Tripeptides, E.g., Tripeptide Thyroliberin (trh), Melanostatin (mif), Etc. Patents (Class 530/331)
  • THERAPEUTIC AGENT FOR PULMONARY SMALL CELL CARCINOMA
    Publication number: 20120232248
    Abstract: The invention aims to clarify further functions of a TCTA protein-derived peptide and provide a novel application of the peptide. The invention provides a therapeutic agent for pulmonary small cell carcinoma or a cell growth inhibitor of pulmonary small cell carcinoma, comprising any peptide described in SEQ ID NOs 1 to 5.
    Type: Application
    Filed: January 25, 2010
    Publication date: September 13, 2012
    Applicant: TOKYO WOMEN'S MEDICAL UNIVERSITY
    Inventors: Shigeru Kotake, Yuki Nanke, Manabu Kawamoto, Toru Yago, Hisashi Yamanaka
  • NOVEL CONJUGATES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    Publication number: 20120225089
    Abstract: Provided herein are cryptophycin conjugates and compositions containing them. Methods of making and using such compounds also are provided.
    Type: Application
    Filed: December 20, 2011
    Publication date: September 6, 2012
    Applicant: SANOFI
    Inventors: Hervé BOUCHARD, Marie-Priscille BRUN, Alain COMMERCON, Jidong ZHANG
  • Inhibitors of the Trypsin-Like Site of the Proteasome and Methods of Use Thereof
    Publication number: 20120214732
    Abstract: The present invention is an inhibitor of the trypsin-like ?2/?2i sites of the proteasome. The inhibitor is characterized as being a peptide-based epoxyketone or vinyl sulfone that contains an arginine or 4-aminomethylene-L-phenylalanine at the C-terminus (i.e., at the P1 position). Methods for using the inhibitor to inhibit the activity of the ?2/?2i site of a proteasome and treat a proteasome-mediated disease or condition are also described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Trustees of Dartmouth College
    Inventors: Alexei Kisselev, Dmitry V. Filippov, Herman Overkleeft
  • NOVEL PEPTIDE FOR AUGMENTING AND EXPRESSION OF BDNF AND PHARMACEUTICAL COMPOSITION FOR PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISEASES INCLUDING ALZHEIMER'S DISEASE OR PARKINSON'S DISEASE, COMPRISING THE SAME
    Publication number: 20120208747
    Abstract: Disclosed are peptides for augmenting the expression of BDNF (brain-derived neurotrophic factor) and a pharmaceutical composition for the prevention and treatment of Alzheimer's disease or Parkinson's disease, comprising the same. The peptides can induce the expression of BDNF in dopamine-reactive human cells, pass easily through the blood-brain barrier thanks to their low molecular weights and are almost free of cytotoxicity. Thus, they are useful in the prevention and treatment of neuropathies such as Alzheimer's disease or Parkinson's disease.
    Type: Application
    Filed: December 31, 2009
    Publication date: August 16, 2012
    Applicant: SUNGYUNKWAN UNIVERSITY FOUNDATION FOR CORPORATE COLLABORATION
    Inventors: Kil Lyong Kim, Hong Gi Kim, Woo Ram Jung, Dong Ik Park, Min Kyoo Shin
  • SYNTHETIC CHOLESTERYLAMINE-LINKER DERIVATIVES FOR AGENT DELIVERY INTO CELLS
    Publication number: 20120208771
    Abstract: Synthetic cholesterylamine-linkers can include derivatives of cholesterol, cholesteryl, or sitosteryl coupled through the linker to an agent for delivery into cells. The cholesterylamines are thought to mimic cholesterol in the capacity and mechanism for enhanced entry into cells. The configuration of the cholesterylamine-linker that is thought to provide for enhanced entry into cells includes a cholesterylamine that is coupled to a linker from the amine, and which linker includes a negative charge at a spatial distance from the amine of the cholesterylamine.
    Type: Application
    Filed: August 12, 2010
    Publication date: August 16, 2012
    Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF KANSAS
    Inventor: Blake R. Peterson
  • Fragment Ligated Inhibitors Selective for the Polo Box Domain of PLK1
    Publication number: 20120202970
    Abstract: Methods for developing non-peptidic inhibitors that target the polo-box domain of PLK1 proteins are described. Methods include developing structure activity relationships for peptidic inhibitors followed by development of non-peptide fragment alternatives for portions of the peptide inhibitors. The non-peptide fragment can provide similar structure activity relationship as the replaced peptide. Fragment alternatives to key binding determinants are identified in an iterative computational and synthetic process facilitated through understanding of the peptide structure-activity relationships. The approach is informed by peptide structure-activity data obtained through synthesis and testing of truncated and mutated analogs of known PBD binding motifs.
    Type: Application
    Filed: February 3, 2012
    Publication date: August 9, 2012
    Applicant: UNIVERSITY OF SOUTH CAROLINA
    Inventors: Campbell McInnes, Doaa Boshra Farag
  • INHIBITORS OF IAP
    Publication number: 20120202750
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Cross-linkers and their uses
    Patent number: 8236319
    Abstract: Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: August 7, 2012
    Assignee: ImmunoGen, Inc.
    Inventors: Ravi V. J. Chari, Robert Yongxin Zhao, Yelena Kovtun, Rajeeva Singh, Wayne Charles Widdison
  • PEPTIDE BASED PEROXIDASE INHIBITORS AND METHODS OF USING SAME
    Publication number: 20120196789
    Abstract: The present invention provides peptide-based peroxidase inhibitors having the formula AA1-AA2-AA3, wherein AA1 is a positively charged, negatively charged or neutral amino acid, AA2 is a redox active amino acid, and AA3 is an amino acid possessing a reducing potential such that AA3 is capable of undergoing a redox reaction with a radical of amino acid AA2 or a retro or retro-inverso analog thereof. The result of such a combination is a highly effective inhibitor of peroxidase activity that has potent anti-inflammatory properties in widely diverse models of vascular disease and injury. Exemplary tripeptides effectively inhibit peroxidase mediated LDL oxidation, increase vasodilation in SCD mice, inhibit eosinophil infiltration and collagen deposition in asthma mice, inhibit acute lung injury, and decrease ischemic injury of the heart.
    Type: Application
    Filed: October 5, 2010
    Publication date: August 2, 2012
    Inventors: Hao Zhang, Yang Shi, Hao Xu, Kirkwood A. Pritchard, JR.
  • HCV PROTEASE INHIBITORS AND USES THEREOF
    Publication number: 20120190614
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: April 10, 2012
    Publication date: July 26, 2012
    Applicant: AVILA THERAPEUTICS, INC.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • ASYMMETRIC SYNTHESIS OF PEPTIDES
    Publication number: 20120190816
    Abstract: The present invention provides a process comprising substitution of an acceptor molecule comprising a group —XC(O)— wherein X is O, S or NR8, where R8 is C1-6 alkyl, C6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor molecule is cyclised such that said nucleophilic substitution at —XC (O)— occurs without racemisation. This process has particular application for the production of a peptide by extension from the activated carboxy-terminus of an acyl amino acid residue without epimerisation.
    Type: Application
    Filed: July 20, 2011
    Publication date: July 26, 2012
    Inventors: Laurence M. Harwood, Ran Yan
  • Water-Soluble Functionalized Fullerenes
    Publication number: 20120183468
    Abstract: Provided herein are water-soluble, functionalized fullerenes, and processes for producing water-soluble, functionalized fullerenes. The process includes sulfonating a fullerene in an acidic solution comprising sulfuric acid to produce a sulfonated fullerene, isolating the sulfonated fullerene from the acidic solution without neutralizing the acidic solution, reacting the sulfonated fullerene with hydrogen peroxide to form a reaction product, and isolating a polyhydroxylated fullerene from the reaction product produced from reacting the sulfonated fullerene with the hydrogen peroxide. The process of producing water-soluble fullerenes further includes functionalizing a polyhydroxylated fullerene with one or more pendant functional groups by reacting the polyhydroxylated fullerene with one or more functional group precursors.
    Type: Application
    Filed: January 17, 2012
    Publication date: July 19, 2012
    Applicant: MARELLE, LLC
    Inventors: Mark Farrell, Michelle Guaragno
  • METHOD FOR IMPROVING BREAD-MAKING PROPERTIES OF RICE FLOUR BREAD DOUGH
    Publication number: 20120177780
    Abstract: This invention provides a method for improving bread-making properties of bread dough using rice flour as the main material. The invention relates to a dough improving agent for rice flour breads, wherein said agent comprises glutathione and a method for making rice flour breads using the same.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 12, 2012
    Applicant: INCORPORATED ADMINISTRATIVE AGENCY NATIONAL AGRICULTURE AND FOOD RESEARCH ORGANIZATION
    Inventor: Hiroyuki Yano
  • Metal Abstraction Peptide (MAP) Tag and Associated Methods
    Publication number: 20120177580
    Abstract: Compositions comprising a tripeptide having the sequence XC1C2; wherein X is any amino acid such that XC1C2 is capable of binding a metal in a square planar orientation or square pyramidal orientation or both; and wherein C1 and C2 are the same or different; and wherein C1 and C2 individually are chosen from a cysteine and a cysteine-like nonnatural amino acid, as well as metal-XC1C2 complexes and methods for forming such complexes.
    Type: Application
    Filed: March 23, 2012
    Publication date: July 12, 2012
    Applicant: University of Kansas
    Inventors: Jennifer Ann Stowell Laurence, Anthony Andrew Vartia, Mary Elizabeth Krause
  • HCV NS3 protease inhibitors
    Patent number: 8216999
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: July 10, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David B. Olsen, Michael T. Rudd, Joseph P. Vacca, Charles J. McIntyre
  • Liquid phase peptide synthesis of KL-4 pulmonary surfactant
    Patent number: 8217142
    Abstract: The invention relates to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu4)4-Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the ?-carbon.
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: July 10, 2012
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ahmed F. Abdel-Magid, Urs Eggmann, Cynthia Anne Maryanoff, Adrian Thaler, Frank J. Villani
  • QUATERNARY ALKYL AMMONIUM BACTERIAL EFFLUX PUMP INHIBITORS AND THERAPEUTIC USES THEREOF
    Publication number: 20120165276
    Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
    Type: Application
    Filed: May 6, 2008
    Publication date: June 28, 2012
    Applicant: Mpex Pharmaceuticals, Inc.
    Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
  • Soluble Nanoparticles as Delivery Systems for Prodrugs
    Publication number: 20120164230
    Abstract: Compounds and methods are disclosed in which a prodrug can be delivered in an elevated oxidative state to cells by means of graphitic nanoparticles to which the prodrug is attached by a hydrophilic polymer and which have been made soluble by a hydrophilic polymer, such as PEG. The graphitic nanoparticle may be a single walled carbon nanotube (SWNT). The prodrug may be a DNA-binding metal-based drug. Exemplified is a platinum(IV) complex c,c,t-[Pt(NH3)2Cl2(OEt)(O2CCH2CH2CO2H)], which is nearly nontoxic to testicular cancer cells, but displays a significantly enhanced cytotoxicity profile when attached to the surface of amine-functionalized soluble SWNTs. An amine functionality on the hydrophilic polymer may be used to link the prodrug.
    Type: Application
    Filed: May 6, 2008
    Publication date: June 28, 2012
    Inventors: Rodney Feazell, Nozomi Nakayama-Ratchford, Hongjie Dai, Stephen J. Lippard
  • ANTI-INFLAMMATORY AGENT FOR ORAL APPLICATION, AND ANTI-INFLAMMATORY PEPTIDE FOR ORAL APPLICATION
    Publication number: 20120157395
    Abstract: Disclosed are a composition having an anti-inflammatory function and a therapeutic method using the composition, both of which are effective for inflammatory diseases such as inflammatory bowel disease. Specifically disclosed are: an anti-inflammatory functional agent for oral application, which comprises a soybean peptide, wherein the soybean peptide contains fractions each having a molecular weight of 500 or less and excluding any free amino acid in an amount of 40 wt % or more and has a free amino acid content of 7 wt % or less; and a therapeutic method using the anti-inflammatory functional agent.
    Type: Application
    Filed: May 12, 2010
    Publication date: June 21, 2012
    Inventors: Masahisa Ibuki, Yoshinori Hasegawa, Yoshinori Mine
  • SELECTIVE CASPASE INHIBITORS AND USES THEREOF
    Publication number: 20120157394
    Abstract: The present invention relates to compounds of Formula I, II, IVC, VIIIC, IXC, or XC and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, II, IVC, VIIIC, IXC, or XC are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases). Processes for synthesizing tripeptides are provided.
    Type: Application
    Filed: May 21, 2010
    Publication date: June 21, 2012
    Applicant: NEW WORLD LABORATORIES, INC.
    Inventors: Jan-Eric Ahlfors, Khalid Mekouar
  • Caveolin peptides and their use as therapeutics
    Publication number: 20120149651
    Abstract: The present invention relates generally to compositions and methods useful for treating various conditions and afflictions, such as inflammation and cancer. More specifically, the present invention relates to compositions and methods of treatment which utilize peptides comprising at least one caveolin scaffolding domain. Even more specifically, the present invention relates to compositions of fusion peptides comprising the antennapedia homeodomain fused to a caveolin scaffolding domain and to methods of using these peptides to treat various conditions and afflictions.
    Type: Application
    Filed: October 30, 2007
    Publication date: June 14, 2012
    Applicant: Yale University
    Inventor: William C. Sessa
  • METHODS RELATED TO THE TREATMENT OF NEURODEGENERATIVE AND INFLAMMATORY CONDITIONS
    Publication number: 20120142615
    Abstract: The invention includes methods of neuroprotection, inducing release of neurotrophic factors, inhibiting the over-activation of innate immune cells, attenuating the toxin-induced death and/or damage of tissues, reducing inflammation, treating an inflammation-related condition, and inhibiting NADPH oxidase, that includes contacting or administering an effective amount of at least one compound of the invention that include: valproic acid, sodium butyrate, and salts thereof; opioid peptides; a peptide comprising the tripeptide GGF; and morphinans, such as naloxone, naltrexone, 3-hydroxy-morphinan and dextromethorphan.
    Type: Application
    Filed: December 13, 2011
    Publication date: June 7, 2012
    Applicants: Human Service
    Inventors: Jau-Shyong Hong, Liya Qin, Guorong Li, Michelle Block, Wei Zhang, Po-See Chen, Giia-Shuen Peng
  • Bimacrocylic HCV NS3 Protease Inhibitors
    Publication number: 20120141414
    Abstract: Inhibitors of the hepatitis C virus (HCV) NS3 protease are provided. In particular, bimacrocyclic compounds and their pharmaceutical compositions for the treatment of HCV infections are provided. Methods of making the bimacrocyclic compounds and their pharmaceutical compositions, and methods of using the compounds for treating HCV infections are also provided.
    Type: Application
    Filed: May 24, 2010
    Publication date: June 7, 2012
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Pavel Majer, Michael Eissenstat, Rongjuan Lu
  • Method and compositions for treating skin
    Patent number: 8193155
    Abstract: A skin care composition comprising at least one keratinocyte CLOCK or PER1 gene activator and at least one DNA repair enzyme; a method for inhibiting damage to human keratinocytes due to environmental aggressors by applying a composition comprising at least one keratinocyte CLOCK or PER1 gene activator and at least one DNA repair enzyme; and a method for repairing DNA damage in human keratinocytes.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: June 5, 2012
    Assignee: ELC Management, LLC
    Inventors: Daniel H. Maes, Nadine A. Pernodet, Lenny Slutsky, Donald F. Collins, Kerri Goldgraben, Edward Pelle, James Timothy McCarthy
  • TRIPETIDE BORONIC ACID OR BORONIC ESTER, PREPARATIVE METHOD AND USE THEREOF
    Publication number: 20120135921
    Abstract: The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
    Type: Application
    Filed: May 17, 2010
    Publication date: May 31, 2012
    Inventors: Runtao Li, Jingrong Cui, Yongqiang Zhu, Shuyang Yao, Zemei Ge, Tieming Cheng
  • PRODRUGS CONTAINING ALBUMIN BINDING PROBE
    Publication number: 20120134977
    Abstract: The present invention provides albumin-binding probes capable of reversibly linking to short-lived amino-containing drugs and non-covalently associating with albumin in-vivo, thereby converting said drugs into inactive reactivable prodrugs having prolonged lifetime in-vivo. The invention further provides conjugates of said probes with amino-containing drugs, as well as pharmaceutical compositions and uses thereof.
    Type: Application
    Filed: June 1, 2010
    Publication date: May 31, 2012
    Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.
    Inventors: Yoram Shechter, Matityahu Fridkin
  • Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
    Patent number: 8188216
    Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a bivalent radical, a —(CH2)t- bivalent radical, or a covalent bond; and where part (T) is a -Y-L-Z- radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.
    Type: Grant
    Filed: October 7, 2004
    Date of Patent: May 29, 2012
    Assignee: Tranzyme Pharma Inc.
    Inventors: Pierre Deslongchamps, Yves Dory, Gilles Berthiaume, Luc Ouellet, Ruoxi Lan
  • NOVEL SPECIFIC HCV NS3 PROTEASE INHIBITORS
    Publication number: 20120129765
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HCV in human patients or other animal hosts.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 24, 2012
    Applicants: GENOSCIENCE, RFS Pharma, LLC
    Inventors: Jerome Courcambeck, Philippe Halfon, Mourad Bouzidi, Steven J. Coats, Richard Anthony Whitaker
  • Novel Peptidase Substrates
    Publication number: 20120129203
    Abstract: The present invention relates to the use of a compound of the following formula (I) for detecting a peptidase activity and/or a variation in pH: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3 and Z4 being independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
    Type: Application
    Filed: July 27, 2010
    Publication date: May 24, 2012
    Applicant: bioMerieux, SA
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Novel Peptidase Substrates
    Publication number: 20120122135
    Abstract: The present invention relates to the use of a compound of the following formula (I), as an enzyme substrate for the detection of a peptidase activity or as a pH indicator: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U is N or N+R and V is CZ6N or N+R or else V is N or N+R and U is CZ6; R is H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3, Z4 and Z5 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.
    Type: Application
    Filed: July 28, 2010
    Publication date: May 17, 2012
    Applicant: bioMerieux, SA
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • HEPATITIS C VIRUS NS3 PROTEASE INHIBITORS
    Publication number: 20120121624
    Abstract: The present invention relates to macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Application
    Filed: July 27, 2010
    Publication date: May 17, 2012
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Nigel J. Liverton, John A. McCauley, Michael T. Rudd
  • PROCESS FOR THE PURIFICATION OF HUMAN GROWTH HORMONE POLYPEPTIDES USING AFFINITY RESINS COMPRISING SPECIFIC LIGANDS
    Publication number: 20120116027
    Abstract: The present invention relates to a novel process for the purification of growth hormone polypeptides, e.g. recombinant human Growth Hormone. The process utilizes an affinity resin comprising a solid phase material having immobilized thereto one or more low-molecular weight synthetic ligands. The affinity resins enable the separation of Growth Hormone from closely related proteins.
    Type: Application
    Filed: November 13, 2009
    Publication date: May 10, 2012
    Inventors: Jakob Ewald Rasmussen, Phaedria Marie St. Hilaire, Michael Roice, Christine Bruun Schioedt, Knud Jørgen Jensen
  • Kokumi-imparting agent
    Patent number: 8173605
    Abstract: The present invention encompasses a method for screening for a kokumi-imparting substance by using the calcium receptor activity as an index, a composition containing a kokumi-imparting substance obtained by the screening method, a method for producing food or drink imparted with kokumi, and food or drink imparted with kokumi.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: May 8, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takeaki Ohsu, Sen Takeshita, Yuzuru Eto, Yusuke Amino, Naohiro Miyamura, Tomohiko Yamanaka, Hiroaki Nagasaki
  • Intermediates for LHRH antagonist synthesis, process for the production, and process for LHRH antagonist production
    Patent number: 8173770
    Abstract: The peptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P1-Ser(P2)-MMeTry(P3)-D-Lys(Nic)-Leu-Lys(iPr,P4)-Pro-D-AlaNH2 and P1-Ser(P2)-NMeTry(P3)-D-Asn-Leu-Lys(iPr,P4)-Pro-D-AlaNH2.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: May 8, 2012
    Assignee: Polypeptide Laboratories A/S
    Inventors: Jon H. Rasmussen, Palle H. Rasmussen, Wolfgang O. Wachs, Stefan Hansen, Jens Fomsgaard
  • PEPTOID COMPOUNDS
    Publication number: 20120108499
    Abstract: The invention relates to new peptoid compounds of formula (I), as well as their use in the treatment of bacterial infections, such as those caused by vancomycin resistant microorganisms, and to compositions thereof.
    Type: Application
    Filed: September 6, 2011
    Publication date: May 3, 2012
    Applicant: University of Wollongong
    Inventors: John BREMNER, Stephen PYNE, Paul KELLER, Dan COGHLAN, Adel GARAS, Helen WITCHARD, Tim BOYLE, Jonathan COATES
  • Antibodies And Epitopes Specific To Misfolded Prion Protein
    Publication number: 20120107321
    Abstract: The present invention relates to antibodies and immunogenic peptides specific to misfolded prion protein (PrP, e g, PrPSc), and uses thereof. The immunogenic peptides comprise the amino acid sequence tyrosine-methionine-leucine (YML). The antibodies or peptides can be used for treating or preventing a disease or disorder associated with misfolded PrP, including cancer. In particular, a IgM monoclonal antibody designated “1A1” was generated using a peptide consisting of the sequence GGYMLGS (i e, SEQ ID NO 8), which corresponds to residues 126-132 of human PrP 1A1 recognizes misfolded PrP, but not normal PrP.
    Type: Application
    Filed: March 2, 2010
    Publication date: May 3, 2012
    Applicant: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventor: Neil R. Cashman
  • CELL-TARGETING NANOPARTICLES AND USES THEREOF
    Publication number: 20120107800
    Abstract: The invention generally refers to a cell-targeting nanoparticle, wherein the cell-targeting nanoparticle is directly conjugated to at least one cysteine-containing peptide, wherein the cysteine-containing peptide is selected from the group consisting of glutathione (GSM, a GSH-containing peptide, and a peptide comprising a nuclear localization signal (NLS) sequence and a transporter sequence, and methods of using the cell-targeting nanoparticle.
    Type: Application
    Filed: September 19, 2011
    Publication date: May 3, 2012
    Inventors: Tamil Selvan SUBRAMANIAN, Padmanabhan Parasuraman, Dominik Janczewski, Kishore K. Bhakoo
  • INHIBITORS OF INTRACELLULAR UROKINASE PLASMINOGEN ACTIVATOR AND METHODS OF USE THEREOF
    Publication number: 20120108494
    Abstract: The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the compositions for treating cancer and for delivering an amiloride conjugate into cancer cells in a subject in need thereof.
    Type: Application
    Filed: August 1, 2008
    Publication date: May 3, 2012
    Applicant: The Regents of the University of California
    Inventors: Fredric A. Gorin, Michael H. Nantz
  • TARGETED BINDING AGENTS DIRECTED TO a5ß1 AND USES THEREOF
    Publication number: 20120107324
    Abstract: The invention relates to targeted binding agents against ?5?1 and uses of such agents. More specifically, the invention relates to fully human monoclonal antibodies directed to ?5?1. The described targeted binding agents are useful in the treatment of diseases associated with the activity and/or overproduction of ?5?1 and as diagnostics.
    Type: Application
    Filed: December 21, 2009
    Publication date: May 3, 2012
    Inventors: Catherine Anne Eberlein, Ian Foltz, Jaspal Singh Kang, Jane Kendrew, Avril Alfred, Simon Thomas Barry
  • NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20120101032
    Abstract: The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IV, IVa, V, Va, VI and VIa, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: October 21, 2011
    Publication date: April 26, 2012
    Applicant: INTERMUNE, INC.
    Inventors: Brad BUCKMAN, Vladimir SEREBRYANY, John B. NICHOLAS, Scott SEIWERT
  • MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS
    Publication number: 20120101031
    Abstract: The present invention relates to novel macrocyclic compounds and methods of treating a hepatitis C infection in a subject in need of such therapy with said macrocyclic compounds. The present invention further relates to pharmaceutical compositions comprising the compounds of the present invention, or pharmaceutically acceptable salts, esters, or prodrugs thereof, in combination with a pharmaceutically acceptable carrier or excipient.
    Type: Application
    Filed: June 7, 2011
    Publication date: April 26, 2012
    Applicants: ENANTA PHARMACEUTICALS, INC., ABBOTT LABORATORIES
    Inventors: Hui-Ju Chen, Keith F. McDaniel, Brian E. Green, Jason P. Shanley, Albert W. Kruger, Jorge Gandarilla, Dennie S. Welch, Russell D. Cink, Steven C. Cullen, Yonghua Gai, Guoqiang Wang, Yat Sun Or
  • Compounds For Enzyme Inhibition
    Publication number: 20120101026
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
    Type: Application
    Filed: December 30, 2011
    Publication date: April 26, 2012
    Applicant: ONYX THERAPEUTICS, INC.
    Inventors: Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser, Kevin D. Shenk, Peggy A. Radel
  • GOLD (III) COMPLEXES WITH OLIGOPEPTIDES FUNCTIONALIZED WITH SULFUR DONORS AND USE THEREOF AS ANTITUMOR AGENTS
    Publication number: 20120101044
    Abstract: The invention concerns Au(III) complexes of the type [AuIIIX2(Pdtc)] (X=halogen, pseudo-halogen; pdtc=peptide-/esterified peptidedithiocarbamato) which are able to both maintain the antitumor properties and the lack of nephrotoxic side-effects of the previously reported Au(III)-dithiocarbamato complexes, together with an improved bioavailability through the peptide-mediated cellular internalization. The Au(III) complexes described have shown a significant biological activity on human tumor cell lines and, thus, they can be advantageously used as antineoplastic agents. The preparation method and use for the treatment of tumor pathologies of the Au(III) complexes of the invention are further described.
    Type: Application
    Filed: March 20, 2009
    Publication date: April 26, 2012
    Inventors: Dolores Fregona, Luca Ronconi, Fernando Formaggio, Q. Ping Dou, Donatella Aldinucci
  • COMPOUNDS FOR ENZYME INHIBITION
    Publication number: 20120101050
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 26, 2012
    Applicant: Onyx Therapeutics, Inc.
    Inventors: Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
  • Hepatitis C virus inhibitors
    Patent number: 8163921
    Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: April 24, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ny Sin, Brian Lee Venables, Paul Michael Scola, Alan Xiangdong Wang
  • Molecular Interactions in Hematopoietic Cells
    Publication number: 20120093873
    Abstract: The invention provides reagents and methods for inhibiting or enhancing interactions between proteins in hematopoietic cells and other cells involved in the mediation of an immune response. Reagents and methods provided are useful for treatment of a variety of diseases and conditions mediated by immune system cells.
    Type: Application
    Filed: September 24, 2010
    Publication date: April 19, 2012
    Applicant: ARBOR VITA CORPORATION
    Inventors: PETER S. LU, JOSHUA D. RABINOWITZ, JOHANNES SCHWEIZER
  • IAP INHIBITORS
    Publication number: 20120094917
    Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Application
    Filed: May 25, 2010
    Publication date: April 19, 2012
    Applicant: TETRALOGIC PHARMACEUTICALS CORP
    Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
  • METHODS AND COMPOSITIONS FOR THE DETECTION OF CANCER
    Publication number: 20120093724
    Abstract: Various embodiments of this invention relate generally to targeted activation and delivery of therapeutic drugs to cells that produce prostate specific antigen (PSA), prostate specific membrane antigen (PSMA) or human glandular kallikrein (hK2). Various further embodiments relate more specifically to PSMA-specific peptide prodrugs that become activated to yield therapeutic drugs. Further aspects of various embodiments of the present invention also relate to methods and compositions for treating or preventing cancers and methods and compositions for detecting and/or imaging cancers.
    Type: Application
    Filed: March 17, 2010
    Publication date: April 19, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Samuel Ray Denmeade, John Thomas Isaacs, Soeren Brogger Christensen
  • COSMETIC AND/OR PHARMACEUTICAL COMPOSITION COMPRISING A RELIEVING PEPTIDIC HYDROLYZATE
    Publication number: 20120094921
    Abstract: The invention concerns a cosmetic or pharmaceutical composition comprising, in a physiologically acceptable medium, a peptide hydrolyzate which is enriched in soothing bioactive peptide. The invention also concerns the use, in a cosmetic composition, of the active principle in accordance with the invention to activate HMG-CoA reductase in skin cells and to prevent or combat skin irritations.
    Type: Application
    Filed: April 15, 2010
    Publication date: April 19, 2012
    Inventors: Claude Dal Farra, Nouha Domloge, Jean-Marie Botto
  • NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
    Publication number: 20120094897
    Abstract: The embodiments provide compounds of the general Formulae I, and II, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: September 14, 2011
    Publication date: April 19, 2012
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert