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7619110 |
Amino acid derived prodrugs of propofol, compositions, uses and crystalline forms thereof
The present invention provides a prodrug of propofol and crystalline forms thereof, methods of making the propofol prodrug and crystalline forms thereof, pharmaceutical compositions of the propofol...
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7611711 |
VEGFR-3 inhibitor materials and methods
The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated...
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7608592 |
HCV inhibitors
The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating...
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7608590 |
HCV NS-3 serine protease inhibitors
Compounds of the formula
where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage...
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7589233 |
L-Threonine derivatives of high therapeutic index
The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the...
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7589066 |
Potent and specific immunoproteasome inhibitors
Compounds and methods of selectively inhibiting an immunoproteasome are described. Also described are methods of treating a cancer, an inflammation, and/or an autoimmune disease and methods of...
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7589065 |
Catalysis of the cis/trans-isomerisation of secondary amide peptide compounds
The present invention is based on the finding that the cis/trans isomerisation of secondary amide peptide bonds in oligo- and polypeptides can be catalytically promoted. This catalysis is effected...
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7585846 |
Compounds for delivering amino acids or peptides with antioxidant activity into mitochondria and use thereof
Disclosed are hydrophilic choline/N-heterocycle ester compounds containing single amino acids, peptides, or derivatives thereof which have the potential to express anti-oxidant activity capable of...
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7579323 |
Hemiasterlin analogs
This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as cytotoxic and anti-mitotic agents.
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7579319 |
Methods for improving the structure and function of arterioles
The present invention relates to the unexpected finding that vessels smaller than even the smallest arteries (i.e. arterioles) thicken, become dysfunctional and cause end organ damage to tissues as...
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7576062 |
Compounds with growth hormone releasing properties
Disclosed are compounds of formula I
wherein R 1 , R 2 , R 5 , R 6 , R 7 , R 8 , G, J, L, M, a, b, c, d, e, and f are as defined in the specification, and compositions containing them. These...
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7553816 |
p-amidobenzylethers in drug delivery agents
Compounds of the formulas
L A n -Z-X—W w D and B Z-X—W w D
wherein: D is...
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7550559 |
Acylsulfonamide compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7544662 |
Polypeptides useful for appetite suppression
The present invention relates to polypeptides obtained from bear derivative isolate which are useful in suppressing appetite. The polypeptides of the present invention are most preferably between...
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7531517 |
Inhibitors of cancer cell, T-cell and keratinocyte proliferation
The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof,
wherein
Y is —NR a R b , —NR c C═ONR a R b, —NR c C═SNR a...
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7521427 |
Peptidyl allyl sulfones
The present disclosure provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the disclosure...
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7514409 |
VLA-4 antagonists
Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated...
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7511039 |
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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7504383 |
Peptide nanostructures encapsulating a foreign material and method of manufacturing same
A composition comprising a material at least partially enclosed by a tubular, spherical or planar nanostructure composed of a plurality of peptides, wherein each of the plurality of peptides...
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7504382 |
Protease inhibitors for coronaviruses and SARS-CoV and the use thereof
Disclosed are protease inhibitors for coronaviruses and SARS-CoV, or picornaviruses, and the use of these protease inhibitors for preventing, reducing, ameliorating and treating a disease or...
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7498406 |
Substantially cell membrane impermeable compound and use thereof
The present invention relates to a compound according to Formula (I): A-(L-Y) p , wherein A comprises at least one substantially cell- membrane impermeable pendant group; L comprises any suitable...
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7491705 |
Alpha-ketoamide derivative, and production method and use thereof
The present invention provides a compound represented by the formula (I):
(wherein
R 1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R...
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7485626 |
Combinations of enzyme inhibitor-containing preparations and the use thereof
The invention comprises a process wherein the DNA synthesis and, thus, the proliferation of mononuclear cells (MNZ) and of T cells as well is inhibited by the simultaneous and combined inhibition...
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7482024 |
Compositions comprising an active agent
The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention...
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7470783 |
Photocleavable protecting groups and methods for their use
Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally...
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7470664 |
HCV NS3 protease inhibitors
The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or...
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7468421 |
Depilatories and agents for external use
This invention relates to depilatories and external preparations, each of which contains endothelin or its agonist, and also to a depilating method characterized by administering endothelin or its...
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7465710 |
Compounds for control of appetite, blood pressure, cardiovascular response, libido, and circadian rhythm
This invention relates generally to dipeptides and tripeptides and to methods for pharmaceutical treatment of mammals using analogs of such dipeptides and tripeptides. More specifically, the...
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7462599 |
Use of effectors of glutaminyl and glutamate cyclases
The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions...
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7459428 |
Method of regulating glucose metabolism, and reagents related thereto
One aspect of the present invention relates to a method for treating Type II diabetes in an animal, comprising conjointly administering to the animal metformin and an inhibitor of...
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7455840 |
Compositions and methods to reduce mutagenesis
The present invention provides methods and compositions for said inhibition of drug resistance. In one embodiment, said invention provides methods and compositions for said inhibition of antibiotic...
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7442394 |
Combined effects of nutrients on proliferation of stem cells
A method and composition for stimulating the proliferation and differentiation of stem cells is used to self-repair injury in mammals. A supplement is administered having an effective dose of...
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7435420 |
Dipeptidyl peptidase IV inhibitors for the treatment of anxiety
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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7432301 |
Use of S-nitrosothiol signaling to treat disordered control of breathing
The present invention is directed to a method of treating disordered control of breathing including the treatment of apnea and hypoventilation associated with congenital or acquired brain stem...
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7429565 |
Antiviral phosphonate analogs
The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such...
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7427601 |
Method for treating tremor
The present invention is directed to the use of a class of peptide compounds for treating essential tremor and other tremor syndromes.
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7427600 |
Active agent delivery systems and methods for protecting and administering active agents
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active...
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7423012 |
Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors
The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts,
which compounds inhibit carboxypeptidase U and...
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7417030 |
Indazole peptidomimetics as thrombin receptor antagonists
The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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7417029 |
Prodrug of an ice inhibitor
This invention describes an ICE inhibitor prodrug (I) having good bioavailability
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel...
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7410951 |
Biologically active peptides and compositions, their use
Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I
wherein Y, n, R 1 , R 2 , R 3 , R 7 ,...
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7407938 |
Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
One embodiment of the invention relates to compounds of the formula I,
in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification. Other embodiments of the invention relate...
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7375086 |
Modulators of Nod2 signaling
The present invention relates to intracellular signaling molecules, in particular the Nod2 protein and nucleic acids encoding the Nod2 protein. The present invention provides methods of identifying...
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7375085 |
Melanocyte-stimulating hormone inhibitors
In the present specification is disclosed a melanocyte-stimulating hormone inhibitory composition which comprises, as the active ingredient, a di- or tripeptide derivative having a certain naphthyl...
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7371729 |
Boronic acid salts useful in parenteral formulations
Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH) 2 . The counter-ion to the boronate may be an alkali metal or derived from a strongly basic organic...
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7368421 |
Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in...
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7354905 |
Prodrugs of thrombin inhibitors
There is provided compounds of formula I,
R 1 O(O)C—CH 2 —(R)Cgl-Aze-Pab-R 2 I
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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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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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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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