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6930200 |
Multicomponent synthesis of amino acids and derivatives thereof
Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R 2 and/or R 3 ) as shown in Formula 1:...
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6884907 |
Hydroxamic acids and acyl hydroxamines as naaladase inhibitors
This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity,...
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6855842 |
Intermediates for making a bezofuran or benzothiophene derivative nitrated in position 5 and uses thereof
The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 1 . The invention also concerns a method for preparing...
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6843917 |
Method for separating in an aqueous medium lanthanides and/or actinides by combined complexing-nanofiltration, and novel complexing agents therefor
The invention relates to the separation of lanthanides and actinides by nanofiltration complexation. The object of the invention is to satisfy the existing need for a simple, efficient and...
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6838574 |
Dicarba-closo-dodecarborane derivatives
A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I):
wherein R 1 represents a...
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6835752 |
Carboxylic acid derivatives, processes for the preparation thereof and pharmaceutical agents comprising the same as active ingredient
A carboxylic acid derivative of formula (1) wherein R 1 is COOH, COOR 6 etc.; A is alkylene etc.; R 2 is alkyl, alkenyl, alkynyl etc.; B is carbocyclic ring or heterocyclic ring; R 4 is...
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6812350 |
Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds
The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that...
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6790978 |
Thyromimetic organic compounds
Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and...
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6780874 |
Enamine derivatives
Enamine derivatives of formula (1) are described: wherein R 1 is a group Ar 1 L 2 Ar 2 Alk- in, which Ar 1 is an aromatic or heteroaromatic group, L 2 is a covalent bond or a linker atom or...
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6761922 |
Sweetener compositions containing aspartyl dipeptide ester compounds
The present invention provides solid and liquid sweetening compositions with a high intensity sweetness containing aspartyl dipeptide ester compounds, processing of making the aspartyl dipeptide...
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6762304 |
Metal catalysts and methods for making and using same
Compounds having the formula: are disclosed. M 1 and M 2 are the same or different and are transition metal atoms or ions; Z 2 and Z 3 , independently, are the atoms necessary to complete a...
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6743914 |
Kinetic resolutions of chiral 2-and 3-substituted carboxylic acids
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...
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6743940 |
4-aminobut-2-ynecarboxylic acid derivatives
There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R 1 and R 2 are each independently of the other hydrogen, C 1 -C 20 alkyl; C 3 -C 12 cycloalkyl;...
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6730518 |
Method for preventing photooxidation or air oxidation in food, pharmaceuticals and plastics
Disclosed is a method of reducing photooxidation or air oxidation in susceptible materials such as food, plastics or pharmaceuticals comprising mixing the material with an antioxidation composition...
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6720424 |
Aminobenzoic acid derivatives
Aminobenzoic acid derivatives represented by Formula (1) as follows: (wherein, R 1 represents a hydrogen atom, a C 1-6 alkyl group, or the like; R 2 represents a hydrogen atom, a C 1-6 alkyl...
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6710205 |
Benzoic acid derivatives, processes for producing the same and drugs containing the same as the active ingredient
An agent comprising the benzoic acid of formula (I) wherein A, B, R 6 , R 7 are carbocyclic ring, heterocyclic ring, etc.; R 1 is hydroxy etc.; R 2 , R 3 , R 4 are alkyl etc.; R 5 , D, E are...
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6706916 |
Optically active amino acid derivatives and processes for the preparation of the same
In producing optically-active amino acid benzyl esters by reacting optically-active amino acids with benzyl alcohols, hydrazines are present in the reaction system, or the compounds are reacted in...
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6699909 |
Aminoindanes
The present invention relates to therapeutically active novel aminoindanes of formula (I). Also provided is a method of preparing compounds of formula (I), and pharmaceutical compositions...
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6680345 |
Salicylic acid salts of salmeterol
The present invention relates to new substituted salicylic acid salts of salmeterol, processes for preparing them and their use
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6677479 |
Substituted fluoroaromatics, process for preparing them and their use
Compounds of the formula (I) and also process for preparing them where substituents X 1 , X 2 , Y and Z are defined as follows: X 1 is H or F X 2 is H or F Y is CI, Br, or I Z is CHO or COOH...
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6656737 |
Isocynate derivatizing agent and methods of production and use
An organic compound useful for detecting the total quantity of isocyanate in an environmental sample is provided. The compound is 9-anthrcenylmethyl-1-piperazinecarboxylate (PAC), an isocyanate...
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6652901 |
Sweetener compositions and uses thereof
The present invention provides compositions containing one or more aspartyl dipeptide derivatives represented by formulas (1) and/or (2) mixed with another high intensity sweetner, such Aspartame,...
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6646157 |
Method for making HBED
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...
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6642398 |
Mono-and disubstituted 3-propyl gamma-aminobutyric acids
The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I The compounds are useful as therapeutic agents in the treatment of epilepsy,...
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6638360 |
Methods for the separation of isomers
Methods for the separation of chaotropic and kosmotropic enantiomers within a racemic mixture are provided. Such methods comprise differentially partitioning the enantiomers into stabilized...
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6627767 |
Amino(oxo) acetic acid protein tyrosine phosphatase inhibitors
or therapeutically acceptable salts thereof, are protein tyrosine kinase PTP1B inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the...
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6620967 |
Ketosis-treating agent
A ketosis-treating agent comprising, as an active ingredient, at least one amino acid selected from valine, isoleucine, serine, glutamine and glutamic acid, or a peptide or protein comprising at...
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6605742 |
Cyclo azaphospha hydrocarbons
Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.
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6603041 |
Bicyclic enamide derivatives
Enamide derivatives of formula (1) are described: wherein R 1 is a group Ar 1 L 2 Ar 2 Alk- in which Ar 1 is an optionally substituted aromatic or heteroaromatic group, L 2 is a covalent bond...
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6590118 |
Aromatic compounds
Disclosed are compounds of formula I wherein A, R 1 , R 2 , R 3 , R 4 and R 5 are described in the specification, pharmaceutical formulations comprising these compounds, the use of these...
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6562967 |
Kinetic resolutions of chiral 2-and-3-substituted carboxylic acids
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...
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6552076 |
Compounds for altering mitochondrial function and cellular responses
Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto. The compounds have the structure ...
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6545018 |
Oxamic acids and derivatives as thyroid receptor ligands
The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and...
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6504052 |
Excitatory amino acid receptor modulators
Compounds of the formula (I) in which R 1 is C 1-10 allyl; C 2-10 alkenyl; C 2-10 alkynyl; phenyl-C 2-10 alkyl or phenyl-C 2-10 alkenyl; and salts and esters thereof, modulate metabotropic...
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6437178 |
O-aminophenolcarboxylic acid and o-aminothiophenolcarboxylic acid
The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure in which: A 1 to A 7 are—independently of one another—H, CH 3 ,...
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6433021 |
Indane compounds and their pharmaceutical use
Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described. In these...
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6403638 |
2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R 1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid...
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6399628 |
N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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6388127 |
Process for preparing cyclic thioamides
The present invention relates to a process for preparing a compound of the formula wherein b, Y and R 3 are defined as above, useful for preparing novel aralkyl and aralkylidene heterocyclic...
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6380249 |
HIV integrase inhibitors
Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the...
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6376707 |
Crystal polymorphism of aminoethylphenoxyacetic acid derivative
The present invention relates to a crystalline polymorph of 2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxy-phenyl)-1-methyleth
yl]amino]ethyl]phenoxy]acetic acid having strong diffraction peaks...
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6339159 |
Optically active α-aminonitrile and process for producing α-amino acid
An aldehyde compound is reacted with an amino compound and hydrogen cyanate in the presence of a chiral zirconium catalyst obtained by mixing a zirconium alkoxide with an optically active...
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6335366 |
Naphthyloxy acetic acid derivatives and a pharmaceutical composition comprising them as an active ingredient
The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR 1 , -(alkylene)CONR 2 R 3 , -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or...
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6329546 |
Caged amino acids
The caged amino acid in accordance with the present invention has the structure represented by the following formula 1: ##STR1## where X and Y each represent a halogen atom, an alkyl group, an...
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6329362 |
Cinnamic acid derivatives
Compounds of formula (1) are described: ##STR1## wherein L 1 is a covalent bond or a linker atom or group; R is a carboxylic acid (--CO 2 H) or a derivative threof; R 6 and R 7 which...
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6326398 |
Oxamic acids and derivatives as thyroid receptor ligands
The present invention provides novel compounds of the Formula ##STR1## and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs...
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6320069 |
Production of optically active ketone
Process for producing an optically active ester by reaction of a racemic alcohol with an optically active amino or tartaric acid derivative, a process for producing an optically active alcohol by...
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6310238 |
O-amino(thio)phenolcarboxylic acids, and their preparation
The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure ##STR1## in which: A 1 to A 7 are--independently of one another--H,...
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6306911 |
Substituted amino acids as neutral sphingomyelinase inhibitors
This invention relates to a series of substituted amino acids of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the...
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6291706 |
Hydrogenation of phthalic acids to cyclohexanedicarboxylic acid
The present invention relates to an improved process for the hydrogenation of phthalic acids over a supported palladium catalyst. Phthalic acids are hydrogenated with improved selectivity in...
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