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7285676 |
Synthesis of chiral 2-alkyl amino acids
Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino...
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7115769 |
Synthesis of 2-alkylcysteine via phase transfer catalysis
Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present...
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6972340 |
Selective protein tyrosine phosphatatase inhibitors
Compounds of formula (I)
or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the...
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6927236 |
Coniosulfides and their derivatives, processes for preparing them, and their use as pharmaceuticals
The present invention relates to compounds of the formula
which are formed during fermentation by the microorganism Coniochaeta ellipsoidea Udagawa, DSM 13856, or by one of its mutations...
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6878845 |
Oligomers from multifunctional acrylates
Oligomers from multifunctional acrylates and organonitro compounds are provided. Films obtained from crosslinked oligomers of the present invention are useful as protective or decorative coatings...
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6770776 |
Synthesis of fluorocarbon compounds
Fluorocarbon compounds are synthesized by reacting a substrate hydrocarbyl compound containing at least one sp 3 -hybridized halophoric carbon atom bearing at least two halogen atom substituents,...
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6559334 |
Polymers chromatographic separation of enantiomers
The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for...
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6495680 |
Helices and nanotubes on folding compositions and method of making same
Helical oligomer and polymer compositions that form nanotubes are described. The compositions comprise a plurality of aromatic substituents linked by at least one amide group. The compositions have...
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6407281 |
Process for producing optically active cysteine derivatives
A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is...
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6180667 |
Esters of acyl L-carnitines and pharmaceutical compositions containing same for treating endotoxic shock
Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally ω-substituted with trialkylammonium,...
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5994539 |
Mercapto acyl aminoacid derivatives endowed with dual ACE-NEP inhibitory activity, useful in the treatment of cardiovascular diseases
Compounds of formula ##STR1## wherein R, R 1 , R 2 , R 3 , R 4 , m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain...
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5945548 |
Process for the synthesis of α-substituted acrylic acids and their application
Process for the synthesis of α-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
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5945451 |
Fluorobutenyl(thio)ethers used as pesticides
The present invention relates to new fluorobutenyl (thio)ethers of the formula (I) ##STR1## in which R 1 represents hydrogen or halogen, R 2 and R 3 independently of one another represent...
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5945408 |
Hydroxyanidino derivatives useful as nitric oxide synthase inhibitors
The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
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5935988 |
Tolerability of pharmaceutically active β-amino acids
The present invention relates to mixtures of α-amino acids and/or derivatives thereof and cyclopentane-β-amino acids and/or derivatives thereof, dipeptides of the abovementioned α-amino acids...
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5863931 |
Amidino derivatives and their use as nitric oxide synthase inhibitors
Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R 1 is a C 1 -6 straight or branched chain alkyl group, a C 2 -6 alkenyl group, a...
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5739140 |
Selected novel aryl acrylics
Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C 1 and C 2 are carbon atoms...
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5637616 |
Method for treating diseases mediated by proteases
A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid,...
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5625085 |
Esters of acyl L-carnitines and pharmaceutical compositons containing same for treating endotoxic shock
Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, straight or branched alkanoyl having 2-26 carbon atoms, optionally ω-substituted with trialkylammonium,...
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5616563 |
Glutathione N-hydroxycarbamoyl thioesters and method of inhibiting neoplastic growth
A compound of the formula ##STR1## with R being hydrogen, alkyl, cycloalkyl or aryl, which may be substituted with halogen or alkyl, and R' and R a being hydroxyl, or --O-alkyl, pharmaceutically...
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5503776 |
N-acylcarnosines and their use as antioxidants
An N-acylamino acid compound represented by the general formula (1): R--CO--(NH--X--CO) n --OR 1 (1) wherein (NH--X--CO) is an amino acid residue, X in (NX--X--CO) is...
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5491169 |
Amino acid derivatives and their therapeutical applications
Compounds having the properties of morphinic substances, particularly anasia, with beneficial effects on behaviour and with peripheral effects without their major drawbacks (tolerence, addiction),...
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5481026 |
Optically active amino acid sulphoxide and amino acid sulphone derivatives
The invention relates to new optically active amino acid derivatives of the general formula (I) ##STR1## in which n, R, R 1 , R 2 , R 3 , X and A have the meaning given in the description, which...
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5466862 |
Low molecular weight polyacetals and polyaldehydes
Low molecular weight polyaldehydes are prepared by converting the acetal groups of the low molecular weight polyacetal to aldehyde groups or by reacting an aldehyde-containing reagent (e.g.,...
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5382679 |
Process for the preparation of glutathione S-acyl derivatives, compounds obtained from said process and an intermediate useful for the preparation thereof
A selective and high yield process for S-acylating glutathione, comprising the eaction between glutathione and an acyl chloride or a carboxylic anhydride in trifluoroacetic acid is described.
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5374765 |
Method for extracting an amino acid ester from a hydrous solution of a mineral acid salt thereof
Disclosed is a method for extracting an amino acid ester from a hydrous solution which comprises adding thereto a water-insoluble organic solvent and then an amount of a base effective to liberate...
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5359128 |
Malic acid derivatives and compositions for the treatment of psoriasis
The invention comprises compositions and methods for the treatment of psoriasis. The compositions comprise compounds of the formula: ##STR1##
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5326755 |
Certain 2,4-pentadienamide pestacides
The present application discloses pesticidally active compounds of formula I: QQ 1 CR 1 CR 2 CR 3 CR 4 C(X 1 )NR 5 R 6 or a salt thereof, wherein Q is an monocyclic aromatic ring,...
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5315031 |
Oligomers with polydiene sequences and photocrosslinkable grafts and their application particularly in coating metals
Oligomers with polydiene sequences and crosslinkable grafts are useful as coatings for protecting metal surfaces as well as inking buffers. The oligomers contain a polydiene sequence of 1-100 diene...
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5292926 |
Cysteine derivatives
This invention relates to cysteine derivatives of the formula[I] and salts thereof. ##STR1## The compounds of this invention are useful for immunomodulator and treatment of liver disorder.
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5274177 |
Glutathione-S-lower fatty acid derivative
This invention relates to a glutathione-S-lower fatty acid derivative of the formula ##STR1## [wherein R 1 is a lower alkyl group which may be substituted; R 2 is a hydrogen atom; R 3 is a...
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5252745 |
Preparation and use of iodopropargyl esters of α-amino acid derivatives as antimicrobial agents
Antimicrobial compounds of the formula ##STR1## wherein R 1 is selected from the group consisting of H, an amine protective group, and a moiety of the formula ##STR2## wherein R 2 , R 5 , and R 6 ...
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5247125 |
Thiol-terminated hydroxyamides
Novel thiol-terminated hydroxyamides, and processes for their preparation and use are provided. These hydroxyamide compounds may be prepared by the reaction of a mercapto-functional alkyl ester,...
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5219886 |
Mercapto-acylamino acids
Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R 7 CO--; R 1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl; R 2 is hydrogen; lower alkyl; cyclolower...
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5214181 |
Amino acid derivatives
This invention relates to novel compounds of the formula [I], which are useful for treatment of various diseases such as immunodeficiency and autoimmune diseases caused by immune disorders,...
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5164526 |
Pleuromutilins
Compounds of formula I ##STR1## wherein R 1 and R 2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally...
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5147868 |
Thienamycin renal peptidase inhibitors
Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical...
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5138071 |
Process for preparing peptides with N-terminal non-proteinogenous amino acids
A process for preparing dipeptides with N-terminal non-proteinogenous amino acids of the formula ##STR1## in which R 1 to R 6 have the meaning stated in the description, from compounds of the...
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5099063 |
Certain phosphinic acid derivatives having antibacterial activity
New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.
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5096700 |
Halogenated aminohexanoates and aminobutyrates antimicrobial agents
The subject invention involves halogenated amino acid derivatives useful as antimicrobial agents having the structure: ##STR1## wherein --R is hydrogen or 2-aminoethyl; --R' is hydroxy, alkoxy,...
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5095114 |
Process for the enantiomer-selective preparation of γ-keto-δ-amino acid derivatives
The invention relates to a process for the enantiomer-selective preparation of γ-keto-δ-amino acid derivatives of the formula I ##STR1## characterized in that a compound of the formula II...
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5073641 |
Prodrug derivatives of carboxylic acid drugs
Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R 1 ...
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5030732 |
Aminoethylphosphinic acid derivatives
Disclosed are some new aminoethylphosphinic acid derivatives useful as antibacterial agents.
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5019285 |
Thioalkanoic acid substituted N,N-dialkylhydroxylamines and stabilized lubricant compositions
Lubricants are stablized against oxidative degradation by the incorporation therein of hydroxylamines substituted with thioalkanoic acid residues of the formula ##STR1## wherein R and R 1 are...
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4978759 |
Process for the stereospecific synthesis of optically pure 4-amino-3-hydroxycarboxylic acid derivatives
The process described makes it possible to obtain optically pure 4-amino-3-hydroxycarboxylic acids by means of a series of stereoselective steps. The starting material is an alpha-amino acid in the...
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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...
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4898977 |
Processes for the preparation of 5-amino-4-hydroxyvaleric acid derivatives
The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R 1 represents hydrogen, optionally...
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4891433 |
Process for the preparation of dibenzothiepin derivative
A novel process for the preparation of 2-(10,11-dihydro-10-oxodibenzo[b, f]thiepin-2-yl)propionic acid which shows high anti-inflammatory and analgetic action is disclosed. The process starts from...
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4886835 |
Alkadiene derivatives, their preparation, and pharmaceutical compositions containing them
Substituted alkadienes of the formula: ##STR1## in which R 1 is hydroxy or acetoxy, R 2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, and R 3 is alkylthio or alkoxy and R 4 is...
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H000645 |
Process for the conversion of maleic acid derivatives to their corresponding fumaric isomers
A process for the isomerization of maleic acid, its monoesters and monoamides in the presence of thiourea in anhydrous conditions at elevated temperature to the corresponding fumaryl forms yields...
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