Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
December 24, 2013
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shouming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
Abstract: The disclosure provides a cell penetrating peptide. The cell penetrating peptide includes an amino acid sequence of Dn, in which D represents an aspartate residue and 2?n?15.
Type:
Grant
Filed:
July 25, 2012
Date of Patent:
December 24, 2013
Assignee:
Kaohsiung Medical University
Inventors:
Hui-Ting Chen, Hsin-Fang Chang, Yan-Hsiung Wang, Chai-Lin Kao
Abstract: An insulin-gold nanocluster, a pharmaceutical composition for treating diabetes comprising the insulin-gold nanocluster, and a method for detecting adipose cells in a tissue by using the insulin-gold nanocluster are provided. Herein, the insulin-gold nanocluster of the present invention comprises: a gold nanocluster, and insulin connecting to the gold nanocluster, wherein the insulin-gold nanocluster emits red fluorescence at maximized wavelength of 670 nm.
Abstract: Embodiments of the present invention are directed to a coated cell comprising a therapeutic cell and a plurality of targeting complexes coating the therapeutic cell and each of said targeting complexes comprising a homing molecule, a lipid moiety, and a spacer having from about 1 to about 10 amino acids and covalently linking the homing molecule to the lipid moiety and wherein the lipid moiety is non-covalently attached to the therapeutic cell. In some embodiments, the therapeutic cell is a stem cell. Embodiments of the invention are directed to methods of coating a therapeutic cell. Embodiments of the invention are directed to methods of treating diseases of the vasculature.
Type:
Grant
Filed:
June 7, 2010
Date of Patent:
November 12, 2013
Assignee:
Cell Targeting, Inc.
Inventors:
Joseph Wagner, Randell Young, David Fink
Abstract: The present invention provides nucleic acid molecules encoding novel red fluorescent proteins from Entacmaea quadricolor and mutants thereof. Also of interest are proteins that are substantially similar to the novel red fluorescent proteins. In addition, host cells, stable cell lines and transgenic organisms comprising the nucleic acid molecules encoding the novel red fluorescent proteins are provided. The subject proteins and nucleic acid compositions find use in a variety of different applications and methods, particularly for labeling of biomolecules, cells, or cell organelles. Finally, kits for use in such methods and applications are provided.
Abstract: The present invention relates to a tyrosine kinase-inducible domain (pKID) and uses thereof. An isolated polypeptide comprising the pKID, and an isolated polynucleotide comprising a nucleic acid sequence encoding the pKID are provided. Also provided are methods for determining tyrosine kinase and/or phosphatase activity in a sample and for identifying an agent that inhibits a tyrosine kinase or phosphatase using a polypeptide comprising the pKID.
Type:
Grant
Filed:
April 1, 2011
Date of Patent:
October 8, 2013
Assignee:
University of Delaware
Inventors:
Neal J. Zondlo, Susan Carr Zondlo, Feng Gao
Abstract: The present invention relates to recombinant albumins fused with poly-cysteine peptide and methods for preparing the same, more precisely recombinant albumins in which cysteines that can be used for drug binding are amplified at N-terminal and C-terminal of the albumin and methods for preparing the same. The recombinant albumin of the present invention demonstrates improved albumin-drug conjugation efficiency when it is used for drug delivery system, indicating that it can effectively deliver a large amount of drug to a target tissue. At the same time, the recombinant albumin of the present invention can be used as an excellent drug deliverer with reduced side effects, compared with the conventional albumin carriers, by regulating the amount of drug conjugated to each unit of albumin by regulating the number of cysteine fused thereto.
Type:
Grant
Filed:
June 2, 2010
Date of Patent:
September 24, 2013
Assignee:
Korea Institute of Science and Technology
Inventors:
Hyung Jun Ahn, Ick Chan Kwon, Kuiwon Choi, Kwangmyeng Kim, Inchan Youn, Sehoon Kim
Abstract: The present invention provides for novel peptides derived from human milk. In aspects of the invention, the peptides are capable, individually or in combination, of evoking an antioxidative stress response, immunomodulation, anti-inflammatory response and anti-pathogenic response. As such the peptides of the invention may be used in food supplements, milk substitutions, infant formula., mother's milk, parenteral nutrition solutions, cell/tissue/organ storage and perfusion solutions and pharmaceutical formulations.
Type:
Grant
Filed:
June 1, 2010
Date of Patent:
August 27, 2013
Inventors:
Kenneth James Friel, Apollinaire Tsopmo
Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.
Type:
Grant
Filed:
March 1, 2010
Date of Patent:
August 20, 2013
Assignee:
Trustees of Tufts College
Inventors:
William W. Bachovchin, Hung-sen Lai, Wengen Wu
Abstract: The embodiments provide Compound KC-7, N-1-[(S)-2-(oxycodone-6-enol-carbonyl-methyl-amino)-2-carbonyl-sarcosine-ethyl amine]-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the \compositions comprise a prodrug, Compound KC-7, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
Abstract: Disclosed here is a method for measuring the kinetics (i.e., the molecular flux rates—synthesis and breakdown or removal rates) of a plurality of proteins or organic metabolites in living systems. The methods may be accomplished in a high-throughput, large-scale automated manner, by using existing mass spectrometric profiling techniques and art well known in the fields of static proteomics and static organeomics, without the need for additional biochemical preparative steps or analytic/instrumental devices.
Type:
Grant
Filed:
March 1, 2012
Date of Patent:
July 9, 2013
Assignee:
The Regents of the University of California
Abstract: Sequence-specific polymers are proving to be a powerful approach to assembly and manipulation of matter on the nanometer scale. Ligands that are peptoids, or sequence-specific N-functional glycine oligomers, allow precise and flexible control over the arrangement of binding groups, steric spacers, charge, and other functionality. We have synthesized short peptoids that can prevent the aggregation of gold nanoparticles in high-salt environments including divalent salt, and allow co-adsorption of a single DNA molecule. This degree of precision and versatility is likely to prove essential in bottom-up assembly of nanostructures and in biomedical applications of nanomaterials.
Type:
Grant
Filed:
January 12, 2011
Date of Patent:
June 11, 2013
Assignee:
Sandia Corporation
Inventors:
David Bruce Robinson, Ronald Zuckermann, George M. Buffleben
Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.
Type:
Grant
Filed:
June 23, 2011
Date of Patent:
April 9, 2013
Assignees:
BioSource Pharm, Inc., Cubist Pharmaceuticals, Inc.
Inventors:
William V. Curran, Christopher M. Liu, Amy C. D. Bombardier, Richard A. Leese, You Seok Hwang, Blaise S. Lippa, Yanzhi Zhang
Abstract: The present invention is directed to the use of the peptide compound Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilizate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.
Type:
Grant
Filed:
September 9, 2008
Date of Patent:
January 8, 2013
Assignee:
mondoBIOTECH Laboratories AG
Inventors:
Dorian Bevec, Fabio Cavalli, Vera Cavalli, Gerald Bacher
Abstract: The present invention is directed to the use of the peptide compound Ac-Arg-Phe-Met-Trp-Met-Arg-NH2 as a therapeutic agent for the prophylaxis and/or treatment of cancer, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, lung diseases, heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artificial mother milk formulation or mother milk substitute containing the peptide Ac-Arg-Phe-Met-Trp-Met-Arg-NH2 optionally together with at least one pharmaceutically acceptable carrier, cryoprotectant, lyoprotectant, excipient and/or diluent.
Type:
Grant
Filed:
September 9, 2008
Date of Patent:
December 25, 2012
Assignee:
mondoBIOTECH Laboratories AG
Inventors:
Dorian Bevec, Fabio Cavalli, Vera Cavalli, Gerald Bacher