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6153391 |
Interruption of binding of MDM2 and P53 protein and therapeutic application thereof
A method for interfering with the binding between p53 and MDM2 or a protein having a p53 binding site analogous to that of MDM2, which method comprises administering a effective amount of a...
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6150325 |
Bicyclic tachykinins antagonists, preparation thereof and their use in pharmaceutical compositions
This invention relates to novel compounds of general formula (I): ##STR1## and to pharmaceutical compositions containing them.
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6146853 |
Cyclic depsipeptide PF 1022G
Known cyclic depsipeptides which are PF 1022F substance and PF 1022H substance, as well as a novel cyclic depsipeptide, PF 1022G substance, are now prepared simultaneously by cultivating a fungal...
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6143739 |
Basic proline-amide derivatives of GE 2270 and GE 2270-like antibiotics
The present invention refers to basic amides derivatives of GE 2270 and GE 2270-like antibiotics of general formula (1), wherein the group GE represents the antibiotic core molecule. The amide...
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6136781 |
LH-RH receptor antagonists
The LH-RH receptor antagonists containing cyclic pentapeptides or salts thereof and novel cyclic pentapeptide or salts thereof are provided. The LH-RH receptor antagonists of the present invention...
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6126916 |
Radiometal-binding peptide analogues
Novel metal binding ligands are disclosed that may be coupled to peptides for use in methods of diagnosis and therapy. Peptides containing the ligands are produced using a method wherein ligand...
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6127519 |
Calcitonin derivatives
Peptides useful in the regulation of calcium metabolism are disclosed. Also disclosed are pharmaceutical compositions of matter containing such peptides as well as a method for the regulation of...
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6123916 |
Therapeutic use of somatostatin peptides
The invention relates to a new pharmaceutical use of somatostatin peptides comprising on the terminal amino group a polyamino polycarboxylic group, in free form or in a pharmaceutically acceptable...
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6117974 |
Libraries of backbone-cyclized peptidomimetics
Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel...
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6111067 |
A-82846-type glycopeptide antibiotics
A82846-related glycopeptide compounds are prepared by treating an antibiotic selected from A82846 components A, B and C with trifluoroacetic acid to remove 1) the α-L-O-4-epi-vancosaminyl group...
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6107273 |
Tumor necrosis factor inhibitors
TNFα antagonist compounds and methods of using the same are disclosed. The compounds comprise a molecular surface that is substantially similar to at least one molecular surface of human TNFα....
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6107275 |
Cyclic Antiplatelet peptides with pseudo-bond
The present invention relates to cyclic peptide analogs containing a pseudo-bond, useful as platelet aggregation inhibitors. An example of a compound of this invention includes Cyclo[AlaΨ[CH 2 ...
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6107274 |
Piperazines as inhibitors of fructose-1,6-bisphosphatase (FBPase)
Compounds of formula A are disclosed: ##STR1## wherein R 1 is aralkyl or cycloalkyl; R 2 is cycloalkylmethyl, alkyl, or aralkyl; R 3 is hydrogen, alkyl, substituted phenyl (including...
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6100377 |
Constrained peptides
Constrained peptides are disclosed which have cyclic portions that contain biologically active regions linked to two linear extensions that each comprise at least one aromatic-group containing...
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6096707 |
Integrin binding peptide and use thereof
Cyclic peptides comprising three colinear amino acids, arginine-lysine-lysine (RKK) are provided that bind to the integrin α2I domain and are potent inhibitors of its interaction with collagens I...
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6096318 |
Antigenically modified HCG polypeptides
Endogenous and exogenous proteins, and fragments thereof, are chemically modified outside the body of an animal so that when injected into the animal they produce more antibodies against the...
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6093692 |
Method and compositions for lipidization of hydrophilic molecules
Fatty acid derivatives of disulfide-containing compounds (for example, disulfide-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for...
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6087330 |
Process to inhibit binding of the integrin α.sub.4 β.sub.1 to VCAM-1 or fibronectin and cyclic peptides therefor
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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6083741 |
Internalisation of DNA, using conjugates of poly-l-lysine and an integrin receptor ligand
Composition comprising DNA associated with a polycation moiety wherein the polycation moiety is itself coupled to an integrin receptor binding moiety is disclosed. Preferably, the integrin receptor...
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6083481 |
Thrombus imaging agents
This invention relates to radiolabeled reagents that are scintigraphic imaging agents for imaging sites of thrombus formation in vivo, and methods for producing such reagents. Specifically, the...
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6080838 |
Peptidomimetic of helix-turn-helix or gamma-turn
A peptidomimetic of the turn in the helix-turn-helix (HTH) motif of DNA-binding proteins was designed and synthesized. Conformational constraint was achieved by an unusual linking of two amino...
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6075006 |
Soluble tachykinin antagonists, the preparation and use thereof
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6066616 |
Somatostatin analogue composition and use in treating breast cancer
The invention provides a pharmaceutical composition comprising a somatostatin analogue, and its use in the treatment of breast cancer. The pharmaceutical composition preferably contains lactic acid...
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6060446 |
Method and composition for treating renal disease and failure
A nutritional composition and methods of using same for treating and preventing renal failure is provided. The nutritional composition includes a therapeutically effective amount of a source...
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6054556 |
Melanocortin receptor antagonists and agonists
Cyclic lactam peptides are disclosed which inhibit at various levels of antagonism the melanocortin 1 receptor (MC1R), melanocortin 3 receptor (MC3R), melanocortin 4 receptor (MC4R), and...
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6051206 |
Radiolabeled somatostatin-derived peptides for imaging and therapeutic uses
This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled...
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6043217 |
Amide derivative of amythiamicin
Novel amide derivatives of amythiamicin are now provided, which are soluble in water and exhibit antibacterial activities, some of which exhibit an excellent antibacterial activity against...
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6043341 |
Cyclic peptide antifungal agents
The present invention provides phosphonylating agents and phosphonylation conditions that are compatible with the acid- and base-sensitive compounds and which promote a regioselective and...
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6043058 |
Preparation of cyclic depsipeptide compounds and a novel cyclic depsipeptide
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6037447 |
Glycopeptide compounds
The present invention is directed to certain glycopeptide dimers in which two glycopeptide units are covalently linked to one another through their disaccharide amine, via a linking radical. This...
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6034056 |
Fibronectin adhesion inhibitors
Cyclic peptides of formula (1): ##STR1## Wherein: AA1 is an L or D amino acid selected from Ile and Leu or amino acid analogue thereof; AA2 is an L amino acid selected from Leu or amino acids...
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6034211 |
β-sheet nucleating peptidomimetics
N-methylated β-sheet nucleating peptidomimetics containing diarylheterocycle β-turn mimics, and methods of making and using them.
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6034058 |
Semi-synthetic alanyl dilemnin analogs
The didemnin class of biologically active cyclodepsipeptides, isolated from the marine tunicate Trididemnun solidum, has shown considerable antitumor, antiviral, and immunosuppressive activities....
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6034057 |
Peptide inhibitors of fibronectine
Cyclic dimeric peptides of formula (I) ##STR1## wherein: peptide 1 and peptide 2 independently represent a tetrapeptide of formula -AA1-AA2-AA3-AA4- juxtaposed in parallel or antiparallel...
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6033879 |
Process for the preparation of substituted aryl lactic acid containing cyclodepsipeptides with 24 ring atoms
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6030943 |
Dehydrodidemnin B as an L-type calcium channel enhancer
This invention relates to a new use discovered for the compound known as Aplidine (dehydrodidemnin B) which has the following structure: Aplidine has been found to be a potent L-type calcium...
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6031071 |
Methods of generating novel peptides
The present invention describes peptides capable of specifically binding to preselected micromolecules or to their natural receptor. The preselected molecules include but are not limited to drugs,...
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6031073 |
Cyclic polypeptides comprising a thioether linkage and methods for their preparation
This invention relates generally to cyclic polypeptides comprising a thioether linkage and methods for their preparation. More particularly, this invention relates to halogenated polypeptides...
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6030944 |
Cyclohexapeptidyl bisamine compounds
Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are...
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6030942 |
Peptides peptide analogs peptidomimetics and other small molecules useful for inhibiting the activity of ribonucleotide reductase
The invention relates to compositions which are useful for inhibiting ribonucleotide reductase enzymes, including the mammalian ribonucleotide reductase enzyme. The compositions include, but are...
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6025466 |
Cyclic hepta-peptide derivative from colonial ascidians, Lissoclinum sp.
A new cyclic heptapeptide, trunkamide A, with antitumor activity has been isolated from a Lissoclinium sp. collected on the Great Barrier Reef, Australia. The structure was determined to be of...
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6022851 |
Lantibiotic related to actagardine, and processes for the preparation and use thereof
The present invention relates to a novel lantibiotic having the formula NH 2 --R-actagardine, where NH 2 --R is the radical of the amino acid alanine, which is formed by the microorganism...
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6022523 |
Radiolabeled platelet GPIIb/IIIa receptor antagonists as imaging agents for the diagnosis of thromboembolic disorders
This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein...
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6017878 |
Nerve growth factor structural analogs and their uses
Cyclic compounds with a 3-dimensional structure that bind at least one neurotrophin receptor (NTR) under physiologic conditions in vitro or in vivo are new. Binding to NTR at least partially mimics...
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6013256 |
Method of preventing acute rejection following solid organ transplantation
The invention provides methods of preventing acute rejection following renal or other solid organ transplantation. The methods entail administering, e.g., intravenously, to a transplant patient a...
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6013627 |
Organic compounds
Cyclopeptolides of formula I ##STR1## wherein A, B, R, Leu, Leu, C, X and Y are as defined, are inhibitors of adhesion molecule expression and are thus useful for treatment of inflammatory and...
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6013626 |
Cryptophycins from synthesis
A cryptophycin compound is provided having the structure: ##STR1## Further provided are methods of producing cryptophycins by total synthesis and methods of using cryptophycins in pharmaceuticals....
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6010679 |
Ternary radiopharmaceutical complexes
This invention provides novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer. The radiopharmaceuticals are...
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6011136 |
Cyclopeptolides
Cyclopeptolides of formula (I), wherein A, B, R 1 Leu, Leu, C, X and Y are as defined, are inhibitors of adhesion molecule, expression and inhibitors of TNF release and are thus useful for...
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6008191 |
Pharmaceutical compositions containing cyclosporin
A novel homogenous alcohol free, free flowing, clear and transparent pharmaceutical composition containing Cyclosporin is disclosed. The amount of Cyclosporin is easily measurable at a wide range...
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