Abstract: The present invention is directed generally to recombinant methods for making a desired polypeptide. These method(s) yield a polypeptide product containing reduced levels of isoform impurities thereof. In particular, the present invention is directed to (1) a recombinant method for preparing growth hormone with reduced isoform impurities thereof and (2) a recombinant method for preparing a growth hormone antagonist, such as pegvisomant, and its protein intermediate, also having reduced isoform impurities thereof. More specifically, the isoform impurities that are decreased by methods of the present invention are the trisulfide and des-phe isoform impurities of growth hormone and growth hormone antagonist (or its intermediate), respectively.
Type:
Grant
Filed:
March 17, 2009
Date of Patent:
April 3, 2012
Assignee:
Pfizer Inc.
Inventors:
Anurag S. Rathore, Stephen B. Lyle, David E. Steinmeyer, Scott I. Allen, John Meyer, Denis M. Boyle, John J. Buckley, Gary V. Johnson
Abstract: The present invention is directed to a pharmaceutical composition comprising 0.5 ng to 20 ?g desmopressin and a pharmaceutically acceptable carrier. The present invention is also directed to a pharmaceutical composition comprising desmopressin and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition is effective to establish a steady plasma/serum desmopressin concentration in the range of from about 0.1 picograms desmopressin per mL plasma/serum to about 10.0 picogram desmopressin per mL plasma/serum. Articles of manufacture and methods of using the above invention are also disclosed.
Abstract: This invention relates to novel peptides, discovered by using phage display technique, that bind to VAP-1 (Vascular Adhesion Protein-1). The invention concerns also peptides useful as VAP-1 ligands. Such peptides constitute a portion of natural proteins that are present in the individual. The invention relates particularly to a peptide chain in the leukocyte surface protein, where said peptide chain is useful as a ligand for the VAP-1 molecule and thus facilitates the binding of leukocytes to the vascular endothelium. Furthermore, the invention relates to pharmaceutical and diagnostic compositions for targeting VAP-1 in vivo.
Abstract: An aqueous solution of calcitonin suitable for intranasal administration comprised of calcitonin, chlorobutanol at a concentration of less than 0.4% weight/weight, and water and having a pH of less than 4 with the proviso that benzalkonium chloride is not present in the solution. The aqueous solution of calcitonin can be used to treat osteoporosis, Paget's bone disease and hypercalcemia.
Type:
Grant
Filed:
September 9, 2010
Date of Patent:
March 20, 2012
Assignee:
Par Pharmaceutical, Inc.
Inventors:
Steven C. Quay, Jorge C. de Meireles, Arati Deshpande, Zenaida O. Go, Anthony P. Sileno
Abstract: The present invention relates to compositions and methods for producing therapeutic oligomeric compounds. In one aspect the invention relates to methods for administering the oligomeric compounds for the treatment and prevention of disease, for example, a fungal infection, bacterial infection, or cancer, in a mammal. In particular, the invention relates to medicaments comprising various novel oligomeric compounds and pharmaceutically acceptable salts thereof. The compounds of the invention may optionally be administered with at least one of a pharmaceutically acceptable excipient, pharmacologically active agent or a combination thereof.
Type:
Grant
Filed:
February 18, 2010
Date of Patent:
March 20, 2012
Assignees:
Centre National de la Recherche Scientifique (SNRS), ImmuPharma France SA
Inventors:
Aude Violette, Jean-Paul Briand, Robert H. Zimmer, Gilles Guichard
Abstract: The subject invention provides dipeptides useful in promoting healthy muscle tissues as well as effective immune responses. The dipeptides of the subject invention are particularly advantageous because they are stable, bioavailable, and can be formulated in an aqueous solution.
Type:
Grant
Filed:
October 17, 2008
Date of Patent:
March 13, 2012
Assignee:
University of Florida Research Foundation, Inc.
Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Type:
Grant
Filed:
April 14, 2005
Date of Patent:
March 6, 2012
Assignee:
Onyx Therapeutics, Inc.
Inventors:
Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
Abstract: The present invention relates to compounds of Formula I, II or III, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
January 9, 2009
Date of Patent:
February 28, 2012
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Zhenwei Miao, Ying Sun, Suanne Nakajima, Datong Tang, Frank Wu, Guoyou Xu, Yat Sun Or, Zhe Wang
Abstract: Linear and cyclic peptidomimetics which bind to one or more melanocortin receptors are provided, which peptidomimetics include at least one ring-constrained amino acid surrogate of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, and y are as defined in the specification, together with methods for synthesizing ring-constrained amino acid surrogates of formula I and peptidomimetics incorporating the same, and methods of use of peptidomimetics in the treatment of various diseases, syndromes and conditions.
Type:
Grant
Filed:
October 3, 2008
Date of Patent:
February 14, 2012
Assignee:
Palatin Technologies, Inc.
Inventors:
Shubh D. Sharma, Margarita Bastos, Wei Yang
Abstract: The invention relates to non-proteolysable oligopeptides that inhibit glycoprotein 41 of the AIDS virus. More specifically, the invention relates to the identification of oligopeptides, particularly hexapeptides, (D), (L) or mixed, preferably D-hexapeptides, which inhibit the binding of a retrovirus to a target cell, thereby providing novel therapies against infection from the human immunodeficiency virus (HIV). The invention also relates to the use of said D-hexapeptides in the form of single components or complex mixtures as prophylactic or therapeutic agents for retroviral infections, especially human immunodeficiency virus type 1 (HIV-1).
Type:
Grant
Filed:
December 29, 2006
Date of Patent:
February 7, 2012
Assignees:
Universidad Del Pais Vasco, Universidad de Valencia
Inventors:
Jose Luis Nieva Escandon, Maria Jose Gomara Elena, Maier Lorizate Nogales, Nerea Huarte Arrayago, Ismael Mingarro Munoz, Enrique Perez Paya
Abstract: The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy.
Type:
Grant
Filed:
June 6, 2008
Date of Patent:
February 7, 2012
Assignee:
University of Maryland, Baltimore
Inventors:
Angela Brodie, Vincent Njar, Gauri Sabnis, Lalji Gediya
Abstract: A generic structure for the peptides of the present invention includes A-X-B-C, where C is a cargo moiety, the B portion includes basic amino acids, X is a cleavable linker sequence, and the A portion includes acidic amino acids. The intact structure is not significantly taken up by cells; however, upon extracellular cleavage of X, the B-C portion is taken up, delivering the cargo to targeted cells. Cargo may be, for example, a contrast agent for diagnostic imaging, a chemotherapeutic drug, or a radiation-sensitizer for therapy. Cleavage of X allows separation of A from B, unmasking the normal ability of the basic amino acids in B to drag cargo C into cells near the cleavage event. X is cleaved extracellularly, preferably under physiological conditions. D-amino acids are preferred for the A and B portions, to minimize immunogenicity and nonspecific cleavage by background peptidases or proteases.
Type:
Grant
Filed:
October 2, 2008
Date of Patent:
February 7, 2012
Assignee:
The Regents of the University of California
Abstract: The invention features peptides for the treatment or prevention of obesity, diabetes or co-morbidities of obesity; for reduction of appetite, food intake, calorie intake, body weight, or body weight gain; and for increase of energy expenditure in a subject.
Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Abstract: It was shown that bombesin 2 (BB2) receptor antagonists typified by RC-3095 are therapeutic agents for irritable bowel syndrome (IBS), and show excellent efficacy in treating both an abdominal symptom and bowel movement disorder. Thus, the present invention provides a therapeutic agent for irritable bowel syndrome (IBS) which comprises, as an active ingredient, a bombesin 2 (BB2) receptor antagonist as well as a method for treating IBS.
Abstract: Disclosed herein are compositions and methods useful for promoting sperm motility, promoting embryonic stem cell formation, promoting trophoblast formation, or promoting neuronal growth. The compositions and methods are based on peptide sequences that bind trophinin, inhibit bystin-mediated arrest of epidermal growth factor (EGF) receptor, and promotes EGF receptor autophosphorylation.
Type:
Grant
Filed:
February 6, 2008
Date of Patent:
January 17, 2012
Assignee:
Sanford-Burnham Medical Research Institute
Abstract: The present invention relates to formulations of a lipid based controlled-release matrix, a polyhydroxy component and a bioactive agent. Such formulation are useful in the delivery of the bioactive compounds. The invention also relates to the use of a polyhydroxy component for increasing the solubility of a bioactive compound, especially a peptide in a lipid-based controlled-release matrix.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
January 17, 2012
Assignee:
Camurus AB
Inventors:
Markus Johnsson, Fredrik Tiberg, Catalin Nistor
Abstract: The present invention relates to gold binding peptides and shape- and size-tunable synthesis of gold nanostructures. The present inventions are very useful for the production of well-designed, gold-based architectures. The size- and shape-specific gold nanostructure materials prepared by the present invention may find use as: highly conductive interconnections for single-electron transistors, catalysts for the oxidation of carbon monoxide; biological and chemical sensors; and as contrasting agents for electron microscopic and medical imaging applications.
Type:
Grant
Filed:
May 4, 2009
Date of Patent:
January 3, 2012
Assignee:
Gwangju Institute of Science and Technology
Inventors:
Hor Gil Hur, Jung Ok Kim, Dae Hee Kim, No Sang Myung
Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
Type:
Grant
Filed:
May 9, 2005
Date of Patent:
January 3, 2012
Assignee:
Onyx Therapeutics, Inc.
Inventors:
Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser, Kevin D. Shenk, Peggy A. Radel
Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective agonists of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Such compounds are useful as medicaments for treatment and prevention of a range of medical conditions characterized by disturbed gastrointestinal motility including, but not limited to, post-surgical gastroparesis and post-operative ileus in combination with opioid-induced bowel dysfunction. These agents are effective for multiple disorders at dose levels equivalent to those required to treat a single disorder.
Type:
Grant
Filed:
July 6, 2007
Date of Patent:
January 3, 2012
Assignee:
Tranzyme Pharma Inc.
Inventors:
Graeme L. Fraser, Hamid R. Hoveyda, Mark L. Peterson