Abstract: 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 impaired wound healing and metabolic diseases of humans and are represented by the general formula and the pharmaceutical salts thereof, in which R is a peptide or a branched or unbranched C1–C9 alkyl chain, a branched or unbranched C2–C9 alkenyl chain, a branched or unbranched C2–C9 alkynyl chain, a C3–C9 cycloalkyl, C4–C9 carbocyclic, C5–C14 aryl, C3–C9 heteroaryl, C3–C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
December 5, 2006
Assignee:
Probiodrug AG
Inventors:
Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
Abstract: The present invention is directed to cyclic peptides of formula (I): X-A1-cyclo(D-Cys-A3-A4-Lys-A6-A7)-A8-Y, or a pharmaceutically acceptable salt thereof. The peptides bind selectively to the somatostatin subtype receptor type-5 and elicit an agonist effect from the somatostatin subtype receptors.
Type:
Grant
Filed:
January 4, 2005
Date of Patent:
December 5, 2006
Assignee:
Societe de Conseils de Recherches et d'Applications Scientifiques SAS
Abstract: This invention provides novel peptides that ameliorate one or more symptoms of atherosclerosis. In certain embodiments, the peptide comprises an amino acid sequence that ranges in length from about 10 up to about 30 amino acids, that comprises at least one class A amphipathic helix, that bears at least one protecting group, that protects a phospholipid against oxidation by an oxidizing agent; and that is not the D-18A peptide. The peptides are highly stable and readily administered via an oral route.
Type:
Grant
Filed:
June 28, 2002
Date of Patent:
December 5, 2006
Assignees:
The Regents of the University of California, The University of Alabama Research Foundation
Inventors:
Alan M. Fogelman, Gattadahalli M. Anantharamaiah, Mohamad Navab
Abstract: The present invention relates to stable pharmaceutical protein formulations that are stabilized using peptide stabilizers selected from the group consisting of Gly-Gly, Gly-Gly-Gly, Gly-Tyr, Gly-Phe, Gly-His, Gly-Asp, Gly-Ala, Ala-Gly, Ala-Ala, derivatives thereof and mixtures thereof. Furthermore, the present invention relates to stable pharmaceutical formulations comprising erythropoietin and peptide stabilizers selected from dipeptides, tripeptides, tetrapeptides, pentapeptides, and mixtures thereof. In addition to peptide stabilizers, the formulations may contain surfactants.
Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.
Type:
Grant
Filed:
February 3, 2004
Date of Patent:
November 21, 2006
Assignee:
The Regents of the University of California
Abstract: The present invention provides a rapid and inexpensive method for extractively isolating acidic lipopeptide antibiotics, such as those having a cyclic peptide or cyclic depsipeptide core, in high yield and purity. In particular, there is provided a method of extracting a variety of acidic lipopeptide antibiotics, directly or indirectly, into water immiscible organic solvents by using a divalent cation chelation procedure.
Type:
Grant
Filed:
March 26, 2004
Date of Patent:
November 21, 2006
Assignee:
Migenix Inc.
Inventors:
Donald B. Borders, Noreen D. Francis, Amedeo A. Fantini
Abstract: Novel peptides with antimicrobial activity are disclosed. The novel peptides are octomeric peptides modified from ?-MSH. The modified ?-MSH antimicrobial peptides disclosed herein may have enhanced activity against microbes over ?-MSH due to modifications in peptide sequence and chirality of amino acids. Due an identified mechanism of action for antimicrobial activity in which cAMP accumulates in the microbial cell, it may be that microbes will not generate resistance to these modified ?-MSH antimicrobial peptides.
Abstract: Compositions comprising at least one peptide copper complex and at least one preservative exhibit chemical stability of the peptide copper complex, as well as resistance and/or toxicity to microbial growth, when the preservative is selected to be a non-formaldehyde-donating preservative. In other embodiments, the present invention is directed to such compositions that are formulated for use as pharmaceuticals and cosmetic products, and to medical devices comprising a disclosed composition. In another aspect, the present invention is also directed to a method for imparting to a composition comprising at least one peptide copper complex, chemical stability as well as resistance and/or toxicity to microbial growth, where the method comprises incorporating a non-formaldehyde-donating preservative in the composition.
Abstract: The present invention is for novel compositions and methods for treating cancer, particularly, for treating cancer in mammals and more particularly in humans. The therapeutic compositions of the present invention include liposome entrapped irinotecan in which the liposome can contain any of a variety of neutral or charged liposome-forming compounds and cardiolipin. The liposomes of the present invention can be either multilamellar vesicles and unilamellar vesicles, as desired.
Abstract: A method to prepare new or unexpected polymorphs of materials which have not been observed, or to obtain a known polymorph under different conditions than those in which it is usually made, by using a laser to cause nucleation and crystal growth to occur in a supersaturated solution in such a way as to obtain a crystal structure which would not normally appear without the use of the laser.
Abstract: The present invention relates to methods and compositions for modifying peptides, polypeptides and proteins with polymers, especially glyco-mimetic polymers, so as to improve their biological activity or pharmacokinetic properties. The invention further provides methods and uses for such polymer-modified peptides, polypeptides and proteins. The invention is particularly suitable for use in the synthesis of polymer-modified synthetic bioactive proteins (FIG. 1D), and of pharmaceutical compositions that contain such proteins.
Type:
Grant
Filed:
July 12, 2001
Date of Patent:
October 10, 2006
Assignee:
Amylin Pharmaceuticals, Inc.
Inventors:
Gerd G. Kochendoerfer, Paolo Botti, James A. Bradburne, Shiah-yun Chen, Sonya Cressman, Christie L. Hunter, Stephen B. H. Kent, Donald W. Low, Jill G. Wilken
Abstract: The present invention relates to three single tryptophan analogs ILPWKLPLLPLRR-amide (IL4) (SEQ ID NO: 1), ILPLKLPWLPLRR-amide (IL8) (SEQ ID NO: 2) and ILPLKLPLLPWRR-amide (IL11) (SEQ ID NO: 3), of Indolicidin, a cationic tridecapeptide amide found in the granules of bovine neutrophils, the analogs having the amino acid only at the 4th, 8th or 11th position from the N-terminal, with leucine at its all other conventional positions, the analogs selectively having only anti-microbial activity and no hemolytic activity of Indolicidin, and thereby providing therapeutic options and a method thereof.
Type:
Grant
Filed:
March 25, 2002
Date of Patent:
October 3, 2006
Assignee:
Council of Scientific and Industrial Research
Abstract: The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide having an isoleucine residue, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by an enzyme associated with the target cell. Methods of making and using the compounds are also disclosed.
Type:
Grant
Filed:
June 11, 2001
Date of Patent:
October 3, 2006
Assignee:
Medarex, Inc.
Inventors:
Lesley B. Pickford, Sanjeev Gangwar, Thomas J. Lobl, Matthew H. Nieder, Geoffrey T. Yarranton
Abstract: The invention relates to GPE analogs, particularly GPE analogs capable of inducing an equivalent physiological effect to GPE within a patient. Such GPE analogs include peptides where the Gly of Gly-Pro-Glu is replaced by any of Ala, Ser, Thr, or Pro; where the Pro of Gly-Pro-Glu is replaced by any of Ala, Ser, Thr, or Gly; and where the Glu of Gly-Pro-Glu is replaced by any of Asn, Asp, or Gln. The GPE analogs of the invention have application in any method of therapy or prophylaxis in which GPE has application. These applications include the treatment of acute brain injury and neurodegenerative disease, including but not limited to injury or disease in the CNS. The GPE analogs will normally be administered as part of a pharmaceutical composition or preparation.
Abstract: The present invention discloses a method of enhancing cardiac contractility in a subject with heart failure. The method consists of administering a compound that inhibits the sarcolemmal sodium/calcium exchanger, whose activity is elevated in heart failure. This method results in correction of cellular calcium handling and enhancement of cardiac contractility to healthy levels. This method can be used for treatment of acute heart failure, cardiogenic shock and congestive heart failure.
Abstract: The present invention relates to methods of treating polycystic ovary syndrome (PCOS) comprising administering glucagon-like peptide-1 (GLP-1), exendin, and analogs and agonists thereof, to subjects suffering therefrom.
Type:
Grant
Filed:
July 30, 2003
Date of Patent:
September 12, 2006
Assignee:
Amylin Pharmaceuticals, Inc.
Inventors:
Nigel Robert Arnold Beeley, Kathryn S. Prickett, Andrew A. Young, David R. Hathaway
Abstract: The present invention provides methods of treating, parasitic infections, thymoma, and lymphoid malignancies in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.
Type:
Grant
Filed:
May 2, 2003
Date of Patent:
September 12, 2006
Assignee:
Praecis Pharmaceuticals, Inc.
Inventors:
Gary L. Olson, Christopher Self, Lily Lee, Charles Michael Cook, Jens Birktoft, Barry Morgan, Christopher C. Arico-Muendel
Abstract: Autographa californica nucleopolyhedrovirus (AcNPV) is a baculovirus widely employed as a vector for the expression of foreign genes and pest control. Although baculoviruses efficiently replicate in the nuclei of arthropod cells, the dynamics and mechanism of DNA replication within the infected cell are still poorly understood. Thus, to study such viral DNA replication, the availability of peptide ligands specific for DNA-binding protein (DBP) is needed. This work resulted in the selection of peptide ligands specifically binding to DBP for AcNPV from the FliTrx™ random peptide display library, which entails the amplification, cloning of the DBP gene from AcNPV, the construction of the expression plasinid for DBP, and the expression and purification of the recombinant His.Tag AcNPV DBP which was used as a target molecule for the selection of the peptide ligands. The affinity of peptide ligands was measured by ELISA procedures.