Abstract: A method has been developed for the preparation of ceralure B1, a potent attractant for the Mediterranean fruit fly. The method utilizes trans-siglure acid as starting material to produce iodolactone which is subsequently reduced to lactone. The lactone is converted to a mixture of epimers ceralure A acid and ceralure B1 acid. The ceralure A acid is recyclized to lactone, leaving epimer ceralure B1 acid intact. Following separation from lactone, the ceralure B1 acid is esterified to produce ceralure B1 of about 92-94% purity. The overall yield is about 58-65%, a significant improvement over currently known methods which result in yields of about 30-33%.

Abstract: Compounds of formula I in the form of their racemates or enantiomers, preferably compounds of formula Ia wherein R4 is C1-C6alkyl, Z is chlorine, bromine or iodine, and X is —OH, chloride, bromide or iodide, or X forms an ester group with the carbonyl substituent, as well as salts of carboxylic acids. The compounds are valuable intermediates for the propagation of &dgr;-amino-&ggr;-hydroxy-&ohgr;-aryl-alkanecarboxamides, which exhibit renin-inhibiting properties and could be used as antihypertensive agents in pharmaceutical preparations.

Abstract: The invention relates to a new process for the synthesis of 1-(aminomethyl)cyclohexyl-acetic acid of formula (I) via the new intermedier 1-(nitromethyl)cyclohexyl-acetic acid derivative of formula (II), wherein R represents hydrogen, benzyl group, diphenylmethyl group or C1-C4 alkyl or alkoxy aromatic ring substituted derivatives thereof.

Abstract: Modified, amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: Double fumarates of L-carnitine or isovaleryl L-carnitine and an amino acid having formula (I) are disclosed which are useful as active ingredients of food supplements, dietary supplements or drugs. wherein: R is hydrogen or isovaleryl; and [A+] is a positively charged amino acid selected from the group consisting of creatine, ornithine, lysine, arginine and histidine.

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: A process for the purification of gabapentin by treatment of a crude aqueous gabapentin hydrochloride solution with a strong cationic ion exchange resin.

Abstract: Amino Acids of formula (1) having high purity, free from the corresponding lactams and chloride anions obtained by reduction of oxyaminoacids of formula (II) 1

Abstract: A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising:

Abstract: The invention relates to stereoisomerically enriched diamines, to metal complexes comprising these diamines and also to their use in a process for asymmetrically reducing ketones using silanes, in particular polymethylhydrosiloxane, as reducing agents.

Abstract: The present invention provides compositions and methods of preparing gabapentin that includes (a) subjecting cyclohexanediacetic acid monoamide to a Hofmann rearrangement to yield a solution comprising an isocyanate intermediate; (b) hydrolyzing the isocyanate intermediate in the presence of an alkali base to form a gabapentin alkali salt; (c) converting the gabapentin alkali salt to a gabapentin-amine salt in a water-miscible polar solvent; (d) adding a basic or weakly basic ion exchange resin to a solution comprising the gabapentin-amine salt; (e) removing the ion exchange resin from the solution; and (f) concentrating the solution to yield gabapentin.

Abstract: This invention relates to novel compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; X is Cl, Br or I; or stereoisomers thereof.

Abstract: The present invention relates to novel prodrugs of gabapentin and to pharmaceutical formulations and sustained release formulations containing the prodrugs.

Abstract: Processes for preparing N-methyl-alanine derivatives and novel intermediates of the process. The derivatives and intermediates are useful for preparing cell-binding agent/maytansinoid complexes.

Abstract: The invention relates to a process for preparing highly functionalized &ggr;-butyrolactams and &ggr;-amino acids by reductive amination of mucohalic acid or its derivatives, and discloses a process for preparing pregabalin, a GABA analog with desirable medicinal activity.

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: The invention relates to amino acids, a method for the production thereof, medicaments containing said amino acids and the use of amino acids in the production of medicaments for treating pain.

Abstract: A compound of the formula 1

Abstract: The present invention provides methods for identifying test substances that bind to the &agr;2&dgr; subunit of a calcium channel.

Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.

Abstract: This invention relates to certain &bgr;-amino acids that bind to the alpha-2-delta (&agr;2&dgr;) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells.

Abstract: The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I 1

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula wherein the variables have the meanings as defined hereinbefore.

Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.

Abstract: The present invention provides compounds of formula Ia and Ib or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.

Abstract: The present invention contains halogenated 2-amino-3,4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention is directed to a method for producing amino acids by reacting halogenated carboxylic acid ester (haloacid esters) with a metal cyanate in the presence of an alcohol and by subsequent acidic saponification of the urethane carbonic acid formed. The method is characterized by the metal cyanate being placed at an elevated temperature in an organic solvent and the other reactants being continuously charged into the mixture over a defined time period.

Abstract: A process for the preparation of gabapentin starting from gabapentin hydrochloride, which comprises the following steps: preparing a gabapentin hydrochloride aqueous solution; adjusting the pH of the solution to or about to gabapentin isoelectric point by addition of a basic compound comprising a monovalent anion; diafiltering the solution through a membrane highly selective for organic compounds with molecular weight higher than 150 and poorly selective for inorganic monovalent ions, to separate the solution into an aqueous permeate containing chloride ions and a retentate containing unsalified gabapentin substantially free from chloride ions; concentrating the retentate by increasing the pressure exerted on the membrane to obtain a concentration of unsalified gabapentin in the retentate not lower than 5%; evaporating the retentate under reduced pressure and at T°<35°; precipitating gabapentin by addition of an alcohol.

Abstract: Described are new crystalline anhydrous forms of gabapentin formed from gabapentin monohydrate. The new crystalline forms provide advantages in the manufacture of the therapeutic agent.

Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration and methods of preparation of the modified amino acid compounds are also provided.

Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: 1

Abstract: An improved process for the preparation of a cyclic amino acid by a novel synthesis is described where benzonitrile is treated with an alkali metal and an amine under Birch reduction conditions to generate in situ an anionic intermediate which is alkylated with an &agr;-haloacetic acid moiety which is subsequently converted to the desired product, as well as valuable intermediates used in the process.

Abstract: Pharmaceutical compositions containing substantially pure and stable gabapentin are disclosed wherein gabapentin contains an anion of a mineral acid, such as chloride, in amounts greater than 20 ppm.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: The invention describes a process for the preparation of pharmaceutical grade gabapentin, consisting of neutralizing an alcoholic solution of gabapentin hydrochloride with basic ion exchange resins and thereafter directly isolating the gabapentin, without requiring either the formation or the isolation of intermediates other than the pharmaceutical grade product.

Abstract: The non-hydrated gabapentin polymorph is prepared by drying an aqueous solution of gabapentin by spray drying or turbo-drying and it is used for the preparation of pharmaceutical grade gabapentin by subjecting the polymorph to crystallisation from solvents.

Abstract: A process for the preparation of gabapentin of formula (I) which comprises: a) reduction of (1-nitromethyl-cyclohexyl)acetonitrile of formula (II)  to give 3-imino-2-aza-spiro[4.5]decan-2-ol of formula (III) b) transformation of compound (III), by alkali treatment, into 2-hydroxy-2-aza-spiro[4.5]decan-3-one of formula (IV) c) reduction of compound (IV) to give 2-aza-spiro[4.5]decan-3-one of formula (V) d) hydrolysis of compound (V) to gabapentin.

Abstract: A process for the production and purification of gabapentin, i.e. 1-(aminomethyl)cyclohexyl-acetic acid, which comprises hydrolysis of 2-aza-spiro[4.5]decan-3-one with HCl, treatment of the resulting product and filtration with acetone, dissolution in water at isoelectric pH and crystallization or digestion in the hot in mixtures of diisopropyl ether with ethanol or methanol.

Abstract: A process for the preparation of gabapentin of formula (I) 1

Abstract: The invention relates to a process for preparing (−)-(1S,4R) N protected 4-amino-2-cylcopentene-1-carboxylate esters represented by the formula (I) wherein R1 and R2 are as described within the specification.

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: This invention is novel processes for the stereoselective preparation of gabapentin analogues.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention relates to novel prodrugs of gabapentin and to pharmaceutical formulations and sustained release formulations containing the prodrugs.

Abstract: The invention provides a compound of formula (I): 1