Abstract: An anti-hypertensive fish protein hydrolysate is provided, wherein the fish is of the genus Salmo or Oncorhynchus, and wherein the fish protein hydrolysate comprises at least 1 peptide selected from the group consisting of: Leu-Ala-Phe, Leu-Thr-Phe, Ile-Ile-Phe, Leu-Ala-Tyr, Ile-Ala-Tyr, Val-Phe-Tyr, Tyr-Ala-Tyr, Val-Leu-Trp, Ile-Ala-Trp, Tyr-Ala-Leu and Tyr-Asn-Arg. Methods of making and methods for using such fish protein hydrolysates are also provided.
Type:
Grant
Filed:
February 14, 2005
Date of Patent:
February 20, 2007
Assignee:
Ocean Nutrition Canada Limited
Inventors:
Harry Stephen Ewart, Dorothy Anne Dennis, Colin Barrow, Michael Anthony Potvin
Abstract: Compounds that modulate natural ? amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a ? amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3–5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a ? amyloid peptide, preferably a retro-inverso isomer of A?17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group.
Type:
Grant
Filed:
September 30, 2003
Date of Patent:
February 13, 2007
Assignee:
Praecis Pharmaceuticals, Inc.
Inventors:
Mark A. Findeis, Malcolm L. Gefter, Gary F. Musso, Ethan R. Signer, James Wakefield, Susan Molineaux, Joseph Chin, Jung-Ja Lee, Michael Kelley, Sonja Komar, Christopher C. Arico-Muendel, Kathryn Phillips, Neil J. Hayward
Abstract: Tuberculosis in an animal is treated by administration of a therapeutically effective amount of an immunomodulator of formula A. In formula (A), n is 1 or 2, R is hydrogen, acyl, alkyl or a peptide fragment, and X is an aromatic or heterocyclic amino acid or a derivative.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
February 6, 2007
Assignee:
SciClone Pharmaceuticals, Inc.
Inventors:
Alexandr A. Kolobov, Andrey S. Simbirtsev, Tat'yana I. Vinogradova, Natal'ya V. Zabolotnyh
Abstract: A peptide of the formula (Xaa)n1-Xaa1-His-Thr-Asp-(Xaa)n2, wherein Xaa is any amino acid; Xaa1 is a hydrophobic amino acid, preferably Gly or Val; n1 is 0–10; and n2 is 0–10; and use thereof in regulating in vivo blood glucose levels in a human or other mammal, particularly in the treatment of Type 2 diabetes in a human. Preferably, the peptide is a tetrapeptide selected from Gly-His-Thr-Asp and Val-His-Thr-Asp. These hypoglycaemic peptides are isolated from human urine and they also have been chemically synthesized.
Type:
Grant
Filed:
June 27, 2002
Date of Patent:
February 6, 2007
Assignees:
International Diabetes Institute, Monash University
Abstract: This invention provides novel peptides that ameliorate one or more symptoms of atherosclerosis. The peptides are highly stable and readily administered via an oral route. In addition, the peptides inhibit osteoporosis. When administered with a statin, the peptides enhance the activity of the statin permitting the statin to be used at significantly lower dosages. In certain embodiments, the peptides range in length from about 10 up to about 30 amino acids, comprise at least one class A amphipathic helix, and protect a phospholipid against oxidation by an oxidizing agent.
Type:
Grant
Filed:
October 16, 2002
Date of Patent:
January 23, 2007
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 provides a composition including an isolated or recombinant peptide component that has osteogenic cell proliferative activity. The peptide, which promotes proliferation of osteoblasts, is useful for treatment of fractures, as a filler in deficient sites of bone, for inhibition of decrease in bone substance related to osteoporosis and periodontic diseases, and for prevention of fractures associated with osteoporosis and rheumatoid arthritis. The peptide, or cells that have been genetically engineered to produce the peptide, can be combined with a bone-compatible matrix to facilitate slow release of the peptide to a treatment site and/or provide a structure for developing bone.
Type:
Grant
Filed:
September 30, 2003
Date of Patent:
January 16, 2007
Assignee:
Ethicon, Inc.
Inventors:
Sridevi Dhanaraj, Anna Gosiewska, Ali Rezania, George A. Heavner, Xuanhan Lin, Chin-Feng Yi
Abstract: The present invention relates to compositions comprising thyroxine (T4) and triiodothyronine (T3). More specifically, the invention relates to thyroxine (T4) and triiodothyronine (T3) compositions that include a peptide carrier and thyroxine (T4) and triiodothyronine (T3) covalently attached to at least one of the N-terminus, the C-terminus, a side chain of the peptide carrier, and/or interspersed within the peptide chain; methods for protecting and administering thyroxine (T4) and triiodothyronine (T3); and methods for treating thyroid disorders.
Type:
Grant
Filed:
May 2, 2002
Date of Patent:
January 16, 2007
Assignee:
New River Pharmaceuticals Inc.
Inventors:
Thomas Piccariello, Lawrence Peter Olon, Alex Saunders Goldstein, James Scott Moncrief, Nancy Johnston Boerth
Abstract: The present invention provides novel ?-O-linked glycoconjugates such as ?-O-linked glycopeptides, as well convergent methods for synthesis thereof. The general preparative approach is exemplified by the synthesis of the mucin motif commonly found on epithelial tumor cell surfaces. The present invention further provides compositions and methods of treating cancer using the ?-O-linked glycoconjugates.
Type:
Grant
Filed:
July 25, 2002
Date of Patent:
January 9, 2007
Assignee:
Sloan-Kettering Institute for Cancer Research
Inventors:
Samuel J. Danishefsky, Dalibor Sames, Samuel Hintermann, Xiao Tao Chen, Jacob B. Schwarz, Peter Glunz, Govindaswami Ragupathi, Philip O. Livingston, Scott Kuduk, Lawrence Williams
Abstract: Compounds of the formula wherein the substitutents are defined as in the specification useful for modulating immune responses in warm-blooded animals.
Abstract: Peptide inhibitors of glycogen synthase kinase-3 (GSK-3) having an amino acid sequence motif of XZXXXS(p)X, wherein S(p)=phosphorylated serine or phosphorylated threonine, X=any amino acid, and Z=any amino acid except serine or threonine. These inhibitors, which are about 7 to 20 amino acids long, are specific for GSK-3 and strongly inhibit the enzyme with an IC50 of about 150 ?M. Also provided are methods of treating biological conditions mediated by GSK-3 activity, such as potentiating insulin signaling in a subject, treating or preventing type 2 diabetes in a patient, and treating Alzheimer's Disease by administering peptide inhibitors. Compositions of these peptide inhibitors and pharmaceutically acceptable carriers are also provided, as is a method for identifying inhibitors of GSK-3. The invention further relates to a computer-assisted method of structure based drug design of GSK-3 inhibitors using a three-dimensional structure of a peptide substrate of GSK-3.
Type:
Grant
Filed:
March 29, 2004
Date of Patent:
January 2, 2007
Assignee:
Tel Aviv University Future Technology Development L.P.
Abstract: The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoproteinemia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis. The compositions of the present invention include dipeptidylpeptidase inhibitors, which are able to inhibit the proteolysis of GLP-1 and accordingly increase the plasma half-life of that hormone. The subject inhibitors may be peptidyl, peptidomimetic (e.g. boronyl peptidomimetics), or non-peptidyl nitrogen containing heterocycles.
Type:
Grant
Filed:
July 28, 2000
Date of Patent:
January 2, 2007
Assignee:
Trustees of Tufts College
Inventors:
William A. Bachovchin, Andrew G. Plaut, Daniel Drucker
Abstract: The present invention provides methods of treating an autoimmune disorder (e.g., lupus erythematosus, multiple sclerosis, myasthenia gravis, vasculitis and diabetes mellitus) in a subject by administering to the subject a therapeutically effective amount of one or more compounds of the invention.
Type:
Grant
Filed:
October 8, 2004
Date of Patent:
January 2, 2007
Assignee:
Praecis Pharmaceuticals, Inc.
Inventors:
Gary L. Olson, Christopher Self, Lily Lee, Charles M. Cook, Jens Birktoft, Barry Morgan, Christopher C. Arico-Muendel
Abstract: Disclosed are glycopeptide derivatives substituted at the C-terminus and/or the R-terminus with a substituent that comprises one or more saccharide groups and a carboxy group; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
March 15, 2005
Date of Patent:
January 2, 2007
Assignee:
Theravance, Inc.
Inventors:
Martin S. Linsell, Paul R. Fatheree, Michael R. Leadbetter, Yan Zhu, J. Kevin Judice
Abstract: A molecular conjugate is provided having the formula: wherein R1 is a de-hydroxyl or de-amino moiety respectively of a hydroxyl-bearing or amino-bearing biologically active molecule or an analog or derivative thereof, and Z is —O— or —NH—, respectively, Y is a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups; and R2 is —CH?CH(W), —CH(OH)CH(OH)W, or —C(O)H, where W can be H, a straight or branched alkyl having 1 to 20 carbons that may be optionally substituted with one or more phenyl, a cycloalkyl optionally substituted with one or more alkyl or phenyl, or an aromatic group optionally substituted with one or more alkyl groups, electron-withdrawing groups, or electron-donating groups.
Type:
Grant
Filed:
November 24, 2004
Date of Patent:
December 26, 2006
Assignee:
Tapestry Pharmaceuticals, Inc.
Inventors:
James D. McChesney, Madhavi C. Chander, Teruna J. Siahaan, Christine R. Xu, Sterling K. Ainsworth
Abstract: A hedgehog conjugate which is characterized in that it contains: a) a polypeptide composed of 10 to 30 hydrophobic amino acids and/or amino acids which form transmembrane helices and are positively charged, b) 1 to 4 aliphatic, saturated or unsaturated hydrocarbon residues with a chain length of 10 to 24 C atoms and with a hydrophobic action or c) a hydrophobic thio compound covalently bound to a hedgehog protein and which has a several-fold increased activity and is suitable as a pharmaceutical agent.
Type:
Grant
Filed:
October 8, 2004
Date of Patent:
December 26, 2006
Assignee:
Curis, Inc.
Inventors:
Angelika Esswein, Kurt Lang, Petra Rueger, Tilmann Seytter
Abstract: A method for treating or reducing the severity of a disease or disorder mediated by a membrane metallopeptidase by administering to a mammal a SMR1-peptide or a pharmaceutically active amount of a SMR1-peptide.
Type:
Grant
Filed:
December 24, 2001
Date of Patent:
December 26, 2006
Assignees:
Institut Pasteur, Centre National de la Recherche Scientifique (C.N.R.S.)
Abstract: Cyclic peptide antibiotics including the loloatins are effective in the treatment of rosacea, particularly when administered in conjunction with an antibiotic such as metronidazole that is effective against anaerobic bacteria.
Abstract: A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB) and wherein R1 is hydrogen, R2 is n-butyl, benzyl or cyclopentylmethyl, R3 is hydrogen, R4 is tert-butyl, iso-butyl, benzyl or methyl, R5 is hydrogen or methyl and R6 is methyl.
Type:
Grant
Filed:
July 29, 2004
Date of Patent:
December 12, 2006
Assignee:
British Biotech Pharmaceuticals, Ltd.
Inventors:
Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
Abstract: Disclosed is a process for preparing a macrocyclic compound of the formula (I): which is carried out using an intermediate of the formula (II): wherein W, R1 through R4, D, A and R12 are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
Type:
Grant
Filed:
April 6, 2004
Date of Patent:
December 12, 2006
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Joerg Brandenburg, Kai Donsbach, Hans-Dieter Ecker, Rogelio Perez Frutos, Fabrice Gallou, Dieter Gutheil, Nizar Haddad, Robert Hagenkoetter, Dirk Kemmer, Jutta Kroeber, Thomas Nicola, Juergen Schnaubelt, Michael Schul, Robert Donald Simpson, Xudong Wei, Eric Winter, Yibo Xu, Nathan K. Yee