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7098024 |
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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7098302 |
Binding peptides specific for the extracellular domain of ErbB2 and uses therefor
The invention provides methods and compositions for diagnosing and treating subjects using EBPs. Specifically disclosed are peptides and peptidomimetics that bind selectively to the extracellular...
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7091314 |
Intermediates and methods for making heptapeptide oxytocin analogues
More efficient and/or economical methods for synthesizing heptapeptide alcohol analogs of oxytocin are provided along with novel intermediates which are useful in synthesizing such oxytocin...
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7091311 |
Peptides and compounds that bind to a receptor
Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and...
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7091313 |
Synthesis of template-fixed β-hairpin loop mimetics
Template-fixed β-hairpin loop mimetics comprising a template corresponding to one of the structures (a), (b), (c), (d), (e), (f), (g), (h) and a template-fixed chain of 4 to 20 α-amino acid...
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7083983 |
Inhibitors of the interaction between P53 and MDM2
The present invention relates to compounds capable of binding to the oncogene protein MDM2, processes for the preparation of such compounds, pharmaceutical preparations comprising such compounds,...
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7084244 |
Conformationally constrained backbone cyclized peptide analogs
Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building...
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7074760 |
Polyacid glycopeptide derivatives
Disclosed are derivatives of glycopeptides that are substituted at the C-terminus with a substituent that comprises two or more (e.g. 2, 3, 4, or 5) carboxy (CO 2 H) groups; and pharmaceutical...
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7071162 |
Combined use of cementum attachment protein and cyclosporin a for improved attachment of dental and orthopedic implants
A method is described for inducing the formation of cementum and a periodontal ligament between a dental implant and bone by administering cementum attachment protein (CAP) together with a...
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7067619 |
Integrin-binding peptides
This invention is directed to novel integrin binding peptides. These peptides bind to α v - of α 5 -containing integrins and can exhibit high binding affinity. They contain one of the following...
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7067508 |
Diaminedithiol derivatives and radiorhenium or radiotechnetium complex thereof; a liver cancer-treating composition comprising the radiorhenium complex and lipiodol; and a kit for preparation of the liver cancer-treating composition
The present invention relates to a novel diaminedithiol derivative or a pharmaceutically acceptable salt thereof; radiorhenium or radiotechneticum complex thereof; a composition for treating liver...
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7067620 |
Antibacterial agents
Novel antibacterial agents that act as multibinding agents are disclosed. The compounds of the invention comprise from 2–10 ligands covalently connected, each of said ligands being capable of...
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7064105 |
Deoxo-proline-containing tamandarin and didemnin analogs, dehydro-proline-containing tamandarin and didemnin analogs, and methods of making and using them
The present invention relates to tamandarin and didemnin analogs which have a deoxo-proline residue or a dehydro-proline residue in their structure. These analogs are useful as anti-cancer agents...
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7063842 |
Compounds and methods for inhibiting the interaction between α-catenin and β-catenin
Modulating agents for inhibiting an interaction between α-catenin and β-catenin are provided. The modulating agents comprise one or more of: (a) a β-catenin HAV motif; (b) a peptide analogue or...
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7060672 |
Cyclosporin analog formulations
The present invention relates to formulations containing cyclosporin analogs that are structurally similar to cyclosporin A, in particular isomeric mixtures of cyclosporin analogs that are...
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7056883 |
Therapeutic agent for soft tissue sarcoma
A therapeutic agent for soft tissue sarcoma (particularly synovial sarcoma), contains a histone deacetylase inhibitor (particularly a compound of formula I) as an active ingredient
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7056884 |
Reduced FK228 and use thereof
The present invention relates to reduced FK228 of the formula (I)
wherein R 1 and R 2 are the same or different and each is a hydrogen atom or a thiol-protecting group, or a salt thereof, and...
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7053047 |
Cyclic pentapeptides and their preparation
This invention relates to cyclic peptides, with the following formula (I) (SEQ ID NO: 1),
cyclo(Xaa-Arg-Pro-Ala-Lys) ...
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7053041 |
Methods and compositions useful for inhibition of αvβ5mediated angiogenesis
The present invention describes methods for inhibiting angiogenesis in tissues using vitronectin α v β 5 antagonists. The α v β 5 -mediated angiogenesis is correlated with exposure to...
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7045591 |
Selective cyclic peptides with melanocortin-4 receptor (MC4-R) agonist activity
Peptides cyclized via disulfide or lactam bridges are disclosed. The peptides exhibit melanocortin-4 receptor agonist activity and are useful for treating obesity.
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7045503 |
Radiometal-binding peptide analogues
Novel metal binding ligands are disclosed that may be coupled to peptides for use in methods of diagnosis and therapy. Peptides containing the ligands are produced using a method wherein ligand...
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7045133 |
VEGF-D/VEGF-C/VEGF peptidomimetic inhibitor
Monomeric monocyclic peptide inhibitors and dimeric bicyclic peptide inhibitors based on exposed loop fragments of a growth factor protein, such as loop 1, 2 or 3 of VEGF-D, and methods of making...
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7041637 |
Echinocandin/carbohydrate complexes
A complex of an echinocandin compound with a carbohydrate is described having improved thermal stability and water solubility. A process for making the echinocandin/carbohydrate complex is also...
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7041786 |
Guanylate cyclase receptor agonists for the treatment of tissue inflammation and carcinogenesis
A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide...
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7041784 |
Apoptotic compounds
The invention provides methods and compositions for enhancing apoptosis of pathogenic cells. The general method comprises the of contacting the cells with an effective amount of an AV peptoid,...
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RE39071 |
Anhydro-and isomer-a-21978c cyclic peptides
Two new groups of A-21978C cyclic peptides, anhydro- and isomer-A21978C peptide derivatives, have antibacterial activity and are useful as intermediates. The two groups are prepared via...
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7030213 |
Conformationally stabilized cell adhesion peptides
Novel synthetic Arg-Gly-Asp containing peptides which have high affinity and specificity for their receptors by virtue of restrictions on their stereochemical conformation. Such restrictions can be...
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7026281 |
Antagonistic analogs of GH-RH inhibiting IGF-I and -II
There is provided a novel series of synthetic analogs of hGH-RH(1–29)NH 2 . These analogs inhibit the activity of endogenous hGH-RH, and therefore prevent the release of growth hormone. The...
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7022669 |
Echinocandin derivatives, method for preparing same and application as antifungal agents
A subject of the invention, in all possible isomer forms as well as their mixtures, is the compounds of formula (I):
in which
either R 1 : H or CH 3 and R 2 : cyclohexyl substituted by an...
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7022667 |
O-derivatized nocathiacin derivatives
The present invention provides compounds of formula I
having potent antibiotic activity, including activity towards Gram-positive bacteria and mycobacteria.
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7018981 |
Cyclic motilin receptor antagonists
The present invention aims to provide cyclic peptide derivatives having motilin receptor antagonist activity and are useful as pharmaceuticals. The present invention provides compounds of general...
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7019110 |
Streptogramin derivatives, preparation method and compositions containing same
Group B streptogramin derivatives of general formula (I) are disclosed:
wherein Ra, Rb, Rc, Rd, R 1 , R 2 and Y are as defined in the description, including preparation methods and...
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7018996 |
Antibiotics AW998A, AW998B, AW998C and AW998D
This invention relates to antibiotics selected from the group AW998A, AW998B, AW998C and AW998D derived from the microorganism Streptomyces designated LL-AW998, which are useful as antibacterial...
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7019109 |
SSTR1-selective analogs
Analogs of SRIF which are selective for SSTR1 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR1 and...
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7015196 |
Basic monocyclic compounds having Nk2 antagonist action, processes for their preparation, and formulations containing them
Basic monocyclic compounds having general formula (I) useful as NK-2 antagonists are described, processes for their preparation and pharmaceutical compositions containing them are also described.
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7015305 |
Process for preparing glycopeptide derivatives
Disclosed are processes for preparing glycopeptide antibiotic derivatives having an amino-containing side chain. The multi-step process is conducted in a single reaction vessel without isolation of...
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7012064 |
Cyclosporins for the treatment of immune disorders
The present invention relates to methods of treating or preventing an inflammatory or immune disorder in a subject while eliminating or reducing the toxicity associated with the administration of...
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7005417 |
Echinocandin derivatives, method for preparing same and use as antifungal agents
A subject of the invention is the compounds of formula (I):
in which
either R 1 and R 2 =H, OH, alkyl optionally substituted, or NR 1 form with the carbon carrying NR 1 R 2 a double bond...
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7001883 |
Cyclized conotoxin peptides
This invention relates to cyclized conotoxin peptides, processes for their preparation and their pharmaceutical use.
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6995238 |
Cyclopeptide derivatives
Disclosed herein is a process for promoting the integration of a biocompatible device or implant into a tissue of a subject. The process comprises covalently bonding to the surface of the device or...
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6995139 |
Cyclic undecapeptide pro-drugs and uses thereof
A pro-drug comprising a cyclic undecapeptide wherein the peptide chain thereof comprises at least one amino acid residue, useful as a medicinal product, including use for treatment of pathological...
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6987167 |
Process for production of the somatostatin analog, octreotide
The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc)...
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6984488 |
Determination and control of bimolecular interactions
Methods of using overlapping peptides for the discovery of discontinuous epitopes, as vaccines, for drug design, for diagnostic purposes and for the elucidation of three-dimensional protein...
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6967238 |
Compounds and methods for modulating cell adhesion
Cyclic peptides comprising a cadherin cell adhesion recognition sequence HAV, and compositions comprising such cyclic peptides, are provided. Methods for using such peptides for modulating...
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6964860 |
Glycopeptide antibiotics
The invention provides compounds of formula
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 6c , R 6d , R 6e and R 7 are defined in the specification. These compounds are useful as...
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6962970 |
Glycopeptide derivatives and pharmaceutical compositions containing the same
Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula:
—R a —Y—R b —(Z) x...
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6962969 |
Compounds and methods for modulating nonclassical cadherin-mediated functions
Modulating agents for inhibiting or enhancing nonclassical cadherin mediated cell adhesion are provided. The modulating agents comprise one or more of: (a) a peptide sequence that is at least 50%...
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6960563 |
Spontaneous emulsions containing cyclosporine
A pharmaceutical composition contains cyclosporine as the active ingredient. More specifically, the composition is an orally administered pharmaceutical formulation in the form of a spontaneous...
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6960564 |
Echinocandin pharmaceutical formulations containing micelle-forming surfactants
Pharmaceutical formulations are described comprising an echinocandin compound or echinocandin/carbohydrate complex and a pharmaceutically acceptable micelle-forming surfactant in a non-toxic...
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6960646 |
Cyclic peptides as potent and selective melanocortin-4 receptors agonists
Cyclic peptides of formula I are potent and selective agonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4...
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