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7615609 |
Preparation of somatostatin peptides
Provided is a process for preparing cyclic somatostatin analogues and the linear intermediates used in this process.
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7611724 |
Method of producing FR901228
Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for...
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7611711 |
VEGFR-3 inhibitor materials and methods
The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated...
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7608681 |
Methods and compositions for prolonging elimination half-times of bioactive compounds
Peptide ligands having affinity for IgG or for serum albumin are disclosed. Also disclosed are hybrid molecules comprising a peptide ligand domain and an active domain. The active domain may...
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7608280 |
Method of producing FR901228
Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for...
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7608242 |
Peptide-chelate conjugates
A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. The peptide-chelate conjugate of the invention may be labelled with a radiometal to...
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7605126 |
Acylaminoheteroaryl hepatitis C virus protease inhibitors
The present invention discloses compounds of formulae I and II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which inhibit serine protease activity, particularly the...
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7601693 |
Composition for treating cancer and use thereof
The present invention provides a cyclic peptide containing RRXR motif. The present invention also provides a composition comprising the said cyclic peptide and a pharmaceutical acceptable carrier....
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7595294 |
Vasoactive intestinal polypeptide pharmaceuticals
Pharmaceutical compositions relating to vasoactive intestinal polypeptides and methods for the treatment of metabolic disorders, including diabetes, insulin resistance, metabolic acidosis and...
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7592433 |
Polynucleotides encoding cyclotide-like structures
The present invention relates to a novel nucleic acid molecule encoding an amino acid sequence, which is capable of forming a cyclic structure. Cyclization may occur within a cell or cell membrane,...
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7592419 |
Macrocyclic inhibitors of hepatitis C virus NS3-serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat...
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7592315 |
Peptide viral entry inhibitors
The present invention provides, inter alia, peptide compositions and methods for treating and preventing Flaviviridae virus (e.g., hepatitis C virus) infections.
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7592308 |
F3W variants of the lantibiotic mersacidin and its use
The present invention relates to methods and products for improved production of the lantibiotic mersacidin. There is provided a method of producing a mersacidin variant which comprises introducing...
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7589170 |
Synthesis of cyclic peptides
This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in...
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7582604 |
Template-fixed peptidomimetics with antibacterial activity
Template-fixed β-hairpin peptidomimetics of the general formula (I), wherein Z is a template-fixed chain of 12 α-amino acid residues which, depend on their positions in the chain (counted...
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7579432 |
Cyclic peptides as G-protein-coupled receptor antagonists
The invention relates to novel cyclic compounds which have the ability to modulate the activity of G protein-coupled receptors. The compounds preferably act as antagonists. In preferred...
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7579322 |
Compositions and methods for promoting myocardial and peripheral angiogenesis
Methods, compositions and devices are disclosed for use in growing new blood vessels to restore or improve blood flow to ischemic tissues and organs of the body. Compositions comprising IGD...
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7569541 |
Method for synthesizing conformationally constrained peptides, peptidomimetics and the use thereof as synthetic vaccines
The present invention relates to methods for synthesizing conformationally constrained peptides and cyclic peptidomimetics obtainable by these methods which are conformationally constrained due an...
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7566765 |
Heterocyclic compounds containing a nine-membered carbon-nitrogen ring
The present invention provides heterocyclic compounds having a nine-membered ring of three repeating C—C—N subunits covalently bound to each other through amide bonds, and variable side groups...
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7566691 |
Vasoactive intestinal polypeptide pharmaceuticals
Pharmaceutical compositions relating to vasoactive intestinal polypeptides and methods for the treatment of metabolic disorders, including diabetes, insulin resistance, metabolic acidosis and...
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7560429 |
Orodispersible dosage forms of desmopressin acetate
Good bioavailability of desmopressin can be obtained by means of an orodispersible pharmaceutical dosage form. Preferred dosage forms comprise desmopressin and an open matrix network which is an...
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7560428 |
Hair growth promoting oligopeptides
The object of the present invention is to provide an oligopeptide having hair growth promoting activity. The present invention provides an oligopeptide which is represented by the formula (I):...
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7553929 |
Cell permeable peptides for inhibition of inflammatory reactions and methods of use
The present invention relates to the delivery of biologically active molecules, such as peptides, into the interior of cells by administering to the cells a complex comprising the molecule linked...
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7550431 |
Spatially-defined macrocycles incorporating peptide bond surrogates
Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit...
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7550430 |
Cationic antimicrobial peptides and compositions
The invention described herein relates to compositions of novel antimicrobial peptides. The peptides of the present invention exhibit high antibacterial activity and low hemolytic activity. The...
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7544364 |
Pharmaceutical compositions containing a glycopeptide antibiotic and a cyclodextrin
Disclosed are pharmaceutical compositions containing a cyclodextrin and a therapeutically effective amount of a glycopeptide antibiotic or a salt thereof. Also disclosed are methods of treating a...
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7541430 |
Peptides for use in treating obesity
Novel cyclic and linear peptides of the formula R 1 —X—X 1 —X 2 —X 3 —X 4 —X 5 —X 6 —X 7 —X 8 —X 9 —X 10 —X 11 —R 2 are useful in the treatment of obesity are provided.
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7538190 |
Methods for the synthesis of two or more dicarba bridges in organic compounds
Described herein are methods for forming two or more dicarba bridges, as well as new compounds containing dicarba bridges.
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7531623 |
Hydrochloride salts of a glycopeptide phosphonate derivative
Disclosed are hydrochloride salts of telavancin having a chloride ion content of from about 2.4 wt. % to about 4.8 wt. %. The disclosed salts have improved stability during storage at ambient...
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7531622 |
Synthesis and characterization of novel systems for guidance and vectorization of molecules of therapeutic interest towards target cells
A method for preparing a grafted homodetic cyclopeptide forming a framework that defines a grafted upper face and grafted lower face, including synthesizing a linear peptide from modified or...
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7531507 |
Acylated nonadepsipeptides containing pyridyl alanine residues
The invention relates to nonadepsipeptides and processes for their preparation, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular bacterial...
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7531506 |
Process for producing trunkamide a compounds
Trunkamide A and other cycloheptapeptides can be made by solid phase synthesis of a linear precursor.
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7521529 |
Differentially protected orthogonal lanthionine technology
The present invention provides a method of synthesizing an intramolecularly bridged polypeptide comprising at least one intramolecular bridge. The present invention further provides a method of...
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7521420 |
Macrocyclic antagonists of the motilin receptor
The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n...
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7517854 |
Melanocortin receptor agonists
Small cyclic peptides of the formula X1-X2-X3-X4-X5-X6-X7-R 1 comprising 7-12 amino acid residues are provided. Said peptides are MC4 receptor agonists, and thus useful in the treatment of obesity...
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7511013 |
Cyclosporin analogues and their pharmaceutical uses
The compounds of the present invention are represented by Formula I, as shown below:
or a pharmaceutically acceptable salt thereof,
with X, R 0 , R 1 , and R 2 defined herein.
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7504378 |
Macrocyclic peptides active against the hepatitis C virus
Compounds of formula (I):
wherein R 1 is (C 1-8 )alkyl, (C 3-7 )cycloalkyl, {(C 1-6 )alkyl-(C 3-7 )cycloalkyl} or Het, which are all optionally substituted from 1 to 3 times with halo, cyano,...
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7501393 |
Pharmaceutical compositions comprising cyclosporins
A composition is described herein comprising cyclosporin A, polysorbate 80, a polyoxyethylene stearate, and an oil; wherein the composition is an emulsion which is ophthalmically acceptable....
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7491794 |
Macrocyclic compounds as inhibitors of viral replication
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide...
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7491695 |
Methods of using macrocyclic modulators of the ghrelin receptor
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue...
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7479481 |
Treatment of ocular diseases and disorders using lantibiotic compositions
Compositions and methods for treating ocular diseases and disorders are provided. The composition can contain at least one lantibiotic, which can be administered topically by injection,...
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7476653 |
Macrocyclic modulators of the ghrelin receptor
The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue...
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7473761 |
Somatostatin analogues
The invention provides cyclo[{4-(NH 2 —C 2 H 4 —NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof,...
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7473760 |
Cyclic peptide compositions for treatment of sexual dysfunction
A cyclic peptide of the structural formula:
or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 5 , R 6 , m, n and p are as defined. Further provided are compositions for...
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7468419 |
Cyclosporin derivatives for the treatment of immune disorders
The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof:
wherein
A is of the formula:
where Q, W, X,...
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7462686 |
On-growth inhibiting compounds
An on-growth inhibiting agent, for the inhibition and/or prevention of on-growth of biological organisms on objects or living beings, includes at least one cyclotide, and a suitable carrier medium....
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7459522 |
Peptide dimers as agonists of the erythropoietin (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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7452965 |
Colon tumor specific binding peptides
Phage display was used to screen peptide libraries that distinguish between well-differentiated (HCT116) and poorly-differentiated colon carcinoma cells (HT29). The screening protocol used...
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7452865 |
Antagonistic analogs of GH RH (2003)
There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH 2 . These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore...
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7452862 |
Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists
Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle...
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