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6180600 |
CD8 antagonists
Compounds that inhibit CD8 mediated T cell activation and that have a molecular surface that corresponds to the molecular surface of human CD8 at amino acids 38-46 and/or 53-56 and/or 60-67 and...
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6180610 |
Tetrapeptide
The peptide X-Arg-Gly-Asp-R-Y wherein X is H or at least one amino acid and Y is OH or at least one amino acid, and R is an amino acid selected from Thr or Cys, or other amino acid, having the same...
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6180095 |
Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents
The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: L 1 is a bifunctional...
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6177408 |
Distamycin derivatives, process for preparing them, and their use as antitumor and antiviral agents
A compound which is a distamycin derivative 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 may be the same or different, are each...
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6177407 |
Methods to increase blood flow to ischemic tissue
The present invention provides methods and kits for increasing blood flow to ischemic tissue, comprising the administration of an effective amount of angiotensinogen, angiotensin I (AI), AI...
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6171578 |
Benzodiazepine derivatives for imaging thrombi
The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled...
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6172044 |
Acylated enol derivative of α-ketoesters and α-ketoamides
This invention relates to acylated enol derivatives of α-ketoesters and α-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors...
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6159940 |
Method for modulating hemopoiesis
A peptide of the formula I X--Glu--Trp--Y (I) wherein X is H or Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal,...
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6159706 |
Application of enzyme prodrugs as anti-infective agents
The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate...
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6159938 |
Serine protease inhibitors comprising α-keto heterocycles
Provided are methods of inhibiting the activity of a serine protease using protease inhibitors that include an alpha-keto heterocycle in their structure. The methods are useful in the treatment of...
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6156732 |
Azole peptidomimetics as thrombin receptor antagonists
Azole derivatives of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.
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6153585 |
Arylsulfonanilide derivatives
The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as...
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6153393 |
Elimination of interference in diagnostic methods by peptides comprising D-amino acids
The invention concerns the use of peptides which are comprised essentially of D-amino acids to eliminate interference in diagnostic methods, a method for eliminating interference in diagnostic...
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6153588 |
Stable non-hygroscopic crystalline form of N-[N-[N-4-(piperidin-4-yl)butanoyl)-N-ethylglycyl] aspartyl]-L-β-cyclohexyl alanine amide
The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspart
yl]-(L)-β -cyclohexyl-alanine...
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6150329 |
Multimeric antithrombotic agents
This invention relates to antithrombotic agents and uses thereof. Specifically, the invention relates to chemical moieties that specifically bind to platelets and inhibit their aggregation,...
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6149925 |
Topical compositions for enhancing glutathione production
The invention provides cosmetic or pharmaceutical compositions for topical application to the skin comprising glutathione-enhancing effective amounts of a glycine compound, a glutamine compound,...
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6150334 |
Serine protease inhibitors-tripeptoid analogs
The present invention relates to certain compounds comprising substituted oxadiazole, thiadiazole and triazole structures which are useful as inhibitors of serine proteases, including human...
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6143715 |
Hepatitis C inhibitor peptide analogues
Compound of formula (I) active against the Hepatitis C virus: ##STR1## wherein B is an acyl derivative; a is 0 or 1; R 6 , when present, is carboxy(lower)alkyl; b is 0 or 1; R 5 , when present, is...
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6143716 |
Liposomal peptide-lipid conjugates and delivery using same
Peptide-lipid conjugates are incorporated into liposomes so as to selectively destabilize the liposomes in the vicinity of target peptidase-secreting cells, and hence, to deliver the liposomes to...
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6143719 |
Bradykinin analogs as selective thrombin inhibitors
Thrombin-induced and ADP-induced platelet and other cell activation is inhibited without affecting thrombin's other proteolytic activity by administration of a bradykinin sequence related analogous...
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6139862 |
Pharmaceutical dipeptide compositions and methods of use thereof
Methods are provided for the therapy of immunodeficient, immunodepressed or hyperactive immune states and for the prevention and treatment of opportunistic infections in such states comprising...
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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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6133233 |
Peptide modulation of reperfusion injury
An in vivo method of reducing reperfusion injury in a mammal resulting from reperfusion of a temporarily occluded blood vessel which comprises the steps of administering into the mammal's...
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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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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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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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6107281 |
Compounds and their combinations for the treatment of influenza infection
Administration of one or more of glutathione, its disulfide dimer, ascorbate-2-phosphate, or N-acetyl-L-cysteine, with or without antioxidants, is suitable for the treatment of influenza virus...
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6107329 |
Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
Compounds of Formula (1) wherein R 6 is carboxy, (C 1 -C 8 )alkoxycarbonyl, benzyloxycarbonyl, C(O)NR 8 R 9 or C(O)R 12 as glucogen phosphorylase inhibitors, pharmaceutical compositions...
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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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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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6096710 |
Collagen-like peptoid residue-containing structures
Synthetic collagen in triple helical conformation and comprising amino acid chains of repeating trimers of highly populated collagen sequences as well as those sequences wherein the proline or...
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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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6096709 |
Use of angiotensin II fragments and analogs thereof in tissue repair
Angiotensin II fragments and analogs thereof are useful in accelerating wound healing. These compounds form the basis of compositions useful for accelerating wound healing, in which the active...
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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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6090782 |
Hemoglobin alpha and beta chain peptide fragments useful for inhibiting stem cell proliferation
Disclosed and claimed are methods for the isolation and use of stem cell inhibiting factors for regulating the abnormal stem cell cycle and for accelerating the post-chemotherapy peripheral blood...
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6087325 |
Peptide-lipid conjugates
Peptide-lipid conjugates are incorporated into liposomes so as to selectively destabilize the liposomes in the vicinity of target peptidase-secreting cells, and hence, to deliver the liposomes to...
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6086878 |
Method of increasing muscle protein and reducing fat in animals
The invention is directed to a method and food product for achieving at least one of the following: increasing muscle protein or reducing fat in an animal. The method comprises administering to the...
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6083917 |
Methods and compositions for the identification, characterization and inhibition of farnesyltransferase
Disclosed are methods and compositions for the identification, characterization and inhibition of mammalian protein farnesyltransferases, enzymes involved in the farnesylation of various cellular...
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6057295 |
Oligopeptides derived from C-reactive protein fragments
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6048854 |
2,3-diaminopropionic acid derivative
The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful...
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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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6046167 |
Peptide YY analogs
The invention provides analogs of PYY. The invention also provides compositions and methods useful for controlling biological activities such as cell proliferation, nutrient transport, lipolysis,...
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