Abstract: Disclosed are Somatostatin receptor ligands comprising a peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and an active agent moiety covalently bonded to the cyclic peptide moiety through a nitrogen atom of a side chain functional group of an internal residue of the cyclic peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and a nanoparticle active agent moiety covalently bonded to the cyclic peptide moiety, pharmaceutical compositions and uses thereof.
Type:
Grant
Filed:
February 3, 2022
Date of Patent:
November 28, 2023
Assignee:
TEL HASHOMER MEDICAL RESEARCH INFRASTRUCTURE AND SERVICES LTD.
Abstract: The present invention relates to acylated GIP analogues which have GIP agonist activity, and their use in the treatment of metabolic disorders.
Type:
Grant
Filed:
April 2, 2021
Date of Patent:
November 14, 2023
Assignee:
Zealand Pharma A/S
Inventors:
Anne Pernille Tofteng Shelton, Pia Nørregaard, Maria Alexandrovna Deryabina, Bjarne Due Larsen, Jacob Ulrik Fog
Abstract: The present disclosure relates to a group of peptide compounds and their use in identifying molecules that stimulate proteasome or immunoproteasome are disclosed herein. Composition matters and methods of uses are within the scope of this disclosure.
Type:
Grant
Filed:
August 13, 2021
Date of Patent:
November 7, 2023
Assignee:
Purdue Research Foundation
Inventors:
Darci Jones Trader, Rachel Anne Coleman
Abstract: The present invention relates to compounds comprising formula I: Amino Acid Sequence-(L)n-DMARD wherein the amino acid sequence comprises QKRAAYDQYGHAAFE-NH2 (SEQ ID NO: 1), DMARD is a disease modifying antirheumatic agent L is a linker unit,—is a covalent bond and n is 0 or 1 and methods of using the compound for treatment of autoimmune diseases. In a preferred embodiment the DMARD is selected from Chloroquine and Hydroxychloroquine.
Abstract: Described herein, in various embodiments, are peptides comprising: (i) a cyclic cell-penetrating peptide sequence (cCPP) and (ii) a CAL-PDZ binding sequence, which is conjugated, directly or indirectly, to an N-terminus of an amino acid in the cCPP, to a C-terminus of an amino acid on the cCPP, or on a side chain of an amino acid in the cCPP. In other embodiments, the peptides further comprise a physiologically cleavable group, wherein after entering the cell, the physiologically cleavable group is reduced, thereby providing a linear peptide. Without being bound by theory, the inventors discovered that the amino acid sequence in the cCPP, which facilities cytosolic delivery of the CAL-PDZ binding sequence also, surprisingly and unexpectedly, synergistically improves binding of CAL-PDZ binding sequence to the CAL-PDZ binding domain. Additionally, the cCPP sequence may also improve selectivity of the CAL-PDZ binding sequence for the CAL-PDZ domain relative to other PDZ binding domains.
Abstract: The present invention relates to the fields of molecular medicine and targeted delivery of therapeutic or diagnostic agents to cells outside the vascular system and into the parenchymal tissue of organs within the body. More specifically, the present invention relates to the methods used to identify membrane receptors or transporters capable of carrying cargo specifically targeted to the parenchymal tissue of the brain and to in vivo enrichment methods for selecting peptides that are transported across the blood-brain barrier (“BBB”), or analogously, across other membrane containing organs or structures, such as liver, spleen, kidney and tumors.
Type:
Grant
Filed:
July 21, 2021
Date of Patent:
September 26, 2023
Assignee:
Ossianix, Inc.
Inventors:
Pawel Stocki, Krzysztof Bartlomiej Wicher, Julia Lynn Rutkowski, Fabrizio Comper, Mykhaylo Demydchuk, Jaroslaw Michal Szary
Abstract: The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.
Abstract: The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
Type:
Grant
Filed:
January 25, 2021
Date of Patent:
September 19, 2023
Assignee:
Novo Nordisk A/S
Inventors:
Thomas Vilhelmsen, Helle Eliasen, Tue Hansen
Abstract: The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
September 19, 2023
Assignee:
Novo Nordisk A/S
Inventors:
Thomas Vilhelmsen, Helle Eliasen, Tue Hansen
Abstract: The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.
Type:
Grant
Filed:
April 13, 2022
Date of Patent:
September 19, 2023
Assignee:
Novo Nordisk A/S
Inventors:
Thomas Vilhelmsen, Helle Eliasen, Tue Hansen
Abstract: A mitochondrial-targeted PARP inhibitor is provided herein, as well as methods of making and using the mitochondrial-targeted PARP inhibitor.
Type:
Grant
Filed:
August 16, 2021
Date of Patent:
September 19, 2023
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Hulya Bayir, Peter Wipf, Tanja Krainz, Robert Clark
Abstract: A biorecognition element for rapid detection of fuel biocontamination. The biorecognition element is a biorecognition element selected from SEQ. ID No. 2 through SEQ. ID No. 24, SEQ. ID No. 22 through SEQ. ID No. 44, SEQ. ID No. 46 through SEQ. ID No. 57, SEQ. ID No. 59 through SEQ. ID No. 196 or SEQ. ID No. 198 through SEQ. ID No. 332.
Type:
Grant
Filed:
May 18, 2021
Date of Patent:
September 12, 2023
Assignee:
United States of America as represented by the Secretary of the Air Force
Inventors:
Oscar N. Ruiz, Thusitha S Gunasekera, Osman Radwan
Abstract: Embodiments of the present disclosure relate to an isolated peptide consisting of a sequence of 3 to 39 amino acids derived from the amino acid sequence SEQ ID NO: 1, said peptide having a sequence of amino acids selected from the group consisting of: a) sequences of 3 to 39 amino acids comprising at least the residues 6 to 8 of SEQ ID NO: 1, and b) sequences of 3 to 39 amino acids having at least 70% identity with said sequence in a).
Type:
Grant
Filed:
January 12, 2018
Date of Patent:
September 12, 2023
Inventors:
Khaddouj Benmoussa, Elsa Bonnafe, Agnès Coste, Jérôme Leprince, Bernard Pipy, Michel Treilhou
Abstract: The invention relates to a glycopolypeptide that includes one or more modified amino acid residues having a sidechain comprising a monosaccharide or an oligosaccharide, wherein the glycopolypeptide binds specifically to a carbohydrate-binding monoclonal antibody with an affinity of less than 100 nM. Immunogenic conjugates that include the glycopolypeptide, and pharmaceutical compositions that include the glycopolypeptide or the immunogenic conjugate are also disclosed. Various method of using the glycopolypeptides, immunogenic conjugates, and pharmaceutical compositions are disclosed, including inducing an immune response, inhibiting viral or bacterial infection, treating a cancerous condition, and detecting a neutralizing antibody.
Abstract: Methodology was developed for transformation of methionine residues into homocysteine derivatives. Methionine residues can undergo alkylation reactions at low pH to yield sulfonium ions, which can then be selectively demethylated to give alkyl homocysteine residues. This process tolerates many functional groups.
Type:
Grant
Filed:
April 27, 2017
Date of Patent:
August 22, 2023
Assignee:
The Regents of the University of California
Inventors:
Timothy J. Deming, Eric G. Gharakhanian
Abstract: The present application provides bifunctional compounds of Formula X or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
Type:
Grant
Filed:
January 29, 2019
Date of Patent:
August 1, 2023
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, Jinhua Wang, Dennis Dobrovolsky
Abstract: Peptidyl IL-2R? ligands and compounds comprising the IL-2R? ligands are disclosed. The IL-2R? ligands and compounds such as synthetic monomers, homodimers, or heteromers and recombinant fusion proteins comprising the IL-2R? ligands can be used as targeting or imaging agents, as diagnostics or to treat cancers and autoimmune diseases.
Type:
Grant
Filed:
January 5, 2022
Date of Patent:
July 4, 2023
Assignee:
MEDIKINE, INC.
Inventors:
William J. Dower, Michael C. Needels, Ronald W. Barrett, Alice V. Bakker, Steven E. Cwirla
Abstract: The present disclosure provides a large combinatorial library of cell-permeable bicyclic peptides. The bicyclic peptides described herein include the first ring consisted of randomized peptide sequences for potential binding to a target of interest while the second ring featured a family of different cell-penetrating motifs, for both cell penetration and target binding. The library was screened against the I?B kinase ?/? (IKK?/?)-binding domain of NF-?B essential modulator (NEMO), resulting in the discovery of several cell-permeable bicyclic peptides which inhibited the NEMO-IKK? interaction, thereby selectively inhibiting canonical NF-?B signaling in mammalian cells and the proliferation of cisplatin-resistant ovarian cancer cells.
Abstract: Provided herein are methods, reagents, and kits for isolating polypeptides, such as a proteome. Also provided herein is a modified trypsin polypeptide that is resistant to autolysis, and that can be selectively-separated from a biological sample once digestion is complete.