Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.

Abstract: The present invention relates to a method for producing N-protected amino acid. Specifically, the present invention provides a method in which a protecting group is introduced to the amino group of an amino acid in a reaction under alkaline condition, and the N-protected amino acid thus generated is then separated from the reaction solution as crystals, without undergoing an extraction step or a concentration step. The present inventors have completed the invention based on the finding that desirable crystals of N-protected amino acids may be obtained without extraction, concentration or recrystallization steps between the initial generation of the N-protected amino acid molecules and the subsequent separation of the crystals, by first adding an water-soluble organic solvent and optionally water to the reaction solution (alkaline) containing the N-protected amino acid, and then neutralizing the solution by an acid.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the cis-alkoxyspirocyclic biphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention relates furthermore to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.

Abstract: The present invention is targeted at a novel coupling method of 1,3-dipolar cycloaddition type which is of particular use for the functionalization of biological molecules, such as, for example, proteins, enzymes or nucleic acids, insofar as it can be carried out in an aqueous medium and at ambient temperature.

Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.

Abstract: A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.

Abstract: Mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs and methods of preparing and methods of using mesophasic forms of (3S)-aminomethyl-5-hexanoic acid prodrugs are provided.

Abstract: Compositions, kits and methods are provided for the treatment or prophylaxis of influenza.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: The present invention relates to ionic liquids of the formula: (Mm+)xH+ynN+R1R2R3R4Z—N(—CHXCOO?)pY2-p or (Mm+)xH+ynP+R1R2R3R4Z—N(—CHXCOO?)pY2-p wherein any one of R1 to R4 independently represents a hydrogen, alkyl, cycloalkyl, aryl or aralkyl group that may be unsubstituted or substituted with one or more groups selected from OH, Cl, Br, F, I, phenyl, NH2, CN, NO2, an ether group, COOR5, CHO, COR5 or OR5, wherein R5 is an alkyl or cycloalkyl group, and wherein two of the groups R1 to R4 together with the N atom may form a heteroaromatic or heterocyclic group such as a pyridinium, pyrrolidinium or imidazolium group; the Z—N(—CHXCOO?)pY2-p is the anion derived from a chelating agent, wherein Z is a group selected from hydrogen, alkyl, an alkyl group optionally substituted with one or more carboxylate groups, hydroxyl groups and/or optionally containing one or more ether functionalities, or Z is a group of the formula —CH2—CHR6—R7—N—(CH2COO?)2, R6 is hydrogen or a C1-C3 alkyl group, R7 is a single bond, a C1-C3

Abstract: The present invention provides 2-azetidinone derivatives, or pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof, comprising formula (I): wherein the substituents are as herein defined. The compounds possess cholesterol absorption inhibitory activity and are accordingly of value in the treatment of disease states associated with hyperlipidaemic conditions.

Abstract: The present invention provides a pharmaceutical composition for use as art NPY Y5 receptor antagonist comprising a compound or the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.

Abstract: The invention relates to novel 4-alkoxy-cyclohexane-1-amino-carboxylic esters of the formula (IV) in which R1 and R2 are as defined in the description, to intermediates and processes for their preparation and to their use as intermediates in the synthesis of insecticidal, acaricidal and herbicidal compounds or pharmaceutically active compounds.

Abstract: The present invention relates to a process for preparing a compound of the formula: wherein R1 is lower alkyl, R4 is hydrogen or lower alkyl, and Z is optionally substituted lower alkyl, optionally substituted lower alkenly, optionally substituted amino, optionally substituted lower alkoxy, optionally substituted carbocyclyl or optionally substituted heterocyclyl.

Abstract: The present invention relates to pharmaceutical compositions of gabapentin tannate in solid dosage form, processes for production of those compositions and methods of use of those compositions. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.

Abstract: Use of neboglamine, (S)-4-amino-N(4,4-dimethyl-cyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.

Abstract: The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of ?, -diaminocarbonyl-?,?-pentamethylene glutarimide.

Abstract: A process for preparing at least one alicyclic carboxylic acid compound by Grignard reaction, the process comprising: reacting magnesium and at least one alicyclic halide compound in at least one solvent to produce at least one alicyclic Grignard reagent; concurrently adding carbon dioxide to the magnesium, the alicyclic halide compound, the solvent, and the alicyclic Grignard reagent, while the alicyclic Grignard reagent is still being produced, to form at least one alicyclic carboxylate magnesium salt; and hydrolyzing the alicyclic carboxylate magnesium salt to form the alicyclic carboxylic acid compound; wherein the alicyclic Grignard reagent and the alicyclic carboxylate magnesium salt are prepared in a one-pot synthesis.

Abstract: Stable compositions containing gabapentin compositions, methods of preparing such compositions, and methods of using such compositions.

Abstract: A polyurethane resin is synthesized from a compound represented by the following Formula (1), a polymerizable composition includes the polyurethane resin, a planographic printing plate precursor includes a photosensitive layer including the composition, and a method produces a diol compound that can be used as a raw material of the polyurethane resin. In Formula (1), R1 and R2 each independently represent a single bond or an alkylene group optionally having a substituent, R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl group, and A represents a divalent or higher linking group, provided that R1 and R2 are not both a single bond.

Abstract: The present disclosure relates to methods of rational genome mining. A method may include narrowing the number of clones that would otherwise need to be screened and/or identifying a gene with a desired catalytic activity. The disclosure also relates to a nitrile hydrolase from Bradyrhizobium japonicum USDA110 first identified by rational genome mining. In addition, the disclosure relates to nitrilase bll6402 and catalytically active variants capable of converting an ?-hydroxy nitriles, a ?-hydroxy nitrile and/or an ?,?-dinitrile to a carboxylic acid.

Abstract: Disclosed is a salt of trans-4-sulfinylamino-1-cyclohexanecarboxylic acid. Also disclosed is a method for producing a salt of trans-4-sulfinylamino-1-cyclohexanecarboxylic acid.

Abstract: A composition comprising a radioactive fluorine-labeled amino acid compound, which is reduced in radiolysis, is provided. A composition is produced by mixing the radioactive fluorine-labeled amino acid compound with a sugar lactone in an amount effective to prevent the radiolysis As the sugar lactone, one selected from the group consisting of ascorbic acid and glucono-?-lactone can preferably be used. The sugar lactone is preferably one selected from the compounds that are acceptable as pharmaceutical additives. The composition preferably contains the sugar lactone in an amount not less than 0.5 ?mol/mL and not more than an amount acceptable for pharmaceutical additives. Preferably, the composition is prepared to have a radioactive concentration in use of 25-125 MBq/mL.

Abstract: The invention relates to 4-hydroxyisoleucine, isomers, analogs, lactones, salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. More particularly, the invention relates to the use of those compounds in the prevention and treatment of disorders of fat metabolism and related syndromes. The invention further relates to the use of those compounds in the prevention and treatment of obesity and related syndromes including, but not limited to, the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight, and more particularly loss of body fat.

Abstract: A process for preparation of gabapentin hydrochloride by converting 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]-undecane into 1,5-diaminoformyl-2,4-dioxo-3-azaspiro[5,5]-undecane at a temperature of 65° C. to 85° C. in the presence of a strong acid, and then carrying out Hofmann rearrangement under an alkaline condition. The starting material of the process is readily available. The process is simple, and can reduce the purification procedure of intermediates, reduce production cost, and obtain product with higher purity.

Abstract: Hyperbranched polymers and methods for preparing the same are disclosed. The polymers are obtained based on monomers synthesized via reacting a substituted or unsubstituted cyclic anhydride with a bifunctional amine.

Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.

Abstract: A process for preparing gabapentin of formula 1, which comprises Formula (I) converting 1-allyl-cyclohexanecarboxaldehyde into 1-allyl-cyclohexanecarbonitrile; ozonizing 1-allyl-cyclohexanecarbonitrile to obtain 1-cyano-cyclohexaneacetaldehyde; acetalizing 1-cyano-cyclohexaneacetaldehyde with a suitable acetalizing agent to give the corresponding acetal and converting the latter into gabapentin.

Abstract: The preparation and use of calcium, barium, magnesium and copper salts of gabapentin enacarbil are described.

Abstract: A process for the preparation of 1,1-cyclohexanediacetic acid monoamide comprising the amination of 1,1-cyclohexanediacetic acid anhydride by reaction with aqueous NH3 at a temperature lower than 30° C. by using a NH3/anhydride molar ratio lower than 3, and the product precipitation through the acidification of the reaction mixture; a precipitation process of 1,1-cyclohexanediacetic acid monoamide; and a process for the synthesis of gabapentin comprising the above preparation of 1,1-cyclohexanediacetic acid monoamide, the Hofmann transposition of the same monoamide, the purification of a gabapentin salt and the crystallization from organic solvent.

Abstract: This invention relates to an improved process for the preparation of amino methyl cyclo alkane acetic acids. This invention particularly relates to an improved process for the preparation of gabapentin (which is chemically known as 1-aminomethyl-1-cyclohexaneacetic acid), which is a very well known agent useful for the treatment of epilepsy and other cerebral disorders. In the chemical series of 1-amino methyl cyclo alkane-1-acetic acids, Gabapentin, which is 1-amino methyl cyclo hexane-1-acetic acid has been developed as a drug having anti convulsive properties.

Abstract: The present invention relates to compounds trans (E) and cis (Z) stereoisomers of 4-t-butyl gabapentin of formula (11) and (12) and a process for the preparation of the said stereoisomers.

Abstract: The present invention relates to a process for the purification of gabapentin. The process relates to the addition of hydrochloric acid to an aqueous solution or suspension of gabapentin, before, during or after the concentration step of that solution, and the subsequent slurry of the gabapentin by the addition of an alcoholic solvent. The so obtained gabapentin has an high purity degree and, in particular, is characterized by a low content of lactam.

Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

Abstract: A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.

Abstract: This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.

Abstract: This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; ?wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.

Abstract: The present invention provides a novel process for preparation of the tannate salt of gabapentin for human and veterinary pharmaceutical use. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. However, the prior art neither discloses nor suggests the preparation of gabapentin tannate. The process for preparing gabapentin tannate includes the mixing of gabapentin and tannic acid together in the presence of one or more solvents. The method may further include the step of selecting the one or more solvents from a group consisting of purified water, ethanol, glycerin, propylene glycol, diethylether, methylene chloride, acetone, isopropyl alcohol and mixtures thereof. The process may also include the steps of isolating and purifying the tannate salt. This may be accomplished by filtration, drying, centrifugation and lyophilization. The process may utilize either natural or synthetic tannic acid.

Abstract: The present invention relates to a novel trisubstituted cyclic thickener or gelator. The present invention further relates to a method for thickening or gelating a solution comprising the use of such a gelator or thickener. A gelator or thickener according to the invention may, for instance, be used for pharmaceutical or cosmetic purposes. It may further be used as a support material in chromatographic materials or catalytically active materials.

Abstract: A process for preparation of gabapentin hydrochloride by converting 1,5-dicyano-2,4-dioxo-3-azaspiro[5,5]-undecane into 1,5-diaminoformyl-2,4-dioxo-3-azaspiro[5,5]-undecane at a temperature of 65° C. to 85° C. in the presence of a strong acid, and then carrying out Hofmann rearrangement under an alkaline condition. The starting material of the process is readily available. The process is simple, and can reduce the purification procedure of intermediates, reduce production cost, and obtain product with higher purity.

Abstract: Used as cooling agents are the compounds of 1/7-isopropyl-4/5-methyl-bicyclo[2.2.2]oct-5-ene derivatives of the formula (I) wherein R1 and R2 are independently hydrogen, hydroxyl, hydroxymethyl, carboxy, or C(O)NHR, wherein R is methyl, ethyl, propyl, isopropyl, or cyclopropyl; with the proviso that R1 and R2 are not both hydrogen.

Abstract: The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula and pharmaceutically acceptable addition salts thereof wherein R1, R1? are independent of each other H or alkyl, R2 is an alkyl and R3, R4 are independent of each other H or an alkanoyl, with the proviso that not both R3 and R4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.

Abstract: In a triterpenic acid having hydroxyl groups, at least one of the hydroxyl groups is phosphorylated to produce a phosphorylated triterpenic acid and/or a salt thereof, thereby improving the solubility of the triterpenic acid in a preparation for external application for the skin and allowing the physiological activity of the triterpenic acid to be exerted satisfactorily. The phosphorylated triterpenic acid is preferably, for example, ursolic acid phosphate and/or a salt thereof. The preparation for external application for the skin is preferably a cosmetic, particularly preferably a quasi-drug.

Abstract: The present application describes deuterium-enriched gabapentin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention provides a process for preparing gabapentin and its intermediates. The process generally involves treating gabapentin lactam with an aqueous solution of hydrobromic acid to yield gabapentin hydrobromide salt as an intermediate, which can be isolated by filtration. The gabapentin hydrobromide salt can then be hydrolyzed with a base, such as an organic amine, to yield gabapentin that can be isolated by filtration.

Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.

Abstract: A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R1 and R2 are each independently lower alkyl.

Abstract: The present invention relates to pharmaceutical compositions of gabapentin tannate in solid dosage form, processes for production of those compositions and methods of use of those compositions. Tannate salts of active pharmaceutical ingredients are used in sustained release applications and to improve certain organoleptic properties such as taste. The process may utilize either natural or synthetic tannic acid.