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8052963 |
[(4-oxo-4H-chromen-3-yl)hydroxymethyl]- or [(4-oxo-4H-chromen-3-yl)methyl]phosphonic acid derivatives
The present invention relates to compounds of the formula (I), where R1 to R3 each, independently of one another, denote H, hydroxyl or alkoxy having 1 to 8 C atoms, R4 denotes alkyl having 1 to 4...
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8003625 |
Phosphoramidate alkylator prodrugs
Phosphoramidate alkylator prodrugs can be used to treat cancer when administered alone or in combination with one or more anti-neoplastic agents.
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7629379 |
Substituted phosphonate fluorescent sensors and use thereof
The invention relates to new compounds of formula (1) wherein R is hydrogen or a linear or branched C1-40alkyl; where X is O, S, or NR1 where R1 is a hydrogen, a linear or branched C1-40 alkyl,...
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7626044 |
Triptolide derivatives and their uses
Triptolide derivatives of Formula (I), their pharmaceutically acceptable salts and optical isomers, Formula (I): wherein, C5 and C6 are connect with each other by a C-C single bond or double bond;...
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7479502 |
2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these...
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7420000 |
Amino phosphonate and amino bis-phosphonate derivatives
Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The...
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7087626 |
Pyrrole derivatives as pharmaceutical agents
Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors. The disclosed invention relates to compounds of the...
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7019024 |
Pharmaceutical for treatment of neurological and neuropsychiatric disorders
The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
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6916831 |
Flavone acetic acid analogs and methods of use thereof
Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and...
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6906007 |
Phenyl-substituted 5,6-dihydropyrone derivatives for use as pesticides and herbicides
The present invention relates to novel phenyl-substituted 5,6-dihydro-pyrone derivatives of the formula (I) in which W, X, Y, Z, G, A, B, Q1 and Q2 are each as defined in the description, to a...
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6864283 |
Oxy-and amino-substituted tetrahydrofuryl derivatives with antitumour activity
Compounds of formula (I) wherein R1is selected from H, C(═O)R′, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or ...
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6737416 |
Phosphonic acid derivative having inhibitory activity against carboxypeptidase B
A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group and the...
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6677461 |
Ligands and asymmetric catalysts made by using the same
A ligand expressed by a general formula (1) in claim 1, wherein R1, R2 and R3 denote substituting groups on aromatic rings, X is P or As, and n is 1 to 3.
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6590107 |
Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides
A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an...
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6566508 |
Fluorogenic compounds and uses therefor
Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when...
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6514953 |
Calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-&lsqb &lsqb (4-aminophenyl)sulfonyl&rsqb (isobutyl)amino&rsqb -1-benzyl-2-(phosphonooxy)propylcarbamate
The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](iso
butyl)amino]-1-benzyl-2-(phosphonooxy)propylcarbamate, to processes for its preparation, and to...
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6515183 |
Chiral diphenyldiphosphines and d-8 metal complexes thereof
Compounds of formula III, wherein R6 und R7 signify identical or different secondary phosphino; R8 is —CH2—OH, —CH2—NH2, —CH2—O—B—FU, —CH2—NH2—B—FU, or —O—B—FU; R9 has the same significance as R8 o...
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6500811 |
Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use
Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes...
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6479471 |
NAALADase inhibitors
The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit...
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6472414 |
Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including...
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6410751 |
Water soluble tri-substituted 1, 2-dioxetane compounds having increased storage stability, synthetic processes and intermediates
Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their...
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6372895 |
Fluorogenic compounds
Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when...
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6365592 |
Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1B (PTP-1B)
The invention encompasses compounds represented by formula I: as well as compositions and methods of treatment. The compounds are inhibitors of the PTP-1B enzyme.
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6362348 |
Additive for inkjet printing, recording solution, method for preventing discoloration and fading of image, and recording sheet
An additive for inkjet printing, comprising a stabilized ascorbic acid derivative. Also disclosed are a recording solution, a method for preventing discoloration and fading of an image, and a...
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6346615 |
Chemiluminescent 1,2-dioxetanes
Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears...
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6333291 |
Optically active diphosphine compound, production intermediate thereof, transition metal complex containing the compound as ligand and asymmetric hydrogenation catalyst containing the complex
This invention provides a novel diphosphine compound which is useful as a ligand of catalysts for asymmetric synthesis reactions, particularly asymmetric hydrogenation reaction. Particularly, it...
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6313159 |
Metabotropic glutamate receptor ligand derivatives as naaladase inhibitors
The present invention relates to metabotropic glutamate receptor ligand derivatives and methods of using the same to inhibit NAALADase enzyme activity, to effect neuronal activities, to inhibit...
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6288280 |
Racemization of atropisomeric bis(phosphine oxide) compounds
A process for the racemization of atropisomeric bis(phosphine oxide) compounds of formula I: ##STR1##in their (S) or (R) or non-racemic form, is useful for preparing optical active bisphosphine...
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6277833 |
Substituted triols
Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.
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6271397 |
L-ascorbic acid-2-phosphoric acid potassium crystal and method for producing the same
A high-purity L-ascorbic acid-2-phosphoric acid potassium crystal having excellent stability, and a method for simply producing the high-purity L-ascorbic acid-2-phosphoric acid potassium in a high...
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6248848 |
Optically active phosphine derivative having at least two vinyl groups, polymer produced using the same as monomer, and transition metal complexes of these
A 2'-diarylphosphino-1,1'-biphenylen-2-yloxy(6,6'-divinyl-1,1'
-binaphthalene -2,2'-diyloxy)phosphine derivative is disclosed, which is represented by general formula (I): ##STR1##wherein Ar is an...
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6150539 |
Triptolide prodrugs having high aqueous solubility
Compounds useful in immunosuppressive and anti-inflammatory treatment are described. The compounds are hydrolyzable triptolide analogs with improved water solubility and generally lower toxicity...
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6133459 |
Method and compositions providing enhanced chemiluminescence from 1,2-dioxetanes
A method and compositions including a 1,2-dioxetane and a fluorescent compound is described. In particular, enzymatic triggering of a triggerable 1,2-dioxetane admixed with a surfactant and the...
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6087513 |
Epoxidation process for aryl allyl ethers
A process for making an aromatic glycidyl ether epoxy compound by contacting an allyl ether made from the hydroxy moiety of a hydroxy-containing aromatic compound with an inorganic or organic...
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6075152 |
Process for preparing isochroman-3-ones
The present invention relates to a process for preparing an isochroman-3-one of the formula (I) by reacting a 1,2-bishalomethylbenzene of the formula (II) ##STR1## in which X is chlorine, bromine...
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6063937 |
Method of making ascorbyl monophosphates
The present invention provides a method of making alkali metal and alkaline earth metal salts of L-ascorbic acid 2-monophosphate comprising reacting a L-ascorbic acid 2-polyphosphate under alkaline...
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6030996 |
Mur D inhibiting compounds, compositions containing such compounds and methods of use
The present invention addresses compounds which inhibit Mur D. The compounds are represented by structural formula 1: ##STR1## wherein: X represents OH, OC1-6 alkyl, O-aryl, O-Har, uridinyl,...
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6028216 |
Asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives
The present invention relates to asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives.
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6025344 |
Certain dioic acid derivatives useful as NAALADase inhibitors
The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit...
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6025345 |
Inhibitors of NAALADase enzyme activity
The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to...
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6008379 |
Aromatic-substituted xanthene dyes
A class of aromatic-substituted xanthene compounds useful as fluorescent dyes is disclosed, the compounds having the general structure where Y1 and Y2 taken separately are selected from the group...
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5990320 |
Optically active diphosphine ligands
Optically active diphosphine ligands of the formula I, ##STR1## where: R1 is hydrogen, C1 -C10 -acyl, C1 -C10 -alkyl, C2 -C10 -alkenyl, each of which may be linear or branched, aryl, arylalkyl, in...
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5965750 |
High- purity tocopherol phosphates, process for the preparation thereof, methods for analysis thereof, and cosmetics
Disclosed herein are a highly purified tocopheryl phosphate and/or a salt thereof (tocopheryl phosphates) wherein a P,P'-bistocopheryl hypophosphate and/or a salt thereof (P,P'-bistocopheryl...
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5962701 |
Chromanylascorbic acid derivatives their preparation and use
Chromanylascorbic acid derivatives of the general formula I ##STR1## where R1 is an organic radical having 1 to 12 C atoms, in particular a methyl group, R2 is an organic radical having 8 to 30 C...
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5929254 |
1,2-dioxetane derivatives
A 1,2-dioxetane derivative of formula (I) for use as a chemiluminescent substrate for immunoassays: ##STR1## wherein R1 is an alkyl group or an aryl group, R2 a hydrogen atom, an alkyl group or an...
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5895819 |
Enzyme substrate
An enzyme substrate is disclosed which comprises a phosphoric ester and an organic acid or a salt thereof having a zinc chelating stability factor constant (log K) of from 8 to 14 in an aqueous...
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5892064 |
Chemiluminescent dialkyl-substituted 1,2-dioxetanes, methods of synthesis and use
A chemiluminescent assay method and compositions are described which use a dialkyl-substituted dioxetane which is deprotected to trigger a chemiluminescent reaction. Chemiluminescent 1,2-dioxetane...
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5886217 |
Method of producing aryl-substituted, amino-acylated phosphonic-acid derivatives with the aid of metal complexes of chiral, amphiphilic ligands
The invention is relates to a method of producing aryl-substituted, amino-acylated phosphonic-acid derivatives with the aid of metal complexes of chiral amphiphilic ligands in that according to the...
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5856522 |
Method of using synthesis of 1,2-dioxetanes and kits therefore
Kits comprising 1,2-dioxetanes which can be cause to chemiluminesce by contact with an enzyme, and the enzyme, are provided for use in optically detectable assays. The assay calls for binding the...
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5856314 |
Thio-substituted, Nitrogen-containing, heterocyclic phosphonate compounds, pharmaceutical compositions, and methods of treating abnormal calcium and phosphate metabolism
The present invention relates to thio-substituted, nitrogen-containing heterocyclic phosphonate compounds, including bisphosphonates, phosphonoalkylphosphinates, phosphonocarboxylates, and...
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