Abstract: A formulation containing a biologically active compound having a structure with hydrogen bonding sites blended with a first polymer having a structure with complementary hydrogen bonding sites and a second polymer that degrades to form degradation products that promote the release of the active compound from the first polymer.
Abstract: The present invention is related to novel bioactive pentapeptides, pentarphins, the main indication of which is enhancing phagocytic activity of macrophages against microbes. In particular, the cyclopentapeptide, cyclo(Val-Lys-Gly-Phe-Tyr), termed cyclopeptarphin, was 100 times more active than tuftsin. Cyclopentarphin was non-toxic even at concentrations 1000 times higher than the minimum active dose, while being non-immunogenic. Furthermore, cyclopentarphin is more stable to enzymatic cleavage in vitro as compared to linear pentarphin and tuftsin and, hence, its life span in vivo is also larger than that of linear peptides. High efficacy and safety of cyclopentarphin enable elaboration of novel drugs that enhance the resistance of human and animal organisms to microbes and micro particles.
Type:
Grant
Filed:
January 21, 2003
Date of Patent:
February 5, 2008
Inventors:
Timo Kalevi Korpela, Elena Navalotskaya, Tatiana Zargarova, Vladimir Zavialov
Abstract: Disclosed are novel insecticidal polypeptides, and compositions comprising these polypeptides, peptide fragments thereof, and antibodies specific therefor. Also disclosed are vectors, transformed host cells, and transgenic plants that contain nucleic acid segments that encode the disclosed ?-endotoxin polypeptides. Also disclosed are methods of identifying related polypeptides and polynucleotides, methods of making and using transgenic cells comprising these polynucleotide sequences, as well as methods for controlling an insect population, such as Colorado potato beetle, southern corn rootworm and western corn rootworm, and for conferring to a plant resistance to a target insect species.
Type:
Grant
Filed:
July 12, 2006
Date of Patent:
January 22, 2008
Assignee:
Monsanto Technology LLC
Inventors:
Mark J. Rupar, William P. Donovan, Chih-Rei Chu, Elizabeth Pease, Yuping Tan, Annette C. Slaney, Thomas M. Malvar, James A. Baum
Abstract: 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 and non-immunogenic, polymeric conjugate group. The conjugates exhibit an excellent macrophage stimulant action and do not require addition solutizing. They can be used in a wide range of applications, in particular for stimulating macrophages, for stimulating antibody synthesis, for combating infection, as an immunostimulant, in particular in relation to tumors, for preventing and treating septicaemic shock, for would healing and as an adjuvant for vaccines.
Type:
Grant
Filed:
July 18, 2003
Date of Patent:
January 8, 2008
Assignee:
GBF Gesellschaft fur Biotechnologische Forschung mbH
Abstract: The present invention relates to cyclic peptides as inhibitors of urokinase binding to the urokinase receptor. Said cyclic peptides are suitable as pharmaceutical active substances for disorders mediated by urokinase and its receptor.
Type:
Grant
Filed:
December 30, 2005
Date of Patent:
January 1, 2008
Assignee:
Wilex AG
Inventors:
Olaf Wilhelm, Horst Kessler, Markus Buergle, Nils Potthoff, Niko Schmiedeberg
Abstract: The present invention features truncated MCH analogs active at the melanin concentrating hormone type 2 receptor (MCH-2R) and uses of such analogs. Truncated MCH analogs described herein include those active at MCH-2R and MCH-1R, and those selectively active at MCH-2R. MCH-2R analogs have a variety of different uses including being used as a research tool and being used therapeutically.
Abstract: Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and/or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).
Type:
Grant
Filed:
July 29, 2004
Date of Patent:
December 25, 2007
Assignee:
Arizona Biomedical Research Commission
Inventors:
Seth D. Rose, Karl J. Okolotowicz, Rosemarie F. Hartman, Jason Houtchens
Abstract: Provided are excellent ?-secretase inhibitors, that is, compounds represented by the general formula (1) or prodrugs thereof: wherein A is amino or protected amino; B1 and B2 are each a single bond, alkylene of 1 to 3 carbon atoms, or the like; D is a single bond, —NHCO, or the like; E is —COOH, tetrazole ring, or the like; n is an integer of 1 to 3; m is an integer of 1 to 3; G is hydroxyl, a group represented by the general formula (2), or the like: in which Z is —NH, -Asp-Ala-NH—, -Asp-Ala-, -Asp-NH—, or the like; L is a 5-to 10-membered ring optionally containing a heteroatom and/or unsaturated bond; X is —COOH, tetrazole ring, or the like; Y is hydrogen, —COOH, or the like; and k is an integer of 1 to 4; and R1, R2, and R3 are each alkyl of 1 to 6 carbon atoms, or the like.
Abstract: The present invention relates to the utilization of peptide analogues of thymulin that are inactive relative to the immune system, not comprising zinc and having anti-pain activity, for manufacturing a medicine for the treatment of pain.
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
December 18, 2007
Assignees:
Centre National de la Recherche Scientifique, Institut National de la Sante et de la Recherche Medicale (INSERM)
Abstract: A composition comprising from about 0.001% to about 0.4% cyclosporin A, a surfactant, and an oil having a specific gravity from 0.8 to 0.95 is disclosed herein.
Type:
Grant
Filed:
July 13, 2005
Date of Patent:
November 20, 2007
Assignee:
Allergan, Inc.
Inventors:
James N. Chang, Orest Olejnik, Bruce A. Firestone
Abstract: The present invention relates to a process for producing efficiently glutamic acid derivatives (including salts thereof) such as monatin by converting a substituted ?-keto acid of formula (1) into a glutamic acid derivative of formula (2) in the presence of an enzyme catalyzing conversion of the same
Abstract: A pharmaceutical composition includes a physiologically active conjugate including a Thymosin alpha 1 (TA1) peptide conjugated to a material which increases half-life of the TA1 peptide in serum of a patient when the conjugate is administered to a patient. The material may be a substantially non-antigenic polymer. In a method of the invention, the substantially non-antigenic polymer is conjugated to a TA1 peptide. Compositions according to the invention are administered to patients in need of immune stimulation.
Abstract: Agonist polypeptide of a receptor protein has been identified. The agonist can be used to facilitate drug and antigen absorption. Suitable routes of administration include oral, nasal, transdermal, and intravenous. Pharmaceutical formulations may comprise a therapeutic agent or an immunogenic agent in combination with the agonist polypeptide.
Abstract: The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial infections and for treating disorders caused by bacterial infections. The present subject matter also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial infections by administering such compounds. The present subject matter also relates to methods of preparing such compounds.
Type:
Grant
Filed:
October 31, 2005
Date of Patent:
November 13, 2007
Assignee:
Array BioPharma, Inc.
Inventors:
Joseph P. Lyssikatos, Steven Mark Wenglowsky
Abstract: The instant invention is directed toward a dermal delivery system composition comprising an aqueous base vehicle including Emu oil, at least one fatty acid alkyl ester, polyethylene glycol, and a gelling agent, in combination with a therapeutically effective amount of at least one species of insulin, and to processes for the manufacture and use thereof.
Abstract: A GLP-1 derivative is provided including an amino acid sequence of GLP-1 (7-35) having deletion, substitution and/or addition of one or more amino acids and having Waa-(Xaa)n-Yaa (in which Waa is Arg or Lys, Xaa is Arg or Lys, n is an integer of 0 to 14, and Yaa is Arg, Arg-NH2, Lys, Lys-NH2 or Hse) added to the C-terminus of the peptide having a GLP-1 activity. These derivatives are highly absorbable via a mucous membrane. The GLP-1 derivative can be conferred with resistance to dipeptidyl peptidase IV by substituting amino acid 8 in its GLP-1 amino acid sequence with Ser, or with resistance to trypsin by substituting amino acids 26 and 34 with Gln and Asn, respectively. The absorption efficiency of the GLP-1 derivatives via mucous membranes can be further improved by preparing a composition using a charge-regulated fat emulsion regulated to be negatively charged thereon.
Abstract: New methods for the treatment of cancer are provided. Null IGF (IGF variants with reduced receptor binding) is administered to subjects having cancer, thereby alleviating the symptoms of the cancer.
Abstract: Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
October 30, 2007
Assignee:
The Trustees of the University of Pennsylvania
Inventors:
Mark I. Greene, Ramachandran Murali, Akihiro Hasegawa
Abstract: A composition is provided to heal burns, wounds and other skin traumas of mammals. The composition is useful to treat sepsis and to improve skin formation as well. The composition comprises an antimicrobial peptide having amino acid sequence FAKKFAKKFKKFAKKFAKFAFAF.