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6844318 |
Peptidase-cleavable, targeted antineoplastic drugs and their therapeutic use
This invention is directed to antineoplastic agents conjugated to enzyme-cleavable peptides comprising the amino acid recognition sequence of a membrane-bound and/or cell-secreted peptidase, and to...
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6841533 |
Conformationally constrained backbone cyclized interleukin-6 antagonists
Novel peptides which are conformationally constrained backbone cyclized antagonists of IL-6, are disclosed. Methods for synthesizing the IL-6 antagonists are also disclosed. Furthermore,...
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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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6838432 |
Treatment of sepsis with TAFI
A method for inhibiting and for reversing the dysfunctional response of vascular endothelial cells to an inflammatory stimulus in a subject in need of such therapy has been developed in which an...
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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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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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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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6815414 |
Pharmaceutical compositions for the treatment of helicobacter pylori-associated disorders
The invention relates to pharmaceutical compositions and methods for treating and/or preventing Helicobacter pylori -associated disorders, particularly disorders of the gastrointestinal tract. The...
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6815426 |
Angiogenesis-inhibitory tripeptides, compositions and their methods of use
This invention pertains to methods and compositions for inhibiting endothelial cell tube formation, the initial step of tumor angiogenesis. More specifically, the present invention relates to...
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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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6812212 |
Assessment of oxidant stress in vitro and in vivo
There is provided a method of assessing oxidant stress by measuring polymerization of proteins. Also provided is a marker for oxidant stress which includes a polymerized protein. A kit for use in...
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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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6803046 |
Sincalide formulations
The invention features sincalide formulations that include an effective amount of sincalide, a bulking agent/tonicity adjuster, a stabilizer, a surfactant, a chelator, and a buffer. The invention...
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6800086 |
Reduced fluence rate PDT
The invention relates to the use of reduced fluence rate PDT to treat neovasculature, particularly choroidal neovasculature (CNV). Reduced fluence rate PDT decreases the likelihood of molecular...
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6800611 |
Metastin derivatives and their use
The invention relates to metastin derivatives represented by the formula: X-AA 1 -AA 2 -AA 3 -AA 4 -Z (I), or a salt thereof, or a pro-drug thereof, which have cancer metastatis suppressing...
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6800612 |
S-nitrosothiols as agents for the treatment of circulatory dysfunctions
The present invention is directed to a S-nitrosothiol derivative of penicillamine or glutathione, of formula I: or its pharmaceutically acceptable salt thereof, in which: A and B are...
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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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6797698 |
Method of treating prolonged critical illness and other conditions having a similar neuroendocrine pattern
A method of treating a subject suffering from a condition involving a blunted anterior pituitary hormone pattern in which Thyroid Releasing-Hormone (TRH) and Growth Hormone-Releasing Peptide (GHRP)...
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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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6794362 |
Asparagine containing elastin peptide analogs
The present invention is directed to a composition which is used to enhance the elasticity and/or appearance of tissue. Specifically, the present invention is directed to a composition formulated...
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6787519 |
Methods of treating disorders related to apoE
The present invention provides methods inhibiting formation of neurofibrillary tangles; and methods for treating disorders relating to apolipoprotein E (apoE) in a subject. The methods generally...
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6784155 |
Inhibitor and stimulator of stem cell proliferation and uses thereof
Disclosed and claimed are methods for the isolation and use of stem cell modulating factors for regulating stem cell cycle and for accelerating the post-chemotherapy peripheral blood cell recovery....
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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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6777389 |
Cosmetic or dermatological use of 7-hydroxylated steroids in combination with elastin derived peptides
The present invention is directed to a composition and method for enhancing the appearance of skin or tissue. The invention is preferably a combination of elastin-derived peptides and steroidal...
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6776984 |
Induced regeneration and repair of damaged neurons and nerve axon myelin
A method of treatment of and composition for human degenerative neurologic diseases discloses the administration of therapeutically amounts of an enhancement agent, such as thrombopoietin, to...
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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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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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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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6737409 |
Dolastatin 10 derivatives
Novel anti-tumor compounds of formula, are disclosed. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), the use of compounds of formula (I) for the treatment of...
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6730660 |
Peritoneal dialysis solutions with polypeptides
The present invention provides an improved dialysis solution. The improved dialysis solution provides for the use of specific polypeptides as an osmotic agent with an additional osmotic agent such...
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6727227 |
Tetrapetide revealing geroprotective effect, pharmacological substance on its basis, and the method of its application
Tetrapeptide L-alanyl-L-glutamyl-L-aspartyl-glycine (SEQ ID NO: 1) of the general formula L-Ala-L-Glu-L-Asp-Gly (SEQ ID NO: 1) is proposed as a biologically active compound with a geroprotective...
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6723703 |
Therapeutic use of aerosolized S-nitrosoglutathione in cystic fibrosis
The present invention is directed to the treatment of cystic fibrosis that involves the administration of a nitrosylating agent, such as S-nitrosoglutathione or ethyl nitrite.
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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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6716818 |
Caspase inhibitors and the use thereof
The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R 1 -R 3 , X and Y are defined herein. The present invention also relates to the...
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6713443 |
Compounds which modify serotoninergic transmission, diagnostic and therapeutic applications
Compounds having the following peptide sequence: X Leu Y, wherein X is H or Ala or Leu-Ser-Ala, Y is OH or peptide sequence having from 1 to 10 amino acids, with the terminal carboxy end being...
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6699838 |
Antiangiogenic peptides
Mammalian kringle 5 fragments and kringle 5 fusion proteins are disclosed as a compounds for treating angiogenic diseases. Methods and compositions for inhibiting angiogenic diseases are also...
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6699835 |
Formulation of boronic acid compounds
The invention relates to the formulation of pharmaceutical compounds. More particularly, the invention provides stable, pharmaceutically acceptable compositions prepared from boronic acid compounds...
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6692753 |
Potentiation of the immune response
A method for stimulating proliferation of T-cells containing cytoplasmic post-prolyl dipeptidase activity; the method, in one aspect, involves contacting the T-cells with an organic compound at a...
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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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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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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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6664231 |
Anti-fungal peptides
The present invention relates generally to anti-fungal peptides derived from or based on Domain III (amino acids 142-169) of bactericidal/permeability-increasing protein (BPI) and in vivo or in...
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6664233 |
Combination therapy including 9-nitro-20(S)-camptothecin and bleomycin
A method for treating a patient having a disease associated with undesirable or uncontrolled cell proliferation such as cancer and restenosis is provided. The method comprises: delivering to the...
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6656911 |
Serine protease inhibitors
The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for...
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6656905 |
Cyclic tetrapeptide compound and use thereof
A cyclic tetrapeptide compound and use thereof. Especially, a compound WF27082, a process for production of the compound by culturing, in a nutrient medium, a WF27082-producing strain belonging to...
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6649587 |
Polyamine analog conjugates and quinone conjugates as therapies for cancers and prostate diseases
Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as...
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