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6916905 |
Dmt-Tic di-and tri-peptidic derivatives and related compositions and methods of use
A compound of formula:
wherein X is a spacer comprising one or more amino acid residues and Y comprises an aromatic group and related compositions and methods of use.
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6911526 |
Compounds that inhibit the interaction between signal-transducing proteins and the GLGF (PDZ/DHR) domain and uses thereof
This invention provides for a composition capable of inhibiting specific binding between a signal-transducing protein and a cytoplasmic protein. This invention also provides a method of identifying...
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6881719 |
β-turn peptidomimetic cyclic compounds
Proteolytically stable small molecule β-turn peptidomimetic compounds have been identified as agonists or antagonists of neurotrophin receptors, such as TrkA. A compound of particular interest...
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6875737 |
Multivalent compounds for crosslinking receptors and uses thereof
Synthetic crosslinking homobivalent and heterobivalent compounds have been designed and developed. These compounds are low in molecular weight, have antagonistic or agonistic activity, and induce...
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6872536 |
Chemotactic peptide antagonists for imaging sites of inflammation
Radiopharmaceuticals comprising molecules that target to N-formyl-methionyl-leucy-phenylalanine (fMLF) receptor on leukocytes in order to target sites of inflammation for diagnostic imaging are...
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6872805 |
Hepatitis C virus inhibitors
The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel...
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6867192 |
Compounds useful in the treatment of inflammatory diseases
There are provided according to the invention, novel compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification, processes for preparing them,...
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6867284 |
Peptide inhibitors of hepatitis C virus NS3 protease
Fluorinated oligopeptides, especially those having 4,4-difluoro-2-amino butyric acid at the C terminus, may be effective inhibitors of hepatitis C virus NS3 protease. Examples of hexapeptides of...
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6858582 |
Composition containing porous microparticle impregnated with biologically-active compound for treatment of infection
Methods and reagents are provided for specifically targeting biologically active compounds such as antiviral and antimicrobial drugs, or prodrugs containing the biologically active compound to...
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6858587 |
Use of tissue factor agonist or tissue factor antagonist for treatment of conditions related to apoptosis
The present invention relates to use of FVII and/or FVIIa and/or another TF agonist and/or FVIIai and/or another TF antagonist in therapeutic treatment of pathological conditions increased or...
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6852697 |
Peptides for treatment of inflammation and shock
Submandibular peptides have been isolated and characterized and provide pharmaceutical compositions for the treatment or prevention of anaphylactic reactions, endotoxic reactions and SIRS-induced...
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6849605 |
Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
A novel method of treating and preventing viral infection is provided. In particular a method of blocking viral infection facilitated by a serine proteolytic (SP) activity is disclosed, which...
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6838475 |
Imidazolidinones as NS3-serine protease inhibitors of hepatitis C virus
The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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6838439 |
Heterocytes as inhibitors of leucocyte adhesion and as VLA-4 antagonists
The present invention relates to compounds of the formula I
which are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to...
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6835714 |
Heterocyclic compounds, intermediates thereof and elastase inhibitors
The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active...
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6828417 |
Polypeptide and process for measuring living body components using the same
A living body component in a sample derived from a living body can be rapidly and accurately measured by reacting the sample with a reagent comprising a combined product of an affinity substance...
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6828302 |
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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6825317 |
Cyclic tetrapeptide derivatives and pharmaceutical uses thereof
The present invention provides a cyclic tetrapeptide derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: wherein each of R 21 and R 22 ...
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6824998 |
Compounds and methods for detecting tripeptidyl protease I
The present invention provides compounds useful for the detection of the enzyme tripeptidyl protease I (TPP-1). The invention also provides methods of making such compounds, methods of using such...
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6818617 |
EC-3, an inhibitor of α4β1 and α4β7 integrins
This invention relates to the identification, purification, and characterization of a novel heterodimeric disintegrin, EC-3, from Echis carinatus viper venom. EC-3 inhibits α4 integrins in an...
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6815425 |
Pharmaceutical composition containing pGLU-GLU-PRO-NH2 and method for treating diseases and injuries to the brain, spinal cord and retina using same
A nueroprotectant composition wherein the active ingredient is pGLU-GLU-PRO-NH 2 or a combination of pGLU-GLU-PRO-NH 2 (EEP) and N-tert-Butyl-α-(2-sulfophenyl)nitrone (SPBN) or other nitrone. A...
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6812208 |
Methods to improve neural outcome
A method for treatment or prophylaxis of a patient suffering from functional symptoms of Parkinson's disease, especially as a consequence of damage to dopaminergic neurons, by administering to the...
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6811996 |
DDS compounds and method for assaying the same
A drug delivery system compound comprising a carboxy(C 1-4 )alkyldextran polyalcohol modified with a saccharide compound and a residue of drug compound bound to the carboxy(C 1-4 )alkyldextran...
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6803044 |
Antimicrobial and anti-inflammatory peptides for use in human immunodeficiency virus
The present invention is directed to a method and pharmaceuticals for treating HIV and secondary infection. One aspect of this invention involves the use of one or more polypeptides with an amino...
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6803370 |
Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such...
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6803466 |
HIV/FIV protease inhibitors having a small P3 residue
With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective...
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6797700 |
Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
The present invention relates to peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated...
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6794365 |
Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
The present invention relates to new malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula...
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6794492 |
Perfluoroalkyl compounds and their methods of use and manufacture
Fluorinated alkyl compounds may be used as reaction intermediates or reaction products in polymerizing amino acid structures into peptides. Fluorinated methyl groups have been found to be...
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6780848 |
Use of GPE to protect glial cells or non-dopaminergic cells from death from neural injury or disease
The tripeptide glycine-proline-glutamine (GPE) may be administered before, or usually after, injury to reduce damage to the central nervous system. GPE appears useful for neuronal rescue...
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6774212 |
Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
The present invention relates to ketoamide and ketoester compounds of Formula (I): wherein W is —NH— or —O—, or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically...
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6770627 |
Piperizine-4-phenyl derivatives as inhibitors of the interaction between mdm2 and p 53
A compound of formula (1), wherein: R 5 is hydrogen, C 1-4 alkyl, R 6 CH 2 — or R 6 C(O)—; R 6 is aryl, heteroaryl, heterocyclyl, aminoC 3-6 alkyl, N-(C 1-4 alkyl)aminoC 3-6 alkyl, NN-(diC...
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6767991 |
Hepatitis C inhibitor peptides
Disclosed herein are hepatitis C viral protease inhibitors of formula (I): wherein a is 0 or 1 ; b is 0 or 1 ; Y is H or C 1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative;...
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6767992 |
Method for producing L-prolyl-L-M-sarcolysyl-L-p-fluorophenylalanine and derivatives thereof
L-prolyl-L-m-sarcolysyl-L-p-fluorophenylalanine, lower alkyl esters and/or acid addition salts thereof are produced. For this purpose, L-p-fluorophenylalanine with a protected carboxyl group is...
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6762166 |
Synthetic complementary peptides and ophthalmologic uses thereof
The present invention is directed to a series of complementary peptides for the pro-gly-pro sequence as antagonists of polymorphonuclear leukocyte chemoattractants. Also provided are applications...
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6759509 |
Branched peptide linkers
Conjugates containing a targeting ligand, such as an antibody, a therapeutically active drug and a branched peptide linker. The branched peptide linker contains two or more amino acid moieties that...
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6753409 |
STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-&lsqb N-&lsqb N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL&rsqb ASPARTYL&rsqb -L-β-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES
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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6753410 |
Investigational compounds
The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or...
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6753316 |
Acryloyl derivatives analogous to distamycin, process for preparing them, and their use as antitumor agents
Compounds which are acryloyl substituted distamycin derivatives of formula (I) wherein: n is 2, 3 or 4; m is 1 or 2; X and Y are the same or different and are selected, independently for each...
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6720306 |
Tetrapartate prodrugs
A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L 1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be...
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6693072 |
Elastase inhibitors
This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P 2 moiety is substituted...
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6693167 |
Peptide-based gemini compounds
New peptide-based Gemini compounds comprising two linked chains (a) each having: (1) a positively charged hydrophilic head, Q 1 or Q 2 formed from one or more amino acids and/or amines, (2) a...
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6693168 |
Chiral cyanoamines and methods of preparation
Methods for preparing chiral non-racemic cyanoamines are provided. The methods are useful, e.g., for preparing chiral amino acids.
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6686335 |
Hydroxamate-containing cysteine and serine protease inhibitors
The present invention is directed to hydroxamate-containing inhibitors of cysteine and serine proteases. Methods for the use of the protease inhibitors are also described.
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6686336 |
N-terminal D(-)-penicillamine peptides as aldehyde sequestration agents
The invention provides a compound of formula I: wherein R 1 -R 3 have any of the values described in the specification; or a salt thereof. The compounds are useful as aldehyde sequestration...
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6683055 |
Low molecular weight inhibitors of complement proteases
Peptide substances, their preparation and their use as complement inhibitors are described. These are in particular substances having a guanidine or amidine radical as a terminal group. In...
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6683154 |
Antimicrobial compositions containing β-amino acid oligomers
Disclosed are antimicrobial compositions containing β-peptides and methods of inhibiting microbial growth in mammals using the compositions. The β-peptides present in the compositions contain...
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6683054 |
Use of melagatran
According to the invention there is provided the use of melagatran, or a pharmaceutically acceptable derivative or prodrug thereof, in the manufacture of a medicament for the treatment of...
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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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6660842 |
Ligand/receptor specificity exchangers that redirect antibodies to receptors on a pathogen
The present invention generally relates to compositions and methods for preventing and treating human diseases including, but not limited to, pathogens such as bacteria, yeast, parasites, fungus,...
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