Abstract: A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.

Abstract: This invention provides new lipoxin analogs, compositions containing analogs, and methods of using these compounds and compositions for treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease. The invention also provides for methods of treating and preventing oral inflammation, including gingivitis, periodontitis, and other forms of periodontal disease with compositions containing COX-2 inhibitors. Further, the invention provides methods for preventing systemic diseases beyond theoral cavity that are related to periodontal disease using the composition containing lipoxin analogs, COX-2 inhibitors, or both.

Abstract: Methods for the reduction of gaseous carbon dioxide emissions from combustion or oxidation reactions are provided. The various methods involve the formation of carbon suboxides and/or polymerized carbon suboxides (PCS), preferentially over gaseous carbon oxides to thereby reduce gaseous carbon dioxide emissions. The various methods can be employed for efficient generation of energy and/or hydrogen. In addition, various methods for the use of polymerized carbon suboxide are disclosed.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: The present invention relates to a pharmaceutical composition useful for treating or preventing inflammatory disease and cell damage, and a method for treating or preventing inflammatory disease and cell damage. The present invention uses the 2-hydroxybenzoic acid derivative represented by the specific chemical formula or its pharmaceutically acceptable salt. The compound of the present invention is useful for treating or preventing cell damage and inflammatory disease including gastritis, gastric ulcer, pancreatitis, colitis, arthritis, diabetes, arteriosclerosis, nephritis, hepatitis, Alzheimer's disease, Parkinson's disease and Lou Gehrig's disease.

Abstract: The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.

Abstract: This invention is directed to a crystalline acid of a lipoxin A4 analog of Formula (II): wherein: R1 is —O—, —S(O)t— (where t is 0, 1 or 2), or a straight or branched alkylene chain; and R2 is aryl (optionally substituted by one or more substituents selected from alkyl, alkoxy, halo, haloalkyl and haloalkoxy) or aralkyl (optionally substituted by one or more substituents selected from f alkyl, alkoxy, halo, haloalkyl and haloalkoxy); and wherein the compound of Formula (II) is a single stereoisomer or any mixture of stereoisomers. This crystalline acid is useful in treating disease-states characterized by inflammation, such as inflammatory and autoimmune disorders or pulmonary or respiratory tract inflammations in humans. Methods of preparing the crystalline acid are also described.

Abstract: The present invention relates to a new process for the resolution of mandelic acid derivatives from racemic mandelic acid derivative mixtures by salt formation with chiral base cyclic amides; to the resolved mandelic acid cyclic amide salts (see, for example, formula IIa), as well as certain other metal and amine salts of the mandelic acid derivatives, and to the use of the resolved mandelic acid derivatives as intermediates suitable for large-scale manufacturing of, for example, pharmaceutical compounds; Formula IIa, wherein R is selected from CHF2, H, C1-6 Alkyl, CH2F, CHCl2 and CClF2; and wherein n is 0, 1 or 2; R1 is H or C1-6 Alkyl and X is H, halo or C1-6 Alkyl.

Abstract: The present invention relates to a process for the resolution of mandelic acid derivative enantiomers from (racemic) mixtures by salt formation (see, for example, formula IIa) with chiral base cyclic amides, and racemisation of the unresolved enantiomer in the same process, wherein an additional racemising base may optionally be used, employing an acid:total base (i.e. cyclic amide and optional additional base) molar ratio of at least 1:1; provided that the cyclic amide base is present in a molar ratio of at least 0.75; and to the use of the resolved mandelic acid derivatives as intermediates suitable for large-scale manufacturing of, for example, pharmaceutical compounds; wherein R is selected from CHF2, H, C1-6 Alkyl, CH2F, CHCl2 and CClF2; and wherein n is 0, 1 or 2; R1 is H or C1-6 Alkyl and X is H, halo or C1-6 Alkyl.

Abstract: The present invention relates to a process for preparing enantiomerically enriched, optionally substituted 2-alkoxy-3-phenylpropionic acids by asymmetrically hydrogenating alkoxycinnamic acids.

Abstract: The present invention is aimed at a process for the preparation of enantiomerically enriched compounds of general formula (I). These are obtained by classical resolution of the corresponding acid using a chiral amino base in organic solvents.

Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.

Abstract: Disclosed is a new process and intermediates for preparing benzazepines of Formula (I): wherein R1 and R2 are as defined herein.

Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.

Abstract: The present invention relates to novel compounds of formula (I), or a salt, solvate, or physiologically functional derivative thereof, to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

Abstract: Provided is a compound represented by the general formula (I) or a salt thereof: wherein, —XY— represents —CH?CH— and the like, between R2 and the carbon atom at 5-position represents a single bond or a double bond, R1 represents a lower alkyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group (wherein a lower alkyl moiety of said lower alkoxycarbonyl group may be substituted with a heterocyclic group) and the like, and R1a represents a hydrogen atom, provided when R1 represents a lower alkoxycarbonyl group and the like, R1a may further represents a lower alkoxycarbonyl group and the like, when between R2 and the carbon atom at 5-position is a single bond, R2 represents a hydroxyl group and the like, and when between R2 and the carbon atom at the 5-position is a double bound, R2 combines with the carbon atom at 5-position to form a hydroxime group (—C(?NOH)) and the like, and R3 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.

Abstract: The present invention relates to a reduced particle size form of the compound (S)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy)phenyl]propanoic acid, as shown in formula (I), or a pharmaceutically acceptable salt thereof or a solvate of either thereof. The invention also concerns methods of treating one or more conditions associated with Insulin Resistance Syndrome using the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in one or more of said conditions. The invention further concerns pharmaceutical compositions containing the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient, as well as processes for the manufacture of the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: A process is provided for the preparation of mandelic acid derivatives. The process comprises the steps of: (a) stereoselectively cyanating a compound of Formula (2) to yield the corresponding cyanohydrin; (b) hydrolyzing the product of step (a) to the corresponding compound of Formula (1). wherein X is a substituent.

Abstract: The present invention relates to novel resolution methods, which are useful in the preparation of enantiomerically enriched intermediates which in their turn are useful in the prepartion of compounds with a pharmacological effect on the insulin resistance syndrome (IRS). It is such a process that the present inventions sets out to define, and more particularly for the preparation of the (S)-enantioner of certain 2-ethoxy-3-(4-hydroxyphenyl)propanoic acids and derivatives thereof.

Abstract: Novel ?-aryl-?-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. The compounds have hypolipidemic, antihyperglycemic uses.

Abstract: The present invention provides a method for producing compound (XIV) useful as an intermediate for pharmaceutical agents efficiently and economically on an industrial scale without using ozone oxidation and highly toxic reagent, and an intermediate used for this method. Particularly, the present invention provides a method for producing a compound having an absolute configuration represented by the formula (XV) and an enantiomer thereof without using a technique such as optical resolution and the like, and an intermediate used for this method. (1) Compound (XIII) as a starting material is led to compound (I), and after introducing a protecting group, subjected to reduction and cyclization to give compound (XIV). Particularly, compound (XIII) as a material is led to compound (I) via compound (XX) to produce compound (XIV).

Abstract: The present invention relates to: a method for producing ?-hydroxycarboxylic acid, which comprises hydrolyzing cyanohydrin in the presence of a hydrocarbon solvent; a method for producing optically active ?-hydroxycarboxylic acid, which comprises: producing optically active cyanohydrin by performing a reaction between a carbonyl compound and hydrogen cyanide, using a solvent comprising at least one organic solvent selected from a group consisting of an alcoholic solvent, an ester solvent, an ethereal solvent and a carboxylic solvent; removing said organic solvent from said reaction solvent; and hydrolyzing the remaining reaction mixture without isolating optically active cyanohydrin; a method for producing optically active ?-hydroxycarboxylic acid, which comprises hydrolyzing optically active cyanohydrin, using at most 10 equivalents of mineral acid relative to said optically active cyanohydrin under the condition that maximum temperature when reacting is 90° C.

Abstract: Glyceric acid compounds of the formula (I) R1R2C(OH)—CR3(OH)—COOX??(I) where R1, R2 and R3 are independently hydrogen, C1-12-alkyl, C6-12-aryl, C7-13-alkaryl or C7-13-aralkyl and X is hydrogen, an alkali metal, an alkaline earth metal/2 or NH4, are prepared by saponification of glycidic acid compounds of the formula (II) where Y is NH2 or OR4 in which R4 is C1-12-alkyl or C7-13-aralkyl, with ring-opening addition of water onto the epoxide ring. Preferably, Y is NH2 and the glycidamide of the formula (II) which is used is prepared by reacting acrylonitriles of the formula (III) R1R2C?CR3CN??(III) with hydrogen peroxide.

Abstract: The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

Abstract: The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).

Abstract: Process for the preparation of optically highly pure (R)- and (S)-&agr;-hydroxycarboxylic acids, in which either isolated, impure (R)- and (S)-&agr;-hydroxycarboxylic acids prepared by acidic hydrolysis of the (R)- and (S)- cyanohydrins obtained by enzyme-catalyzed addition of a cyanide group donor to the corresponding aldehydes or ketones are recrystallized in an aromatic hydrocarbon, optionally in the presence of a cosolvent, and optically highly pure (R)- and (S)-&agr;-hydroxycarboxylic acids having an optical purity of over 98%ee are obtained or the hydrolysis solution obtained by acidic hydrolysis of the (R)- and (S)-cyanohydrins is treated directly with an aromatic hydrocarbon, optionally in combination with a cosolvent, and is then extracted at hydrolysis temperature, whereupon after cooling of the organic phase the corresponding chemically and optically highly pure (R)- and (S)-&agr;-hydroxycarboxylic acids having an optical purity of over 98%ee crystallize out.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: An industrially advantageous process for producing optically active 4-amino-2-methylbutane-1-ol which is useful as an intermediate in synthesizing optically active medicines and pesticides. Racemic 4-amino-2-methylbutane-1-ol is treated with an optically active organic acid. The diastereomeric salt thus obtained is crystallized out and subjected to solid-liquid separation to give optically active 4-amino-2-methylbutane-1-ol. The diastereomeric salt of optically active 4-amino-2-methylbutane-1-ol with an optically active reagent for optical resolution is decomposed by bringing into contact with a solvent and an alkali and subjected to solid-liquid separation, thereby recovering the optically active 4-amino-2-methylbutane-1-ol from the filtrate. Further, the filtration residue containing the alkali salt of the reagent for optical resolution obtained by the solid-liquid separation is brought into contact with a solvent and an acid.

Abstract: Glyceric acid compounds of the formula (I)

Abstract: A process is provided for the preparation of mandelic acid derivatives.

Abstract: The present invention relates to a production method of (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid which comprises optical resolution of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid with an optically active amine of the formula (VIII) wherein R2 is 3,4-dimethoxyphenyl or 2-chlorophenyl. According to the present invention, (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid useful as a starting material of a pharmaceutical agent can be efficiently produced with a high optical purity and a relatively high total yield.

Abstract: A new process for the preparation of specific aromatic aldehydes by ozonolysis of aromatic alkenes is provided. This new process can be advantageously integrated into a synthesis of specific chiral diols using aromatic aldehydes of this type.

Abstract: A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.

Abstract: The present invention relates to novel resolution methods, which are useful in the preparation of enantiomerically enriched intermediates which in their turn are useful in the prepartion of compounds with a pharmacological effect on the insulin resistance syndrome (IRS). It is such a process that the present inventions sets out to define, and more particularly for the preparation of the (S)-enantioner of certain 2-ethoxy-3-(4-hydroxyphenyl)propanoic acids and derivatives thereof.

Abstract: A &ohgr;-substituted phenyl-prostaglandin of formula (I), a process for the preparation thereof, a mediciament comprising it as active ingredient (all symbols have the same meaning as described in the specification). The compounds of the formula (I) bind strongly in PGE2 receptor (especially subtype EP4) and therefore are useful for the prophylaxis and/or treatment of immune diseases (autoimmune diseases (amyotrophic lateral sclerosis (ALS) etc.), post-transplantation graft rejection, etc.), asthma, abnormal bone formation, neurocyte death, pulmopathy, hepatopathy, etc. They are also related to sleeping disorders and platelet coagulations, and therefore they are also applicable to these diseases.

Abstract: Compounds having the general structure: which are useful for the treatment of a variety of diseases and conditions, such as bone disorders.

Abstract: Compositions and methods for the treatment of dry eye and related diseases utilizing 6-keto-PGF1&agr; and its analogs are disclosed.

Abstract: The present invention relates to compounds of formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A malic acid or oxalacetic acid derivative is represented by the following formula (1): wherein ring Z is an alicyclic carbon ring; each of Ra and Rb is independently a hydrogen atom, a metal atom, or an organic group; and Y is a hydroxyl group or an oxygen atom, where ring Z is a bridged carbon ring or a monocyclic carbon ring having eight or more members when Y is an oxygen atom. The alicyclic carbon ring includes, for example, cyclooctane ring and adamantane ring. This compound is a novel malic acid derivative having an alicyclic group bonded to a carbon atom at the 3-position, or a novel oxalacetic acid derivative having a specific alicyclic group bonded to a carbon atom at the 3-position.

Abstract: Compounds having a structure according to the following formula: are effective in treating disorders such as bone disorders and glaucoma in a subject in need thereof.

Abstract: The present invention provides a compound of formula I or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, —(CH2)h—C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted —(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted —(CH2)h—C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h—C3-8 cycloalkenyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted —(CH2)h-heterocyclic ring, substituted and unsubstituted —(CH2)i—X—R4 (X is —O—, —S(═O)j—, —NR7—, —S(═O)2NR8—, or —C(═O)—), and —(CH2)iCHR5R6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.

Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

Abstract: A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical prepartions containing it and the use of the compound in clinical conditions associated with insulin resistance.

Abstract: The invention relates to a method of preparing 2- and 4-hydroxymandelic acid by condensing glyoxylic acid with phenol. The glyoxylic acid is reacted with phenol, after which the formed reaction mixture or the phenol, the 2- and 4-hydroxymandelic acid respectively are elution-separated in a column comprising an anion exchange resin, wherein first the excess phenol is separated, followed by the separation of the 4-hydroxymandelic acid and finally the 2-hydroxymandelic acid, both in the form of acid and salt, depending on the eluent used.