Cyan-416D and Cyan-416E to their production by fermentation of Acremonium sp. NRRL 30631 to methods for recovery and concentration from the crude solutions, and to a process for purification and to semisynthetic ethers of Cyan-416B.

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: An NF-?B inhibitor having as an active ingredient a benzoquinone derivative represented by the general formula (1) wherein R1, R2, and R3 are each independently H, alkyl having 1 to 5 carbons, or alkoxy having 1 to 5 carbons; R4 is H, hydroxymethyl, alkyl, or carboxyl which is optionally esterified or amidated; Z is represented by the formula (A); and, n is an integer from 0 to 6, or its hydroquinone form or a pharmaceutically acceptable salt thereof.

Abstract: A polyhydroxyalkanoate that comprises a unit represented by the following chemical formula (1): wherein R1 is a substituent of an aromatic ring selected from the group consisting of H, CH3, C2H5, CH3CH2CH2, (CH3)2CH, (CH3)3C, a halogen atom, CN, NO2, COOR?, and SO2R?, wherein R? is selected from the group consisting of H, Na, K, CH3, and C2H5, and R? is selected from the group consisting of OH, a halogen atom, ONa, OK, OCH3, and OC2H5; and x represents an integer of 1 to 8 being the same or different each other in the polyhydroxyalkanoate. A method for producing the polyhydroxyalkanoate is also provided.

Abstract: Compounds of formula Ia, Ib and Ic, (Ic), in which R, R1 and R2 are e.g. phenyl, naphthyl, anthracyl, phenanthryl or a heterocyclic radical, are suitable as photoinitiators which accumulate at the surface of coatings.

Abstract: It is to provide a process for synthesizing an intended fluorine-containing compound having a geminal difluoro structure with a high yield, by subjecting a carbonyl compound which is readily available to a two-stage reaction.

Abstract: This invention relates to a novel process to obtain highly pure 4-(cyclopropylcarbonyl)-?,?-dimethylphenylacetic acid of Formula I through crystallization from a mixture of para and meta regioisomers of Formula I and II in cyclohexane, whereby the amount of undesired meta isomer, 3-(cyclopropylcarbonyl)-?,?-dimethylphenylacetic acid of Formula II is decreased to below 0.5%. The compound of Formula I is a key intermediate for the preparation of high purity terfenadine carboxylate, which is a known antihistaminic.

Abstract: A ferulic acid derivative represented by the general formula (1); a process for preparing a ferulic acid derivative represented by the general formula (1), comprising reacting ferulic acid or an ester thereof represented by the general formula (2) with a dihalomethane represented by the general formula CH2X2, wherein X is a halogen atom; and an ultraviolet light-absorbent composition comprising the ferulic acid derivative. Since the ultraviolet light absorbent composition is not only excellent in the ultraviolet light absorption but also very stable against heat, the ultraviolet light absorbent composition can be suitably used as cosmetics which especially require long-term stability.

Abstract: Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a group Ar1L2Ar2Alk- in which: Ar1 is an optionally substituted aromatic or heteroaromatic group; L2 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted arylene or heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH?C(R)— or ?in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; X is an —O— or —S— atom or —N(R2)— group in which: Rx, Ry and Rz which may be the same or different is each a hydrogen atom or an optional substituent; or Rz is an atom or group as previously defined and Rx and Ry are joined together to form an optionally substituted spiro linked cycloaliphatic or heterocycloaliphatic group; and the salts, solvates, hydrates and N-oxides thereof.

Abstract: An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.

Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: Process for making a pharmaceutical composition, comprising: a compound of formula (1) in crystalline form: 1

Abstract: The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.

Abstract: Aldehydes containing a difluorooxymethylene bridge, of the general formula I

Abstract: An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.

Abstract: The present invention provides a new fluorine-containing acetophenone derivative useful as a photo initiator, and a surface layer material containing the fluorine-containing acetophenone derivative. The present invention provides inexpensively an article with a hard coat excellent in anti-staining property, lubricity, scratch resistance and abrasion resistance, and provides a method for forming the hard coat.

Abstract: A process for the preparation of 2-oxocarboxylic acid esters represented by the following general formula (I), comprising by oxidizing a 2-hydroxycarboxylic acid ester represented by the following general formula (II) in the presence of a nitroxyl radical represented by the following general formula (III), a hypochlorite, a metal bromide and water with the pH of the reaction system being kept within the range of 5 to 7: 1

Abstract: The invention relates to a process for preparing optically active 5-hydroxy-3-ketoesters of formula A1 or A2, 1

Abstract: The present invention provides a process for transesterification of ketoester using polyaniline salt as catalyst, said process comprising reacting a keto ester with an alcohol in presence of a catalyst at a temperature range of 50 to 120° C. for a period in the range of 4 to 24 hours and separating the esters from the reaction mixture.

Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.

Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.

Abstract: The invention relates to a process for the manufacture of a compound of formula 1

Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1

Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.

Abstract: An unsaturated derivative at the 4-position of 6-tert-butyl-1,1-dimethylindane corresponding to the following formula: in which: X represents: a divalent radical of formula: and Y represents a divalent radical of following formula: R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue selected from the group consisting of residues deriving from glucose, galactose, mannose and glucuronic acid or an amino acid residue deriving from lysine, glycine and aspartic acid, r′ and r″, which are identical or different, represent H, low

Abstract: To provide a novel polyhydroxyalkanoate and a manufacturing method by a microorganism capable of substantially reducing unintended monomer units and obtaining the polyhydroxyalkanoate in a high yield. A microorganism capable of synthesizing a novel polyhydroxyalkanoate having 3-hydroxy-substituted benzoylalkanoic acid as a monomer unit using a substituted benzoylalkanoic acid as a material is cultured in the medium containing a substituted benzoylalkanoic acid, then the polyhydroxyalkanoate produced in the cultured bacteria is extracted and recovered.

Abstract: A novel anthracene derivative useful as an additive to a radiation-sensitive resin composition is disclosed.

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: A method for the preparation and purification of compounds using a novel support, a tetrabenzo [a, c, g, i]-fluorene group (Tbf) comprising reacting a building block (A) containing a Tbf group (Tbf-A), with a second building block (B), to afford an intermediate compound (Tbg-A-B) followed by purifying the intermediate compound by adsorption on a carbon support, removing the intermediate compound from the support with a solvent and repeating the previous reactions using the required number of building blocks to synthesize the compounds followed by removal of the Tbf group to afford the desired compounds.

Abstract: The present invention relates to novel amino acid esters of arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.

Abstract: Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates.

Abstract: An improved process for preparing carboxylic acid esters from acid chlorides, acid bromides or acids and alcohols provides for performing the esterification in the presence of the adduct (onium salt) of the corresponding carboxylic acid and 1,5-diazabicyclo[4.3.0]-non-2-ene or 1,8-diazabicyclo[5.4.0]-undec-7-ene. Alternatively, it is possible to operate in the presence of the corresponding carboxylic acid and an onium salt of the corresponding carboxylic acid.

Abstract: This invention relates to compounds of Formula (I) where Z is an amine, alcohol or derivative thereof, and the ketone analog thereof.

Abstract: Disclosed is a novel class of compounds of formula (I) wherein V, A, Y, Z, R1, E, X and D are as defined in the specification. These compounds act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor, the compounds are suitable for treating or preventing glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

Abstract: The present invention relates to methods for preparing &bgr;-ketoester fragrance pro-accords from activated acyl units, 1,3-dioxan-4,6-diones and fragrance raw material alcohols. The first step involves contacting an activated acyl unit, preferably an acid chloride, with a 1,3-dioxan-4,6-dione, an example of which is Meldrum's acid, to form a 2-acyl 1,3-dioxan-4,6-dione which is then reacted with a fragrance raw material alcohol to form the final &bgr;-ketoester fragrance pro-accord. The resulting &bgr;-ketoester fragrance pro-accords are suitable for use in laundry detergent, personal care, and other formulations wherein aesthetic fragrance materials are employed.

Abstract: The present invention is directed to novel substituted &agr;-hydroxy acid thereof, represented by the general Formula I: where R1-R5, X and Z are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: A process for the transformation of an organic molecule catalyzed by a ligand-metal complex, is conducted in compressed CO2 as a solvent, wherein the complex comprises a perfluorinated group. Further, a process for the polymerization of a monomer containing two or more polymerizable groups, optionally together with another copolymerizable monomer, to give a cross-linked polymer in the form of essentially spherical particles, is conducted in compressed CO2 as a solvent, typically in the presence of a surfactant.

Abstract: The present invention relates to the field of organic synthesis and more specifically to a process for the preparation of Michael-adducts, as defined below, by reacting a &bgr;,&bgr;- or a &agr;,&bgr;-disubstituted, or a &agr;,&bgr;,&bgr;-trisubstituted, &agr;,&bgr;-unsaturated ketone (I) with a &bgr;-ketoester or a &bgr;-diketone (II) in presence of a suitable catalyst of formula M(X)n, according to scheme 1: 1

Abstract: Adipic acid diester is caused to react with alkoxide M(OR)n, wherein R is an alkyl group and M is an alkali metal or alkaline earth metal, the reaction product is successively subjected either to coupling with halomethylstyrene followed by carbonylation, or to coupling with 2-(halomethylphenyl)propionic acid or its ester followed by decarboxylation and hydrolysis. With this process, it is possible to produce more efficiently a specific 2-substituted propionic acid, loxoprofen.