Abstract: The present invention provides oral pharmaceutical compositions that enable the successful delivery of drugs in a pharmaceutically effective amount, particularly poly (amino acids) such as peptides, peptidomimetics and proteins. e.g. hormones to a subject via oral administration to accomplish the desired therapeutic effect. The oral pharmaceutical composition comprising a poly (amino acid) as the active ingredient, e.g. a peptide or protein, shows a rapid disintegration and/or dissolution such that the active ingredient is able to attain a therapeutic effect.
Type:
Grant
Filed:
May 21, 2015
Date of Patent:
April 18, 2017
Assignee:
Novartis AG
Inventors:
Moise Azria, Simon David Bateman, Anasuya Ashok Ghosh, Shoufeng Li, Alan Edward Royce
Abstract: The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.
Type:
Grant
Filed:
September 26, 2013
Date of Patent:
April 11, 2017
Assignee:
President and Fellows of Harvard College
Abstract: The technology described herein is directed to agents that reduce the level of oxidant-modified ET-B Cys405, Cys403, or Cys402 and the identification and use of such agents for, e.g. to treat hypertension.
Type:
Grant
Filed:
April 3, 2013
Date of Patent:
March 28, 2017
Assignee:
The Brigham and Womens's Hospital, Inc.
Inventors:
Bradley Maron, Joseph Loscalzo, Jane Leopold
Abstract: A method modulating adhesion and migration of at least one cadherin expressing cell includes administering a cadherin modulating agent to the at least one cadherin expressing cell in an amount effective to modulate cell adhesion and migration. The cadherin modulating agent includes a small molecule peptidomimetic of a peptide or cyclic peptide that comprises a cadherin cell adhesion recognition sequence. The cadherin modulating agent can promote or inhibit neurite outgrowth when applied to at least one neuron disposed on a substrate coated with a cadherin molecule.
Type:
Grant
Filed:
July 16, 2009
Date of Patent:
March 21, 2017
Assignee:
Case Western Reserve University
Inventors:
Susann Brady-Kalnay, Susan Burden-Gulley
Abstract: Peptides are provided that comprise less than 24 amino acids. The peptides have an amino acid sequence selected from the group consisting of: (a) an amino acid sequence having from 4 to 6 contiguous amino acids of a reference sequence PEPTIDE 1; (b) an amino acid sequence substantially identical to the sequence defined in (a); and (c) a variant of the amino acid sequence defined in (a). Also provided is a non-myristoylated MANS peptide. Various methods of using the peptides are also provided.
Abstract: Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.
Type:
Grant
Filed:
August 30, 2012
Date of Patent:
March 21, 2017
Assignee:
Trustees of Tufts College
Inventors:
William W. Bachovchin, Hung-sen Lai, Sarah E. Poplawski
Abstract: The invention provides a method of making a peptide or peptide derivative comprising the amino acid sequence comprising imfwydcye or a variant amino acid sequence comprising one, two, three, four, five or six amino acid substitutions in imfwydcye.
Abstract: A method for treating a patient suffering from one of septic shock, acute kidney injury, severe hypotension, cardiac arrest, and refractory hypotension, but not from myocardial infarction, is provided. The method includes administering a therapeutically effective dose of Angiotensin II, or Ang II, to the patient.
Type:
Grant
Filed:
December 16, 2009
Date of Patent:
February 21, 2017
Assignee:
The George Washington University a Congressionally Chartered Not-for-Profit Corporation
Abstract: Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.
Type:
Grant
Filed:
October 2, 2015
Date of Patent:
February 7, 2017
Assignee:
Allergan, Inc.
Inventors:
Michael E. Garst, William Robert Carling, David Arthur Scowen, Michael E. Stern, Christopher S Schaumburg
Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).
Abstract: The present invention cationic amphiphilic polyproline helices (CAPHs) compounds having increased hydrophobicity and cellular internalization as antimicrobial agents. Antimicrobial compositions and methods of using the same are also provided.
Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
Type:
Grant
Filed:
September 24, 2014
Date of Patent:
December 13, 2016
Assignees:
POLYPHOR LTD., UNIVERSITAT ZURICH
Inventors:
Jürg Zumbrunn, Steven J. Demarco, Sergio Lociuro, Jan Wim Vrijbloed, Frank Gombert, Reshmi Mukherjee, Kerstin Moehle, Daniel Obrecht, John Anthony Robinson, Heiko Henze, Barbara Romagnoli, Christian Ludin
Abstract: The disclosure provides methods of treating X-linked hypophosphatemia, related bone demineralization and renal phosphate wasting disorders in a mammalian subject. The methods comprise administering to the subject an effective amount of a polyarginine peptide.
Abstract: The invention relates to a stable, pharmaceutically acceptable, aqueous formulation of TNF-binding protein, comprising a TNF-binding protein, a buffer and an isotonicity agent.
Type:
Grant
Filed:
December 15, 2014
Date of Patent:
December 6, 2016
Assignee:
ARES TRADING S.A.
Inventors:
Fabrizio Samaritani, Alessandra Del Rio, Rita Agostinetto
Abstract: Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.
Type:
Grant
Filed:
September 12, 2014
Date of Patent:
November 29, 2016
Assignee:
Enteris BioPharma, Inc.
Inventors:
Nozer M. Mehta, William Stern, James P. Gilligan
Abstract: The present invention describes the use of a composition including or constituted by at least one element chosen from: a specific protein including or consisting of the amino acid sequence SEQ ID NO: 5, and a protein homologous to the specific protein, for the preparation of a medicament intended for the prevention or treatment of pathologies associated with a viral infection or an inflammation.
Type:
Grant
Filed:
March 4, 2010
Date of Patent:
November 15, 2016
Assignees:
CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURG, UNIVERSITE DE LA MEDITERRANEE
Inventors:
Eric Chabriere, Mikael Elias, Olivier Rohr, Christian Schwartz
Abstract: Various embodiments provide materials and methods for synthesizing protocells for use in targeted delivery of cargo components to cancer cells. In one embodiment, the lipid bilayer can be fused to the porous particle core to form a protocell. The lipid bilayer can be modified with targeting ligands or other ligands to achieve targeted delivery of cargo components that are loaded within the protocell to a target cell, e.g., a type of cancer. Shielding materials can be conjugated to the surface of the lipid bilayer to reduce undesired non-specific binding.
Type:
Grant
Filed:
February 20, 2015
Date of Patent:
November 1, 2016
Assignees:
STC.UNM, Sandia Corporation
Inventors:
C. Jeffrey Brinker, Carlee Erin Ashley, Xingmao Jiang, Juewen Liu, David S. Peabody, Walker Richard Wharton, Eric Carnes, Bryce Chackerian, Cheryl L. Willman
Abstract: The present invention refers to a microemulsion formulation suitable for preventing assembly of amphiphilic drug molecules which may cause hypersensitivity reactions and other unwanted side effects.
Type:
Grant
Filed:
January 5, 2010
Date of Patent:
October 18, 2016
Assignee:
AZAD Pharma AG
Inventors:
Fabio Carli, Elisabetta Chiellini, Van Van Khov-Tran, Mihran Baronian