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RE38828 |
Parevins and tachytegrins
The present invention provides a new class of broad-spectrum antimicrobial peptides effective against a wide variety of microbes, including bacteria, viruses, retroviruses, fungi, yeast and protozoa.
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6951652 |
Vaccine for prevention of gram-negative bacterial infections and endotoxin related diseases
A vaccine is disclosed which is useful for protecting a host from Gram negative infections and the effects of endotoxin, therefore preventing sepsis and septic shock. The vaccine is prepared by...
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6951840 |
Lipoglycopeptide antibiotics
Provided are novel lipoglycopeptides exhibiting bacterial signal peptidase inhibitory activity. Also provided are actinomycete strains that produce these lipoglycopeptides, methods of producing...
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6943145 |
Compounds and method for the prevention and treatment of diabetic retinopathy
The invention provides peptide derivatives designed to deliver peptides having growth factor inhibitory activity, especially somatostatin analogs, to the retina by sequential metabolism. The...
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6939946 |
Ring modified cyclic peptide analogs
A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the...
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6939947 |
N1-modified glycopeptides
The present invention is directed to N 1 -acylated derivatives of desleucylA82846B. These derivatives are useful as antibacterials.
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6936586 |
Synthetic IL-10 analogues
The nonapeptide NH2-Ala-Tyr-Met-Thr-Met-Lys-Ile-Arg-Asn-COOH (SEQ ID NO: 1) and related molecules are useful as IL-10 agonists.
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6927208 |
Cyclosporin with improved activity profile
The invention relates to a novel cyclosporin, the pharmaceutical use thereof and a pharmaceutical composition containing it.
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6916784 |
Cyclic peptide antifungal agents and process for preparation thereof
Provided are compounds of the formula (1):
wherein R′ is hydrogen, methyl or NH 2 C(O)CH 2 —;
R″ and R′″ are independently methyl or hydrogen; R adn R y are independently...
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6914122 |
Macrocyclic NS-3 serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties
The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention...
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6911428 |
Diaryl peptides as NS3-serine protease inhibitors of hepatitis C virus
The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus. A particularly preferred compound is of the formula:
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6911526 |
Compounds that inhibit the interaction between signal-transducing proteins and the GLGF (PDZ/DHR) domain and uses thereof
This invention provides for a composition capable of inhibiting specific binding between a signal-transducing protein and a cytoplasmic protein. This invention also provides a method of identifying...
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6906170 |
Anti-inflammatory peptides derived from IL-2 and analogues thereof
Synthetic anti-inflammatory peptides derived from the sequence of IL-2 are provided. Parent peptides of the sequences Ile-Val-Leu, Glu-Phe-Leu-Asn-Arg-Trp-Ile-Thr (SEQ ID NO:1) and Arg-Met-Leu-Thr...
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6900176 |
Pest control agents/depsipeptides
The present invention relates to the use of 24-membered cyclodepsipeptides of the formula (1)
in which R 1 and R 2 are as defined in the description,
for controlling animal pests in...
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6890902 |
Cytotoxic modified lactoferrin peptides
The present invention provides a modified lactoferrin peptide which is cytotoxic, 7 to 25 amino acids in length, with three or more cationic residues and which has one or more extra bulky and...
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6884774 |
Cyclic hexapeptide derivatives
This invention relates to new polypeptide compound represented by the general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description or a salt thereof which has...
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6884868 |
Cyclic hexapeptides having antibiotic activity
This invention relates to new polypeptide compound represented by general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description or a salt thereof which has...
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6881577 |
Method for improving transfection efficiency
The invention relates to a method for improving transfection efficiency through the use of K16-peptides. In addition, the invention further relates to novel K16-peptides, including a K16-CYC peptide.
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6878804 |
Synthesis of template-fixed β-hairpin loop mimetics
Template-fixed β-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 α-amino acid...
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6875740 |
Combination of a cyclic hexapeptide with antifungal drugs for treatment of fungal pathogens
There is described antifungal combination use of known antifungal agents such as the azoles or polyenes in combination with a lipopeptide compound antifungal agent. More particularly, the invention...
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6872804 |
Glycopeptide disulfide and thioester derivatives
Disclosed are disulfide and thioester derivatives of glycopeptides and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as...
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6872702 |
Inhibitors for urokinase receptor
The present invention concerns peptides as inhibitors of the binding of urokinase to the urokinase receptor. These peptides, which are preferably cyclic, are suitable as pharmaceutical agents for...
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6872803 |
Peptides
The present invention provides peptides represented by the following formula (A):
wherein Q represents a physiologically active peptide moiety; X each represents the same or different α-amino...
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6872713 |
Antiprotozoal saponins
Saponins of formula (I), a stereoisomeric form thereof or a pharmaceutically acceptable addition salt thereof, wherein R 1 to R 12 have the meaning given in the description, can be isolated from...
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6866837 |
Radiolabeled peptides for the diagnosis and treatment of breast and prostate tumors and metastases of such tumors
Compounds and methods for the diagnosis and treatment of tumors, including breast and prostate tumors and metastases thereof using radiolabelled peptides that bind to GRP receptors. The peptides...
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6864233 |
Fungicidal echinocandin derivatives and their preparation
The invention concerns compounds of general formula (I) wherein: R 1 represents a hydrogen atom, a hydroxy radical, Ob or Ncd; A represents an oxygen atom, a CH 2 radical or a NH radical; B...
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6858585 |
Cyclic depsipeptides and drugs containing the same as the active ingredient
Cyclic depsipeptides represented by the formula
wherein:
R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15-carbon atoms; A, B,...
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6852689 |
Methods for administration of antibiotics
The invention provides methods for administering a therapeutically effective amount of daptomycin while minimizing skeletal muscle toxicity. The methods provide daptomycin administration at a...
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6846804 |
Construction of a structural variant of sublancin to facilitate its isolation and use in bioremediation of environmental contamination by gram-positive spore formers such as bacillus anthrasis
A sublancin peptide variant having a Gly-His peptide sequence fused to the C-terminal end of the mature sublancin peptide provides an affinity tag facilitating increased purification of the peptide...
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6846802 |
Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising N-cyclic P2 moieties
The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention...
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6841533 |
Conformationally constrained backbone cyclized interleukin-6 antagonists
Novel peptides which are conformationally constrained backbone cyclized antagonists of IL-6, are disclosed. Methods for synthesizing the IL-6 antagonists are also disclosed. Furthermore,...
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6841530 |
Semi-synthetic studies toward didemnin analogues
Disclosed are semi-synthetic methods for the preparation of Didemnin Analogs. The compounds of this type are illustrated in Formula (I).
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6831150 |
Reductive alkylation process
The invention provides a novel reductive alkylation method useful for selectively alkylating saccharide-amines of glycopeptide antibiotics.
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6831061 |
Apicidin-derivatives, their synthetic methods and anti-tumor compositions containing them
A substituted apicidin derivative, a method of synthesis therefore, and an anti-tumor composition comprising the same are disclosed. The substituent of the derivative is preferably semicarbazone,...
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6828299 |
Polyhydroxy glycopeptide derivatives
Disclosed are polyhydroxy derivatives of glycopeptides and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial...
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6828302 |
Therapeutic uses of depsipeptides and congeners thereof
Depsipeptides and congeners thereof are disclosed having the following structure: wherein m, n, p, q, X, R 1 , R 2 and R 3 are as defined herein. These compounds including FR901228, have...
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6825317 |
Cyclic tetrapeptide derivatives and pharmaceutical uses thereof
The present invention provides a cyclic tetrapeptide derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: wherein each of R 21 and R 22 ...
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6821950 |
Cyclic agonists and antagonists of C5a receptors and G protein-coupled receptors
The present invention relates to novel cyclic or constrained acyclic compounds which modulate the activity of G protein-coupled receptors and are useful in the treatment of conditions mediated by G...
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6818614 |
Compounds having antifungal activity
A compound of the following chemical structure (I) which exhibits antifungal activity and is useful in treating and preventing fungal infectious diseases:
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6815437 |
Streptogramines, their preparation and compositions containing them
Group A streptogramin derivatives of formula (I): the salts thereof, and mixtures of stereoisomers thereof, as well as processes for preparing them and pharmaceutical compositions comprising...
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6809177 |
Process for the conversion of echinocandin class of peptides to their c4-homotyrosine monodeoxy analogues
The invention relates to a process for the conversion of echinocandin class of peptides to their C4-homotyrosine monodeoxy analogues, particularly mulundocandin to deoxymulundocandin, which...
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6809075 |
Elastin peptide analogs and uses of same incombination with skin enhancing agents
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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6809077 |
Cyclosporin analogs for the treatment of autoimmune diseases
The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof: In particular, residue A maybe represented by either...
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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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6794489 |
Compositions and methods for treatment of sexual dysfunction
Compositions and methods are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction. In one...
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6793925 |
Pseudomycin natural products
The invention relates to pseudomycin natural products including pseudomycins A′ and B′, methods for making such pseudomycins, and methods employing antifungal activity of these pseudomycins....
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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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6790935 |
Cyclosporin derivatives and method for the production of said derivatives
The invention relates to cyclosporin derivatives, whereby the peptide chain thereof comprises at least one pseudo-proline type non-natural amino acid radical. The invention also relates to a method...
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6790829 |
Cyclic decapeptide antibiotics
Several cyclic decapeptides having antibiotic activity are disclosed. The decapeptides are active against both gram positive and gram negative bacteria.
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6784156 |
Cyclosporins for the treatment of respiratory diseases
The present invention relates to novel semisynthetic cyclosporin analogs of Formula (I): X is absent, —C1-C6 alkyl-, or —C3-C6 cycloalkyl- Y is selected from the group consisting of: (i)...
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