Cyclic Peptides Patents (Class 530/317)
  • Patent number: 11524980
    Abstract: The present invention relates to echinocandin cyclopeptides and to methods for preparing echinocandin cyclopeptides.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: December 13, 2022
    Assignee: Cidara Therapeutics, Inc.
    Inventors: David Hughes, Martin Patrick Hughes, Robert Michael Hughes, Balasingam Radhakrishnan, Yannick Borguet, Steven McIntyre
  • Patent number: 11464877
    Abstract: The present invention relates to a prostate-specific membrane antigen (PSMA)-specific binding protein, wherein the PSMA-specific binding protein is a lipocalin 2 (Lcn2)-derived binding protein and binds to PSMA with a KD of 10 nM or lower. The present invention also relates to a nucleic acid molecule encoding the PSMA-specific binding protein of the invention, a vector comprising said nucleic acid molecule of the invention and a host cell transformed with the vector. Furthermore, the invention relates to a method of producing the PSMA-specific binding protein of the invention, the method comprising culturing the host cell of the invention under suitable conditions and isolating the PSMA-specific binding protein produced. The present invention further relates to a protein conjugate comprising the PSMA-specific binding protein of the invention, or the PSMA-specific binding protein produced by the method of the invention.
    Type: Grant
    Filed: July 17, 2019
    Date of Patent: October 11, 2022
    Inventors: Arne Skerra, Antonia Richter, Volker Morath, Cyril Barinka, Jakub Ptacek
  • Patent number: 11447524
    Abstract: Disclosed herein is a cyclic peptide polymer. R1, R2, and R3 are organic groups. Each R4 is a covalent bond, methylene, ethylene, n-propylene, or n-butylene. Each X is —NH—, —O—, or —O—CO—. The values m and n are nonnegative integers having a sum of at least 1. The value p is an integer greater than 1. The cyclic peptide polymer may be made by providing a first cyclic peptide monomer having a protecting group on the X group, covalently binding the —CO—OH group of the first cyclic peptide monomer to a solid support having a carboxylic acid-reactive group, converting the protecting group to —XH, reacting the —XH group with the —CO—OH group of an additional cyclic peptide monomer, optionally repeating the converting and reacting steps with further additional cyclic peptide monomers, and cleaving the cyclic peptide polymer from the solid support.
    Type: Grant
    Filed: November 19, 2020
    Date of Patent: September 20, 2022
    Assignee: The Government of the United States of America, as represented by the Secretary of the Navy
    Inventors: Kenan P. Fears, Manoj K. Kolel-Veetil
  • Patent number: 11421001
    Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
    Type: Grant
    Filed: September 4, 2020
    Date of Patent: August 23, 2022
    Assignees: UNIVERSITAET ZUERICH, POLYPHOR LTD.
    Inventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
  • Patent number: 11331369
    Abstract: The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof wherein each of R1, R2, R3, R4, L1, and L2, are as defined herein. The present invention also contemplates compositions and methods of treatment as an endoparasiticide with a Formula (1) compound.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: May 17, 2022
    Assignee: Zoetis Services LLC
    Inventors: Michael P. Curtis, Susan M. Sheehan, Graham M. Kyne, Matthew W. Bedore, Richard A. Ewin, Paul D. Johnson, Tom L. McTier, Christoper S. Knauer, Rajendran Vairagoundar
  • Patent number: 11286280
    Abstract: Methods preventing, ameliorating or treating cytokine storm or inflammatory disease, indications, conditions and syndromes by administration of a therapeutically effective amount of a melanocortin-1 receptor-specific cyclic peptide or pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 13, 2020
    Date of Patent: March 29, 2022
    Assignee: Palatin Technologies, Inc.
    Inventors: Wei Yang, Yi-Qun Shi
  • Patent number: 11279963
    Abstract: The invention concerns a compound characterised by a mono(2-hydroxyethyl) terephthalic acid (MHET) and bis(2-hydroxyethyl) terephthalic acid chemically bonded to a saccharide. Furthermore, the invention concerns a corresponding compound which is used as a synthesis component for polymers or fine chemicals.
    Type: Grant
    Filed: March 23, 2017
    Date of Patent: March 22, 2022
    Assignee: Julius-Maximilians-Universität Würzburg
    Inventors: Jürgen Seibel, Malte Timm
  • Patent number: 11214602
    Abstract: The invention is directed to modified Coversin polypeptides which exhibit leukotriene or hydroxyeicosanoid binding activity and reduced or absent C5 binding relative to the unmodified Coversin polypeptide; to nucleic acid molecules encoding said modified Coversin polypeptides; vectors and host cells comprising said nucleic acid molecules; and methods of treating or preventing diseases or conditions mediated by a leukotriene or hydroxyeicosanoid in a subject comprising administering said modified polypeptides or nucleic acids to a subject.
    Type: Grant
    Filed: April 20, 2018
    Date of Patent: January 4, 2022
    Assignee: Volution Immuno Pharmaceuticals, SA
    Inventor: Miles Andrew Nunn
  • Patent number: 10857242
    Abstract: A fluorescent tracer for targeting tumors, comprises: at least one first fluorophore fluorescing in a range of wavelengths of between 700 and 1000 nm, a targeting assembly comprising at least two identical targeting molecules, and a cyclic oligopeptide: configured so as to define a mean plane defining a first upper face and a second lower face, comprising at least one first lysine amino acid residue on the second lower face, the targeting molecules being fixed to the first upper face of the mean plane, the fluorophore being fixed to the second lower face of the mean plane via a spacer arm connecting a carbon of the sequence of the at least three double bonds and the lysine amino acid residue of the oligopeptide.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: December 8, 2020
    Assignee: FLUOPTICS
    Inventor: Pascal Gayet
  • Patent number: 10800822
    Abstract: Synthetic histatins composed of combinations of functional domains of natural histatins separated by exogenous linkers are described as are methods of using endogenous and synthetic histatins for the treatment of ocular diseases or conditions.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: October 13, 2020
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventor: Vinay Aakalu
  • Patent number: 10787486
    Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: September 29, 2020
    Assignees: UNIVERSITAET ZUERICH, POLYPHOR LTD.
    Inventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
  • Patent number: 10639380
    Abstract: The invention pertains to inhibitors bindable to regions of a virus. More particularly, the invention relates to inhibitors bindable to regions of flaviviral envelope glycoprotein, or flaviviral virus E protein, a class II viral E protein. Even more particularly, the invention relates to peptides inhibitory to virus-to-cell fusion and virus entry into animal cells. The invention also contains methods of determining said inhibitors, bindable to regions of the flaviviral E protein complex, (e.g., those of dengue and zika viruses) as candidates for in vivo anti-viral compounds that are also resistant to degradation by peptidases and thus extraordinarily suitable for oral, in addition to other, routes of administration.
    Type: Grant
    Filed: December 6, 2016
    Date of Patent: May 5, 2020
    Assignee: ENNAID THERAPEUTICS, LLC
    Inventors: Scott F. Michael, Sharon Isern
  • Patent number: 10555243
    Abstract: A Discovery Signal (DS) processing method and device is provided. In the method, at least one of the following operations is executed on each component signal of a DS: determining a configuration manner of each component signal; performing pattern modification on each component signal; and determining a transmission manner of each component signal or each pattern-modified component signal.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: February 4, 2020
    Assignee: XI'AN ZHONGXING NEW SOFTWARE CO., LTD.
    Inventors: Hanqing Xu, Yajun Zhao, Linmei Mo
  • Patent number: 10494403
    Abstract: A cyclopeptide is disclosed, which is represented by the following formula (I) or (I?): wherein R1 and G? are defined in the specification. In addition, a pharmaceutical or cosmetic composition comprising the same and a method for preparing the same are also disclosed.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: December 3, 2019
    Assignee: CIPHORE BIOMED TECHNOLOGY LIMITED COMPANY
    Inventor: Po-Ruay Chen
  • Patent number: 10478501
    Abstract: The present invention relates to a pharmaceutical composition of oligopeptides, preferably cyclic oligopeptides, said composition further comprising one or more lipophilic and/or amphiphilic compounds, in the presence or absence of water as the main ingredients, the use of the lipophilic and/or amphiphilic compounds for making pharmaceutical compositions of said oligopeptides, and methods of making said pharmaceutical composition.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: November 19, 2019
    Assignee: Merck Patent GmbH
    Inventors: Simon Goodman, Christiane Amendt, Marcus Eber
  • Patent number: 10471162
    Abstract: Disclosed herein are collagen-targeted imaging agents for positron emission tomography and related imaging methods using the collagen-targeted imaging agents. The collagen-targeted imaging agent is a cyclic polypeptide comprising a cyclic main body, wherein the cyclic main body comprises at least one S—S bond; at least two branches, wherein each of the at least two branches comprises at least three amino acids; and a linker, wherein the linker is capable of linking an imaging reporter.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: November 12, 2019
    Assignee: The General Hospital Corporation
    Inventors: Pauline Desogere, Peter Caravan
  • Patent number: 10464975
    Abstract: The present invention provides methods of designing and making structurally stabilized anti-microbial peptides for the prophylaxis and treatment of infection. Methods are also disclosed for designing stabilized anti-microbial peptides that are selectively lytic/cytotoxic to bacteria, allowing for internal use of anti-microbial peptides without mammalian membrane disruption and cytotoxicity.
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: November 5, 2019
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Rida Mourtada, Gregory H. Bird
  • Patent number: 10450344
    Abstract: Provided are an antibody-binding polypeptide as set forth in any one of SEQ ID NOS: 1 to 18 and an adsorption material of an antibody or antibody derivative in which the antibody-binding polypeptide is immobilized on a water-insoluble carrier. These antibody-binding polypeptide and adsorption material have excellent antibody binding properties and selectivity, and also excellent alkali resistance and temporal stability.
    Type: Grant
    Filed: March 27, 2017
    Date of Patent: October 22, 2019
    Assignee: FUJIFILM Corporation
    Inventor: Koichi Minami
  • Patent number: 10421782
    Abstract: A series of cationic cyclic peptides, useful for the treatment of infectious diseases in both human and veterinary clinical/surgical environment are described herein. The peptides of the invention have a length of 15 to 21 amino acids, and show a sequence A-B-C-D-C?-B?-A?, wherein units A and A? correspond to —NH2 terminal and —COOH terminal regions; units B and B? correspond to cyclizable amino acids containing sulfur; units C and C are sequences of 5 amino acids selected among hydrophobic amino acids, basic amino acids and amino acids forming hydrogen bonds; unit D is a dipeptide consisting of glycine and one basic amino acid. Said peptides show significant antibacterial activity, associated with high stability and resistance to the action of bacterial endopeptidases, and weak or null toxicity against eukaryotic cells.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: September 24, 2019
    Assignee: ICF S.r.l.
    Inventors: Maria Cristina Baroni, Clotilde Silvia Cabassi, Antonello Romani
  • Patent number: 10253067
    Abstract: Methods for treating liquid cancer, determined to lack a p53 deactivation mutation, in a subject are provided. Also provided are peptidomimetic macrocycles for use in treatment of a liquid cancer, determined to lack a p53 deactivation mutation, in a subject.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: April 9, 2019
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Hubert Chen, David Allen Annis, Yong Chang, Manuel Aivado, Karen Olson, Chris Viau
  • Patent number: 10144765
    Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: December 4, 2018
    Assignees: POLYPHOR LTD., UNIVERSITAET ZUERICH
    Inventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
  • Patent number: 10072045
    Abstract: Novel antibacterial lipopeptides, pharmaceutical compositions, and methods for their preparation and use are described.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: September 11, 2018
    Assignee: RAMAPO PHARMACEUTICALS, INC.
    Inventor: Haiyin He
  • Patent number: 10064913
    Abstract: The present invention relates to peptides, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated cytotoxic T cell (CTL) peptide epitopes, alone or in combination with other tumor-associated peptides that serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses. The present invention relates to 95 novel peptide sequences and their variants derived from HLA class I molecules of human tumor cells that can be used in vaccine compositions for eliciting anti-tumor immune responses.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: September 4, 2018
    Assignee: IMMATICS BIOTECHNOLOGIES GMBH
    Inventors: Toni Weinschenk, Jens Fritsche, Steffen Walter, Peter Lewandrowski, Harpreet Singh
  • Patent number: 9896487
    Abstract: Isolated polypeptides that possess an a-sheet structure are disclosed that can be used to treat or diagnose amyloid diseases.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: February 20, 2018
    Assignee: University of Washington Through Its Center For Commercialization
    Inventors: Valerie Daggett, Gene Hopping
  • Patent number: 9856294
    Abstract: The invention relates to novel cyclodecapeptide compounds having formula (I) for use as drugs and, more specifically, for use in the diagnosis, prevention and/or treatment of neurodegenerative diseases, such as Wilson's disease and Alzheimer's disease, and for use in the diagnosis, prevention and/or treatment of poisoning with metal ions, such as copper and mercury ions. The invention also relates to pharmaceutical compositions comprising at least one compound having formula (I) as an active principle.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: January 2, 2018
    Assignees: Commissariat A L'Energie Atomique Et Aux Energies Alternatives, Universite Joseph Fourier
    Inventors: Pascale Delangle, Anaïs Pujol, Pascal Dumy, Olivier Renaudet, Michel Ferrand
  • Patent number: 9782454
    Abstract: This invention relates to novel compositions comprising analogs of naturally occurring polypeptides, wherein the analog comprises an ?-amino acid and at least one ?-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: October 10, 2017
    Assignee: LONGEVITY BIOTECH, INC.
    Inventors: Scott J. Shandler, Samuel H. Gellman
  • Patent number: 9731048
    Abstract: An isolated peptide is disclosed. The peptide comprises a titanium oxide binding amino acid sequence connected to a heterologous biologically active amino acid sequence via a beta sheet breaker linker, wherein: (i) the titanium oxide binding amino acid sequence is selected to bind coordinatively with titanium oxide; (ii) the titanium oxide binding amino acid sequence is selected to induce a beta sheet structure; and (ii) the titanium oxide binding amino acid sequence binds to titanium oxide with a higher affinity than said biologically active amino acid sequence binds to the titanium oxide under physiological conditions. Use of the peptides and titanium devices comprising same are also disclosed.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: August 15, 2017
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Hanna Rapaport, Anna Gittelman
  • Patent number: 9678083
    Abstract: The invention is directed towards novel amino acid based compounds, which may be isotopically enriched, and methods of use of such compounds for characterizing one or more molecules of a sample by mass spectrometry, the method comprising: (a) reacting the one or more molecules with the compound; and (b) characterizing the one or more molecules by mass spectrometry.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: June 13, 2017
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Jarrod A. Marto, Scott B. Ficarro, Manor Askenazi
  • Patent number: 9670262
    Abstract: The present invention relates to modified SAK gene having amino acid SEQ ID 2. The present invention further relates to process for cloning and expressing modified SAK gene fusion protein which imparts improved stability to the heterologous protein of interest. Further the invention relates to process of purification of recombinant heterologous proteins from bacterial inclusion bodies using modified SAK.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: June 6, 2017
    Assignee: LUPIN LIMITED
    Inventors: Shardul Salunkhe, Bhaskarjyoti Prasad, Praveen Muneshwar, Anjali Apte Deshpande, Sriram Padmanabhan
  • Patent number: 9644224
    Abstract: The invention provides methods and compositions for production of a cyclic polymer in a cell free system. In general, the methods of the invention involve ligating first and second recombinant intein domains to a linear synthetic polymer to form a compound containing the structure: D1-X(n)-D2, where D1 is a first catalytic domain of an intein; D2 is a second catalytic domain of an intein; where the second catalytic domain has at its N-terminus a first reactive site for the intein; and X(n) is a polymer of a number n of monomer X, where the polymer N-terminus has a second reactive site for the intein. D1-X(n)-D2 compounds autocatalytically cyclize the X(n) polymer to produce a cyclic polymer. The invention finds use in a variety of drug discovery, clinical and therapeutic applications.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: May 9, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventor: Todd M. Kinsella
  • Patent number: 9637538
    Abstract: A monoclonal chimeric immunoglobulin wherein the heavy chains and the light chains are human by nature in their constant parts, in particular, the heavy chain constant parts are chosen from the group formed of the heavy chain constant parts of an IgA, of an IgG or of an IgM and the light chain constant parts are chosen from the group formed of the kappa chains and the lambda chains, and the light chain and the heavy chain variable parts are chosen from the group formed of monoclonal antibodies specific to monomorphic epitopes of HLA class I antigens and monoclonal antibodies specific to monomorphic epitopes of HLA class II antigens. A process for standardization of the screening and for quantification of anti-HLA antibodies in a liquid medium is also described.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: May 2, 2017
    Assignees: UNIVERSITE PAUL SABATIER TOULOUSE III, CENTRE HOSPITALIER UNIVERSITAIRE DE TOULOUSE, INVIVOGEN
    Inventors: Antoine Blancher, Nicolas Congy, Jean-Gerard Tiraby, Daniel Drocourt
  • Patent number: 9636407
    Abstract: A caspofungin composition includes caspofungin acetate and at least one amino acid, where the composition is a solid. The solid composition may be made by forming a liquid mixture including a solvent, caspofungin acetate and the amino acid(s), and lyophilizing the liquid mixture.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: May 2, 2017
    Assignee: FRESENIUS KABI USA, LLC
    Inventors: John Zhiqiang Jiang, Arunya Usayapant, David Bowman, Keith Kwok, Joel Peterson
  • Patent number: 9630993
    Abstract: The present invention provides cyclic peptides comprising a dimer of peptides, each peptide comprising a sequence corresponding to the HER2 splice variant HER2Delta16, wherein the cyclic peptide is cyclized via a disulfide bond between the peptides and via an amino acid linking the peptides. The invention also provides methods of making antibodies that specifically bind to HER2Delta16 homodimers using said cyclic peptides.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: April 25, 2017
    Assignee: NESTEC S.A.
    Inventor: Nicholas Chi-Kwan Ling
  • Patent number: 9617309
    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
    Inventors: Gregory L. Verdine, Kazuhiro Hayashi
  • Patent number: 9599603
    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
  • Patent number: 9561259
    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
  • Patent number: 9527896
    Abstract: Cross-linked peptides related to human p53 and bind to HMD2 or a family member of HDM2 useful for promoting apoptosis, e.g., in the treatment of and identifying therapeutic agents that binding to HMD2 or a family member of HDM2.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: December 27, 2016
    Assignees: DANA-FARBER CANCER INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Federico Bernal, Loren D. Walensky, Gregory L. Verdine, Stanley J. Korsmeyer
  • Patent number: 9505816
    Abstract: A series of stapled BCL-2 family peptide helices were identified as able to target the survival protein MCL-I with high affinity and a subset with unprecedented selectivity. Agents and methods for selective pharmacologic neutralization of MCL-I are provided for drug discovery and therapeutic uses, including use in overcoming the apoptotic resistance of cancer and other diseases associated with impaired cell death.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: November 29, 2016
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Michelle L. Stewart
  • Patent number: 9505805
    Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: November 29, 2016
    Assignee: SYNERGY PHARMACEUTICALS, INC.
    Inventor: Kunwar Shailubhai
  • Patent number: 9494588
    Abstract: A protein produced by an expression system that includes a nucleic acid sequence that encodes an MHC class I heavy chain. The MHC class I heavy chain comprises an alpha-1 helix and an alpha-2 helix. The nucleic acid sequence has a disulfide bridge formed between the alpha-1 helix and the alpha-2 helix in the MHC class I heavy chain. Amino acid 139 is substituted by a cysteine so as to provide Cys-139. Amino acid 84 is substituted by the cysteine so as to provide Cys-84 or amino acid 85 is substituted by the cysteine so as to provide Cys-85. The disulfide bridge is formed between the alpha-1 helix and the alpha-2 helix in the MHC class I heavy chain between Cys-139 and Cys-84 or between Cys-139 and Cys-85. The protein comprises an anchor element selected from a natural biotinylation sequence, a polyhistidine sequence, or a polyarginine sequence.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: November 15, 2016
    Assignee: JACOBS UNIVERSITY BREMEN GGMBH
    Inventors: Sebastian Springer, Martin Zacharias
  • Patent number: 9493510
    Abstract: The present invention relates to inhibitors of protein-protein interactions (PPI). Specifically, the present invention relates to a structural informatics approach to designing peptidomimetic macrocycles containing an amino acid “warhead” for ligand-directed covalent modification of cysteine and lysine-containing proteins for the treatment of diseases such as cancer. Further included is the targeting of components of the BCL2 signaling pathway, specifically BCL2-A1 and MCL-1.
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: November 15, 2016
    Assignee: NOLIVA THERAPEUTICS LLC
    Inventors: Renato T. Skerlj, Andrew C. Good
  • Patent number: 9399664
    Abstract: The process described herein discloses purification process of a secondary metabolite produced by fermentation route. The process involves selective removal of impurities at various stages of washings, charcoalization followed by crystallization. The product is closely related to class of echinocandins and is found to be potent antifungal compound & a key ingredient in the synthesis of antifungal drugs.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: July 26, 2016
    Assignee: Biocon Limited
    Inventors: Kushal Rastogi, Onkar Prakash Santan, Nitin Sopanrao Patil, Rakesh Bhaiyyaram Mendhe
  • Patent number: 9399077
    Abstract: The present invention concerns compounds and methods of labeling peptides or other molecules with 18F or 19F or any other suitable radionuclide of use, for example, in PET or NMR in vivo imaging. A targeting molecule such as a protein or a peptide is linked to a substituted metallocene complex which is reacted with the 1gF or 19F shortly before performing the PET or NMR in vivo imaging on the patient. The labeled molecule is then used for targeting a cell, tissue, organ or pathogen to be imaged or detected.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: July 26, 2016
    Assignee: Aptenia S.r.l.
    Inventors: Guiseppe Zanoni, Alessio Porta, Marco Pazzi, Andrea Gandini, Wolfgang Karl-Diether Brill
  • Patent number: 9370549
    Abstract: The present invention relates to compositions and methods for treating diseases associated with dyslipidemia, including hypercholesterolemia, hypertriglyceridemia, steatohepatitis, atherosclerosis, obesity, hyperglycemia, metabolic syndrome, and related aspects of and conditions associated with metabolic syndrome. The compositions and methods disclosed herein are useful for regulating the lipid balance (lipid homeostasis) in a subject. Compositions and methods including a Nuclear Transport Modifier may be administered to a subject to modulate the transport of transcription factors, mediated by nuclear import adaptors, into the nucleus of a cell resulting in a decrease in cholesterol and triglyceride levels in the blood and liver, a decrease in atherosclerotic lesion size, a decrease in body weight and in hyperglycemia, a reduction of fatty liver inflammation, and an improvement in liver function.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: June 21, 2016
    Assignee: Vanderbilt University
    Inventors: Jack J. Hawiger, Ruth Ann Veach, Jozef Zienkiewicz, Yan Liu, Robert D. Collins, Amy S. Major
  • Patent number: 9358267
    Abstract: The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: June 7, 2016
    Assignee: Cubist Pharmaceuticals LLC
    Inventors: Thomas J. Kelleher, Jan-Ji Lai, Joseph P. DeCourcey, Paul D. Lynch, Maurizio Zenoni, Auro R. Tagliani
  • Patent number: 9334306
    Abstract: The present invention is directed to C-type lectin-like molecule-1 (CLL1) specific ligand peptides, comprising the amino acid motif LR(S/T), and methods of their use, e.g., for imaging detection for diagnosis of leukemia and the presence of leukemic stem cells (LSCs) and targeted therapy against leukemia mediated at least in part by CLL1-expressing LSCs.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: May 10, 2016
    Assignee: The Regents of the University of California
    Inventors: Chong-xian Pan, Hongyong Zhang
  • Patent number: 9328139
    Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: May 3, 2016
    Assignee: University of South Carolina
    Inventors: Campbell McInnes, Shu Liu
  • Patent number: 9321779
    Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 26, 2016
    Assignee: UniTris Biopharma Co., Ltd.
    Inventors: Fuyao Zhang, Xiaoming Shen, Gaoqiang Hu, Piaoyang Sun
  • Patent number: 9321809
    Abstract: A compound as represented by Formula (I) is provided, wherein groups are defined in the description. The compound is used as HCV protease inhibitor for treating HCV infection.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: April 26, 2016
    Assignee: GINKGO PHARAMA CO., LTD.
    Inventors: Ben Li, Li Chen, Peibing Zhai, Tao Jiang
  • Patent number: 9309288
    Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 12, 2016
    Assignee: ADVANCED ACCELERATOR APPLICATIONS
    Inventors: Annarita Del Gatto, Laura Zaccaro, Carlo Pedone, Michele Saviano