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6127339 |
Peptide for binding thereto a low density lipoprotein
Disclosed is a peptide for binding thereto a low density lipoprotein, which has an amino acid sequence represented by the formula (I) or (II) and which has an electric charge (E) satisfying the...
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6127340 |
Serine protease inhibitors
This invention is directed to peptide inhibitors of serine proteases, espcecially thrombin, in which the P1-P2 natural amide linkage is replaced by another bond. Exemplary thrombin inhibitors have...
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6124431 |
Peptide derivatives
A peptide derivative represented by the following formula or a salt thereof ##STR1## wherein A represents a hydrogen atom, and B represents a phenyl group substituted with a hydroxyl group; said...
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6121241 |
Anticoagulant peptide aldehyde derivatives
This invention relates to peptide aldehyde derivatives of formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represent a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents...
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6121239 |
Peptide substrates for the identification of factor Xa
Peptide substrates selected from the group consisting of (i) the tri- and tetra-peptides of the formula Q-A 1 -A 2 -Gly-A 4 -R (I) having SEQ ID NO: 1 in which Q is a...
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6121240 |
Urokinase receptor ligands
Compounds of the invention inhibit urokinase plasminogen activator or uPAR: ##STR1## where R 10 is --CH(R 9 )XCH(R 1 )(R 11 ) or a capping group, where X is NR 12 , CR 12 R 15 , O, S, SR 12 , or...
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6120768 |
Dota-biotin derivatives
A radionuclide-chelator conjugate composition for detecting and/or treating lesions in a patient in a pre-targeting protocol which comprises pre-targeting the target cell, tissue, or pathogen with...
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6117840 |
CS-1 peptidomimetics, compositions and methods of using the same
The present invention contemplates a peptide that inhibits the binding between the VLA-4 receptor expressed on inflammatory leukocytes and the fibronectin CS-1 peptide expressed on endothelial...
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6110896 |
Peptidyl compounds and their therapeutic use
Tripeptidyl derivatives having a SH or acylS group and which are amides, have therapeutic utility via MMP or TNF inhibition.
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6107489 |
Extended lifetimes in vivo renin inhibitors
Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting...
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6103870 |
CS-1 peptidomimetic, compositions and methods of using the same
The present invention contemplates a peptide that inhibits the binding between the VLA-4 receptor expressed on inflammatory leukocytes and the fibronectin CS-1 peptide expressed on endothelial...
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6100238 |
Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors
The present invention relates to certain substituted oxadiazole nonpeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated...
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6096861 |
Peptide-peptoid metal complexes
A chemical complex comprising divalent metal ions, preferably Ca +2 ions, and peptide-peptoid trimers in a fixed ratio and having a centrosymmetric crystalline structure wherein three divalent...
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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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6096712 |
Kininogen inhibitors
Kininogenase inhibiting peptides or peptide analogues with C-terminal related to agmatine or noragmatine.
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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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6090785 |
Substituted N-carboxyalkylpeptidyl derivatives as antidegenerative agents
Novel N-carboxyalkylpeptidyl compounds represented by the formula ##STR1## which are found to be useful inhibitors of matrix metalloendoproteinases which degrade major components of articular...
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6087119 |
Method for determining the catalytic activity of factor IXa
A method for the determination of factor IXa in a sample solution using a measurable factor IXa substrate and a water-miscible alcohol and measuring the cleavage of the factor IXa substrate as a...
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6084065 |
Oligopeptides with fungicidal activity
The present invention relates to oligopeptidic compounds having the general formula (I): K--[--A--] z --[--B--] w --L (I) The compounds having general formula (I) are...
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6069232 |
Polyfluoroalkyl tryptophan tripeptide thrombin inhibitors
This invention relates to polyfluoroalkyl tryptophan tripeptides and to compositions containing them. The compounds are highly selective thrombin inhibitors which provide anticoagulant effects...
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6051683 |
Immune regulating peptides and method of obtaining them
The invention relates to medicine, specifically, to methods of obtaining biologically active substances with immuno-regulating properties, and can be used in medicine and veterinary science and in...
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6051684 |
Methods of treating neurodegenerative disorders using protease inhibitors
Methods of use of compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds provided for use in the methods are those of the...
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6048841 |
Peptidyl compounds
Peptidyl compounds having an imidazole substituent have therapeutic utility via their inhibitory effect on metalloproteinases and tumour necrosis factor.
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6048840 |
Hypoglycaemic peptides
This invention relates to novel insulin-potentiating hypoglycaemic compounds.
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6046289 |
Propenamide derivatives containing Arg-Gly-Asp polymers obtained therefrom
A propenamide derivative of the formula (I) having, as an essential structural unit, an adhesive peptide represented by the formula (II) in the side chain or salts thereof: Formula (I): R 1 R 2 ...
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6046168 |
Peptide inhibits blood triglyceride level
The present invention relates to a peptide having the amino acid sequence shown in the sequence listing; an agent for inhibiting elevations of triglyceride levels in blood comprising the above...
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6037325 |
Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases including human neutrophil elastase,...
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6034067 |
Serine protease inhibitors
The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can...
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6034215 |
3-amino-2-oxo-1-piperidnercetic derivatives as enzyme inhibitors
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof,...
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6034066 |
Cysteine protease inhibitors for use in treatment of IGE mediated allergic diseases
The invention provides compounds for use in the treatment of allergic diseases including juvenile asthma and eczema. The compounds can inhibit IgE mediated reaction to major environmental and...
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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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6034216 |
Low molecular weight peptidomimetic growth hormone secretagogues
The present invention comprises growth hormone releasing peptides/peptidomimetics (GHRP) capable of causing release of growth hormone from the pituitary. Compositions containing the GHRP's of this...
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6030946 |
Reversible cysteine protease inhibitors
Cysteine protease inhibitors are provided.
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6030950 |
Pharmaceutical therapeutic use of glutathione derivative
Methods of adjusting or maintaining the intracellular levels of glutathione of a subject are provided. The subject is treated by administering an effective amount of an acetyl derivative of...
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6030619 |
Molecular mimetics of meningococcal B epitopes
Molecular mimetics of unique epitopes of Neisseria meningitidis serogroup B ("MenB") are disclosed. Compositions containing such molecular mimetics can be used to prevent MenB or E. coli K1 disease...
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6028110 |
Succinyl hydroxamic acid, N-formyl-N-hydroxy amino carboxylic acid and succinic acid amide derivatives as metalloprotease inhibitors
A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO 2 H group and R 1 , R 2 , R 3 , R 4 , R 5 are as defined in the specification, or a...
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6027711 |
Structurally determined metallo-constructs and applications
A metallo-construct, which may be a peptide, is provided for use as a biological, therapeutic, diagnostic imaging, or radiotherapeutic agent, and for use in library or combinatorial chemistry...
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6025472 |
N-substituted glycine derivatives as enzyme inhibitors
The present invention discloses peptide aldehydes which are potent inhibitors of factor Xa, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of...
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6024938 |
Lyophilized imaging agent formulation comprising a chemotactic peptide
A lyophilized imaging agent formulation and methods for making same are disclosed, such formulations comprise a targeting molecule such as antibody or chemotactic peptide, a linker such as...
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6022860 |
Immobilized and activity-stabilized complexes of LHRH antagonists and processes for their preparation
In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over...
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6020312 |
Synthetic antibiotics
Compositions of the current invention are directed toward inhibiting the growth of microorganisms, particularly fungi. The compositions consist of chemically-synthesized antibiotics comprising...
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6017537 |
Formyl methionyl peptide vaccine adjuvant
The present invention relates to immunological adjuvants comprised of the N-formyl methionyl peptide fMLP. FMLP, when used as an adjuvant in accordance with the present invention, provides for an...
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6015791 |
Serine protease inhibitors-cycloheptane derivatives
The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors,...
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6015879 |
Peptide and peptide analog protease inhibitors
Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided Among the compounds are those of formulae I and II:...
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6015877 |
Compounds for inhibition of proteolysis
Compounds used to treat cancer which inhibit carboxy terminal proteolysis of proteins having a carboxyl-terminal -CAAX motif (C=cysteine, A=aliphatic amino acid, and X=any amino acid). The...
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6013462 |
Glutathione analogs as reagents
Compounds of the formula ##STR1## or the alkyl (1-6C), alkenyl (1-6C), or arylalkyl (7-12C) amides or salts including the cycloamido forms thereof; wherein n is 1 or 2; wherein when n is 1, X...
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6008196 |
Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase, and to novel processes for making the same. As inhibitors of human neutrophil elastase,...
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6004757 |
Substrate specificity of a protein kinases
The invention provides a method for determining an amino acid sequence motif for a phosphorylation site of a protein kinase. In the method of the invention, a protein kinase is contacted with an...
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6001813 |
Val-pro containing α-keto oxadiazoles as serine protease inhibitors
The present invention relates to certain substituted oxadiazole tripeptides, which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated...
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6001811 |
Serine protease inhibitors--N-substituted derivatives
The present invention relates to oxadiazole, thiadiazole, and triazole peptoids that are inhibitors of serine protease, specifically human neutrophil elastase; which proteases are useful in...
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