Polymer Supported Synthesis, E.g., Solid Phase Synthesis, Merrifield Synthesis, Etc. Patents (Class 530/334)
  • Patent number: 10597715
    Abstract: Provided herein are methods and compositions for the sequencing of long nucleic acids, such as DNA. The methods and compositions are suited for the spatial labeling and sequencing of long nucleic acid molecules.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: March 24, 2020
    Assignee: Centrillion Technology Holdings
    Inventors: Wei Zhou, Filip Crnogorac, Glenn McGall, Jian Cao
  • Patent number: 10342846
    Abstract: The invention provides pharmaceutical compositions and method of using the compositions, wherein the compositions comprise liposomes or micelles that contain one or more targeting peptides and/or anticancer drugs. In various embodiments, the components of the liposomes can include a) a phospholipid and optionally a lipid that is not a phospholipid; b) a pegylated lipid; c) a peptide-ethylene glycol (EG)-lipid conjugate wherein the peptide is a targeting ligand, and d) one or more drug-conjugated lipid, encapsulated drugs, or a combination thereof. The peptide-EG-lipid conjugate can be, for example, a compound of Formula (I) or Formula (II). The ethylene glycol (EG) segments of the peptide-EG-lipid conjugate can be, for example, EG6 to about EG36; and the EG segment can be conjugated to one or more lysine moieties.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: July 9, 2019
    Assignee: University of Notre Dame du Lac
    Inventors: Zihni Basar Bilgicer, Jonathan Ashley, Tanyel Kiziltepe Bilgicer, Jared Stefanick, Nathan J. Alves
  • Patent number: 9579382
    Abstract: The present disclosure relates to the use of a recombinant LAG-3 or derivatives thereof in order to boost a monocyte-mediated immune response, in particular to elicit an increase in the number of monocytes in blood. This finds use in the development of novel therapeutic agents for the treatment of an infectious disease or cancer.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: February 28, 2017
    Assignee: IMMUTEP
    Inventor: Frédéric Triebel
  • Patent number: 9211522
    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: September 23, 2014
    Date of Patent: December 15, 2015
    Assignee: CEM Corporation
    Inventors: Jonathan McKinnon Collins, Joseph Joshua Lambert, Michael John Collins
  • Patent number: 9192601
    Abstract: Provided herein are methods and compositions for improving muscle performance and increasing endurance. Agonists of AMP-activated protein kinase (AMPK) and agonists of peroxisome proliferator-activated receptor delta (PPAR?) can be used in such treatments.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: November 24, 2015
    Assignee: Salk Institute for Biological Studies
    Inventors: Ronald M. Evans, Vihang A. Narkar, Reuben J. Shaw, Michael Downes, Ruth T. Yu
  • Patent number: 9180206
    Abstract: This invention provides a pharmaceutical preparation for DDS containing a pharmaceutical agent fixed by bonding to a monomolecular layer that is covalently bonded to a magnetic particle surface, (a) by reacting an alkoxysilane compound with the magnetic microparticle surface by dispersing a magnetic microparticle in a liquid mixture including an epoxy-containing alkoxysilane compound, a silanol condensation catalyst, and a non-aqueous organic solvent; (b) by washing the microparticle surface with an organic solvent to remove remaining surplus alkoxysilane compound for producing an epoxy-containing monomolecular layer that is covalently bonded to the microparticle surface; and (c) by fixing an imino-containing pharmaceutical agent such as a protein, amino acid, enzyme, antibody, antibiotic, antimicrobial, or contrast medium by reaction with the epoxy group.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: November 10, 2015
    Assignee: EMPIRE TECHNOLOGY DEVELOPMENT LLC
    Inventor: Kazufumi Ogawa
  • Patent number: 9164517
    Abstract: A pressure gauge may be coupled to a supply line which carries liquid from a bottle to either one or more mixing vessels and/or one or more reactors in a combinatorial processing tool. A control device may monitor the pressure measured by the pressure gauge, and the control device may be configured to change the pressure supplied to the bottle based on a comparison of the measured pressure to a predetermined pressure value. The control device may adjust the pressure provided to the bottle using a pressure regulator coupled to the pressure source. By changing the pressure provided to the bottle, the control device may maintain a relatively constant flow rate of fluids from the liquid source into one or more mixing vessels and/or the one or more reactors.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: October 20, 2015
    Assignee: Intermolecular, Inc.
    Inventors: Rajesh Kelekar, Gaurav Verma, Kurt Weiner
  • Patent number: 9139437
    Abstract: Embodiments described herein generally relate to the separation of carbon nanotubes by reversible gelation.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: September 22, 2015
    Assignee: Empire Technology Development LLC
    Inventor: Seth Adrian Miller
  • 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: 8940865
    Abstract: Disclosed are two myocardial peptides, whose amino acid sequences are Trp-Ser-Asn-Val-Leu-Arg-Gly-Met-Gly-Gly-Ala-Phe and Lys-Gly-Ala-Trp-Ser-Asn-Val-Leu-Arg-Gly-Met-Gly-Gly-Ala-Phe respectively, wherein the latter can be obtained by extracting from myocardial peptides solution. The myocardial peptides can be used in the produce of a medicament for preventing and/or treating myocardial ischemia.
    Type: Grant
    Filed: July 15, 2008
    Date of Patent: January 27, 2015
    Assignee: Dalian Zhen-Ao Pharmaceutical Co, Ltd.
    Inventors: Yusong Chen, Shu Li, Risheng Wang, Qiang Liang, Zheng Zeng, Xiaohong Qian, Dong Cao, Huimin Liang
  • Publication number: 20140374238
    Abstract: A precision volumetric liquid dispensing instrument is disclosed that includes two pressure sensors and a fluid passageway with a defined volume portion in communication with the two sensors for receiving and distributing liquid in relatively small volumes. One of the pressure sensors is positioned to measure pressure at one portion of the defined volume portion of the fluid passageway and the other of the gas pressure sensors is positioned to measure gas pressure at a different portion of the defined volume portion of the passageway. At least one valve is in communication with the passageway for moving fluids into or out of the defined volume portion of the fluid passageway, and a processor carries out a step selected from the group consisting of (i) calculating the volume of the liquid based upon the measured pressure and (ii) metering a liquid into the defined volume portion of the fluid passageway until the measured pressure indicates that a desired volume of fluid is in the fluid passageway.
    Type: Application
    Filed: June 20, 2013
    Publication date: December 25, 2014
    Inventors: David L. Herman, Joseph J. Lambert
  • 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: 8883964
    Abstract: The invention provides modified collagen and related therapeutic and diagnostic methods.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: November 11, 2014
    Assignee: The Johns Hopkins University
    Inventors: Michael Yu, Jennifer H. Elisseeff, Allen Yi-Lan Wang, Hyeseung Janice Lee, Xiao Mo
  • 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
  • Patent number: 8853325
    Abstract: The present invention is directed to alkanal derivatives of water-soluble polymers such as poly(ethylene glycol), their corresponding hydrates and acetals, and to methods for preparing and using such polymer alkanals. The polymer alkanals of the invention are prepared in high purity and exhibit storage stability.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: October 7, 2014
    Assignee: Nektar Therapeutics
    Inventor: Antoni Kozlowski
  • Publication number: 20140256596
    Abstract: The invention describes peptide ligands specific for human plasma Kallikrein.
    Type: Application
    Filed: October 8, 2012
    Publication date: September 11, 2014
    Applicant: BICYCLE THERAPEUTICS LIMITED
    Inventors: John Tite, Edward Walker, Catherine Stace, Daniel Teufel
  • Patent number: 8828542
    Abstract: Nanoparticles can include a core linked to a polymerizable moiety that can be polymerized, cross-linked or cured. The polymerizable nanoparticles can be included in a composition for a polymerization, cross-linking or curing reaction in an amount and disposition sufficient for inhibiting or preventing volume shrinkage during polymerization, cross-linking or curing reaction. Also, the nanoparticles can be included with monomers, dendrimers, oligomers or polymers in the compositions that can be reacted to form a polymerized, cross-linked or cured product.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: September 9, 2014
    Assignee: Korea University Research and Business Foundation
    Inventor: Dong Hoon Choi
  • Patent number: 8809262
    Abstract: The invention relates to multimeric forms of antimicrobial peptides, for example, defensin peptides. The multimeric forms of defensin peptides possesses antimicrobial activity and may be formulated into antimicrobial compositions, pharmaceutical compositions, eyedrop composition, contact lens solution compositions for coating medical devices and the like. The invention also relates to the use of these multimeric forms of peptides, e.g. multimeric forms of defensin peptides for inhibiting and/or reducing the growth of microorganisms in general, including in a host. The invention further relates to a method of preparing multimers of peptides derived from defensins, for example hBD3.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: August 19, 2014
    Assignees: Singapore Health Service Pte Ltd., Agency for Science, Technology and Research
    Inventors: Roger W. Beuerman, Shouping Liu, Jing Li, Lei Zhou, Chandra Shekhar Verma, Donald Tan
  • Patent number: 8802819
    Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: August 12, 2014
    Assignee: Lonza Ltd.
    Inventors: Fernando Albericio, Michèle Cristau, Matthieu Giraud, Miriam Gongora Benitez, Judit Tulla-Puche
  • Publication number: 20140213509
    Abstract: ?-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa7, Xaa8, Xaa13 and Xaa14 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
    Type: Application
    Filed: June 6, 2012
    Publication date: July 31, 2014
    Applicant: POLYPHOR AG
    Inventors: Daniel Obrecht, Frank Otto Gombert, Johann Zimmermann
  • Patent number: 8791294
    Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D-mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: July 29, 2014
    Assignee: BCN Peptides, S.A.
    Inventors: Llorenç Rafecas Jane, Antoni Riera Escale, Rosario Ramon Albalate, Monica Alonso Xalma
  • Publication number: 20140206841
    Abstract: Apparatus and methods utilizing infrared energy for heating reactions associated with peptide synthesis, such as activation, deprotection, coupling, and cleavage. Thorough agitation of the contents of reaction vessels during heating and real-time monitoring and adjustment of temperature and/or reaction duration are also described. Existing peptide synthesizers may be retrofitted to include an infrared energy source.
    Type: Application
    Filed: January 18, 2013
    Publication date: July 24, 2014
    Applicant: Protein Technologies, Inc.
    Inventors: Mahendra Menakuru, Alexander Waddell
  • 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: 20140154737
    Abstract: The invention provides a cross-linked poly-?-lysine polymer. The poly-?-lysine and cross linker are linked by amide bonds and may the cross linker has at least two functional groups capable of reacting with an alpha carbon amine of poly-?-lysine. The polymer is suitably insoluble in water and other solvents and is provided in particulate form. The invention provides a particulate support comprising the cross-linked poly-?-lysine polymer and the polymer may provide the particle itself or be coated on a particle for example silica. The polymer is useful in a wide range of applications including wound treatment, as a medical diagnostic comprising a particulate support and a functional material bound or retained by the support and solid phase synthesis of peptides, oligonucleotides, oligosaccharides, immobilisation of species, cell culturing and in chromatographic separation.
    Type: Application
    Filed: April 20, 2012
    Publication date: June 5, 2014
    Applicant: SPHERITECH LTD
    Inventor: Donald Wellings
  • Publication number: 20140155565
    Abstract: The present invention relates to a hydrophilic crosslinked polymer, preferably in the form of porous particles, and to the preparation and use thereof. The polymer according to the invention is produced by polymerisation from chain-forming hydrophilic vinyl ethers and crosslinking, preferably heterocyclic divinyl ethers.
    Type: Application
    Filed: February 5, 2014
    Publication date: June 5, 2014
    Applicant: Merck Patent GmbH
    Inventors: Matthias JOEHNCK, Eckhard SABROWSKII
  • Patent number: 8742028
    Abstract: The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: June 3, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Kripa S. Srivastava, Matthew R. Davis
  • 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
  • Publication number: 20140094567
    Abstract: The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided.
    Type: Application
    Filed: October 20, 2011
    Publication date: April 3, 2014
    Applicant: LONZA LTD
    Inventors: Fernando Albericio, Michèle Cristau, Matthieu Giraud, Miriam Gongora Benitez, Judit Tulla-Puche
  • Publication number: 20140086981
    Abstract: Peptides of general formula (I): R1—Wn—Xm-AA1-AA2-AA3-AA4-AA5-AA6-Yp—Zq—R2 their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, a preparation process, cosmetic or pharmaceutical compositions which contain them and their use in the treatment and/or care of conditions, disorders and/or diseases which improve or are prevented by PGC-1? modulation.
    Type: Application
    Filed: March 23, 2012
    Publication date: March 27, 2014
    Inventors: José María García Antón, Nuria Almiñana Domenech, Antonio Vicente Ferrer Montiel
  • Patent number: 8669356
    Abstract: The invention provides a universal linker capable of synthesizing nucleic acid having a phosphate group at the 3? terminal, a universal support carrying the linker, and a synthesis method of nucleic acid using the universal support. The linker for solid phase synthesis of nucleic acid contains a compound represented by at least one of the following formulae wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: March 11, 2014
    Assignees: Nitto Denko Corporation, National University Corporation Nagoya University
    Inventors: Yoshihiro Hayakawa, Masaki Tsukamoto, Kenjiro Mori, Kenjiro Minomi, Eri Maeta, Tatsuya Konishi
  • Publication number: 20140058062
    Abstract: [Technical Promblem] To provide a method for manufacturing that enables to obtain a targeted glycopeptide harboring a sialyl sugar chain in high yield without decomposing sialic acid at a non-reducing terminal of sugar chain when the glycopeptide is synthesized by a Boc solid phase synthesis method. [Solution to Problem] The present invention is characterized in that the Boc-sialylglycosylated amino acid derivative used in Boc solid phase synthesis method is one where the carboxyl group of the sialic acid at the sugar chain non-reducing terminal is protected with a phenacyl group.
    Type: Application
    Filed: March 5, 2012
    Publication date: February 27, 2014
    Applicant: Glytech, Inc.
    Inventors: Yasuhiro Kajihara, Masumi Murakami, Kazuyuki Ishii
  • Publication number: 20140051828
    Abstract: The present invention relates to a method for preparing a peptide having a stable, internally constrained alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region and a method of stabilizing an alpha-helical, beta-sheet/beta-turn, 310-helical, or pi-helical region within a peptide structure. The resulting peptides and methods of using them are also disclosed.
    Type: Application
    Filed: April 23, 2013
    Publication date: February 20, 2014
    Inventor: New York University
  • Patent number: 8652484
    Abstract: The present invention relates to methods and compositions for pretargeting delivery of therapeutic agents. In preferred embodiments, the pretargeting method comprises: a) administering a bispecific antibody with a first binding site for a disease-associated antigen and a hapten on a targetable construct; b) administering a targetable construct comprising at least one therapeutic agent. In preferred embodiments, the bispecific antibody is made by the dock-and-lock (DNL) technique. In a more preferred embodiment, the targetable construct comprises one or more SN-38 moieties.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Immunomedics, Inc.
    Inventors: William J. McBride, Christopher A. D'Souza, Chien-Hsing Chang, David M. Goldenberg
  • Patent number: 8623995
    Abstract: Polypeptides labelled with a donor and acceptor pair of dyes selected from a dibenzorhodamine dye and a diamino-benzophenoxazine dye are peptide conjugates which are useful for intracellular and bead-based assays with fluorescence detection. Peptide conjugates with a caspase-recognition site undergo cleavage into peptide fragments which may be detected, located, and quantitated by the changes in fluorescence. Intracellular cleavage of peptide conjugates is correlated with apoptosis.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: January 7, 2014
    Assignee: Applied Biosystems, LLC
    Inventors: Xiongwei Yan, Sheri Miraglia, Pau Miau Yuan
  • Publication number: 20130345397
    Abstract: A method for preparing a peptide or peptides containing a dicarba bridge, comprising: (i) providing a reactable peptide having at least two complementary metathesisable groups or two or more reactable peptides having at least two complementary metathesisable groups between them; (ii) subjecting the reactable peptide or reactable peptides to metathesis to form a reactable peptide or peptides having at least one unsaturated dicarba bridge; and (iii) adding one or more further amino acids to one or both ends of at least one of the reactable peptides.
    Type: Application
    Filed: May 25, 2011
    Publication date: December 26, 2013
    Inventor: Andrea Robinson
  • Publication number: 20130338044
    Abstract: A bifunctional linker and method of use is provided that has a spacer molecule with a functional group on one end configured to couple to the surface of a substrate and a function group on the other end that is configured couple to a biomolecule and methods of use. The preferred bifunctional linker has a poly(ethylene glycol) spacer ranging from 3 to 20 ethylene glycol units that has a silane functional group to react with a substrate and an azide functional group that can couple to a biomolecule that includes an alkyne group. The preferred linker can produce an azide-derivatized glass surface in one step and the azide functional group of the spacer can in sequence conjugate with a biomolecule using click chemistry, which can be conducted at low temperature and in aqueous solution.
    Type: Application
    Filed: June 10, 2013
    Publication date: December 19, 2013
    Inventors: Jiayu Liao, Yongfeng Zheng
  • Publication number: 20130324699
    Abstract: A new method of synthesizing GLP-1 peptide is devised.
    Type: Application
    Filed: April 29, 2013
    Publication date: December 5, 2013
    Applicant: LONZA AG
    Inventor: Lonza AG
  • Publication number: 20130289241
    Abstract: A method for preparing exenatide by solid-phase synthesis, including: 1) mixing an Fmoc-Rink amide AM resin with a deprotecting agent to obtain a Rink amide AM resin; 2) condensing an Fmoc-Ser(tBu)-OH with the Rink amide AM resin to obtain an Fmoc-Ser(tBu)-Rink amide AM resin; 3) repeating the Fmoc deprotection and the condensation between an amino acid and a polypeptide on the resin, and condensing an amino acid with a polypeptide on the resin from the C-terminal to the N-terminal, to form a polypeptide resin; and 4) separating the polypeptide and the resin on the polypeptide resin.
    Type: Application
    Filed: April 26, 2012
    Publication date: October 31, 2013
    Applicant: SHANGHAI AMBIOPHARM, INC.
    Inventors: Juncai BAI, Guoqing ZHANG, Ruoping ZHANG
  • Patent number: 8569452
    Abstract: The present invention relates to novel phalloidin derivatives and their fluorescent dye conjugates. These new compounds may be used in studies of actin dynamics in living systems. The present invention also relates to methods for preparing such compounds. The synthesis routes combine solid-phase and solution phase peptide synthesis, and has great advantage for efficient preparation of a diverse library of the phalloidin derivatives, especially for the synthesis of phalloidin.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: October 29, 2013
    Assignee: American Peptide Company, Inc.
    Inventors: Baosheng Liu, Jianheng Zhang
  • Patent number: 8552133
    Abstract: The present invention relates to a controlled metathesis-driven polymerization process which is particularly useful for the synthesis of biological polymers such as peptides and polymers. The invention also provides metathesisable supports, groups and linkers for use in the process.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: October 8, 2013
    Assignees: Syngene Limited, Monash University
    Inventors: Andrea Robinson, Rebecca Dee Garland
  • Patent number: 8546532
    Abstract: The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: October 1, 2013
    Assignee: Declion Pharmaceuticals, Inc.
    Inventors: Dustan Bonnin, Eric Zanelli, Thomas Mathers
  • Patent number: 8546533
    Abstract: The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 1, 2013
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de Montpellier 1, Universite Jagellone, Universite Montpellier 2—Sciences et Techniques
    Inventors: Jean Martinez, Pawel Zajdel, Maciej Pawlowski, Gilles Subra
  • Publication number: 20130184436
    Abstract: An apparatus is provided for the semi-automated parallel synthesis of multiple peptides. The apparatus includes an array of nozzles, each positioned above or adjacent a separate reaction container, two or more liquid reservoirs, each reservoir coupled to the liquid dispenser(s), and base chamber(s) connected to the reaction containers for removing liquid there from. The addition and removal of liquids may be controlled by programmable electromagnetic valves. The apparatus may also be used for other parallel solid phase reactions. A method is also provided for synthesizing multiple polypeptides or other macromolecules, for example by using the above apparatus, wherein multiple common steps are performed automatically while reactants are added manually.
    Type: Application
    Filed: October 11, 2012
    Publication date: July 18, 2013
    Applicant: Nanjingjinsirui Science & Technology Biology Corporation
    Inventor: Nanjingjinsirui Science & Technology Biology Corporation
  • Publication number: 20130172529
    Abstract: The invention relates to a method for obtaining thymosins and/or the pharmaceutically acceptable salts thereof by means of solid-phase synthesis on polymeric supports, which comprises the steps of linearly synthesizing the thymus-derived peptides in solid phase, incorporating at least one Thr or Ser in the sequence, in pseudoproline dipeptide form, obtaining the thymosins by treating the peptidyl resin with trifluoroacetic acid, and purifying the thymosins by RP-HPLC. The present invention also protects the isolated and/or purified compound obtained by means of said method and also the use thereof in the preparation of a medicinal product.
    Type: Application
    Filed: November 9, 2012
    Publication date: July 4, 2013
    Applicant: BCN PEPTIDES S.A.
    Inventor: BCN Peptides S.A.
  • Publication number: 20130143251
    Abstract: The present invention discloses a process for preparing ubiquinated peptide conjugates comprising a ubiquitin peptide residue UR attached at its C-terminus to a substrate peptide via a native isopeptide bond, this process comprising combining Native Chemical Ligation (NCL) and solid phase peptide synthesis (SPPS). Further are disclosed ubiquinated peptide conjugates containing a native isopeptide bond, as well as various uses thereof.
    Type: Application
    Filed: June 1, 2011
    Publication date: June 6, 2013
    Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITY
    Inventors: Ashraf Brik, Ajish Kumar, Leslie Erlich, Liat Spasser
  • Patent number: 8415454
    Abstract: A process for manufacturing a cyclic peptide which comprises providing a cyclic peptide bonded to a Merrifield-type resin and cleaving the cyclic peptide from the Merrifield type resin by transesterification.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: April 9, 2013
    Assignee: Solvay (Société Anonyme)
    Inventors: Satish Joshi, Shima Joshi, Bernhard Freimann, Manuel Ramos, Roland Callens
  • Patent number: 8410247
    Abstract: Water soluble reagents and methods for the formation of an amide bond between a phosphinothioester and an azide in an aqueous medium. The phosphinothioester is generated using a water-soluble phosphinothiol reagent. This reaction allows formation of an amide bond between a wide variety of chemical species including amino acids, peptides or protein fragments in an aqueous solution. Of particular interest, this reaction allows for the formation of an amide bond in a physiological setting. In a specific embodiment, this invention provides reagents and methods for peptide ligation in an aqueous medium. The reaction eliminates the need for a cysteine residue and is traceless leaving no residual atoms in the ligated peptide product.
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: April 2, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Ronald T. Raines, Annie Tam, Matthew B. Soellner
  • Patent number: 8378072
    Abstract: The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the modulation of unwanted immune responses, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: February 19, 2013
    Assignee: Declion Pharmaceuticals, Inc.
    Inventor: Dustan Bonnin
  • Publication number: 20130041132
    Abstract: The present invention discloses latent thioester functionalities attached to the C-terminus of a first polypeptide, or a first fragment thereof having a Cys residue at its N-terminus, and a process using this functionality for the preparation of polypeptide thioesters, in particular of ubiquitin thioesters, this process comprising preparing a polypeptide or a fragment thereof, being attached to a latent thioester functionality, which can then be ligated with a second polypeptide fragment, followed by selective activation of the latent thioester functionality group, to provide the requested polypeptide thioester. There are also provided the polypeptides obtained by this method, specific unnatural amino acids useful to be incorporated within the polypeptide thioesters, and kits for preparing them.
    Type: Application
    Filed: February 9, 2011
    Publication date: February 14, 2013
    Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITY
    Inventors: Ashraf Brik, Mahmood Haj-Yahya, Ajish Kumar, Leslie Erlich, Liat Spasser
  • Patent number: 8314208
    Abstract: A method is disclosed for carrying out peptide synthesis comprising deprotecting an Fmoc-protected amino acid with piperazine while applying microwave irradiation to the deprotection reaction.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: November 20, 2012
    Assignee: CEM Corporation
    Inventor: Jonathan M. Collins