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6136787 |
Interleukin 1β protease and interleukin 1β protease inhibitors
There is disclosed an isolated polypeptide and derivatives thereof having protease biological activity for human precursor IL-1β and for a substrate comprising: R 1 -Asp-R 2 -R 3 wherein R 1 ...
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6133324 |
Use of perillyl alcohol in organ transplantation
Perillyl alcohol and its monoterpene derivatives used alone or in combination with existing immunosuppressive agents, such as cyclosporine A and azathioprine, to provide methods and compositions...
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6127342 |
Method for preventing or treating a lung disease caused by active oxygen and free radical injury
The present invention provides a preventive or therapeutic agent for tissue injury caused by active oxygens and free radicals, having for its effective component γ-L-glutamyl-L-cysteine ester...
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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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6126939 |
Anti-inflammatory dipeptide and pharmaceutical composition thereof
The present invention is directed to peptides of the formulas (i) Xaa-Yaa-Arg, wherein either Xaa is any amino acid residue and Yaa is Glu or Xaa is absent and Yaa is any amino acid residue with...
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6124264 |
Heterocyclic compounds
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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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6117841 |
Substituted peptidylamine calcium channel blockers
The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to...
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6117887 |
Inhibition of 26S and 20S proteasome by indanones
This invention is novel indanone compositions useful for inhibiting cell proliferation disorders in mammals.
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6117842 |
Fibrinogen receptor antagonists
Compounds of this invention have the formula: X--(CH 2 ) n --C(O)NH--A--C(COOR 5 )R 3 R 4 or a pharmaceutically acceptable salt thereof, e.g. ##STR1## which are useful for inhibiting fibrinogen...
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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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6110923 |
Method for treating cancer using novel substituted purinyl derivatives with immunomodulating activity
The present invention covers a method of treatment of cancer, in particular, colon carcinoma, comprising the step of administering the compound N2-(6-dimethylamino...
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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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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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6096711 |
Hsp72 induction and applications
Disclosed herein is a method for inducing Hsp72 production in a cell. The method involves contacting the cell transiently with a proteasome inhibitor in an amount sufficient to induce Hsp72...
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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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6093696 |
Tyrosine derivatives
Tyrosine derivatives of formula (1) are described: ##STR1## in which R is (1) a group R 1 X 1 -- where R 1 is an optionally substituted alkyl or aromatic group, and X 1 is a covalent bond or a...
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6090786 |
Serine proteases, their activity and their synthetic inhibitors
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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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6060452 |
Analogs of L-Glu-L-Trp having pharmacological activity
This invention provides analogs of L-Glu-L-Trp and methods of using them for immunomodulation and treatment of pathological neovascular conditions. The analogs include the substitution of a carbon...
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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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6057297 |
Inhibitor compounds of zinc-dependent metalloproteinases associated with pathological conditions, and therapeutic use thereof
Peptidomimetic compounds capable of inhibiting zinc-dependent metalloproteinases to treat pathological conditions associated with activation of endogenous metalloproteinases in mammals.
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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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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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6030946 |
Reversible cysteine protease inhibitors
Cysteine protease inhibitors are provided.
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6030640 |
Oligoglycine compound, fibrous microtube of oligoglycine compound and process of producing fibrous microtube
A lipid represented by the following formula: MO--(CO--CH 2 --NH) p --CO--(CH 2 ) n --CO--(NH--CH 2 --CO) q --OM wherein M represents a hydrogen atom or an alkali metal, n is an integer 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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6024734 |
Treatment methods using homeopathic preparations of growth factors
The present invention comprises homeopathic dilutions of growth factors and methods for their use. Disorders which may be effectively treated with the compositions of the present invention include...
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6025333 |
Treatment of CNS tumors with metalloprotease inhibitors
The present invention relates to genes and their encoded proteins which regulate neurite growth and the diagnostic and therapeutic use of such proteins (termed herein neurite growth regulatory...
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6020309 |
Pharmaceuticals based on papillomaviruses
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6017887 |
Peptide, peptide analog and amino acid 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), (II) and...
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6017888 |
Stimulation of hair growth by peptide copper complexes
Peptide-copper complexes are disclosed which stimulate the growth of hair on warm-blooded animals. In one aspect of this invention, the peptide-copper complexes are dipeptides or tripeptides...
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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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6015792 |
Specific eatable taste modifiers
Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
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6007819 |
Methods of inducing immunity using low molecular weight immune stimulants
The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other...
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6004933 |
Cysteine protease inhibitors
The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and...
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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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6001817 |
Pharmaceutical composition comprised of cisplatin, and processes for making and using same
A pharmaceutical composition, comprising cisplatin, a special carrier and, optionally, customary pharmaceutical excipients, is disclosed. The preparation of this pharmaceutical composition is also...
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5998379 |
Serine protease inhibitors-proline analogs
The present invention relates to certain substituted oxadiazole, thiadiazole, and triazole peptoids that are useful as inhibitors of serine proteases, in particular human neutrophil elastase....
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5994406 |
Geminal cationic surfactants of the type Nα Nω bis (Nα-acyl-arginin) α,ω diamino alkyl dichlorohydrates as antimicrobial agents
Surfactants having general formula (II) ##STR1## wherein X=8-14; n=2-8. The process for obtaining such surfactants comprises the following steps; a) producing nitroarginin; b) producing N α...
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5981492 |
Substituted 5-membered ring heterocycles, their preparation and their use
The present invention pertains to 5-ring heterocycles of general formula (I), wherein W, Y, Z, B, D, E and R as well as b, c, d, e, f, g, and h are as indicated in the description; to methods for...
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5981470 |
Uterine fibroid treatment
The use of a) an angiotensin-converting enzyme (ACE) inhibitor such as Captopril or Enalapril, b) an angiotensin II-receptor antagonist such as Saralasin or Losartan, or c) a renin inhibitor, such...
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5977073 |
Nutrient composition for treatment of immune disorders
A composition and method for its use in treatment of an immune disorder in a mammal. The composition includes, in relative amounts, between 50 and 3000 mg of a purified compound selected from...
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5977075 |
N-aroylamino acid amides as endothelin inhibitors
The present invention relates to the compounds of formula (I) ##STR1## wherein R is carboxy, esterified carboxy, carbamoyl, N-(alkyl or aryl)-carbamoyl, cyano, 5-tetrazolyl or CONH--SO 2 --R 4 ;...
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5977074 |
Inhibitors of β-amyloid protein production
This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease...
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5977070 |
Pharmaceutical compositions for the nasal delivery of compounds useful for the treatment of osteoporosis
A pharmaceutical composition for the nasal delivery of compounds useful for treating osteoporosis, comprising an effective amount of a physiologically active truncated analog of PTH or PTHrp, or...
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5972897 |
Acylated enol derivatives as prodrugs of elastase inhibitors
This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and...
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