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6254850 Metal complexes, suitable for use in diagnosis and therapy  
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...
6229011 N-aroylphenylalanine derivative VCAM-1 inhibitors  
Compounds of the formula: ##STR1## 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...
6040432 Metal complexes, of DTPA derivatives suitable for use in diagnosis and therapy  
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...
6017918 Phenyl glycine compounds and methods of treating atherosclerosis and restenosis  
The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the...
5658943 Phenylalanine derivatives as endothelin antagonists  
Novel antagonists of endothelin are described, as well as novel intermediates used in their preparation, methods for the preparation and pharmaceutical compositions of the same, which are useful in...
5510522 Synthesis of N-formyl-3,4-di-t-butoxycarbonyloxy-6-(trimethylstannyl)-L-phenylalanine ethyl ester and its regioselective radiofluorodestannylation to 6- .sup.18 F!fluoro-1-dopa  
A process for forming a 6-fluoro derivative of compounds in the L-Dopa family comprising the steps of protecting the groups attached to the benzene ring in the compound followed by serially...
5338859 Process for the production of calcium salts of hydantoic acids  
The present invention provides a process for the production of calcium salts of hydantoic acids and which comprises the steps of reacting a hydantoin with a calcium base material such as calcium...
5288898 N-methylphenylserine alkyl ester derivatives and uses thereof  
As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an α-adrenergic and β-adrenergic agent to stimulate the α-adrenergic and...
5254726 No-carrier-added (NCA) aryl (18E) fluorides via the nucleophilic aromatic substitution of electron rich aromatic rings  
A method for synthesizing no-carrier-added (NCA) aryl [ 18 F] fluoride substituted aromatic aldehyde compositions bearing an electron donating group is described. The method of the present...
5246943 Substituted 1,2,3,4-tetahydroisoquinolines with angiotensin II receptor antagonist properties  
This invention relates to novel substituted 1,2,3,4-tetrahydroisoquinolines which are useful in the treatment of vascular restenosis, various disorders of the central nervous system, in the...
5194663 Aromatic derivatives of butyric acid, a process for their preparation and their use in cosmetics and in human and veterinary medicine  
An aromatic derivative of butyric acid has the formula ##STR1## These aromatic derivatives of butyric acid are useful in human and veterinary medicines as well as in cosmetic compositions.
5041637 Process for the synthesis of optically active aminoacids  
New process for the synthesis of optically active aminoacids of formula ##STR1## by treating compounds of formula ##STR2## which an optically active alcohol of formula R 4 --OH ...
5013868 Process for treating amphoteric amino acids  
The present invention relates to a process for treating amphoteric amino acids, and/or amphoteric amino acid derivatives in a fluid bed, whereby in order to maintain fluidizing conditions one adds...
4962223 Process for the synthesis of the levodopa  
New process for the synthesis of the levodopa, L-(-)-2-amino-3-(3,4-dihydyphenyl)propionic acid, drug used in the treatment of the Parkinson's disease. The process consists in resolving with...
4929755 Process for making an optically active mixture of an N-acyl-amino acid or ester containing at least two chiral centers  
In the process of hydrocarboxylating an α-enamide with CO and H 2 O or an organic hydroxyl compound to produce an N-acyl-α-amino acid or ester, respectively, the improvement comprising using as...
4888043 Herbicidal amino-mesityl cyclohexane-1,3-dione compounds  
The invention concerns compounds of the formula I ##STR1## wherein: Z is selected from hydrogen, alkyl, alkanoyl, sulfamoyl, carboxy and trifluoroacetamido; Y is selected from various carboxy or...
4879398 Process for producing 2,6-disubstituted tyrosine  
A process for making 2,6-disubstituted tyrosine by the noble metal coupling of a disubstituted aromatic halide or diazonium salt with an amino-protected 2-aminoacrylic acid to form a...
4837332 Process for blocking amino acids with the tertiary-alkoxycarbonyl group  
Amino acid salt having at least one unblocked amino group and comprising at least one cation which has a nitrogen cationic atom is reacted with 1-(tertiary-alkoxycarbonyl)imidazole in the liquid...
4833273 Process for the resolution of 1-aminoindanes  
An improved process for the resolution of 1-aminoindanes into the R-isomer on a large scale is described. The resolving agent used in the process is R-N-acetyl-3,4-dimethoxyphenylalanine. The...
4769486 Method for racemizing an optically active amino acid  
A method for racemizing an optically active amino acid, which comprises heating the optically active amino acid in an aqueous solution under an alkaline condition in the presence of an alkali metal...
4740615 Process for purified amino acids  
A process for the recovery in substantially pure form of an amino acid represented by the formula ##STR1## from an aqueous production mixture by a low pressure temperature gradient chromatographic...
4716246 Process for L-dopa  
A process for the preparation of (S)- or L-3-(3,4-dihydroxyphenyl)alanine (L-dopa) is described. The process utilizes water as reaction process solvent and proceeds via formation of an intermediate...
4695588 Fluorinated amino acids  
Novel substituted α-fluoromethyl-α-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.
4675439 Preparation process of N-acylphenylalanines  
A process for preparing an N-acylphenylalanine represented by the formula (II): ##STR1## wherein R 3 and R 4 mean individually a hydrogen atom or an alkyl, alkoxy, phenoxy, hydroxy or...
4661510 α-allenic-α-amino acids as enzyme inhibitors  
Novel α-allenic-α-amino acids which are enzyme inhibitors of the suicide or k cat type are disclosed herein.
4638086 Process for the racemization of optically active aminoacids  
The racemization of optically active aminoacids (including their N-acyl derivatives) by heating with carboxylic acids takes place particularly readily with carboxylic acids of low volatility. Only...
4634775 Optically active 3,4-bis-(diphenylphosphino)-pyrrolidine, and rhodium complexes, containing it as chiral ligands  
There are described new optically active 3,4-bis-(diphenylphosphino)-pyrrolidines of the formula ##STR1## wherein Ph is a phenyl group and R is hydrogen, an alkyl group, an arylalkyl group or an...
4613691 Preparation of amino acids from unsaturated hydantoins  
Amino acids can be easily prepared by reducing unsaturated hydantoins to the corresponding saturated hydantoins by hydrogenating the unsaturated hydantoin using either Raney Nickel catalyst in the...
4612388 Process for producing N-acylphenylalanines  
Disclosed herein is a process for producing an N-acyl-substituted or unsubstituted phenylalanine comprising hydrolyzing a 2-substituted-4-substituted or unsubstituted benzylidene-5-oxazolone with...
4508921 Process for preparation of alpha-alkyl amino acids  
A process for preparing α-alkyl amino acids by enantioretentive α-alkylation of α-amino acids is described. The products are bioactive compounds including some useful as therapeutic agents.
4480109 Process for producing threo-3-(3,4-dihydroxyphenyl)serine  
A process for producing an optically active threo-3-(3,4-dihydroxyphenyl)serine represented by the formula ##STR1## which is useful as a remedy for peripheral orthostatic hypotension or as an...
4452783 Derivatives of substituted phenylacetic acids and compositions containing them  
Aminoacid and peptide derivatives of the formula: A--NH--R 1 --CO] x [NH--R 2 --CO] y NH--R 4 --COOH in which A, R 1 , R 2 , x and y have the meanings specified in claim 1 for formula I, and...
4453007 Method for increasing the purity of amphoteric compound compositions  
Provided is a method of increasing the purity of amphoteric compound compositions. The method is: (a) providing an amount of a crude amphoteric compound composition, (b) using a portion of the...
4440936 Rhodium-phosphine chiral hydrogenation catalysis of acetophenone, atropic acid, and alpha-acylamidoacrylic acids and esters thereof  
The chiral phosphine ligand (R)-1,2-bis(diphenylphosphino)-1-cyclohexylethane, when complexed to Rh(I), functions as a superior chiral hydrogenation catalyst. The chiral phosphine ligand is more...
4436910 Process for the production of aqueous solutions of sodium salts of α- a  
Aqueous solutions of sodium salts of α-aminocarboxylic acids practically free of foreign salts are produced by saponifying the corresponding hydantoin at a temperature between 110° C. and 180°...
4421767 Compounds and methods for treating depression  
Compounds of the formula: ##STR1## wherein: X is fluorine, chlorine, or bromine; R is the group R 2 as defined below; R 1 is a group of the formula: ##STR2## or the group R 2 as defined...
4404392 Resolution of α-pivaloyloxyethyl-(S)-3-(3,4-dihydroxyphenyl)-2-methylalantinate into its α and β isomers  
Resolution of the α and β isomers of α-pivaloyloxyethyl-(S)-3-(3,6-dihydroxyphenyl)-2-methylalan inate is accomplished by; (a) forming the (+) hydrogen tartrate salt of the mixture; (b)...
4401676 Novel α-amino acids  
Novel α-ethynyl- and α-vinyl 3,4-disubstituted phenylalanines are disclosed. The compounds have pharmaceutical activity.
4380646 Method for the N-acylation of aminocarboxylic acids  
A process is disclosed for the prparation of an acylated aminocarboxylic acid which comprises contacting an aminocarboxylic acid, its alkali metal or alkaline earth metal salt with a low alkyl...
4339589 Preparation of 4-substituted oxazolidin-5-ones  
Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxazolinone-(5) compounds in an...
4288601 Fluorination process  
A process for preparing α-fluoromethyl amino acids is disclosed. The process utilizes SF 4 and BF 3 or AlCl 3 in HF to effect the fluorination.
4264771 Alkylation of substituted oxazolinone-(5) compounds  
Manufacture of 4-substituted oxazolinone-(5) compounds, which are intermediates for α-substituted aminoacids, by alkylation of 2-substituted or 3,4-disubstituted oxozolinone-(5) compounds in an...
4230893 1,1-Di(4-hydroxy-3-methoxyphenyl)-2-alkoxypropane  
4-Hydroxy-3-methoxyphenylacetone, an intermediate for methyldopa, has been prepared from reacting two moles of guaiacol and one mole of a 2-alkoxy propanol followed by basic elimination to form the...
4124533 Metal coordination complexes containing optically active phosphine or arsine ligands  
Process for the homogeneous catalytic hydrogenation of β-substituted-α-acylamido-acrylic acids which yields, after hydrogenation, an optically active mixture. The process comprises the...
4120867 Monoradioiodinated phenolic esters, acids and amines  
Monoradioiodinated derivatives of compounds employed in a radioassay prepared from precursors which are either active esters, amino acids, or amines, including a phenolic or imidazole substituent...
4111933 Protection of functional groups during reaction and their subsequent restoration  
In the process for preparing an organic compound of the formula A' -- X in which X is an amino group, a hydroxyl group or a carboxyl group, and A' is the remainder of the molecule, from an...
4087520 Lowering blood pressure with new L-3-(3,4-dihydroxyphenyl)-2-methyl-alanine peptides  
An L-3-(3,4-dihydroxyphenyl)-2-methyl-alanine peptide of the formula ##STR1## wherein A is an alkylene radical which can be substituted by a hydroxyl group or by a phenyl radical which optionally...
4020060 7-[α-Amino- ω-(3,4-methylenedioxyphenyl)acylamido]cephalosporanic acid derivatives  
Novel 7-[α-amino-ω-(3,4-methylenedioxyphenyl)acylamido]cephalosp oran ic acid derivatives are prepared which are useful as antibacterial agents.
4010181 Process for the asymmetric hydrogenation of a substituted acrylic acid or ester thereof  
Optically active diphosphines of the formula, ##STR1## in which the phosphinomethyl groups are trans to each other, form rhodium complexes useful as catalysts in hydrogenating substituted acrylic...
4005127 L-Dopa process and intermediates  
A process for the preparation of 3-(3,4-dihydroxyphenyl)-L-alanine (L-DOPA) wherein α-acetamido-4-hydroxy-3-alkoxy-cinnamic acid acetate is subjected to catalytic asymmetric hydrogenation to yield...
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