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6656911 |
Serine protease inhibitors
The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for...
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6649587 |
Polyamine analog conjugates and quinone conjugates as therapies for cancers and prostate diseases
Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as...
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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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6649593 |
Modulators of SREBP processing
Compounds, compositions and methods are provided for the inhibition of S1 protease and for the modulation of cholesterol homeostasis in a cell.
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6645939 |
Substituted β-alanine derivatives as cell adhesion inhibitors
β-Alanine derivatives of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These...
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6642375 |
Fluorescent substances
The present invention provides a fluorescent substance which is represented by a formula: A-B-C wherein A is a residue of natural or synthetic nucleotide, oligonucleotide, polynucleotide, or...
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6638912 |
Peptide compositions mimicking TGF-β activity
Compositions suitable for pharmaceutical administration are provided in which one compound is a small peptide mimic of TGF-β. More preferably, pharmaceutical compositions of the present invention...
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6638941 |
Conformationallly constrained peptidomimetics as β-turn templates and modulators of SH3 domains
Spirolactam compounds useful as inhibitors of protein-protein interactions modulated by SH3 domains are disclosed. Compounds of the invention are also useful as β-turn mimetics. Also disclosed are...
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6635738 |
Compounds which prevent neuronal cell death and uses thereof
The present invention provides for a compound having the structure: (AA 1 ) n -Cys-(AA 2 ) m wherein n=0,1,2,3,4 or 5 and m=0,1,2,3,4 or 5, provided the sum of (n+m) is greater than or equal to...
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6632921 |
Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents
Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans ....
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6627604 |
Memno peptides, process for their preparation and use thereof
The invention relates to novel peptide derivatives, called memno peptides, of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and (A)n have the meaning herein, obtainable...
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6627732 |
Glutathione derivatives and their dosage forms
The present invention provides a glutathione derivative having a dramatically enhanced hematopoiesis promoting effect in the living body represented by the formula (I): where A represents H or a...
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6624147 |
Inhibitors of prenylated pyrophosphate consuming enzymes
Novel peptide-like FPP-analogues suitable for inhibiting protein:prenyl transferases, such as protein:geranylgeranyl transferase-1, and other prenyl pyrophosphate-consuming enzymes such as squalene...
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6624142 |
Trimethyl lock based tetrapartate prodrugs
The invention is directed primarily to compounds of Formula I: wherein: R 1 is a polymeric residue; L 1 is a bifunctional linking group; Y 1 and Y 2 are independently O, S or NR 7 ; R 2-7 ...
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6624290 |
Azapeptides useful in the treatment of Hepatitis C
The present invention relates to azapeptide compounds represented by the formula: pharmaceutical compositions containing such compounds, and the use thereof in the treatment of Hepatitis C viral...
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6620911 |
Anti-cryptococcal peptides
Antifungals based on dolasatin 10 and four structural modifications thereof (herein “peptides”) and methods of treating a host afflicted with a fungi-induced infection are herein described. In...
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6617426 |
Cysteinyl protease inhibitors
Amino acid di- and tri-peptide analogs having C-terminal vinylic groups, pharmaceutical compositions containing the analogs and methods of treating diseases using cysteinyl protease inhibitors;...
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6617310 |
Phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines
This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or...
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6613876 |
β-polypeptide foldamers of well-defined secondary structure
Disclosed are β-peptides containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the α and β carbons of the peptide backbone. The β-peptides adopt stable helical and...
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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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6610658 |
Modulators of &mgr -amyloid peptide aggregation
Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely...
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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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6602856 |
Antagonists of alpha-melanocyte stimulating hormone and methods based thereon
Peptide antagonists of α-melanocyte stimulating hormone are disclosed, together with methods of inhibiting the effects of α-melanocyte stimulating hormone on cells or tissues sensitive to that...
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6600015 |
Selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity
Peptides that selectively stimulate melanocortin-4 (MC-4) receptor activity are disclosed. In one embodiment, the peptides are of formula I:
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6596845 |
Cinnamoyl distamycin analogous derivatives, process for their preparation, and their use as antitumor agents
Compounds which are cinnamoyl distamycin derivatives of formula (I), wherein n is 2, 3, or 4; R 0 is C 1 -C 4 alkyl or C 1 -C 3 haloalkyl; R 1 and R 2 , which are the same or different, are...
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6593455 |
Tripeptide amides that block viral infectivity and methods of use thereof
Embodiments relate to the discovery that tripeptide amides, which correspond to viral capsid sequences, can be used to inhibit viral infection, including human immunodeficiency virus (HIV)...
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6593454 |
Methods for identifying inhibitors of methionine aminopeptidases
Methods are provided for detecting methionine aminopeptidase (MAP) activity and for detecting inhibitors of MAP. The methods utilize a peptide comprising an N-terminal methionine which can be...
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6593300 |
(3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta
The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C 1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C 1-2 ...
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6589937 |
Peptides and nootropic agent
New peptides represented by the following general formula (wherein X is OH or NH 2 , R is an amino acid residue selected from Arg, His, Lys, Methyl-Arg or Methyl-Tyr, n is an integer of 1-4, and...
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6586405 |
Non-covalent inhibitors of urokinase and blood vessel formation
Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have P1 a group having an...
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6586403 |
Treating allergic reactions and inflammatory responses with tri-and dipeptides
This invention relates to methods and compositions of tripeptides and dipeptides having anti-inflammatory activities that can be used for the treatment of allergic and inflammatory reactions. A...
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6579971 |
Method of producing 3,4-dehydroprolines and 3,4-dehydropiperidines
A process for preparing compounds of the formula I in which R is hydrogen, C 1 -C 6 -alkoxy, —NHC 1 -C 6 -alkyl, —N(C 1 -C 6 -alkyl) 2 , OH, NH 2 R 1 is hydrogen, C 1 -C 6 -alkyl, Me 3 Si,...
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6576614 |
Peptide analogs as irreversible interleukin-1β protease inhibitors
Disclosed are compounds, compositions, and methods for inhibiting interleukin-1β protease activity, wherein the compounds are α-substituted methyl ketones having formula (I) as set forth herein....
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6576613 |
Title inhibitors of urokinase
Novel inhibitors of urokinase are provided which have an arginine or arginine mimic aldehyde or an arginine ketoamide group at P1. These compounds are useful in vitro for monitoring plasminogen...
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6566508 |
Fluorogenic compounds and uses therefor
Disclosed are novel coumarin based fluorogenic compounds useful in assaying for biological activity. Specifically, these fluorogenic compounds exhibit fluorescence at particular wavelengths when...
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6566493 |
Peptidomimetics containing 6-peptidylamino-1-naphthalenesulfonamide moieties
Compounds of the following formula are disclosed, wherein R 1 is a peptide and R 2 is an amino acid or peptide as disclosed herein: The compounds are inhibitors of activated protein C.
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6566336 |
Compounds alkylating specific base sequence of DNA and method for synthesizing the same
The invention provides a compound recognizing the minor group of hydrogen bonds between base pairs and being capable of forming a covalent bond with bases. The inventive compound can recognize a...
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6562783 |
Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
The invention provides a compound of formula (I): or salts or hydrates thereof, useful as beta-secretase inhibitors. The invention further relates to a method of reducing plaque formation,...
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6552168 |
Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
The invention encompasses the novel class of compounds represented by formula I, which are caspase-3 inhibitors. The invention also encompasses certain pharmaceutical compositions for treatment...
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6551998 |
Antimicrobial agents
Antimicrobial compounds of formula I are disclosed: R 1 —X—R 2 wherein X is a group comprising of from about 4 to about 10 amino acids, wherein at least one of the amide (—CONH—) linkages...
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6548479 |
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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6548638 |
Peptoid and nonpeptoid containing α-keto oxadiazoles as serine protease inhibitors
The present invention relates to certain substituted oxadiazole peptoids and nonpeptoids useful as inhibitors of serine proteases, especially human neutophil elastase (HNE). Compounds of the...
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6548637 |
Ligands for opioid receptors
The present invention provides compounds, and pharmaceutical preparations thereof, that bind selectively to mammalian opioid receptors. The present set of compounds comprises full agonists, partial...
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6548048 |
Lipopeptide stabilized microbubbles as diagnostic/therapeutic agents
Novel membrane-forming amphiphilic lipopeptides comprising one or more peptide moieties containing 2-50 aminoacyl residues and one or more hydrocarbon chains containing 5-50 carbon atoms. Such...
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6541454 |
Phosphonates, biphosphonates and pharmaceutical compositions containing them
A method for treating patients having calcium related disorders includes using di- or tripeptide derivatives of bisphosphonates to enhance oral bioavailability of such compounds.
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6537967 |
Pentamer peptide amide, ALGPGNH2, which inhibits viral infectivity and methods of use thereof
The present invention relates to the discovery that a specific pentamer peptide amide, which corresponds to a viral capsid sequence, can be used to inhibit viral infection, including human...
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6534283 |
Method for treatment and prevention of physiological shock
Shock is a life threatening complication in situations associated with trauma including burns, surgery, ischemia, sepsis, and other critical care applications. Shock is induced by pancreatic...
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6524553 |
Quinolone vitronectin receptor antagonist pharmaceuticals
The present invention describes novel compounds of the formula: (Q) d —L n —C h , useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of...
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6511959 |
Use of calcium-activated neutral protease (CANP) inhibitors in pharmaceutical preparations
The invention provides to the use of inhibitors of calcium-activated neutral proteases (CANPs) and their pharmaceutically acceptable addition salts or their active subunits in the field of tumor...
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