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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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6774103 |
Compounds for deactivating phospholamban function on Ca-ATPase (phospholamban inhibitors)
This invention relates to determining the three-dimensional structure of the cytosolic domain of phospholamban (PLB) and its active site from NMR data of sufficiently high resolution for the...
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6774104 |
Stabilized pharmaceutical composition in lyophilized form
A stabilized pharmaceutical composition in lyophilized form comprising: a cyclic polypeptide compound represented by the general formula (I): wherein R 1 is a hydrogen atom or an acyl group and...
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6750199 |
Antimicrobial sulfonamide derivatives of lipopeptide antibiotics
The present invention provides antimicrobial sulfonamide derivatives of lipopeptide antibiotics, pharmaceutical compositions of antimicrobial sulfonamide derivatives, methods for making...
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6750321 |
Insulin-like growth factor agonist molecules
Peptides are provided that inhibit the interaction of an IGF with any one of its binding proteins and not to a human IGF receptor. These IGF agonist peptides are useful to increase serum and tissue...
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6743776 |
Cyclohexapeptides having antimicrobial activity
This invention relates to new polypeptide compounds represented by general formula [I]: wherein R 1 and R 2 are as defined in the description and pharmaceutically acceptable salt thereof which...
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6737403 |
Derivatives of laspartomycin and preparation and use thereof
The present invention provides laspartomycin core peptides, laspartomycin core peptide derivatives, antimicrobial laspartomycin derivatives, methods for making laspartomycin core peptides, methods...
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6737241 |
Methods for screening for transdominant intracellular effector peptides and RNA molecules
Methods and compositions for screening for intracellular transdominant effector peptides and RNA molecules selected inside living cells from randomized pools are provided.
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6730776 |
WF14573 or its salt, production thereof and use thereof
The present invention provides a new antimicrobial compound WF14573, and a process for producing WF14573 by (a) culturing a WF14573A and/or B-producing microorganism in a nutrient medium and...
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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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6720305 |
Injectable formulations containing ramoplanin
The present invention relates to a pharmaceutical composition for intravenous administration that contains ramoplanin or a member of the ramoplanin family.
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6713580 |
Quaternary amino acids on solid supports
The present invention relates to novel templates useful for generating novel compounds and to compounds produced utilizing the templates. The templates comprise quaternary amino acids that may be...
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6713604 |
Process to inhibit binding of the integrin α4β1 , to VCAM-1 fibronectin and cyclic peptides thereof
The present invention is directed to an isolated and purified cyclic peptide of from 5 to about 13 residues modeled after a portion of the CS1 peptide. A peptide of this invention preferably has...
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6706192 |
Purification process
Object of the invention is a process for the chromatographic purification of cyclosporin A from a crude product containing cyclosporin complex by using a column filled with silica gel and by the...
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6706862 |
Backbone-cyclized BPI peptidomimetics
Novel backbone-cyclized BPI peptide analogs and methods of making the same by the use of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic...
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6703480 |
Peptide dimers as agonists of the erythropoientin (EPO) receptor, and associated methods of synthesis and use
Novel peptide dimers are provided that bind and activate the erythropoietin receptor (EPO-R) or otherwise act as an EPO agonist. The novel compounds have a first peptide chain R 1 and a second...
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6696412 |
High purity lipopeptides, Lipopeptide micelles and processes for preparing same
The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential...
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6696413 |
Pharmaceutical preparation with cyclosporin A
The invention relates to a pharmaceutical preparation which consists of or contains cyclosporin A, an emulsifying α-tocopherol derivative, an ethoxylation product of vegetable oils, fatty acids or...
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6696409 |
Neuropeptide Y agonists
A ligand for a neuropeptide Y receptor which has the formula: Ac-Ala-Arg-Ala-Ala-Leu-Asn-Ala-Ala-Thr-Arg-Gln-Arg-Tyr-NH 2 (SEQ ID NO:1), or...
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6689749 |
Neuropeptides originating in scorpion
The invention provides a peptide capable of blocking voltage-gated K + channels and inhibiting IL-2 production, which is represented by an amino acid sequence of: ...
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6677376 |
Non-peptidic cyclophilin binding compounds and their use
The invention relates to non-peptidic compounds that possess bioactive properties, such as the ability to protect neuronal cells from otherwise lethal treatments or the ability to promote the...
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6677429 |
Echinocandin derivatives, preparation method and application as anti-fungal agents
A compound of Formula I in which R 1 and R 2 =H, OH, alkyl optionally substituted, or NR 1 forms with the carbon bearing NR 1 R 2 a double bond and R 2 is Xra, X being O, NH or N-alkyl and Ra...
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6673769 |
Lanthionine bridged peptides
Disclosed are lanthionine bridged peptides having the structure methods of their preparation and their use as pharmacologically active agents.
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6670446 |
N1 modified glycopeptides
Described herein are N′-acylated derivatives of desleucylA82846B. The compounds are useful as antibacterial agents.
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6670142 |
Method for screening combinatorial bead library, capturing cells from body fluids, and ligands for cancer cells
The invention includes a cell-growth-on-bead assay for screening a one-bead-one-compound combinatorial bead library to identify synthetic ligands for cell attachment and growth or proliferation of...
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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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6664231 |
Anti-fungal peptides
The present invention relates generally to anti-fungal peptides derived from or based on Domain III (amino acids 142-169) of bactericidal/permeability-increasing protein (BPI) and in vivo or in...
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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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6664367 |
Stable analogs of bioactive peptides containing disulfide linkages
Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c)...
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6660466 |
Di-nitrogen heterocycle compositions
Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as...
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6660832 |
Macrocyclic compounds and preparation methods thereof
The present invention is directed to macrocyclic compounds of the formula (I) wherein Q, X, R 1 and R 5 are as defined herein. Compounds of the invention are useful for therapeutic and...
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6660835 |
Lead substances and their use as therapeutics
The present invention relates to peptides, which are useful in treating Staphylococcus infections. More particularly, the inventive peptides interfere with the regulation of the agr system of...
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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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6645934 |
Peptide with radio protective effect
The invention makes available a peptide having a radioprotective effect that comprises a modified form and/or an optionally modified fragment of the Bowman-Birk protease inhibitor (BBI).
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6630123 |
Method to enhance tissue accumulation of radiolabeled compounds
Administration of a radioisotopic compound by infusion over a period of time greater than two hours, preferably greater than twelve hours, greatly increases the maximum radioactivity that...
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6630569 |
Ectoparasiticide agents
The present invention relates to the ectoparasiticidal use of cyclic depsipeptides of the formula (I) in which R 1 , R 2 , R 3 , R 4 , X 1 , X 2 , X 3 and X 4 are substituents described...
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6624144 |
Matrix metalloproteinase inhibitors and down-regulators
The present invention relates to novel matrix metalloproteinase (MMP) inhibitors and down-regulators, to a process for the preparation of these inhibitors, to pharmaceutical compositions comprising...
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6617425 |
Peptides
The invention provides novel β-peptides comprising 2 or more different β-amino acid residues, preferably compounds of formula I wherein the R residues, X and n are as defined. Compounds of the...
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6613738 |
Cyclic lipopeptide from Cryptosporiopsis quercina possessing antifungal activity
A unique lipopeptide antimycotic, termed Cryptocandin, is described from Cryptosporiopsis cf quercina, an endophytic fungus. Cryptocandin with a molecular mass of 1079 contains equimolar...
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6610826 |
Cyclopeptide derivatives with integrin inhibitor properties
Compounds of the formula I R—Q—X I, in which R, Q, and X are as defined herein, can be used as integrin inhibitors. In particular, compounds of formula I are suitable for the treatment of...
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6610822 |
Purification process
There is disclosed a process for purifying a natural product using a two-phase, multi-solvent system followed by vacuum concentration and back extraction. The method allows for the removal of...
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6610821 |
Compounds and methods for modulating endothelial cell adhesion
Cyclic peptides comprising a cadherin cell adhesion recognition sequence HAV, and compositions comprising such cyclic peptides, are provided. Methods for using such peptides for modulating...
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6608027 |
Macrocyclic peptides active against the hepatitis C virus
The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R 21 , R 22 , R 3 , R 4 , D...
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6602849 |
Cyclic somatostatin analogs
The present invention is directed to cyclic derivatives containing an imidazole cis amide bond mimetic which bind selectively to somatostatin receptor subtypes and the use thereof in treating...
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6593453 |
Activated peptides and conjugates
Novel activated peptides and conjugates thereof, useful in diagnostic assays and therapeutics, and processes for the preparation thereof are disclosed.
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6590073 |
Formation and anion-exchange of crystalline echinocandin ammonium salts
A method is described for forming a crystalline Echinocandin nucleus salt from its mixed broth and/or partially purified process streams by the steps of nanofiltration to form a concentrate,...
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6586393 |
Antibiotics GE 23077, pharmaceutically acceptable salts and compositions, and use thereof
The invention relates to an antibiotic substance of microbial origin, arbitrarily denominated GE23077 complex and the individual factors which constitute it, a mixture of said factors in any...
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6583265 |
Cyclosporins
The present invention relates to novel cyclosporins, processes for their preparation, their use as pharmaceuticals and pharmaceutical compositions comprising them. The novel cyclosporins are...
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6583114 |
Fracture healing using pthrp analogs
This invention provides methods of bone healing and fracture repair comprising administering to a patient in need thereof an effective amount of a polypeptide analog of parathyroid hormone related...
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