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7601845 |
Optically detectable organophosphonates
The invention relates to compounds having general formula I
in which X represents an optically detectable moiety, n is an integer with 1≦n≦20, R 1 is an unbranched or branched alkyl group...
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7560584 |
Immunomodulatory compounds and methods of use thereof
The present invention is directed to novel compounds that function as immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases, to novel adjuvant...
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7514556 |
Inhibitors of β-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase...
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7504388 |
Methods employing and compositions containing defined oxidized phospholipids for prevention and treatment of atherosclerosis
Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders,...
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7429575 |
N-(phosphonoalkyl)-amino acids, derivatives thereof and compositions and methods of use
The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a...
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7408075 |
Synthesis of phosphocholine ester derivatives and conjugates thereof
Aspects of the present invention include methods of synthesizing phosphocholine analogues and the phosphocholine conjugates formed therefrom and their use in preventing infections caused by...
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7378538 |
Compound having phosphorylcholine group, polymer thereof and process for producing the same
A compound of the invention is a specific compound having a phosphorylcholine group, and a polymer of the invention comprises at least 1 mol % of repeating units with a phosphorylcholine group and...
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7153842 |
Florfenicol prodrug having improved water solubility
The present invention discloses phosphate esters of florfenicol (prodrugs) and florfenicol analogs having superior water solubility that are hydrolyzed to florfenicol or the respective florfenicol...
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7141557 |
Lipid analogs for treating viral infections
A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an...
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7135584 |
Lipid analogs for treating viral infections
A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpes virus, is disclosed. The method comprises administering to a subject in need of such treatment an...
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7101864 |
Compositions comprising oxophosphonate-based metalloproteinase inhibitors
The present invention relates to compositions useful for treating or controlling disease states or conditions associated with zinc containing proteinases, especially metalloproteinases. The active...
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7034176 |
Aminopropylphosphinic acids
Intermediates used in the preparation of compounds of formula I,
or a stereoisomer thereof, or a pharmaceutically acceptable form of either selected from the group consisting of a salt, a...
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6911553 |
Osteoblast-specific mitogens and drugs containing such compounds
The invention is directed to compounds of formula (I) wherein R 1 alkyl, alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; and the physiologically safe salts, esters,...
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6846925 |
Colchinol derivatives as angiogenesis inhibitors
The invention related to colchinol derivatives of the formula (I): Wherein: R 1 ; R 2 and R 3 are each independently hydroxy, phosphoryloxy (—OP 3 H 2 ), C 1-4 alkoxy or an in vivo hydrolysable...
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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 R 1 represents hydrogen atom, an alkyl group, a substituted alkyl group and...
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6593312 |
Cyclic α-amino-&ggr -hydroxyamide compounds
A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R 1 and R 4 , which may be identical or different, each...
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6576766 |
Signal transduction inhibitors, compositions containing them
This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediate by one or more molecular interactions involving a...
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6576627 |
Phosphonic acid derivatives having carboxypeptidase b inhibitory activity
A compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof: wherein R 1 represents hydrogen atom, an alkyl group, a substituted alkyl group and...
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6569899 |
4-aminobutanoic acid derivatives and drugs containing these derivatives as the active ingredient
Aminobutylic acid derivatives of the formula (I) wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds...
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6506739 |
Bis-(N,N'-bis-(2-haloethyl)amino)phosphoramidates as antitumor agents
Bis-(N,N′-bis-(2-haloethyl)amino)phosphoramidates, pharmaceutical compositions containing them, methods of treatment using them, and processes for their preparation. The compounds possess...
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6498150 |
Low molecular weight cell, bone marrow and immune stimulants
The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other...
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6495533 |
Drugs containing phosphoric acid derivatives as the active ingredient
The present invention relates to phosphoric acid derivatives represented by general formula (I), wherein each symbol is as defined in the description and nontoxic salts thereof. Because of having...
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6432933 |
Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such...
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6391866 |
(α-aminophosphino) peptides derivative and compositions containing same
The invention concerns (α-aminophosphino) peptide derivative compounds of general formula (I) wherein: R 1 and R 2 represent each a hydrogen atom or together form an imine with the adjacent...
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6235727 |
Sulfonylaminophosphinic and sulfonylaminophosphinic acid derivatives, methods for their preparation and use
Compounds of the formula I ##STR1## 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...
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6150344 |
Hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases
Compounds of Formula I ##STR1## are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases...
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6136798 |
Compounds inhibiting the association of the PDGF receptor and phosphatidylinositol 3-kinase and their use
The present invention provides compounds that inhibit the association of platelet-derived growth factor and phosphatidylinositol 3-kinase. The present invention also provides pharmaceutical...
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6075159 |
Phosphite, a process for producing the same and a use thereof
A phosphite represented by the formula (I): ##STR1## wherein n repesents 1 or 2; A represents alkylene; B represents a direct bond or alkylene; one of Y and Z represents a hydroxyl group, alkoxy or...
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6002029 |
Antiviral prodrugs
Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.
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5968916 |
Fluoroalkenyl compounds and their use as pest control agents
Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of...
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5916922 |
Phenyl glyoxamides as SPLA2 inhibitors
A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA 2 mediated release of fatty acids for treatment of conditions such as septic shock.
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5849725 |
Phosphorylated derivatives of compositions having anti-inflammatory or analgesic activity and a method for the preparation thereof
The principal activity of the amides of ethanol-β-aminophosphoric acid with active moieties having anti-inflammatory and analgesic activity (FANS) remains substantially unchanged but they have...
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5741923 |
Ethylenically unsaturated compounds
An improved process for producing ethylenically unsaturated phosphate ester compounds, especially 2-(methacryloyloxyethyl)-2' (trimethylammoniomethyl) phosphate, (HEMA-PC) comprises a two step...
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5707967 |
Pain relief compositions
Disclosed are compositions containing either aspartame or monosodium glutanate combined with an amino acid.
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5703263 |
Process for making chiral alpha-amino phosphonates and selected novel chiral alpha-amino phosphonates
This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates...
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5686633 |
Inks, particularly for ink jet printing
Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R 1 , R 2 , R 3 , R 4 , R 3 ' and R 4 ' are as defined in claim...
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5659061 |
Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities
The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are...
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5639732 |
Phosphorous-containing cysteine and serine protease inhibitors
The present invention is directed to novel phosphorous-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.
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5627173 |
Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders
Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and...
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5616745 |
Lipopolyamines, their preparation and their use
New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R 1 and R 2 : aliphatic radical containing...
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5574025 |
Inhibitors of prenyl-protein transferases
The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained...
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5556710 |
Metal coating useful for rendering the surface of the metal biocompatible
Compounds of formula (I), in which the groups R are hydrogen or C 1 -4 alkyl, n is from 2 to 4, X is alkylene, poly(ethoxy) or an aryl-containing group, Y is a valence bond or a divalent functional...
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5543396 |
Proline phosphonate derivatives
Peptidyl derivatives of diesters of α-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like,...
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5516767 |
Phosphinyloxy propanaminium inner salt derivatives
Compounds of the formula ##STR1## where X 1 and X 2 are independently O or S, and R 1 is as defined in the description R 2 , R 3 , and R 4 are each independently straight or branched...
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5508463 |
α-aminophosphonates
Novel α-aminophosphonates are provided along with processes and intermediates for their preparation. In preferred embodiments, scalemic α-aminophosphonates are prepared by the stereoselective...
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5476847 |
Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors
Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene; R 1 , R 2 , R 3 and R 4 are H,...
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5476671 |
Synthetic ceramides and their use in cosmetic compostions
A novel pseudoceramide which has improved dispersibility in aqueous solutions and which can be produced by an economical manufacturing process. The process for producing new pseudoceramides and...
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5468732 |
Phosphorus containing renin inhibitors
Phosphorus containing polypeptides as renin inhibitors, useful as antihypertensive agents.
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5451573 |
Substituted cyclohexane derivatives for the treatment of diseases
Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R 3 , R 4 , R 5 , Y and Z have the meanings indicated,...
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5436245 |
Phosphate substituted amino or imino acids useful as antihypertensives
Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein: X...
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