Containing Only Normal Peptide Links In The Ring, I.e., Homodetic Cyclic Peptides Patents (Class 530/321)
  • Patent number: 11008366
    Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: May 18, 2021
    Assignee: AILERON THERAPEUTICS, INC.
    Inventors: Vincent Guerlavais, Noriyuki Kawahata
  • Patent number: 10703780
    Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
    Type: Grant
    Filed: September 10, 2018
    Date of Patent: July 7, 2020
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Vincent Guerlavais, Noriyuki Kawahata
  • Patent number: 10689419
    Abstract: Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R1-R7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described.
    Type: Grant
    Filed: September 11, 2018
    Date of Patent: June 23, 2020
    Assignee: ONKURE, INC.
    Inventors: Anthony D. Piscopio, Xiaoyong Fu, Feng Shi, Huayan Liu, Zhifeng Li
  • Patent number: 10357537
    Abstract: The present invention relates to a pharmaceutical composition comprising a cyclotide for use in immune suppression as well as to a method for immune suppression comprising the step of administering an effective amount of a pharmaceutical composition comprising such a cyclotide to a subject in need thereof. The present invention also relates to a pharmaceutical composition comprising a cyclotide for use in treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation. Likewise, the present invention also relates to a method for treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: July 23, 2019
    Assignees: Medizinische Universitat Wien, Universitatsklinikum Freiburg
    Inventors: Christian Werner Gruber, Carsten Gruendemann
  • Patent number: 9988433
    Abstract: The present disclosure provides a method of covalently modifying a biological macromolecule, the method comprising subjecting a reaction mixture comprising: (a) a biological macromolecule comprising one or more thiol groups; and (b) a molecule comprising one or more olefin or alkyne moieties to a radical reaction under conditions sufficient to produce the covalently modified biological macromolecule. The present disclosure also provides a method of covalently modifying a biological macromolecule, the method comprising subjecting a reaction mixture comprising: (a) a molecule comprising one or more thiol groups; and (b) a biological macromolecule comprising one or more olefin or alkyne moieties to a radical reaction under conditions sufficient to produce the covalently modified biological macromolecule. The present disclosure further provides a covalently modified biological macromolecule prepared by any of the disclosed methods.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: June 5, 2018
    Assignee: Mosaic Biosciences, Inc.
    Inventors: Alexei Kazantsev, Peter D. Mariner, Martin Stanton
  • Patent number: 9511024
    Abstract: The present invention provides new amino lipids and a convenient method for synthesizing these compounds. These (cationic) amino lipids have good properties as transfection agents. The method is an economic versatile two step synthesis allowing the preparation of various amino lipids thus leading to the assembly of a combinatorial library of transfection agents. Moreover, the present invention provides lipid particles (liposomes) containing said amino lipids and their use for delivering bioactive agents into cells. The invention encompasses also the use of lipid particles containing the cationic amino lipids as medicament.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: December 6, 2016
    Assignee: INCELLA GMBH
    Inventors: Gary Davidson, Pavel Levkin, Linxian Li, Yi Su, David Zahner
  • Patent number: 9505804
    Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: November 29, 2016
    Assignee: AILERON THERAPEUTICS, INC.
    Inventors: Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
  • Patent number: 9453052
    Abstract: The present invention relates to a pharmaceutical composition comprising a cyclotide for use in immune suppression as well as to a method for immune suppression comprising the step of administering an effective amount of a pharmaceutical composition comprising such a cyclotide to a subject in need thereof. The present invention also relates to a pharmaceutical composition comprising a cyclotide for use in treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation. Likewise, the present invention also relates to a method for treating or preventing a disorder selected from the group consisting of (i) an autoimmune disorder; (ii) a hypersensitivity disorder; and (iii) a lymphocyte-mediated inflammation.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: September 27, 2016
    Assignees: Universitatsklinikum Freiburg, Medizinische Universitat Wien
    Inventors: Christian Werner Gruber, Carsten Gruendemann
  • Publication number: 20150139950
    Abstract: The disclosure concerns the use of cyclophilin inhibitors in the treatment of chronic Hepatitis C virus infection.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventor: Claudio Avila
  • Patent number: 9035022
    Abstract: Cyclic CRF antagonist peptides having improved properties of “drugability”. The peptides are 33 residues in length with a lactam bond between the residues in position 22 and 25; however, they may be N-terminally shortened by up to 3 residues.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: May 19, 2015
    Assignee: Salk Institute for Biological Studies
    Inventor: Jean E. F. Rivier
  • Patent number: 9029321
    Abstract: Methods and compositions are presented for use in diagnostic, imaging or targeting of therapeutic agents to treat obesity/adiposity-associated disorders, where such as compositions and methods identify and use peptides to selectively target adipose tissue stromal cells in mammals, both in vitro and in vivo.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: May 12, 2015
    Assignee: Board of Regents of the University of Texas
    Inventors: Mikhail G. Kolonin, Alexes Daquinag, Yan Zhang
  • Publication number: 20150126450
    Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.
    Type: Application
    Filed: April 16, 2013
    Publication date: May 7, 2015
    Inventors: Kent Kirshenbaum, Paul Michael Levine, Michael John Garabedian
  • Publication number: 20150125491
    Abstract: The present invention relates to novel cyclic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
    Type: Application
    Filed: March 28, 2013
    Publication date: May 7, 2015
    Applicant: Aurigene Discovery Technologies Limited
    Inventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra
  • Publication number: 20150119318
    Abstract: The present invention provides an isolated peptide having an amino acid residue sequence that comprises at least one human cytomegalovirus glycoprotein B (HCMV-gB) sequence segment, each HCMV-gB sequence segment consisting of at least 8 and not more than 60 consecutive amino acid residues from residues 146 to 315, residues 476 to 494 of SEQ ID NO: 1, or from a sequence variant of residues 146 to 315 or 476 to 494 of SEQ ID NO: 1 that has at least 70% sequence identity thereto. The peptides of the invention are useful for treating, preventing, or inhibiting a herpesvirus (e.g., Herpes Simplex Virus-1, Human Cytomegalovirus, and the like) infection in a subject.
    Type: Application
    Filed: July 9, 2014
    Publication date: April 30, 2015
    Applicant: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
    Inventors: Lilia I. Melnik, Robert F. Garry, Cindy A. Morris
  • Publication number: 20150119551
    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: Application
    Filed: September 11, 2014
    Publication date: April 30, 2015
    Applicants: President and Fellows of Harvard College, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Federico BERNAL, Loren D. WALENSKY, Gregory L. VERDINE
  • Publication number: 20150118213
    Abstract: The present invention is directed to compounds useful in stabilizing thrombin activity, thrombin compositions comprising the compounds, methods of using the compounds and methods of identifying compounds capable of stabilizing thrombin activity. The compounds are preferably isolated peptides comprising or interacting with the gamma loop of thrombin.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 30, 2015
    Inventors: Nadav Orr, Yair Pilpel, Sivan Doron
  • Publication number: 20150111815
    Abstract: The present invention relates to a compound of formula (I): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; a method for treating or preventing a viral infection using the same.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 23, 2015
    Inventors: Zhuang SU, Zhengyu LONG, Zhennian HUANG, Suizhou YANG
  • Patent number: 9012604
    Abstract: The present invention relates to a triazanonane derivative indicated by the chemical formula 1 below, or a pharmaceutically acceptable salt thereof, and a method for preparing same, and the triazanonane derivative according to the present invention forms a complex with a metal-fluoride and displays an effect of increasing the labeling efficiency up to 78-90% when labeling F-18, thus enabling use in various radioactive medicine labeling (In the chemical formula 1, R1, R2, A. E. X, n and m are as defined in the present description.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: April 21, 2015
    Assignee: Snur & DB Foundation
    Inventors: Jae Min Jeong, Dinesh Shetty, Dong Soo Lee, June-Key Chung, Myung Chul Lee
  • Publication number: 20150104415
    Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis C virus infection.
    Type: Application
    Filed: April 11, 2012
    Publication date: April 16, 2015
    Applicants: DEBIOPHARM INTERNATIONAL SA, NOVARTIS AG
    Inventors: Claudio Avila, Rafael Crabbe
  • Publication number: 20150105335
    Abstract: The present invention provides, among other things, novel peptides and compositions for treating disease.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 16, 2015
    Inventor: Richard Franklin
  • Publication number: 20150087577
    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: Application
    Filed: September 24, 2014
    Publication date: March 26, 2015
    Applicants: Universität Zürich, POLYPHOR LTD.
    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
  • Patent number: 8987414
    Abstract: Provided herein are peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: March 24, 2015
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Vincent Guerlavais, Christopher R. Conlee, Scott Paul Lentini
  • Publication number: 20150080549
    Abstract: An object of the present invention is to provide methods of discovering drugs effective for tough targets, which have conventionally been discovered only with difficulty. The present invention relates to novel methods for cyclizing peptide compounds, and novel peptide compounds and libraries comprising the same, to achieve the above object.
    Type: Application
    Filed: December 28, 2012
    Publication date: March 19, 2015
    Inventors: Shiori Kariyuki, Takeo Iida, Miki Kojima, Ryuichi Takeyama, Mikimasa Tanada, Tetsuo Kojima, Hitoshi Iikura, Atsushi Matsuo, Takuya Shiraishi, Takashi Emura, Kazuhiko Nakano, Koji Takano, Kousuke Asou, Takuya Torizawa, Ryusuke Takano, Nozomi Hisada, Naoaki Murao, Atsushi Ohta, Kaori Kimura, Yusuke Yamagishi, Tatsuya Kato
  • Patent number: 8981049
    Abstract: Improved methods of native chemical ligation are provided. The methods involve reacting a thioacid (e.g. a peptide thioacid) with an aziridinyl compound (e.g. an aziridinyl peptide) under mild conditions without the use of protecting groups, and without requiring that a cysteine residue be present in the ligation product. Initial coupling of the thioacid and the aziridinyl compound yields a ligation product which contains an aziridinyl ring. Subsequent opening of the aziridinyl ring (e.g. via a nucleophilic attack) produces a linearized and modified ligation product.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: March 17, 2015
    Assignee: Washington State University
    Inventor: Philip Garner
  • Publication number: 20150065433
    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: Application
    Filed: November 6, 2014
    Publication date: March 5, 2015
    Applicant: ALLERGAN, INC.
    Inventors: Catherine Simone Victoire Frydrych, William Robert Carling, Michael E. Garst, Michael E. Stern, Christopher S. Schaumburg
  • Publication number: 20150065434
    Abstract: Provided herein are cyclic peptide inhibitors of lysine-specific demethylase 1. These cyclic peptides have the potential to treat cancer, diabetes, cardiovascular disease, and neurological disorders.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Patrick M. WOSTER, Isuru R. KUMARASINGHE
  • Publication number: 20150056165
    Abstract: The present invention relates to novel cyclosporine analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.
    Type: Application
    Filed: August 26, 2014
    Publication date: February 26, 2015
    Inventors: Yat Sun Or, Guoqiang Wang, Jiang Long, In Jong Kim
  • Publication number: 20150056209
    Abstract: Provided herein are peptide mimotopes that are useful for generating antibodies and in the preparation of vaccines and diagnostics for treating and diagnosing coronary artery disease.
    Type: Application
    Filed: April 18, 2013
    Publication date: February 26, 2015
    Inventors: Joseph L. Witztum, Sotirios Tsimikas, Christoph Binder, Shahzada Amir
  • Publication number: 20150057234
    Abstract: Disclosed is a hydrate of a compound as shown in Formula I. In formula I, R represents H or a cation capable of forming a pharmaceutically acceptable salt. The mass percentage of water in the hydrate is more than 8%. The hydrate has good stability. Moreover, disclosed are a preparation method and a use thereof.
    Type: Application
    Filed: March 29, 2013
    Publication date: February 26, 2015
    Inventors: Shidong Liu, Zhaoli Zhang, Xiusheng Wang, Xiao Zhang, Zhijun Tang, Xiaoming Ji
  • Publication number: 20150057235
    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: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Kunwar SHAILUBHAI, Gary S. JACOB
  • Publication number: 20150051153
    Abstract: An environmentally sensitive membrane binding polypeptide, pH (low)-sensitive membrane peptide (pHLIP) has improved insertion kinetics balanced with solubility to selectively target acidic tissues.
    Type: Application
    Filed: July 13, 2011
    Publication date: February 19, 2015
    Inventors: Yana K. Reshetnyak, Oleg A. Andreev, Donald M. Engelman
  • Publication number: 20150050256
    Abstract: The invention provides lantibiotics geobacillin I and geobacillin II from Geobacillus thermodenitrificans, compositions comprising the lantibiotics, and methods of use of the lantibiotics.
    Type: Application
    Filed: February 7, 2013
    Publication date: February 19, 2015
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Wilfred A. van der Donk, Neha Garg, Yuki Goto, Weixin Tang
  • Publication number: 20150045290
    Abstract: Biosurfactants produced by a strain of Bacillus sp and to uses thereof. A composition comprising the biosurfactants, and a method for producing the biosurfactants. A method for obtaining a biosurfactant, and a device for implementing the method. The production of biopesticides or biosurfactants for the phytosanitary industry, and in the fields of the food, cosmetics, pharmaceutical and oil industries and the environment.
    Type: Application
    Filed: October 3, 2012
    Publication date: February 12, 2015
    Applicant: Universite Lille 1-Sciences ET Technologies-USTL
    Inventors: Francois Coutte, Philippe Jacques, Didier Lecouturier, Jean-Sebastien Guez, Pascal Dhulster, Valerie Leclere, Max Bechet
  • Publication number: 20150045302
    Abstract: A product comprising a peptide that comprises a motif selected from a group consisting of isoDGR, NGR and DGR, wherein the peptide cyclised by joining the N- and C-termini of its main chain and wherein the cyclic peptide is joined to albumin.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 12, 2015
    Inventors: Angelo Corti, Flavio Curnis
  • Publication number: 20150045293
    Abstract: Described herein are melanocortin analogs having enhanced activity and transport.
    Type: Application
    Filed: March 12, 2013
    Publication date: February 12, 2015
    Inventor: Kenneth Allen Gruber
  • Publication number: 20150045288
    Abstract: The present invention relates to anti-contaminant composition comprising a cell-free fermentation product of one or more Bacillus subtilis strains (e.g., selected from the group consisting of: 22C-P1, 15A-P4, 3A-P4, LSSA01, ABP278, BS 2084 and BS 18); wherein said fermentation product comprises one or more compounds selected from the group consisting of: a lipopeptide, a polyketide, a bacillibactin, a bacilysin, an anticapsin, a plantazolicin, a LCI, a homologue of a plantazolicin and a homologue of a LCI. In addition, the present invention further relates to methods of preparing the compositions, methods of using the composition, products comprising the composition and uses thereof.
    Type: Application
    Filed: February 20, 2013
    Publication date: February 12, 2015
    Inventors: Tina Mygind, George H. Weber, Connie Benfeldt, Ashley Ann Hibberd, Rebecca Joy Landrum, Panagiotis Chanos, Gregory R. Siragusa, Matthew James Hundt
  • Publication number: 20150045310
    Abstract: Compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. Pharmaceutical compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. A method for treating cancer is provided.
    Type: Application
    Filed: February 4, 2013
    Publication date: February 12, 2015
    Inventors: A. James Link, Siyan Zhang
  • Publication number: 20150038404
    Abstract: This invention relates to novel macrocyclic compounds (e.g., those delineated in the formulae herein), pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the protease elastase.
    Type: Application
    Filed: February 22, 2013
    Publication date: February 5, 2015
    Inventors: Hendrik Luesch, Valerie J. Paul, Lilibeth A. Salvador
  • Publication number: 20150038403
    Abstract: The present invention provides mimetics of erythropoietin that bind to the erythropoietin receptor and that are suitable for use in pharmaceutical compositions. The present invention also provides methods of treatment using the mimetics of erythropoietin as well as methods of making the mimetics of erythropoietin.
    Type: Application
    Filed: May 11, 2012
    Publication date: February 5, 2015
    Inventors: Hendrik Mario Geysen, Cyrille V. Gineste
  • Publication number: 20150038673
    Abstract: The present invention relates to novel ?-AR homologous cyclopeptide-mutants comprising only two cysteine residues able to form an intramolecular linkage, to linear peptides that can form these cyclopeptide-mutants and to nucleic acid molecules encoding these cyclopeptide-mutants and linear peptides. Moreover, vectors and recombinant host cells comprising said nucleic acid molecule and a method for producing the disclosed cyclopeptide-mutants are provided. Further provided is a composition comprising the peptides, nucleic acid molecules, vectors or host cells of the invention. The present invention also relates to therapeutic and diagnostic means, methods and uses taking advantage of the peptides of the invention and to means, methods and uses for detecting anti-.beta.-adrenergic receptor antibodies like anti-?1-adrenergic receptor antibodies.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 5, 2015
    Inventors: Roland Jahns, Valerie Jahns, Martin Lohse, Viacheslav Nikolaev
  • Publication number: 20150038430
    Abstract: The present invention provides biologically active peptidomimetic macrocycles for the treatment of cell proliferative disorders such as cancer and immunoproliferative disease.
    Type: Application
    Filed: July 8, 2014
    Publication date: February 5, 2015
    Inventors: Huw M NASH, David Allen ANNIS, Rosana KAPELLER-LIBERMANN, Tomi K. SAWYER, Noriyuki KAWAHATA, Jiawen HAN
  • Publication number: 20150037302
    Abstract: The present invention relates to a method of producing biosurfactants, such as surfactin, comprising culturing at least one biosurfactant-producing microbe in a liquid culture medium comprising vinasse as a carbon source. Methods of using the crude biosurfactant containing culture broth in tertiary oil recovery and as antibacterial compositions in tertiary oil recovery are also described. Methods of using the culture broth residue after isolation of the biosurfactants as fertilizer and compositions for this use are also described.
    Type: Application
    Filed: January 25, 2013
    Publication date: February 5, 2015
    Inventors: Michael Paul Bralkowski, Sarah Ashley Brooks, Stephen M. Hinton, David Matthew Wright, Shih-Hsin Yang
  • Publication number: 20150038672
    Abstract: Targeting agents are derived from coupling together formed imaging amino acids or formed multi-modal, multi-chelating metal, multi-dye imaging agents, or combinations of these, that may be conjugated directly, or activated, or attached to linkers to which targeting groups, such as peptides, proteins, antibodies, aptamers, or small molecule inhibitors, may be conjugated in the final steps of the synthesis to form a wide variety of TMIAs.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Applicant: Rochester Institute of Technology
    Inventors: Hans F. Schmitthenner, Stephanie Beach, Chelsea Weidman, Taylor Barrett
  • Publication number: 20150030669
    Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.
    Type: Application
    Filed: March 11, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
  • Publication number: 20150030566
    Abstract: Compositions containing one or more tyrocidines, tryptocidines, phenycidines and/or gramicidin S, or derivatives and analogues thereof, are described for controlling antimicrobial growth on plants, plant material or plant growth media, and methods for controlling or preventing the growth of microbial pathogens, and in particular fungal pathogens, on plants, plant parts and plant material are described herein. The active agents used to control these pathogens are tyrocidines, tryptocidines, phenycidines and/or gramicidin S, or derivatives, analogues or modifications thereof.
    Type: Application
    Filed: August 22, 2013
    Publication date: January 29, 2015
    Inventors: Marina Rautenbach, Abré De Beer, Anscha Mari Troskie, Johan Arnold Vosloo
  • Publication number: 20150023917
    Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis B and Hepatitis D virus infections.
    Type: Application
    Filed: July 28, 2014
    Publication date: January 22, 2015
    Applicant: NOVARTIS AG
    Inventor: Nikolai Naoumov
  • Publication number: 20150024998
    Abstract: In one aspect, the invention relates to isolated compounds useful as antifungal agents, for example, compounds having a structure represented by a formula: wherein R1 is hydrogen or hydroxyl; wherein R2 is hydrogen, a-xylose or ?-xylose; and wherein R3 and R4 are each hydrogen or together oxygen, or a pharmaceutically acceptable salt thereof; methods of isolating and purifying same; pharmaceutical compositions comprising same; agricultural compositions comprising same; and methods of treating and/or preventing fungal infections using same. In one aspect, R2 is not hydrogen or ?-xylose when R1 is hydroxyl and R3 and R4 are together oxygen. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 20, 2012
    Publication date: January 22, 2015
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Eric W. Schmidt, Joseph O. Falkinham, Peter W. Jeffs
  • Patent number: 8933195
    Abstract: The invention provides histone deacetylase (HDAC) inhibitors shown as Formula I, where R1 to R8 are as defined in the specification. The invention also provides methods for synthesis of these compounds and applications of these compounds in preparing pharmaceuticals for preventing or treating mammal diseases related to the dysregulation of HDAC.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: January 13, 2015
    Assignees: Nanjing Yoko Biomedical R & D Ltd., Nanjing Xingang Medical Co., Ltd., Nanjing Yoko Pharmaceutical Co., Ltd.
    Inventors: Sheng Jiang, Shang Li, Zhiyi Yao, Yiwu Yao, Feng Zhang, Yang Chao, Hai Ye, Min Chen
  • Publication number: 20150011465
    Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula I: The peptoids demonstrate antimicrobial activity and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals including humans where microbial invasion is involved. The present cyclic and linear peptoids are particularly valuable as their effect is rapid, broad in spectrum and mostly indifferent to resistance provoked by standard antibiotics.
    Type: Application
    Filed: September 9, 2014
    Publication date: January 8, 2015
    Inventors: Kent Kirshenbaum, Sung Bin Shin
  • Publication number: 20150011728
    Abstract: The present invention relates to peptides having one or more stable, reversibly and internally-constrained HBS ?-helices.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 8, 2015
    Applicant: NEW YORK UNIVERSITY
    Inventors: Paramjit S. Arora, Stephen E. Miller