Abstract: Compounds of formula 1 and 1-1, 1

Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selec

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: GABA-related pro-drugs of the formula (III) are provided that when administered to humans or other mammals provide an increased duration of active compound in the plasma compared to compounds of corresponding structure in which labile groups are not present.

Abstract: A novel process for the preparation of N,N′-bis[2,3-dihydroxypropyl]-5-[(hydroxyacetyl) methylamino]-2,4,6-triiodo-1, 3-benzenedi carboxamide of formula (I), commonly known as lomeprol, a novel non-ionic contrast agent which shows very good safety and contrast effectiveness.

Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.

Abstract: The invention concerns a method for preparing methionine aminoamide. The invention also concerns the preparation of methionine without co-production of salts, from an aqueous solution containing essentially methionine aminonitrile by producing during a first step aminoamide followed by two complementary steps.

Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.

Abstract: The present invention relates to novel intermediates for the hemisynthesis of taxanes and to their processes of preparation. The compounds of the present invention include precursor compounds of taxane side chains.

Abstract: Process for the preparation of amino acid derivatives of the general formula I where R1-R4 are as defined herein, from the corresponding malonic acid monoester amides of the general formula II  by Hofmann degradation using a hypohalite in an aqueously basic medium, which comprises carrying out the reaction in the presence of an alcohol or amine and using the hypohalite in amounts of from 1.0 to 1.5 equivalents and the base in amounts of from 0.8 to 4.0 equivalents per mole of starting material II.

Abstract: The present invention relates to a process for preparing a compound of the formula wherein b, Y and R3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic lactams and imides which are selective agonists and antagonists of serotonin 1 (5-HT1) receptors.

Abstract: Disclosure is a method for preparing &agr;-aspartyl-&bgr;-cyclohexylalaninamide, comprising carrying out a first step of amide formation of an &agr;-aspartyl phenylamine ester of general formula (II) wherein: R is a C1-C4 alkyl radical, and then performing a catalytic hydrogenation of the resulting &agr;-aspartyl phenylalaninamide ammonium salt, optionally released previously from its salt, and optionally transforming it into an addition acis salt.

Abstract: Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.

Abstract: The present invention provides a method and composition for treating or preventing pathogenic effects in a mammal caused by intracellular calcium overload, comprising administering to a mammal a mixture of sodium co-transport dependent amino carboxylic acids or their physiologically acceptable salts in an amount sufficient to substantially saturate sodium-dependent amino carboxylic acid transport mechanisms of a cell's plasma membranes. Administration of these amino carboxylic acids can advantageously treat or prevent cell lysis and irreversible cell damage caused by intracellular calcium overload, especially in mammals suffering from a disease condition associated with or resulting from insufficient tissue oxygenation.

Abstract: This invention is to develop novel transition metal catalysts for the practical synthesis of important chiral molecules. The invention emphasizes asymmetric catalysis based on chiral bidentate phosphine ligands with cyclic ring structures which could be used to restrict conformational flexibility of the ligands and thus the efficiency of chiral transfer can be enhanced through the ligand rigidity.

Abstract: A process for the combinatorial preparation of a substance library from n different compounds in an array of n different reaction solutions at n spatially separate reaction sites, in which at each of the n reaction sites

Abstract: 2,3-Di-substituted trans olefinic N-heteroaromatic or urido propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: The present invention relates to new malonic acid derivatives of the formula 1, 1

Abstract: Novel aminobutyric acids derivatives and methods for protecting crops against fungal diseases by applying to the crops or their locus a composition containing an effective amount of said derivatives.

Abstract: A method for recovering amino acids, which comprises supplying a mixed solution containing inorganic acid salts, amino acids and non-electrolytes such as saccharides to a first-step resin layer comprising an Na type or K type strongly acidic ion exchange resin; separating an effluent into at least a first fraction containing coloring matters, acidic amino acids and ashes, a second fraction containing neutral amino acids and saccharides, and a third fraction containing betaines; supplying the second fraction to a second-step resin layer comprising at least one resin selected from the group consisting of NH4 type, Ca type and Mg type strongly acidic ion exchange resins, and optionally further supplying it to a third-step resin layer comprising an Mg type or Ca type strongly acidic ion exchange resin different from the resin of the second-step resin layer, thereby recovering various kinds of amino acids contained in an effluent.

Abstract: An aminopolycarboxylic acid compound represented by the following formula or analogous thereof: The aminopolycarboxylic acid compound of the present invention can be used as a chelating agent for various metals, which is excellent in the biodegradability and masking effect on metals.

Abstract: The preparation of a mono-cationic salt of N,N′-bis(2-hydroxybenzyl)-ethylenediamine-N,N′-diacetic acid (HBED) and HBED itself is disclosed. In particular, the invention relates to the hydrolysis of the t-butyl ester of HBED with a weak acid, such as formic acid, to form HBED, and the subsequent reaction with an equimolar amount of a base to form the mono-cationic salt.

Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: The present invention provides N-alkylaspartyl dipeptideester compounds and salts thereof, such as N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which provide high degrees of sweetness in comparison to conventional products, compositions and products containing the novel aspartyl dipeptide ester compounds and method of producing the novel aspartyl dipeptide ester compounds.

Abstract: Disclosure is a method for preparing &agr;-aspartyl-&bgr;-cyclohexylalaninamide, comprising carrying out a first step of amide formation of an &agr;-aspartyl phenylamine ester of general formula (II) 1

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.

Abstract: A description is given of new chiral phosphine ligands containing amino acid groups and having the formula I where R1 is hydrogen, a C1-C7-alkyl radical, a C6-C10-aryl radical or a monovalent metal, preferably sodium or potassium, R2 is hydrogen or a C1-C7-alkyl radical, R3 is hydrogen or an —NR5R6 radical, where R5 and R6 are identical or different and are hydrogen or C1-C7-alkyl or C6-C10-aryl radicals, m is 0 or 1, with the exception of the compounds in which R5 and R6 are hydrogen and at the same time R2 is hydrogen, R4 is phenyl and R1 is methyl or benzyl and a process for their preparation. These phosphine ligands are suitable as constituents of metal complexes which can be used as catalysts for reactions to form C—C, C—H, C—N, C—Si or C═O bonds.

Abstract: Use in the prevention and/or in the treatment of neurodegenerative diseases of 2-amino-4-phenyl-4-oxo-butyric acid derivatives which act as kynureninase enzyme inhibitors and/or kynurenine-3-hydroxylase enzyme inhibitors.

Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).

Abstract: The invention relates to diethylenetriaminepentaacetic acid derivatives, their complexes and complex salts, containing an element of atomic numbers 20-32, 39-51 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and antidotes and process for their production.

Abstract: The invention relates to glutarimides of formula (I): in which Ar represents a phenyl non substituted or substituted one or more times with one of the substituents selected from a halogen atom, a hydroxyl, a (C1-C4)alkoxy, a trifluoromethyl, a (C1-C4)alkyl, said substituents being identical or different; a pyridyl group; a thienyl group and X is methylene or ethylene, their salts and their enantiomers, as well as their method of preparation and their use for the preparation of the corresponding 3,3-disubstituted piperidines.

Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.

Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.

Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.

Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.

Abstract: The invention relates to a compound having the general Formula I: including its salts, where Z is either the group having the general Formula II: where R1 is alkyl having 1-4 C atoms, alkoxyalkyl having 2-5 C atoms or aryloxyalkyl whose alkyl group has 1-4 C atoms, R2 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms, R3 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2, Y is H2 or O and L is a luminophoric moiety in a position para or meta to the nitrogen, or is the group having the general Formula III: where n is 2 or 3, R4 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms, R5 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and L is a luminophoric moiety in a position para or meta to the nitrogen, or is the group having the general Formula IV: where R6 is alkyl having 1-3 C atoms or phenyl, R7 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and L is a luminophoric moiety in a position para

Abstract: A substance PF1191 having an inhibitory activity to kainic acid toxicity represented by the following formula (I) which is obtained by incubating a fungus belonging to the genus Eupenicillium and isolating the product thus produced from the culture by solvent extraction, adsorption column chromatography, gel filtration, etc.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).

Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention 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 tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.

Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an .alpha.-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.

Abstract: Amino acids are derivatized for use in peptide synthesis by conversion to N-carboxyanhydrides that are N-proected by either a trityl or a phenylfluorenyl group.

Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an .alpha.-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.

Abstract: The present invention provides a skin external preparation comprising a compound of the formula (1), (2), (3) or (4). ##STR1## wherein X represents COOH, etc., Z represents CONH.sub.2, etc. and R.sup.1 and R.sup.7 individually represent a hydrogen atom, etc.The above-described compound has excellent effects, for example, for preventing or alleviating skin aging or inhibiting hair growth.

Abstract: The invention provides analogs of PYY. The invention also provides compositions and methods useful for controlling biological activities such as cell proliferation, nutrient transport, lipolysis, and intestinal water and electrolyte secretion.

Abstract: A sulfur-containing amino acid compound having a high inhibitory activity on LTA.sub.4 hydrolase which is represented by the following formula: ##STR1## wherein R.sup.1 represents H, alkyl, optionally substituted phenyl alkyl, alkanoyl or optionally substituted benzoyl; R.sup.2 represents ester, amide or carboxyl; R.sup.3 represents hydroxyl, alkyl, halogenoalkyl, alkoxy, halogenoalkoxy, alkylthio, optionally substituted phenyl, optionally substituted phenoxy, optionally substituted phenylthio, halogen atom, alkylsulfonyl, halogenoalkylsulfonyl, nitro or cyano; R.sup.4 represents alkyl; A.sup.1 represents alkylene; and A.sup.2 represents alkylene.