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7335644 |
Anti-hypertensive molecules and process for preparation thereof
The present invention relates to novel anti-hypertensive molecules. The present invention also provides a process for the preparation of novel antihypertensive molecules. The present invention...
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7335645 |
Effectors of dipeptidyl peptidase IV for topical use
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula
wherein
A is an amino acid having at least one functional...
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7323447 |
Hepatitis C virus inhibitors
The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which inhibit the function of the NS3 protease (also referred to herein as “serine...
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7323448 |
Antibacterial agents
Compounds of formula (I) or a pharmaceutically or veterinarily acceptable salts thereof
wherein R 1 represents hydrogen, C 1 -C 6 alkyl or C 1 -C 6 alkyl substituted by one or more halogen...
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7320960 |
Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7320961 |
Method for treating a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate
The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1...
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7316996 |
Bisacyloxypropylcysteine conjugates and the use thereof
The invention provides lipopeptide conjugates in which a cysteine that is double-substituted by a fatty acid is bonded by means of the carboxyl group to a highly soluble, physiologically compatible...
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7297681 |
Growth hormone secretagogues
The invention relates to compounds of formula I
which are useful for elevating the plasma level of growth hormone in a mammal as well as for the treatment of growth hormone secretion...
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7291599 |
Use of inhibitors of enzymes having activities of amino peptidase N and/or dipeptidyl peptidase IV and of pharmaceutical preparations thereof for a therapy and prevention of chronical neurodegenerative diseases
The invention relates to a process for the treatment of neurodegenerative diseases wherein mis-folded proteins accumulate in characteristic lesions and contribute substantially to a pathogenesis...
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7288526 |
Dipeptide and related compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7288527 |
Inhibition of allergic contact dermatitis by N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester
It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) and/or one of its lower alkyl derivatives can be used to treat allergic contact dermatitis associated with...
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7288525 |
Method for lowering serum homocysteine
The present invention provides a method for reducing the amount of homocysteine in the blood of an individual. The method comprises administering to the individual a composition comprising a...
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7285525 |
Suppression of immune response via inhibition of cathepsin S
Methods and products for suppressing a class II MI-IC-restricted immune response in a mammal, or in mammalian cells, are described. The methods depend upon inhibiting invariant chain proteolysis by...
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7282484 |
Anti-tumor agents
A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula I, to...
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7276484 |
Dipeptide inhibitors of β-secretase
Dipeptide derived inhibitors of the β-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of Aβ peptide in a...
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7271152 |
Compounds and methods for the modulation of CD154
The present invention relates to compounds that are capable of modulating CD154 mobilization and that are useful for stabilizing the thrombotic process and reducing the activation of cells involved...
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7265118 |
Regulation of substrate activity
A method for regulating substrate activity in vivo is useful for the treatment of medical disorders such as inflammation, arteriolosclerosis and angiogenesis. The method involves the administration...
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7262170 |
Pharmaceutical composition for reducing vaginal acidity and treatment of vaginitis, and the use thereof
A composition is disclosed for treating a patient suffering from abnormally high acidity in the vagina, wherein the vaginal pH value is lower than 4.0. The composition consists essentially of: (a)...
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7250401 |
Therapeutic compositions
A method is provided for the preparation of compounds of the formula (R 1 )(R 2 )NC(═X)S(O) n R 3 or (R 1 )(R 2 )NC(═X)OS(O) n R 3 , wherein R 1 , R 2 and R 3 , X and n have any of the...
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7244711 |
Association of calpain inhibitors and reactive oxygen species trapping agents
The invention concerns a pharmaceutical composition comprising, as active principle, at least a calpain inhibiting substance and at least a substance trapping reactive oxygen species (ROS), and...
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7241796 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering...
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7232803 |
Antimicrobial compounds and formulations
The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having...
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7229969 |
Combinations of enzyme inhibitors and the use thereof
Combination of inhibitors of dipeptidyl peptidase IV (DP IV) and enzymes having the same substrate specificity (DP IV-analogous enzymatic activity) and inhibitors of alanyl aminopeptidase...
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7217695 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Peptidomimetic inhibitors of post-proline cleaving enzymes
The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using...
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7214664 |
Peptidyl prodrugs that resist P-glycoprotein mediated drug efflux
Dipeptide, and tripeptide and tetrapeptide ester derivatives of bioactive agents are provided wherein the parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful...
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7208171 |
Injectable and bioadhesive polymeric hydrogels as well as related methods of enzymatic preparation
The invention is related to biomimetic gels that are prepared enzymatically, using a transglutaminase to cross-link polymer-peptide conjugates of rational design.
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7186695 |
Treatment of arthritis with arsenoxide compounds
The present invention provides a method of treatment and/or prophylaxis of arthritis in a vertebrate comprising administering to said vertebrate in need of said treatment and/or prophylaxis a...
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7183252 |
Indole peptidomimetics as thrombin receptor antagonists
The invention is directed to novel indole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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7183260 |
C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to...
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7179792 |
Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least one other active ingredient and the use of the product
The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I
in which the radicals have the meanings defined herein, or a pharmaceutically acceptable salt or...
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7176185 |
Short peptide carrier system for cellular delivery of agent
A dipeptide or tripeptide carrier system for active agent delivery to cells has an N-terminus natural amino acid and an active agent covalently bonded to a side chain of one of the remaining amino...
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7173013 |
Treatment of tuberculosis using immunomodulator compounds
Tuberculosis in an animal is treated by administration of a therapeutically effective amount of an immunomodulator of formula A. In formula (A), n is 1 or 2, R is hydrogen, acyl, alkyl or a peptide...
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7169752 |
Compounds and compositions for prevention of overdose of oxycodone
The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to an opioid such as oxycodone in a manner that substantially decreases the potential of...
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7166580 |
Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7166579 |
Prodrugs of DP IV-inhibitors
Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds...
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7163921 |
Peptide derivatives and medicinal compositions
The present invention to novel nociceptin receptor agonists which are peptide derivatives represented by the following general formula (1):
(in which A is alkylene, —CH 2 ) n CO— or a...
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7163923 |
Peptide deformylase activated prodrugs
This invention provides a method for inhibiting the growth of a microorganism that expresses Peptide Deformylase by contacting the microorganism with an effective amount of the compound described...
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7157430 |
(Substituted)acyl dipeptidyl inhibitors of the ICE/CED-3 family of cysteine proteases
This invention is directed to novel (substituted) acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as...
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7153835 |
Anti-inflammatory peptides
Methods for inhibiting an inflammatory reaction in a mammal and pharmaceutical compositions are provided. The methods comprise administering to the mammal an effective amount of a peptide of the...
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7151088 |
Neuroprotective dietary supplement
The invention relates to a novel dietary supplement mixture having improved neuroprotective activity and preventing, ameliorating or counteracting neurodegeneration and preventing, counteracting...
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7148199 |
Arginyl-glutamine dipeptide for treatment of pathological vascular proliferation
The subject invention provides dipeptides useful in preventing pathological proliferation of blood vessels. The dipeptides of the subject invention are particularly advantageous because they are...
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7148198 |
Antibacterial agents
A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme:
wherein A represents a group of formula (IA) or...
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7144866 |
Avermectin derivatives
Provided is a compound represented by the general formula (I) or a salt thereof:
wherein, —X Y— represents —CH═CH— and the like, between R 2 and the carbon atom at 5-position...
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7144854 |
Long lasting anti-angiogenic peptides
Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly...
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7144865 |
Compositions and methods for treating obesity
The present invention relates to dietary supplementing methods useful for controlling obesity. More particularly, the invention relates to methods of administration of compositions containing...
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7144856 |
Inhibitors of dipeptidyl peptidase I
The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I)which can be used in the treatment of malignant cell degeneration, immune diseases...
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7132392 |
Inhibition of cell motility and angiogenesis by inhibitors of Grb2-SH2-domain
Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by...
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7132104 |
Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders
The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression,...
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7125872 |
β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are...
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7122335 |
Compounds and methods to enhance rAAV transduction
Agents and methods to alter rAAV transduction, including agents and methods to enhance rAAV transduction, are provided. For instance, the invention provides methods to identify agents that enhance...
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