Synthesis Of Peptides Patents (Class 530/333)
  • Patent number: 10308677
    Abstract: An improved method for coupling carboxylic acids and amines is disclosed that includes the steps of combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid, a carbodiimide, an activator additive, and a base, and carrying out the activation and coupling at a temperature greater than 30° C.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: June 4, 2019
    Assignee: CEM Corporation
    Inventors: Jonathan M. Collins, Sandeep Kumar Singh
  • Patent number: 10005755
    Abstract: The invention relates to a process for the preparation of a ketone of a general formula 1 with X being Cl or Br, in particular with X being Cl, with Y being F, Cl, Br, I or H, in particular with Y being F, comprising the steps of: activation of a carboxylic acid by using a peptide coupling agent, coupling of the activated carboxylic acid with a malonic acid derivative providing a ?-ketoester precursor and converting the ?-ketoester precursor to the ketone of the general formula 1.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: June 26, 2018
    Assignee: CORDON PHARMA INTERNATIONAL GMBH
    Inventors: Ilia Freifeld, Gerhard Jas, Kurt Kesseler, Richard Robert Dauer
  • Patent number: 9982035
    Abstract: This invention relates pro-coagulant serpin molecules engineered by modification of the P4, P2, P1 and/or P1? residues within the reactive center loop (RCL) to display increased specificity for anticoagulant proteases. These modified serpin molecules may be useful in therapy, for example as pro-coagulants for the treatment of bleeding.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: May 29, 2018
    Assignee: Cambridge Enterprise Limited
    Inventors: James Andrew Huntington, Stéphanie Polderdijk, Trevor Baglin
  • Patent number: 9976166
    Abstract: The present invention relates to binding fusion protein compositions comprising targeting moieties linked to extended recombinant polypeptide (XTEN), binding fusion protein-drug conjugate compositions, and XTEN-drug conjugate compositions, isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of using such compositions in treatment of diseases, disorders, and conditions.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: May 22, 2018
    Assignee: AMUNIX OPERATING INC.
    Inventors: Volker Schellenberger, Joshua Silverman, Chia-wei Wang, Benjamin Spink, Willem P. C. Stemmer, Nathan C. Geething
  • Patent number: 9605026
    Abstract: The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: March 28, 2017
    Assignees: NEW YORK UNIVERSITY, THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION, THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Paramjit S. Arora, Quintin Pan, Anna Mapp
  • Patent number: 9493509
    Abstract: The present invention provides novel peptidomimetic macrocycles and methods for their preparation and use, as well as amino acid analogs and macrocycle-forming linkers, and kits useful in their production. Macrocycles of the invention include triazole moieties that crosslink amino acid side chains. The cross links can stabilize a secondary structure of a peptidomimetic macrocycle, such as an ?-helix.
    Type: Grant
    Filed: April 2, 2015
    Date of Patent: November 15, 2016
    Assignee: AILERON THERAPEUTICS, INC.
    Inventor: Huw M. Nash
  • Patent number: 9416156
    Abstract: Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising ?-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the ?-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with ?-amino acid residues, and the ?-amino acid residues are distributed in a repeating pattern.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: August 16, 2016
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: William S. Horne, Samuel H. Gellman, Lisa M. Johnson
  • Patent number: 9347961
    Abstract: A test kit for the quantitative determination of narcotic drugs comprising (A) series of sealed vessels, each vessel containing a deuterium free isotopologue of a narcotic drug in exactly defined concentrations and quantities, wherein the isotopologue differs from vessel to vessel and—wherein the quantities of the isotopologue differ from vessel to vessel or are the same for all vessels; and/or (B) series of sealed vessels, each vessel containing in exactly defined concentrations and quantities the same isotopologue in quantities which differ from vessel to vessel; wherein the free isotopologues are selected from narcotic drugs; prodrugs, salts, solvates, hydrates and polymorphs and contain at least three stable isotopes selected from the group consisting of 13C, 15N and 18O in the molecule with a degree of labeling of at least 95 mol-%; the use of the test kit and a method for quantitatively determining narcotic drugs.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: May 24, 2016
    Assignee: CHIRON AS
    Inventors: Morten Salihi Karlsen, Huiling Liu, Jon Eigill Johansen
  • Patent number: 9330932
    Abstract: Some embodiments include a method in which a mixture of polynucleotide structures comprises a set of surface shapes. Surface shapes of some polynucleotide structures are complementary to surface shapes of other polynucleotide structures. The complementary surface shapes lock together along interfaces between adjacent polynucleotide structures to incorporate the polynucleotide structures into a polynucleotide mask. The polynucleotide mask is used during fabrication of features associated with a semiconductor substrate. Some embodiments include a method in which a semiconductor substrate comprises registration regions configured to adhere individual polynucleotide structures to specific locations of the semiconductor substrate. The adhered polynucleotide structures are incorporated into a polynucleotide mask which is used during fabrication of features associated with the semiconductor substrate.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: May 3, 2016
    Assignee: Micron Technology, Inc.
    Inventors: Scott E. Sills, Gurtej S. Sandhu
  • Patent number: 9284348
    Abstract: Disclosed are a carrier for use for separation purpose and a method for separation of a compound which enable a chemical reaction to be performed in a liquid phase, enable a compound of interest to be separated from the liquid phase after the completion of the reaction readily, enable the separated compound to be evaluated by structural analysis or the like while the compound being bound to the carrier, and enable the compound to be separated from the carrier readily. A carrier for separation which has a reaction site capable of reacting with other compound on a benzene ring, and a long-chain group having a specified carbon atom(s) at each of the ortho-position and the para-position of the reaction site through an oxygen atom.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: March 15, 2016
    Assignee: JITSUBO Co., Ltd.
    Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
  • Patent number: 9267123
    Abstract: Disclosed herein are methods and compositions for correction and/or mutation of genes associated with Parkinson's Disease as well as clones and animals derived therefrom.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: February 23, 2016
    Assignees: Sangamo BioSciences, Inc., Whitehead Institute for Biomedical Research
    Inventors: Rudolf Jaenisch, Josee Laganiere, Frank Soldner, Lei Zhang
  • Patent number: 9133237
    Abstract: The present invention relates to a method for preparing a cyclic peptide with antiparasite activity and anticancer activity. The invention also relates to this peptide as an antiparasite agent, for example in the treatment of toxoplasmosis and as an anticancer agent. The invention also relates to the use of this cyclic peptide for treating organs ex vivo before transplantation.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: September 15, 2015
    Assignees: UNIVERSITE JOSEPH FOURIER (GRENOBLE 1), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, (INSERM) INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE
    Inventors: Yung-Sing Wong, Mohamed-Ali Hakimi, Alexandre Bougdour, Hervé Pelloux, Danièle Maubon
  • Patent number: 9115179
    Abstract: The present invention relates to methods of preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof. Particularly, the present invention relates to a process for the synthesis of ?-turn cyclic peptidomimetic compounds of formula I: where R1, R2, R3, R4, R5, R6, R7, L2, X, Y and n are as defined in the specification. The present invention provides a more efficient route for preparing ?-turn cyclic peptidomimetic compounds and intermediates thereof.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: August 25, 2015
    Assignee: Mimetogen Pharmaceuticals Inc.
    Inventors: Teresa Lama, Jeanick Pascal
  • Patent number: 9035021
    Abstract: The invention provides cyclo[{4-(NH2—C2H4—NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Benzyl)-Phe], optionally in protected form, or a pharmaceutically acceptable salt or complex thereof, which has interesting pharmaceutical properties.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: May 19, 2015
    Assignee: Novartis AG
    Inventors: Rainer Albert, Wilfried Bauer, David Bodmer, Christian Bruns, Ivo Felner, Heribert Hellstern, Ian Lewis, Mark Meisenbach, Gisbert Weckbecker, Bernhard Wietfeld
  • Patent number: 9029507
    Abstract: The present invention relates to analytical methods such as molecular weight determination of polypeptide, in particular Glatiramer acetate. The present invention further relates to an improved process for preparation of polypeptides or pharmaceutically acceptable salts thereof, particularly Glatiramer acetate also known as Copolymer-1. The present invention further relates to characterization of Glatiramer acetate by peptide mapping.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: May 12, 2015
    Assignee: USV Limited
    Inventors: Dhananjay Govind Sathe, Avinash Venkatraman Naidu, Subramanian Sundaram, Anindya Sibnath Bhattacharyya, Rakesh Shekhawat, Divya Lal Saksena, Sukumar Ramanujam, Sanjay Vyankatrao Patil
  • Patent number: 9029503
    Abstract: The invention mainly relates to a method for manufacturing a polypeptide of formula: X1—X?—X2??(III) X1 and X2 each representing a peptide fragment, and X? representing an amino acid residue comprising a thiol function, said method comprising at least one step of ligation reaction between a polypeptide of formula: X1—N(CH2CH2SH)2??(I) and a polypeptide of formula: H—X?—X2.??(II) The invention also relates to the polypeptides of formula (I) themselves and the method for obtaining them, as well as resin supports suitable for obtaining them.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: May 12, 2015
    Assignees: Centre National de la Recherche Scientifique, Institut Pasteur de Lille
    Inventors: Oleg Melnyk, Reda Mhidia, Julien Dheur, Nathalie Ollivier
  • Patent number: 8981055
    Abstract: The present invention relates to an improved process for the preparation of Micafungin.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: March 17, 2015
    Assignee: Xellia Pharmaceuticals APS
    Inventors: Solvi Gunnes, Harald Halvorsen
  • Patent number: 8980845
    Abstract: The present invention relates to a process for the enzymatic production of a dipeptide composition from a cyanophycin (CGP) or CGP-like polymer preparation by degrading the polymer preparation with an CGPase, a CGPase particularly adapted for said process, and the use of cyanophycin (CGP) or CGP-like polymers or fragments thereof, notably a dipeptide composition obtained by the process as defined above, as pharmaceutical composition, medicament, or as food or feed substitute.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: March 17, 2015
    Assignee: Westfälische Wilhelms-Universität Münster
    Inventors: Ahmed Sallam, Alexander Steinbüchel
  • 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
  • Patent number: 8980581
    Abstract: The invention provides certain embodiments relating to methods and compositions for incorporating non-natural amino acids into a polypeptide or protein by utilizing a mutant or modified aminoacyl-tRNA synthetase to charge the non-natural amino acid to a the corresponding tRNA. In certain embodiments, the tRNA is also modified such that the complex forms strict Watson-Crick base-pairing with a codon that normally forms wobble base-pairing with unmodified tRNA/aminoacyl-tRNA synthetase pairs.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: March 17, 2015
    Assignee: California Institute of Technology
    Inventors: Pin Wang, Inchan Kwon, Soojin Son, Yi Tang, David Tirrell
  • Patent number: 8975370
    Abstract: The present invention relates to a chimeric inhibitor protein of a protease comprising an inhibiting polypeptidic sequence and at least one polypeptidic sequence of a substrate-enzyme interaction site specific for a protease. Other objects of the invention are to provide a purified and isolated DNA sequence encoding the chimeric inhibitor protein of a protease, an expression vector characterized in that it comprises said purified and isolated DNA sequence, a eukaryotic or prokaryotic host cell transformed with this expression vector and a method of producing a chimeric inhibitor protein.
    Type: Grant
    Filed: April 5, 2004
    Date of Patent: March 10, 2015
    Assignee: Universite de Lausanne
    Inventors: David Deperthes, Sylvain Cloutier
  • Patent number: 8969516
    Abstract: This invention relates to a method of hydrolysis of the peptide bond between R1 and B in a specific designed amino acid sequence R1BXJZR3R2, where R1 represents a polypeptide of interest, R2 represents a sequence capable of specific binding to another component or molecule or another domain which needs to be cleaved, R3 represents an optional short peptide sequence, B represents a residue capable of accepting an acyl group, J represents a residue capable of metal ion binding, and X and Z represent amino acid residues, wherein the said method is based on a novel molecular mechanism of peptide bond hydrolysis, occurring in a specific complex of this metal ion with the BXJZ sequence. This method can be used to remove BXJZR3R2 domains in recombinant polypeptides, such as sequences capable of specific binding to another component or molecule to yield pure, unmodified R1 polypeptides of interest.
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: March 3, 2015
    Assignee: Instytut Biochemii I Biofizyki Pan
    Inventors: Wojciech Bal, Edyta Kopera, Artur Krezel, Aleksandra Wyslouch-Cieszynska
  • Publication number: 20140357841
    Abstract: A method for stabilizing an alpha helix of a polypeptide includes steps of: (1) connecting an unnatural amino acid to an amino terminus of the polypeptide and end-capping via an acetylation; (2) processing a product of the step (1) with a thiolene reaction and obtaining a polypeptide compound having a modification of thioether side chains; (3) oxidizing the polypeptide compound having the modification of the thioether side chains, and obtaining a polypeptide compound having a modification of R-configured sulfoxide side chains or S-configured sulfoxide side chains; (4) separating and purifying a product of the step (3), and obtaining the modification of the R-configured sulfoxide side chains. CD diagrams show that, via chiral sulfoxide side chains, the method has good performance on stabilizing the alpha helix of the polypeptide and good tolerance to a polypeptide sequence.
    Type: Application
    Filed: January 26, 2014
    Publication date: December 4, 2014
    Applicant: Peking University Shenzhen Graduate School
    Inventors: Zigang Li, Qingzhou Zhang
  • Patent number: 8895696
    Abstract: Methods for building peptide chains containing sulfonyl modified amines at the N-terminus, or, within amino acid side chains, of a growing peptide in a solid-phase peptide synthesis are described. Further, compositions having a sulfonyl modified amine attached to the N-terminus, or within an amino acid side chain, of a polypeptide containing three or more amino acid residues are described.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: November 25, 2014
    Assignee: The University of Toledo
    Inventors: Steven J. Sucheck, Rommel S. Talan, Partha Karmakar
  • Patent number: 8895694
    Abstract: The invention relates to protracted Glucagon-Like Peptide-1 (GLP-1) derivatives and therapeutic uses thereof. The GLP-1 derivative of the invention comprises a modified GLP-1(7-37) sequence having a total of 2-12 amino acid modifications, including Glu22 and Arg26, and being derivatised with an albumin binding residue or pegylated in position 18, 20, 23, 30, 31, 34, 36, 37, or 39. These compounds are useful in the treatment or prevention of diabetes type 2 and related diseases. The compounds are potent, stable, have long half-lives, a high affinity of binding to albumin, and/or a high affinity of binding to the extracellular domain of the GLP-1 receptor (GLP-1R), all of which is of potential relevance for the overall aim of achieving long-acting, stable and active GLP-1 derivatives with a potential for once weekly administration.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: November 25, 2014
    Assignee: Novo Nordisk A/S
    Inventors: Jane Spetzler, Lauge Schäffer, Jesper Lau, Thomas Kruse, Patrick William Garibay, Steffen Reedtz-Runge, Henning Thøgersen, Ingrid Pettersson
  • Patent number: 8877252
    Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: November 4, 2014
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Steven G. Wright, Troy Christensen, Thean Yeoh, Michael E. Rickey, Joyce M. Hotz, Rajesh Kumar, Henry R. Costantino
  • Patent number: 8871904
    Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: October 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, Minzhang Chen, John E. Cochran, Adam Looker, Valdas Jurkauskas
  • Patent number: 8871903
    Abstract: Methods to synthesize self-assembling peptides embedded with complex organic electronic subunits are provided.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: October 28, 2014
    Assignee: The Johns Hopkins University
    Inventors: John D. Tovar, Allix M. Sanders
  • Publication number: 20140315791
    Abstract: Described is a method of fabricating biologically active, unnatural polypeptides. The method includes the steps of selecting a biologically active polypeptide or biologically active fragment thereof having an amino acid sequence comprising ?-amino acid residues, and fabricating a synthetic polypeptide that has an amino acid sequence that corresponds to the sequence of the biologically active polypeptide, but wherein about 14% to about 50% of the ?-amino acid residues found in the biologically active polypeptide or fragment of step (a) are replaced with ?-amino acid residues, and the ?-amino acid residues are distributed in a repeating pattern.
    Type: Application
    Filed: January 8, 2014
    Publication date: October 23, 2014
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: William S. Horne, Samuel H. Gellman, Lisa M. Johnson
  • Patent number: 8865658
    Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one aromatic amine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one alkylated amine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: October 21, 2014
    Assignee: AMBRX, Inc.
    Inventors: Zhenwei Miao, Junjie Liu, Thea Norman
  • Patent number: 8859731
    Abstract: A method of selectively introducing a substituent into a protein proximal to a binding site on the protein for a homing peptide, comprising: (a) contacting the protein with a compound comprising a homing peptide having the ability to bind to the binding site of the protein; and (b) allowing a moiety on the protein proximal to the binding site to react with the compound comprising the homing peptide, thereby to transfer the substituent G onto the protein.
    Type: Grant
    Filed: April 12, 2011
    Date of Patent: October 14, 2014
    Assignee: Novo Nordisk A/S
    Inventors: Mikael Kofod-Hansen, Henning Ralf Stennicke, Soeren Oestergaard, Henrik Oestergaard
  • Patent number: 8859730
    Abstract: A chemoselective chemical ligation method is disclosed. The method joins two peptide segments efficiently to produce a larger peptide or protein, by generating a natural peptide bond (Xaa-Ser and Xaa-Thr) at the ligation site (Xaa represents any 5 amino acid). The method requires two steps (FIG. 1 (a)): a) reacting the starting peptide(s) to form an acetal intermediate with an acetal group at the ligation site; b) converting said acetal intermediate to a desired peptide or protein with said natural peptide bond.
    Type: Grant
    Filed: August 12, 2009
    Date of Patent: October 14, 2014
    Inventor: Xuechen Li
  • Patent number: 8859727
    Abstract: A nanoparticle-polypeptide complex comprising a bioactive polypeptide in association with a nanoparticle, wherein the bioactive polypeptide is modified by the addition of a chemical moiety that facilitates cellular uptake of the protein. The polypeptide can be a protein or a peptide. In some embodiments, the amino acid sequence of the protein or peptide is derived from the amino acid sequence of a tumor suppressor gene product.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: October 14, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Jacki Lin, Ralph Arlinghaus, Tong Sun, Lin Ji, Bulent Ozpolat, Gabriel Lopez-Berestein, Jack A. Roth
  • Publication number: 20140296479
    Abstract: The present invention is characterized by a D-Aptamer-Like Peptide (D-Aptide) or retro-inverso Aptide which specifically binds to a target comprising: (a) a structure stabilizing region comprising parallel, antiparallel or parallel and antiparallel D-amino acid strands with interstrand noncovalent bonds; and (b) a target binding region I and a target binding region II comprising randomly selected n and m D-amino acids, respectively, and coupled to both ends of the structure stabilizing region. The D-Aptide or retro-inverso Aptide has the sequence of the same or opposite direction to L-Aptide, wherein the stability to proteases is improved while maintaining the affinity to a target compared with L-Aptide. The D-Aptide of the present invention has substantially the same target affinity and a remarkably improved stability compared with L-Aptide which is different from a general technical knowledge.
    Type: Application
    Filed: April 6, 2012
    Publication date: October 2, 2014
    Applicant: GWANGJU INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Sang-Yong Jon, Sung-Hyun Kim
  • Patent number: 8846862
    Abstract: An instrument and method for accelerating the solid phase synthesis of peptides are disclosed. The method includes the steps of deprotecting a protected first amino acid linked to a solid phase resin by admixing the protected linked acid with a deprotecting solution in a microwave transparent vessel while irradiating the admixed acid and solution with microwaves, activating a second amino acid, coupling the second amino acid to the first acid while irradiating the composition in the same vessel with microwaves, and cleaving the linked peptide from the solid phase resin by admixing the linked peptide with a cleaving composition in the same vessel while irradiating the composition with microwaves.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: September 30, 2014
    Assignee: CEM Corporation
    Inventors: Jonathan McKinnon Collins, Joseph Joshua Lambert, Michael John Collins
  • Publication number: 20140275481
    Abstract: Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Mark David Simon, Bradley L. Pentelute, Andrea Adamo, Patrick Louis Heider, Klavs F. Jensen
  • Patent number: 8816050
    Abstract: A method is provided for the synthesis of glycopeptides using a sugar assisted ligation strategy, wherein an N-terminal peptide portion in the form of a thioester is coopled with a C-terminal peptide portion bearing a carbohydrate moiety comprising a thiol group.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: August 26, 2014
    Inventors: Chi-Huey Wong, Ashraf Brik, Yu-Ying Yang, Simon Ficht, Richard Payne
  • Patent number: 8802818
    Abstract: Prostaglandin-F2 alpha (PGF2?) receptor (FP) modulators of formula I, as well as the use of PGF2? receptor modulators for the treatment of conditions associated with FP activity such as preterm labor and colorectal cancer, are disclosed.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: August 12, 2014
    Inventors: William D. Lubell, Sylvain Chemtob, Terence E. Hebert, Audrey Claing, Stephane Laporte, Carine B. Bourguet, Eugenie Goupil, Xin Hou, Danae Tassy
  • Patent number: 8796418
    Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.
    Type: Grant
    Filed: September 18, 2008
    Date of Patent: August 5, 2014
    Assignees: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
    Inventors: Loren D. Walensky, Gregory L. Verdine, Susan Korsmeyer
  • Patent number: 8791234
    Abstract: Peptide ligands for transporting therapeutic agents across the intestinal epithelial barrier that ordinarily are inadequately absorbed and must be delivered by alternative means, which contain an isolated amino acid sequence wherein at least one pair of amino acids are of an opposite charge and the pair members are separated by a spacer of 1-12 amino acid residues including at least one hydrophobic amino acid, and wherein the length of the amino acid sequence is greater than 5 and less than 20 amino acids. Pharmaceutical compositions for gastro-intestinal delivery and methods for the gastrointestinal delivery of poorly absorbed therapeutic agents are also disclosed.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 29, 2014
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Patrick J. Sinko, Xiaoping Zhang, Zoltan Szekely
  • Patent number: 8791236
    Abstract: A method for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.
    Type: Grant
    Filed: January 28, 2014
    Date of Patent: July 29, 2014
    Assignee: Novo Nordisk A/S
    Inventors: Caspar Christensen, Rune Severinsen, Anders Klarskov Petersen, Steffen Kidal, Claus U. Jessen, Peter Madsen, Henrik Valore, Tina Moeller Tagmose, Jan Lindy Soerensen
  • Publication number: 20140206596
    Abstract: The present invention discloses a design for a molecular delivery vehicle capable of delivering a molecular payload to a target cell and its intracellular compartments. Also disclosed are highly pH-sensitive nanoconstruct that takes advantage of the requirement of cationic charge for internalization of CPPs to mask the non-specific internalization, compositions containing nanoconstruct, and methods for forming the same.
    Type: Application
    Filed: January 16, 2014
    Publication date: July 24, 2014
    Applicant: University of Southern California
    Inventors: Wei-Chiang SHEN, Jennica KRANKEL, Likun FEI
  • Patent number: 8765910
    Abstract: The invention relates to a method for producing C-terminal amidated dibasic or polybasic peptides, consisting in reacting two peptides in the presence of trypsin biologically active enzymes and, if necessary, in purifying the thus obtainable compounds of formula (I) by means of protein chemistry.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: July 1, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Sebastian Rissom, Paul Habermann, Christophe Salagnad, Frank Zocher, Laure Landric-Burtin
  • Patent number: 8759259
    Abstract: Embodiments of the invention are directed to a one-bead-two-compound method for the creation of encoded cyclic peptoid libraries. This scheme is useful for the creation of cyclic peptoid microarrays since only the cyclic peptoid, not the linear encoding molecule, contains an attachment residue and thus can be spotted onto an activated substrate.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: June 24, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Yong-Uk Kwon, Thomas Kodadek
  • Publication number: 20140170064
    Abstract: Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [125I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Charles Andrew Boswell, Leslie A. Khawli, Jan Marik, Simon Williams
  • Publication number: 20140162339
    Abstract: The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein said peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting said peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized ?-helical structure; and (2) contacting said crosslinked stabilized ?-helical structure with MDM2.
    Type: Application
    Filed: October 31, 2013
    Publication date: June 12, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: GREGORY L. VERDINE, CHRISTIAN E. SCHAFMEISTER
  • Patent number: 8748575
    Abstract: Therapeutic peptides having guanylyl cyclase C agonist activity are disclosed. The therapeutic peptides are analogues of the E. coli STa peptide with non-natural amino acid, isosteric or D-amino acid substituents. The therapeutic peptides are useful in the treatment of chronic ideopathic constipation, inflammatory bowel disease, and other diseases. Pharmaceutical compositions comprising the therapeutic peptides are also disclosed.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: June 10, 2014
    Assignee: Combimab, Inc.
    Inventors: Henry Wolfe, Reinhard Ebner
  • Patent number: 8741576
    Abstract: Heteroclitic analogs of Class I epitopes are prepared by providing conservative or semi-conservative amino acid substitutions at positions 3 and/or 5 and/or 7 of these epitopes. The analogs are useful in eliciting immune responses with respect to the corresponding wildtype epitopes.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: June 3, 2014
    Assignee: Epimunne Inc.
    Inventors: Shabnam Tangri, Alessandro Sette, Glenn Ishioka, John D. Fikes
  • Patent number: 8735354
    Abstract: Disclosed herein are peptide amphiphiles for use in producing a natural endothelium mimicking nanomatrix. The disclosed natural endothelium mimicking nanomatrix can be used to coat medical devices such as vascular stents to promote endothelializaiton and inhibit restenosis and thrombosis. 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: Grant
    Filed: July 2, 2009
    Date of Patent: May 27, 2014
    Assignee: UAB Research Foundation
    Inventors: Ho-Wook Jun, Meenakshi Kushawaha, Brigitta C. Brott, Peter Anderson
  • Patent number: RE46830
    Abstract: A novel method for synthesizing a Hirulog peptide is devised.
    Type: Grant
    Filed: March 17, 2015
    Date of Patent: May 8, 2018
    Assignee: Polypeptide Laboratories Holding (PPL) AB
    Inventors: Anne-Sophie Droz, Jasmine Schnidrig, Nicole Studer, Stéphane Varray, Corinne Wenger, Oleg Werbitzky