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6673772 |
Dipeptide compounds and their use as antiviral agents
A novel dipeptide compound inhibiting the enzymatic activity of HIV protease and an anti-AIDS medicine comprising this dipeptide compound as an effective component represented by formula (I) ...
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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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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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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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6642259 |
Immune stimulating dietary supplement and method of use thereof
The immune system of middle aged and elderly individuals is stimulated with a dietary supplement. The dietary supplement includes Vitamin E, Vitamin B6 and conjugated linoleic acid. The dietary...
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6642253 |
Thrombin inhibitors comprising an aminoisoquinoline group
The invention relates to a compound having the formula (I) wherein R 1 is cyclopentyl, cyclohexyl or a branched (3-4C)alkyl; R 2 is cyclohexyl or phenyl; R 3 is H or methyl; and A is an...
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6642201 |
Use of a dipeptide for stimulating repair processes
L-Lys-L-Glu dipeptide is proposed for use in medicine for preparation of a drug capable of stimulating repair processes. According to the invention, the pharmaceutical peptide preparation capable...
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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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6635621 |
Cysteine protease inhibitors
This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases,...
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6635620 |
Hydroxyproline derivatives
The present invention relates to hydroxyproline derivatives represented by the following general formulas and the therapeutic agent containing the same for the impaired organs and tissues. ...
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6630487 |
Treatment of insulin resistance with growth hormone secretagogues
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in...
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6630451 |
Benzimidazolone peptidometics as thrombin receptor antagonist
The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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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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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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6617311 |
Regulation of tyrosine hydroxylase
This invention relates to methods of regulating the effect of tyrosine hydroxylase (TH). In particular it relates to increasing the effective amount of TH in the central nervous systems (CNS) for...
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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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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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6605590 |
Oligomers and oligomeric segments of alpha-hydroxy carboxylic acids and alpha-amino acids
An enzymatic synthesis and composition of α-hydroxy carboxylic acid and α-amino acid or peptide co-oligomers is disclosed wherein a residue of the α-hydroxy carboxylic acid is linked to a...
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6602514 |
Use of ectoine or ectoine derivatives in cosmetic formulations
The use of one or more compounds chosen from the compounds of the formulae Ia and Ib the physiologically compatible salts of the compounds of the formulae Ia and Ib and the stereoisomeric forms...
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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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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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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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6576628 |
3-aryl-succinamido-hydroxamic acids, methods for producing said acids and medicaments containing the same
The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) and its salt, ester and derivative thereof, along with...
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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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6566337 |
Compounds with growth hormone releasing properties
This invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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6566338 |
Caspase inhibitors for the treatment and prevention of chemotherapy and radiation therapy induced cell death
The use of caspase inhibitors for treating, ameliorating, and preventing non-cancer cell death during chemotherapy and radiation therapy and for treating and ameliorating the side effects of...
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6562789 |
Histidine derivatives, preparation process, and their use as free antiradical agents
The invention relates to novel histidine derivatives corresponding to the general formula (I) below: in which: R denotes a linear or branched, saturated or unsaturated alkyl radical containing...
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6552038 |
Anticoagulant agents
This invention relates to a compound of the Formula I X—C(O)—Y—G—R I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof,...
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6551999 |
Angiogenesis inhibitor
An angiogenesis inhibitor comprising a cysteine protease inhibitory compound. As the preferable cysteine protease inhibitory compound, epoxysuccinic acid compounds, peptide halohydrazide compounds,...
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6548480 |
Phosphonic acid derivatives with metallopeptidase inhibitory activity
Compounds of formula (I) wherein R is an alkyl, aryl or arylalkyl group wherein the aryl is phenyl naphthyl or heterocycle; R 1 and R 2 , the same or different, are hydrogen atoms or alkyl groups;...
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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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6548481 |
Effectors of dipeptidyl peptidase IV
Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired...
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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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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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6534536 |
Alkylsulfonamido heterocyclic thrombin inhibitors
Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl,...
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6531449 |
Hexahydropyrazolo&lsqb 4,3,-c&rsqb pyridine metabolites
The invention provides metabolites of the compound...
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6531130 |
Treatment of demyelinating autoimmune disease with ordered peptides
Compositions and methods are provided for the treatment of demyelinating autoimmune disease. Therapeutic doses are administered of an ordered peptide comprising a repeated motif {SEQ ID NO: 1} [ 1...
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6528489 |
Mycotoxin derivatives as antimitotic agents
The present invention provides a treatment for mammalian diseases characterized by aberrant cell proliferation. The treatment consists of administering therapeutically active dosages of antibiotic...
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6525025 |
Gamma-ketoacid dipeptides as inhibitors of caspase-3
This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases. The invention also encompasses certain pharmaceutical compositions...
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6525017 |
Using glutathiane to protect neurons from injury
A method for identifying agents useful for protection of a human neuron from injury. The method includes the steps of providing a cell which has NMDA receptor; selecting a agent potentially useful...
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6521659 |
Compositions containing a substituted indolealkanoic acid and an angiotensin converting enzyme inhibitor
Disclosed are methods of reducing serum glucose and triglyceride levels and for inhibiting angiogenesis, the methods comprising administration of substituted indolealkanoic acids to patients in...
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6506732 |
Enzymatic hydrolysate of milk proteins
The present invention relates to a mixture of soluble hydrophobic peptides of an enzymatic hydrolysate of milk having skin hydrating properties and percutaneous absorption levels of 4 to 5%. The...
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6506733 |
Compounds and compositions as protease inhibitors
Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins...
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6500804 |
Method for the improvement of islet signaling in diabetes mellitus and for its prevention
The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic...
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6500802 |
Peptidyl-2-amino-1-hydroxyalkanesulfonic acid cysteine protease inhibitors
The present invention is directed to novel peptidyl-2-amino-1-hydroxyalkanesulfonic acid inhibitors of cysteine proteases. Methods for the use of the protease inhibitors are also described.
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6500803 |
Factor VIIa inhibitors
The present invention relates to compounds of formula I, in which R 1 , R 2 , R 91 , R 92 , R 93 , R 94 , R 95 , R 96 , R 97 , r, s, and t have the meanings indicated in the claims. Compounds of...
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6495522 |
Substituted alpha-hydroxy acid caspase inhibitors and the use thereof
The present invention is directed to novel substituted α-hydroxy acid thereof, represented by the general Formula I: where R 1 -R 5 , X and Z are defined herein. The present invention also...
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