Cyclic Peptides Patents (Class 530/317)
  • Patent number: 10253067
    Abstract: Methods for treating liquid cancer, determined to lack a p53 deactivation mutation, in a subject are provided. Also provided are peptidomimetic macrocycles for use in treatment of a liquid cancer, determined to lack a p53 deactivation mutation, in a subject.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: April 9, 2019
    Assignee: Aileron Therapeutics, Inc.
    Inventors: Hubert Chen, David Allen Annis, Yong Chang, Manuel Aivado, Karen Olson, Chris Viau
  • Patent number: 10144765
    Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: December 4, 2018
    Assignees: POLYPHOR LTD., UNIVERSITAET ZUERICH
    Inventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
  • Patent number: 10072045
    Abstract: Novel antibacterial lipopeptides, pharmaceutical compositions, and methods for their preparation and use are described.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: September 11, 2018
    Assignee: RAMAPO PHARMACEUTICALS, INC.
    Inventor: Haiyin He
  • Patent number: 10064913
    Abstract: The present invention relates to peptides, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated cytotoxic T cell (CTL) peptide epitopes, alone or in combination with other tumor-associated peptides that serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses. The present invention relates to 95 novel peptide sequences and their variants derived from HLA class I molecules of human tumor cells that can be used in vaccine compositions for eliciting anti-tumor immune responses.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: September 4, 2018
    Assignee: IMMATICS BIOTECHNOLOGIES GMBH
    Inventors: Toni Weinschenk, Jens Fritsche, Steffen Walter, Peter Lewandrowski, Harpreet Singh
  • Patent number: 9896487
    Abstract: Isolated polypeptides that possess an a-sheet structure are disclosed that can be used to treat or diagnose amyloid diseases.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: February 20, 2018
    Assignee: University of Washington Through Its Center For Commercialization
    Inventors: Valerie Daggett, Gene Hopping
  • Patent number: 9856294
    Abstract: The invention relates to novel cyclodecapeptide compounds having formula (I) for use as drugs and, more specifically, for use in the diagnosis, prevention and/or treatment of neurodegenerative diseases, such as Wilson's disease and Alzheimer's disease, and for use in the diagnosis, prevention and/or treatment of poisoning with metal ions, such as copper and mercury ions. The invention also relates to pharmaceutical compositions comprising at least one compound having formula (I) as an active principle.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: January 2, 2018
    Assignees: Commissariat A L'Energie Atomique Et Aux Energies Alternatives, Universite Joseph Fourier
    Inventors: Pascale Delangle, Anaïs Pujol, Pascal Dumy, Olivier Renaudet, Michel Ferrand
  • Patent number: 9782454
    Abstract: This invention relates to novel compositions comprising analogs of naturally occurring polypeptides, wherein the analog comprises an ?-amino acid and at least one ?-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: October 10, 2017
    Assignee: LONGEVITY BIOTECH, INC.
    Inventors: Scott J. Shandler, Samuel H. Gellman
  • Patent number: 9731048
    Abstract: An isolated peptide is disclosed. The peptide comprises a titanium oxide binding amino acid sequence connected to a heterologous biologically active amino acid sequence via a beta sheet breaker linker, wherein: (i) the titanium oxide binding amino acid sequence is selected to bind coordinatively with titanium oxide; (ii) the titanium oxide binding amino acid sequence is selected to induce a beta sheet structure; and (ii) the titanium oxide binding amino acid sequence binds to titanium oxide with a higher affinity than said biologically active amino acid sequence binds to the titanium oxide under physiological conditions. Use of the peptides and titanium devices comprising same are also disclosed.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: August 15, 2017
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Hanna Rapaport, Anna Gittelman
  • Patent number: 9678083
    Abstract: The invention is directed towards novel amino acid based compounds, which may be isotopically enriched, and methods of use of such compounds for characterizing one or more molecules of a sample by mass spectrometry, the method comprising: (a) reacting the one or more molecules with the compound; and (b) characterizing the one or more molecules by mass spectrometry.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: June 13, 2017
    Assignee: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Jarrod A. Marto, Scott B. Ficarro, Manor Askenazi
  • Patent number: 9670262
    Abstract: The present invention relates to modified SAK gene having amino acid SEQ ID 2. The present invention further relates to process for cloning and expressing modified SAK gene fusion protein which imparts improved stability to the heterologous protein of interest. Further the invention relates to process of purification of recombinant heterologous proteins from bacterial inclusion bodies using modified SAK.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: June 6, 2017
    Assignee: LUPIN LIMITED
    Inventors: Shardul Salunkhe, Bhaskarjyoti Prasad, Praveen Muneshwar, Anjali Apte Deshpande, Sriram Padmanabhan
  • Patent number: 9644224
    Abstract: The invention provides methods and compositions for production of a cyclic polymer in a cell free system. In general, the methods of the invention involve ligating first and second recombinant intein domains to a linear synthetic polymer to form a compound containing the structure: D1-X(n)-D2, where D1 is a first catalytic domain of an intein; D2 is a second catalytic domain of an intein; where the second catalytic domain has at its N-terminus a first reactive site for the intein; and X(n) is a polymer of a number n of monomer X, where the polymer N-terminus has a second reactive site for the intein. D1-X(n)-D2 compounds autocatalytically cyclize the X(n) polymer to produce a cyclic polymer. The invention finds use in a variety of drug discovery, clinical and therapeutic applications.
    Type: Grant
    Filed: December 10, 2010
    Date of Patent: May 9, 2017
    Assignee: RIGEL PHARMACEUTICALS, INC.
    Inventor: Todd M. Kinsella
  • Patent number: 9636407
    Abstract: A caspofungin composition includes caspofungin acetate and at least one amino acid, where the composition is a solid. The solid composition may be made by forming a liquid mixture including a solvent, caspofungin acetate and the amino acid(s), and lyophilizing the liquid mixture.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: May 2, 2017
    Assignee: FRESENIUS KABI USA, LLC
    Inventors: John Zhiqiang Jiang, Arunya Usayapant, David Bowman, Keith Kwok, Joel Peterson
  • Patent number: 9637538
    Abstract: A monoclonal chimeric immunoglobulin wherein the heavy chains and the light chains are human by nature in their constant parts, in particular, the heavy chain constant parts are chosen from the group formed of the heavy chain constant parts of an IgA, of an IgG or of an IgM and the light chain constant parts are chosen from the group formed of the kappa chains and the lambda chains, and the light chain and the heavy chain variable parts are chosen from the group formed of monoclonal antibodies specific to monomorphic epitopes of HLA class I antigens and monoclonal antibodies specific to monomorphic epitopes of HLA class II antigens. A process for standardization of the screening and for quantification of anti-HLA antibodies in a liquid medium is also described.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: May 2, 2017
    Assignees: UNIVERSITE PAUL SABATIER TOULOUSE III, CENTRE HOSPITALIER UNIVERSITAIRE DE TOULOUSE, INVIVOGEN
    Inventors: Antoine Blancher, Nicolas Congy, Jean-Gerard Tiraby, Daniel Drocourt
  • Patent number: 9630993
    Abstract: The present invention provides cyclic peptides comprising a dimer of peptides, each peptide comprising a sequence corresponding to the HER2 splice variant HER2Delta16, wherein the cyclic peptide is cyclized via a disulfide bond between the peptides and via an amino acid linking the peptides. The invention also provides methods of making antibodies that specifically bind to HER2Delta16 homodimers using said cyclic peptides.
    Type: Grant
    Filed: May 14, 2015
    Date of Patent: April 25, 2017
    Assignee: NESTEC S.A.
    Inventor: Nicholas Chi-Kwan Ling
  • Patent number: 9617309
    Abstract: The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: April 11, 2017
    Assignee: President and Fellows of Harvard College
    Inventors: Gregory L. Verdine, Kazuhiro Hayashi
  • Patent number: 9599603
    Abstract: A method modulating adhesion and migration of at least one cadherin expressing cell includes administering a cadherin modulating agent to the at least one cadherin expressing cell in an amount effective to modulate cell adhesion and migration. The cadherin modulating agent includes a small molecule peptidomimetic of a peptide or cyclic peptide that comprises a cadherin cell adhesion recognition sequence. The cadherin modulating agent can promote or inhibit neurite outgrowth when applied to at least one neuron disposed on a substrate coated with a cadherin molecule.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: March 21, 2017
    Assignee: Case Western Reserve University
    Inventors: Susann Brady-Kalnay, Susan Burden-Gulley
  • Patent number: 9561259
    Abstract: Disclosed herein are novel analogs of cyclosporin, pharmaceutical compositions containing them, and methods for their use in the treatment of dry eye and other conditions.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: February 7, 2017
    Assignee: Allergan, Inc.
    Inventors: Michael E. Garst, William Robert Carling, David Arthur Scowen, Michael E. Stern, Christopher S Schaumburg
  • Patent number: 9527896
    Abstract: Cross-linked peptides related to human p53 and bind to HMD2 or a family member of HDM2 useful for promoting apoptosis, e.g., in the treatment of and identifying therapeutic agents that binding to HMD2 or a family member of HDM2.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: December 27, 2016
    Assignees: DANA-FARBER CANCER INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: Federico Bernal, Loren D. Walensky, Gregory L. Verdine, Stanley J. Korsmeyer
  • Patent number: 9505805
    Abstract: The invention provides novel guanylate cyclase-C agonist peptides and their use in the treatment of human diseases including gastrointestinal disorders, inflammation or cancer (e.g., a gastrointestinal cancer). The peptides can be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The gastrointestinal disorder may be classified as either irritable bowel syndrome, constipation, or excessive acidity etc. The gastrointestinal disease may be classified as either inflammatory bowel disease or other GI condition including Crohn's disease and ulcerative colitis, and cancer.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: November 29, 2016
    Assignee: SYNERGY PHARMACEUTICALS, INC.
    Inventor: Kunwar Shailubhai
  • Patent number: 9505816
    Abstract: A series of stapled BCL-2 family peptide helices were identified as able to target the survival protein MCL-I with high affinity and a subset with unprecedented selectivity. Agents and methods for selective pharmacologic neutralization of MCL-I are provided for drug discovery and therapeutic uses, including use in overcoming the apoptotic resistance of cancer and other diseases associated with impaired cell death.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: November 29, 2016
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Michelle L. Stewart
  • Patent number: 9494588
    Abstract: A protein produced by an expression system that includes a nucleic acid sequence that encodes an MHC class I heavy chain. The MHC class I heavy chain comprises an alpha-1 helix and an alpha-2 helix. The nucleic acid sequence has a disulfide bridge formed between the alpha-1 helix and the alpha-2 helix in the MHC class I heavy chain. Amino acid 139 is substituted by a cysteine so as to provide Cys-139. Amino acid 84 is substituted by the cysteine so as to provide Cys-84 or amino acid 85 is substituted by the cysteine so as to provide Cys-85. The disulfide bridge is formed between the alpha-1 helix and the alpha-2 helix in the MHC class I heavy chain between Cys-139 and Cys-84 or between Cys-139 and Cys-85. The protein comprises an anchor element selected from a natural biotinylation sequence, a polyhistidine sequence, or a polyarginine sequence.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: November 15, 2016
    Assignee: JACOBS UNIVERSITY BREMEN GGMBH
    Inventors: Sebastian Springer, Martin Zacharias
  • Patent number: 9493510
    Abstract: The present invention relates to inhibitors of protein-protein interactions (PPI). Specifically, the present invention relates to a structural informatics approach to designing peptidomimetic macrocycles containing an amino acid “warhead” for ligand-directed covalent modification of cysteine and lysine-containing proteins for the treatment of diseases such as cancer. Further included is the targeting of components of the BCL2 signaling pathway, specifically BCL2-A1 and MCL-1.
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: November 15, 2016
    Assignee: NOLIVA THERAPEUTICS LLC
    Inventors: Renato T. Skerlj, Andrew C. Good
  • Patent number: 9399664
    Abstract: The process described herein discloses purification process of a secondary metabolite produced by fermentation route. The process involves selective removal of impurities at various stages of washings, charcoalization followed by crystallization. The product is closely related to class of echinocandins and is found to be potent antifungal compound & a key ingredient in the synthesis of antifungal drugs.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: July 26, 2016
    Assignee: Biocon Limited
    Inventors: Kushal Rastogi, Onkar Prakash Santan, Nitin Sopanrao Patil, Rakesh Bhaiyyaram Mendhe
  • Patent number: 9399077
    Abstract: The present invention concerns compounds and methods of labeling peptides or other molecules with 18F or 19F or any other suitable radionuclide of use, for example, in PET or NMR in vivo imaging. A targeting molecule such as a protein or a peptide is linked to a substituted metallocene complex which is reacted with the 1gF or 19F shortly before performing the PET or NMR in vivo imaging on the patient. The labeled molecule is then used for targeting a cell, tissue, organ or pathogen to be imaged or detected.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: July 26, 2016
    Assignee: Aptenia S.r.l.
    Inventors: Guiseppe Zanoni, Alessio Porta, Marco Pazzi, Andrea Gandini, Wolfgang Karl-Diether Brill
  • Patent number: 9370549
    Abstract: The present invention relates to compositions and methods for treating diseases associated with dyslipidemia, including hypercholesterolemia, hypertriglyceridemia, steatohepatitis, atherosclerosis, obesity, hyperglycemia, metabolic syndrome, and related aspects of and conditions associated with metabolic syndrome. The compositions and methods disclosed herein are useful for regulating the lipid balance (lipid homeostasis) in a subject. Compositions and methods including a Nuclear Transport Modifier may be administered to a subject to modulate the transport of transcription factors, mediated by nuclear import adaptors, into the nucleus of a cell resulting in a decrease in cholesterol and triglyceride levels in the blood and liver, a decrease in atherosclerotic lesion size, a decrease in body weight and in hyperglycemia, a reduction of fatty liver inflammation, and an improvement in liver function.
    Type: Grant
    Filed: May 6, 2015
    Date of Patent: June 21, 2016
    Assignee: Vanderbilt University
    Inventors: Jack J. Hawiger, Ruth Ann Veach, Jozef Zienkiewicz, Yan Liu, Robert D. Collins, Amy S. Major
  • Patent number: 9358267
    Abstract: The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: June 7, 2016
    Assignee: Cubist Pharmaceuticals LLC
    Inventors: Thomas J. Kelleher, Jan-Ji Lai, Joseph P. DeCourcey, Paul D. Lynch, Maurizio Zenoni, Auro R. Tagliani
  • Patent number: 9334306
    Abstract: The present invention is directed to C-type lectin-like molecule-1 (CLL1) specific ligand peptides, comprising the amino acid motif LR(S/T), and methods of their use, e.g., for imaging detection for diagnosis of leukemia and the presence of leukemic stem cells (LSCs) and targeted therapy against leukemia mediated at least in part by CLL1-expressing LSCs.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: May 10, 2016
    Assignee: The Regents of the University of California
    Inventors: Chong-xian Pan, Hongyong Zhang
  • Patent number: 9328139
    Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D1 groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: May 3, 2016
    Assignee: University of South Carolina
    Inventors: Campbell McInnes, Shu Liu
  • Patent number: 9321779
    Abstract: The present invention relates to an intermediate, as represented by formula (I), for synthesizing caspofungin, and a preparation method thereof. The intermediate enables efficient preparation of caspofungin.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 26, 2016
    Assignee: UniTris Biopharma Co., Ltd.
    Inventors: Fuyao Zhang, Xiaoming Shen, Gaoqiang Hu, Piaoyang Sun
  • Patent number: 9321809
    Abstract: A compound as represented by Formula (I) is provided, wherein groups are defined in the description. The compound is used as HCV protease inhibitor for treating HCV infection.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: April 26, 2016
    Assignee: GINKGO PHARAMA CO., LTD.
    Inventors: Ben Li, Li Chen, Peibing Zhai, Tao Jiang
  • Patent number: 9309288
    Abstract: The present invention is related to new peptide antagonists of ?v?3 receptor, designed on the basis of the crystal structure of integrin ?v?3 in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the ?v?3 receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for ?v?3-targeted therapy and imaging.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 12, 2016
    Assignee: ADVANCED ACCELERATOR APPLICATIONS
    Inventors: Annarita Del Gatto, Laura Zaccaro, Carlo Pedone, Michele Saviano
  • Patent number: 9273098
    Abstract: Lactam-bridged melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes, including obesity, modulation of feeding behavior, related metabolic syndrome, sexual dysfunction, male erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: March 1, 2016
    Assignee: Palatin Technologies, Inc.
    Inventors: Xin Chen, Wei Yang
  • Patent number: 9273099
    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: October 4, 2011
    Date of Patent: March 1, 2016
    Assignees: PRESIDENT AND FELLOWS OF HARVARD COLLEGE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Loren D. Walensky, Stanley J. Korsmeyer, Susan Korsmeyer, Gregory Verdine
  • Patent number: 9233318
    Abstract: A purification method of the compound represented by formula 1 is provided, which includes the following steps: (1) loading crude compound 1 on macroporous adsorbent resin, (2) washing the macroporous adsorbent resin with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water, (3) eluting with an aqueous solution, an organic solvent or a mixture solution of organic solvent and water. The purified compound represented by formula 1 is obtained.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: January 12, 2016
    Assignee: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.
    Inventors: Zhonghao Zhuo, Zhijun Tang, Tianhui Xu, Ming Li, Xiaoming Ji, Xiaoliang Gao
  • Patent number: 9155696
    Abstract: A liquid pharmaceutical composition comprising a biodegradable polymer, polyethylene glycol having a molecular weight of less than 600 Daltons, a pharmaceutically active agent and less than 0.5% of an biologically acceptable organic solvent.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 13, 2015
    Assignee: Novartis AG
    Inventor: Karin Schönhammer
  • Patent number: 9096647
    Abstract: A non-aqueous single pot synthesis of [18F]SFB is set forth. The [18F]SFB produced with this method is then used, for example, to label a peptide or an engineered antibody fragment (diabody) targeting human epidermal growth factor receptor 2 (HER2) as representative examples of labeled compounds for use as an injectable composition to locate abnormal tissue, specifically tumors within an animal or human using a PET scan.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: August 4, 2015
    Assignee: The Regents Of The University Of California
    Inventors: Sebastian Olma, Clifton Kwang-Fu Shen
  • Patent number: 9090655
    Abstract: Disclosed is an antimicrobial peptide having an amino acid sequence of formula presented as (P1)M(nA1X1X2)N(P2)X, wherein P1 is selected from the group consisting of basic amino acids including Arg and Lys; A1 is selected from the group consisting of aromatic amino acids including Trp, Phe and Ala; X1 is selected from the group consisting of basic amino acids or nonpolar amino acids, including Arg, Lys, Val, Leu, Ala and Ile; X2 is selected from the group consisting of basic amino acids or nonpolar amino acids, including Arg, Lys, Val, Leu, Ala and Ile; P2 is selected from the group consisting of basic amino acids including Arg and Lys; and the numbers of M and X are respectively 0˜2; when N>2, A1 is Ala and the Ala residues are less than N?2.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: July 28, 2015
    Assignee: RISE TECHNOLOGY CO., LTD.
    Inventors: Jya-Wei Cheng, Kuo-Chun Huang, His-Tsu Cheng, Hui-Yuan Yu
  • Patent number: 9073963
    Abstract: The invention relates to compositions which are useful for inhibiting prostaglandin F2? receptor. The compositions include, but are not limited to, linear peptides, peptide analogs, and peptidomimetics. Methods of using the compositions of the invention to treat preterm labor and dysmenorrhea are disclosed.
    Type: Grant
    Filed: April 15, 2009
    Date of Patent: July 7, 2015
    Assignees: Universite De Montreal, Theratechnologies, Inc.
    Inventors: Krishna Peri, Felix Polyak, William Lubell, Eryk Thouin, Sylvain Chemtob
  • Patent number: 9067968
    Abstract: The invention provides tight junction protein modulators, compositions comprising the same, and uses thereof. In particular, the invention provides tight junction protein modulators that modulate the second extracellular loop of tight junction proteins, such as occludin or claudin.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: June 30, 2015
    Assignee: The Regents of the University of Colorado, a body corporate
    Inventors: Margaret C. Neville, Neal Beeman, Robert S. Hodges
  • Publication number: 20150148290
    Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 28, 2015
    Inventors: Eric Marsault, Carl St-Louis
  • Patent number: 9040487
    Abstract: The present invention relates to a cyclosporine emulsion containing: i) a cyclosporine ii) a natural oil (long chain triglyceride) iii) a phosphatidylcholine, iv) glycerol, v) a pharmaceutically tolerable alkali salt of a free fatty acid, vi) a medium chain triglyceride-oil vii) optionally, hydrochloric acid or sodium hydroxide for pH adjustment viii) water.
    Type: Grant
    Filed: September 30, 2011
    Date of Patent: May 26, 2015
    Assignee: NEUROVIVE PHARMACEUTICAL AB
    Inventor: Eskil Elmér
  • 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
  • Publication number: 20150133305
    Abstract: The present invention is directed to methods, for example phage display assays, for bioengineering peptides that bind to individual distinct nucleotides. Also provided are peptides engineered by such methods. Specifically, cyclic peptides that bind individual distinct nucleotides are provided herein.
    Type: Application
    Filed: November 7, 2008
    Publication date: May 14, 2015
    Inventors: Mineo Yamakawa, Joseph V. Kosmoski, Deane C. Little
  • Publication number: 20150133630
    Abstract: An object of the present invention is to provide molecules that bind to a target molecule in a pH dependent manner and a screening method for selecting such molecules. Provided is a screening method for selecting peptides that bind to a target molecule at a first pH and do not bind thereto at a second pH, including a step of preparing a peptide library in which each mRNA contains at least one special amino acid that undergoes a pH-dependent change in the charge of the side chain thereof, a step of bringing the peptide library into contact with the target molecule and incubating them under the first pH condition and selecting peptides that bind to the target molecule, and a step of selecting, from the peptides which have bound to the target molecule, peptides that do not bind to the target molecule under the second pH condition.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 14, 2015
    Applicant: The University of Tokyo
    Inventors: Hiroaki Suga, Takeo Iida
  • Publication number: 20150132374
    Abstract: A modified release composition comprising cyclosporin A for oral administration. The composition may comprise a core and a modified release coating, wherein the core comprises a hydrogel-forming polymer matrix and cyclosporin A. The composition may be in the form of a minibead. The compositions provide a pharmacokinetic profile and dissolution profile which provides release of cyclosporin A in the lower GI tract whilst minimising systemic exposure. Also disclosed are uses of the composition in the treatment of conditions affecting the lower GI tract, particularly the colon.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Applicant: SIGMOID PHARMA LIMITED
    Inventors: Ivan Coulter, Vincenzo Aversa, Mónica Rosa
  • Publication number: 20150132220
    Abstract: Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases.
    Type: Application
    Filed: January 8, 2015
    Publication date: May 14, 2015
    Inventors: Philip E. Thorpe, Jin He
  • Publication number: 20150132355
    Abstract: The present invention relates generally to tissue differentiation factor (TDF) analogs. More specifically, the invention relates to structure-based methods and compositions useful in designing, identifying, and producing molecules which act as functional modulators of TDF-like receptors. The invention further relates to methods of detecting, preventing, and treating TDF-associated disorders.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Inventors: William D. Carlson, Peter C. Keck, Michael Sworin, Dattatreyamurty Bosukonda
  • Patent number: 9029501
    Abstract: Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: May 12, 2015
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Thilo J. Heckrodt, Rajinder Singh
  • Publication number: 20150125423
    Abstract: The present invention provides novel peptide immunogens comprising influenza virus matrix 2 protein epitopes and related compositions and methods. The present invention relates to a composition comprising a peptide immunogen useful for the prevention and treatment of an influenza virus-mediated disease. The invention also relates to vaccines, immunogenic products and immunogenic compositions containing the peptide immunogens.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Inventors: Jennifer Mitcham, Matthew Moyle
  • Patent number: 9023808
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: May 5, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Agustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Milsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alverez, Bjorn Olaf Classon, Hans Kristian Wallberg