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6803466 |
HIV/FIV protease inhibitors having a small P3 residue
With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective...
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6800611 |
Metastin derivatives and their use
The invention relates to metastin derivatives represented by the formula: X-AA 1 -AA 2 -AA 3 -AA 4 -Z (I), or a salt thereof, or a pro-drug thereof, which have cancer metastatis suppressing...
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6797461 |
Tryptase substrates and assay for tryptase activity using same
The invention is directed to synthetic polypeptide substrates for tryptase enzymes and assays for tryptase activity that utilize the synthetic polypeptide substrates. The preferred synthetic...
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6797807 |
Compounds and methods for cancer therapy
Methods for using modulating agents to enhance or inhibit occludin-mediated cell adhesion in a variety of in vivo and in vitro contexts are provided. Within certain embodiments, the modulating...
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6794492 |
Perfluoroalkyl compounds and their methods of use and manufacture
Fluorinated alkyl compounds may be used as reaction intermediates or reaction products in polymerizing amino acid structures into peptides. Fluorinated methyl groups have been found to be...
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6794362 |
Asparagine containing elastin peptide analogs
The present invention is directed to a composition which is used to enhance the elasticity and/or appearance of tissue. Specifically, the present invention is directed to a composition formulated...
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6784155 |
Inhibitor and stimulator of stem cell proliferation and uses thereof
Disclosed and claimed are methods for the isolation and use of stem cell modulating factors for regulating stem cell cycle and for accelerating the post-chemotherapy peripheral blood cell recovery....
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6780968 |
Monocyclic compounds with four bifunctional residues having NK-2 antagonist action
Disclosed are monocyclic compounds containing four bifunctional residues linked together via peptide or pseudopeptide bonds of the general formula (I): having tachykinin receptor antagonist...
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6774212 |
Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
The present invention relates to ketoamide and ketoester compounds of Formula (I): wherein W is —NH— or —O—, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically...
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6773704 |
Methods of treating vascular disease associated with cystatin C deficiency
The invention provides methods of treating and preventing vascular diseases, by inhibiting cysteine proteases active at sites of vascular injury, particularly cathepsins K and S, by administering...
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6767890 |
Peptides having anti-cancer and anti-inflammatory activity
A pentapeptide is disclosed having the generic formula A-A-A-B-C (SEQ ID NO:2) wherein A is a non-polar amino acid, B is a polar amino acid, and C is a charged amino acid. In a preferred embodiment...
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6767991 |
Hepatitis C inhibitor peptides
Disclosed herein are hepatitis C viral protease inhibitors of formula (I): wherein a is 0 or 1 ; b is 0 or 1 ; Y is H or C 1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative;...
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6767897 |
Therapeutic uses of tri-, tetra-, penta-, and polypeptides
Novel uses of certain peptides to treat patients suffering from neurological or psychiatric disorders are disclosed. The peptides include the tripeptide hormone MIF and compounds made by...
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6765086 |
Self-aligning peptides modeled on human elastin and other fibrous proteins
A polypeptide is provided that has a secondary structure characterized by at least three beta-sheet/beta-turn structures, and that is not a naturally occurring fibrous protein. Such polypeptides,...
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6762166 |
Synthetic complementary peptides and ophthalmologic uses thereof
The present invention is directed to a series of complementary peptides for the pro-gly-pro sequence as antagonists of polymorphonuclear leukocyte chemoattractants. Also provided are applications...
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6759509 |
Branched peptide linkers
Conjugates containing a targeting ligand, such as an antibody, a therapeutically active drug and a branched peptide linker. The branched peptide linker contains two or more amino acid moieties that...
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6756041 |
Process for preparing conjugate vaccines including free protein and the conjugate vaccines, immunogens, and immunogenic reagents produced by this process
A process for preparing a protein-polysaccharide conjugate includes reacting a protein with a polysaccharide to produce a mixture including a protein-polysaccharide conjugate and free protein. At...
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6753410 |
Investigational compounds
The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or...
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6753316 |
Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each...
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6750058 |
Transfecting peptide vector, composition containing same and applications
The invention concerns transfecting peptide vector, a composition containing said vector and their applications for treating and preventing diseases in human beings and animals. Said vector for...
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6750202 |
Phosphinate peptide analogs for the treatment of fibrotic disorders
The invention relates to a method of treating a fibrotic disease, comprising administering to a mammal an effective amount of a phospinate-peptide analog of the general formula (I).
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6743769 |
Antimicrobial peptides and derived metapeptides
The peptides and derivative metapeptides based upon natural antimicrobial peptides have potent and broad spectrum activity against pathogens exhibiting multiple antibiotic resistance. In addition,...
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6740639 |
Inclusion complees of a high potent opioid peptide, pharmaceutical compositions and method of treatment
The invention provides novel inclusion complexes of highly potent opioid peptide of L-Tyrosyl-D-alanyl-glycyl-N-methylphenylalanyl-glycyl-isopro
pylamide with cyclodextrin, pharmaceutical...
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6737409 |
Dolastatin 10 derivatives
Novel anti-tumor compounds of formula, are disclosed. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), the use of compounds of formula (I) for the treatment of...
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6727227 |
Tetrapetide revealing geroprotective effect, pharmacological substance on its basis, and the method of its application
Tetrapeptide L-alanyl-L-glutamyl-L-aspartyl-glycine (SEQ ID NO: 1) of the general formula L-Ala-L-Glu-L-Asp-Gly (SEQ ID NO: 1) is proposed as a biologically active compound with a geroprotective...
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6723830 |
Short peptides which selectively modulate the activity of protein kinases
Peptides which are peptide derivatives of the αD region of a protein kinase can modulate the activity of protein kinases. The activity of a protein kinase in a subject can be modulated by...
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6720306 |
Tetrapartate prodrugs
A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L 1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be...
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6716809 |
Mage-A3 peptides presented by HLA class molecules
The invention describes HLA class II binding peptides encoded by the MAGE-A3 tumor associated gene, as well as nucleic acids encoding such peptides and antibodies relating thereto. The peptides...
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6716810 |
Composition and method for regulation of body weight and associated conditions
Described are methods and compositions for regulating body weight and/or regulating the rate of weight gain or loss, and particularly, for treating or preventing obesity. Specifically, methods of...
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6713445 |
Peptides for treatment of HIV infection
The HIV-1 envelope protein gp120 is toxic to rodent and human neurons by indirect mechanisms requiring accessory glial cells. Chemokines are known to block gp120 interactions with chemokine...
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6706487 |
Monoclonal antibody and the method of using the antibody
Chimeric, humanized and other IL-18 mAbs, derived from high affinity neutralizing mAbs, pharmaceutical compositions containing same, methods of treatment and diagnostics are provided.
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6703483 |
Compounds useful in pain management
Compounds of the formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds...
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6699838 |
Antiangiogenic peptides
Mammalian kringle 5 fragments and kringle 5 fusion proteins are disclosed as a compounds for treating angiogenic diseases. Methods and compositions for inhibiting angiogenic diseases are also...
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6693072 |
Elastase inhibitors
This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P 2 moiety is substituted...
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6693167 |
Peptide-based gemini compounds
New peptide-based Gemini compounds comprising two linked chains (a) each having: (1) a positively charged hydrophilic head, Q 1 or Q 2 formed from one or more amino acids and/or amines, (2) a...
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6689753 |
β sheet breaker peptide analogs that inhibit β pleated sheet formation in amyloid β-peptide
The present invention provides peptide analogs and peptide mimetics that inhibit pleated sheet formation in amyloid β-peptide, pharmaceutical compositions thereof and their therapeutic use. The...
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6686445 |
Synthetic antineoplastic agents derived from dolastatin 15 and methods of making same
A composition of matter, denominated herein as 12 a-r , having the structural formula set forth below: wherein R is selected from the group consisting of: a) R=NHPh; b) R=NHCH 2 Ph; c) R=NH(CH 2...
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6686336 |
N-terminal D(-)-penicillamine peptides as aldehyde sequestration agents
The invention provides a compound of formula I: wherein R 1 -R 3 have any of the values described in the specification; or a salt thereof. The compounds are useful as aldehyde sequestration...
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6682740 |
Peptides derived fram complement peptide C3a sequence and antiallergic compositions comprising them
Peptides corresponding partially or entirely to positions 50-77 of the sequence of the complement-derived peptide C3 a and analogs thereof are capable of inhibiting IgE-mediated triggering and/or...
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6683154 |
Antimicrobial compositions containing β-amino acid oligomers
Disclosed are antimicrobial compositions containing β-peptides and methods of inhibiting microbial growth in mammals using the compositions. The β-peptides present in the compositions contain...
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6683048 |
Compounds and methods for stimulating gene expression and cellular differentiation
Modulating agents for inhibiting an interaction between α-catenin and β-catenin are provided. The modulating agents comprise one or more of: (a) a β-catenin HAV motif; (b) a peptide analogue or...
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6670326 |
Depsipeptide compound
This invention relates to a novel compound which has a cytotoxic activity and TGF-β like activity for human cancer cells and is useful as an antitumor agent and to a pharmaceutical composition...
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6664368 |
Inhibition of nuclear import by backbone cyclic peptide analogs
The design and the synthesis of backbone cyclic peptide analogs which functionally mimic the nuclear localization signal (NLS) region of macromolecules is disclosed. The principles of the invention...
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6664372 |
Azatide peptidomimetics
Peptidomimetic azatides and combinatorial oligoazitide libraries are produced by means of a stepwise synthesis. Combinatorial library construction of this new biomimetic polymer provides a means to...
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6656905 |
Cyclic tetrapeptide compound and use thereof
A cyclic tetrapeptide compound and use thereof. Especially, a compound WF27082, a process for production of the compound by culturing, in a nutrient medium, a WF27082-producing strain belonging to...
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6649395 |
Tyrosine-containing cyclophilin and related methods
The present invention relates to the use of these cyclophilins, hereinafter referred to as ‘tyrosine-containing’ cyclophilins, in a method for identifying compounds capable of binding to and/or...
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6649746 |
Biological production of stable glutamine, poly-glutamine derivatives in transgenic organisms and their use for therapeutic purposes
The invention provides a bioproduction of glutamine rich peptides. These peptides are used for rehydration and nutrition therapy in patients and for enhanced nutrition in animals. The peptides may...
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RE38313 |
Soluble polypeptide fractions of the LAG-3 protein, production method, therapeutic composition, anti-idiotype antibodies
Soluble polypeptide fraction consisting of all or part one of at least one of the four immunoglobulin-type extracellular LAG-3 protein domains (amino acids 1-159, 160- 230 239 , 240-330...
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6638912 |
Peptide compositions mimicking TGF-β activity
Compositions suitable for pharmaceutical administration are provided in which one compound is a small peptide mimic of TGF-β. More preferably, pharmaceutical compositions of the present invention...
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6638941 |
Conformationallly constrained peptidomimetics as β-turn templates and modulators of SH3 domains
Spirolactam compounds useful as inhibitors of protein-protein interactions modulated by SH3 domains are disclosed. Compounds of the invention are also useful as β-turn mimetics. Also disclosed are...
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