Containing Only Normal Peptide Links In The Ring, I.e., Homodetic Cyclic Peptides Patents (Class 530/321)
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Publication number: 20120219574Abstract: The present invention provides for the identification of an antigen surrogate to the native antigens for the autoimmune disease pemphigus vulgaris. Ligands are discovered using large random peptoid or cyclic peptoid libraries that are screened against known antibodies to autoimmune diseases. The ligands may be useful as drugs in the treatment of such diseases and can also be used in combination with the concomitant removal of T-cells associated with autoimmune disorders.Type: ApplicationFiled: April 10, 2012Publication date: August 30, 2012Applicant: OPKO Pharmaceuticals, LLCInventors: Phillip FROST, Thomas Kodadek
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Publication number: 20120214748Abstract: The invention relates to peptides of the general formula (I) GX1CSX2SX3PPX4CX5PD (SEQ ID NO: 20), where X1 is Y, M, W, I, V, or A; X2 is R or K; X3 is Y, F, I, M, L, E, D, or H; X4 is V, I, or H; and X5 is I, V, Y, F, or W; and to the pharmaceutically acceptable salts, esters or prodrugs of the peptides according to general formula (I). In addition, the invention relates to pharmaceutical preparations, kits containing the preparations, and to procedures using the peptides and preparations.Type: ApplicationFiled: May 25, 2010Publication date: August 23, 2012Inventors: Peter Gal, Gabor Pal, Kocsis Andrea Parisne, Peter Zavodszky
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Publication number: 20120214745Abstract: Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporin and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.Type: ApplicationFiled: February 22, 2012Publication date: August 23, 2012Applicant: Isotechnika Pharma Inc.Inventors: Salvaraj Naicker, Randall W. Yatscoff, Robert T. Foster
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Publication number: 20120214968Abstract: 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: ApplicationFiled: February 10, 2012Publication date: August 23, 2012Inventors: Baosheng Liu, Jianheng Zhang
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Publication number: 20120208746Abstract: Methods of predicting the response in a patient infected with hepatitis C virus (HCV) to a treatment regime involving the use of a cyclophilin-binding compound are described which provide for improvements in treatments, pharmaceutical compositions, dosing regimen, assays, kits, and other aspects of the art.Type: ApplicationFiled: January 12, 2012Publication date: August 16, 2012Applicant: Scynexis Inc.Inventors: Samuel Earl HOPKINS, Yves Joseph Ribeill, Bernard Scorneaux
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Publication number: 20120196808Abstract: The present application relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of inter alia shock conditions as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.Type: ApplicationFiled: March 1, 2012Publication date: August 2, 2012Applicant: FERRING B.V.Inventors: Kazimierz Wisniewski, Claudio Schteingart, Regent LaPorte, Robert Felix Galyean, Pierre Riviere
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Publication number: 20120196749Abstract: A cyclosporin derivative of general Formula (I) or a pharmaceutically compatible salt thereof, which have a pharmaceutical effectiveness, for example in the case of chronic inflammatory diseases. The cyclosporin derivatives are preferably free from a peptide section capable of passing through the membrane of a biological cell.Type: ApplicationFiled: February 15, 2012Publication date: August 2, 2012Inventors: Gunter Fischer, Miroslav Malesevic, Frank Erdmann, Jan Kühling, Michael Bukrinsky, Stephanie Constant
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Publication number: 20120190816Abstract: 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: ApplicationFiled: July 20, 2011Publication date: July 26, 2012Inventors: Laurence M. Harwood, Ran Yan
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Publication number: 20120183954Abstract: Chemically reactive dyes that are intramolecularly crosslinked with a water-soluble bridge, their bioconjugates and their uses are described. Reactive fluorescent dyes that have a water-soluble bridge are superior to those of conjugates of spectrally non-crosslinked dyes or the dyes that are crosslinked with a hydrophobic bridge. The invention includes reactive fluorescent dyes, their biological conjugates and uses.Type: ApplicationFiled: July 12, 2011Publication date: July 19, 2012Applicants: AAT BIOQUEST, INC., BECTON, DICKINSON AND COMPANYInventors: Zhenjun Diwu, Qinglin Meng, Jinfang Liao, Haitao Guo, Timothy Dubrovsky, Barnaby Abrams
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Publication number: 20120171227Abstract: The present invention provides methods, compositions and applications for efficient, site-specific drug delivery using pro-drug complexes comprising therapeutic agents and one or more functional groups (e.g., imaging agents, targeting agents, and trigger agents). In particular, the present invention relates to pro-drug complexes comprising one or more functional groups conjugated with a therapeutic agent (e.g., a chemotherapeutic agent), methods of synthesizing the same, as well as systems and methods utilizing the therapeutic and diagnostic compositions (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).Type: ApplicationFiled: June 30, 2010Publication date: July 5, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: James R. Baker, JR., Baohua M. Huang, Thommey P. Thomas
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Publication number: 20120157385Abstract: A conjugate which comprises a cyclosporin moiety of formula (I) linked to one or more mitochondrial targeting groups, or a pharmaceutically acceptable salt thereof: wherein: A represents or, B represents methyl or ethyl, one Of R1 and R1 represents hydrogen and the other represents methyl, R2 represents ethyl or isopropyl, R3 represents hydrogen or methyl, and R4 represents —CH2CH(CH3)CH3, —CH2CH(CH3)CH2CH3, —CH(CH3)CH3 or —CH(CH3)CH2CH3.Type: ApplicationFiled: July 19, 2010Publication date: June 21, 2012Applicant: UCL Business PLCInventors: David Selwood, Martin Crompton
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Publication number: 20120157371Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: December 12, 2011Publication date: June 21, 2012Inventors: Chongxi YU, Lina Xu, Yuhua Chen, Binbing Yan, Shiqian Tu
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Publication number: 20120142893Abstract: The present invention concerns a method for separation of the antifungal cyclic hexapeptides Pneumocandin B0 from Pneumocandin C0 using a hydrophilic stationary phase and a hydrophobic mobile phase.Type: ApplicationFiled: August 11, 2010Publication date: June 7, 2012Applicant: Xellia Pharmaceuticals ApSInventor: Anders Brunsvik
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Publication number: 20120141788Abstract: The present invention relates a process for the precipitation of an organic compound, wherein: (a) a solution (I) of the organic compound in a first solvent is introduced via a first inlet into a closed type mixing chamber; (b) a precipitation agent (II) is introduced, simultaneously with step (a), via a second inlet into the closed type of mixing chamber; (c) the solution (I) of the organic compound and the precipitating agent (II) are mixed thereby forming a precipitate of the organic compound and a liquid phase; and (d) discharging the precipitate of the organic compound and the liquid phase via a single outlet from the closed type mixing chamber.Type: ApplicationFiled: September 19, 2007Publication date: June 7, 2012Inventor: Huibert Albertus Van Boxtel
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Publication number: 20120135939Abstract: 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: ApplicationFiled: October 11, 2011Publication date: May 31, 2012Applicant: ALLERGAN, INC.Inventors: Michael E. Garst, William Robert Carling, David Arthur Scowen, Michael E. Stern, Christopher S. Schaumburg
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Patent number: 8188216Abstract: 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: GrantFiled: October 7, 2004Date of Patent: May 29, 2012Assignee: Tranzyme Pharma Inc.Inventors: Pierre Deslongchamps, Yves Dory, Gilles Berthiaume, Luc Ouellet, Ruoxi Lan
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Patent number: 8187605Abstract: Embodiments of the present invention provide for novel peptides of use for detection and/or inhibition of anti-?1-adrenergic receptor antibodies. Certain embodiments concern uses of cyclic and/or linear peptides. In other embodiments, the present invention relates to novel peptides of use in diagnostic and/or pharmaceutical compositions. Some embodiments concern diagnosing and/or treating cardiac conditions. Cardiac conditions of the instant invention can concern infectious heart disease, non-infectious heart disease, ischemic heart disease, non-ischemic heart disease, inflammatory heart disease, myocarditis, cardiac dilatation, idiopathic cardiomyopathy, idiopathic dilated cardiomyopathy, immune-cardiomyopathy, heart failure, and any cardiac arrhythmia condition.Type: GrantFiled: March 31, 2006Date of Patent: May 29, 2012Assignee: Julius-Maximillians-Universität WürzburgInventors: Roland Jahns, Valérie Jahns, Martin J. Lohse, Dieter Palm
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Publication number: 20120130146Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising the continuous administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agent or therapy forms that have synergistic efficacy when administered consecutively with said ligands, such as chemotherapeutic agents and or radiation therapy.Type: ApplicationFiled: May 25, 2010Publication date: May 24, 2012Applicant: Merck Patent GmbHInventors: Martin Andreas Picard, Ullrich Bethe, Matthias Dotzauer, Elizabeth Cohen-Jonathan Moyal
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Publication number: 20120130017Abstract: There is provided a novel process for preparing polyamides (in particular cyclic and hairpin polyamides) comprising the step of coupling an amine with a Boc-protected amino acid monomer in the presence of diphosgene and/or triphosgene. Such a process may be performed on a solid or solution phase.Type: ApplicationFiled: April 28, 2010Publication date: May 24, 2012Applicant: UNIVERSITY OF LEICESTERInventors: Wu Su, Glenn Ashley Burley
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Publication number: 20120100562Abstract: The invention provides methods and compositions for modulating the Wnt signaling pathway, in particular by interfering with binding of Dkk1 or SOST with LRP5 and/or LRP6.Type: ApplicationFiled: October 19, 2011Publication date: April 26, 2012Applicant: Genentech, Inc.Inventors: Eric Bourhis, Andrea Cochran, Yingnan Zhang
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Patent number: 8153759Abstract: Disclosed are a compound represented by the general formula (I) below and a polymer compound obtained by polymerizing such a compound. R1-Gly-Lac-Pro-R2 ??(I): where -Gly-Lac-Pro- represents a structure represented by the following formula (II), R1 represents a hydrogen atom, or an amino acid, a polypeptide or a hydroxycarboxylic acid which are linked through an amide bond, R2 represents a hydroxyl group, or an amino acid or a polypeptide which are linked through an amide bond, or a hydroxycarboxylic acid which is linked through an ester bond.Type: GrantFiled: August 10, 2007Date of Patent: April 10, 2012Assignee: National University Corporation Gunma UniversityInventors: Hiroyuki Oku, Yuya Shimoda, Aya Inoue, Chie Takayama, Keiichi Yamada, Ryoichi Katakai
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Publication number: 20120077732Abstract: The present invention relates to cyclic peptides, comprising alternating D- and L- amino acids and wherein the peptide possesses immunomodulatory activity. The present invention also relates to pharmaceutical compositions comprising the cyclic peptides and to methods for the treatment of disease.Type: ApplicationFiled: November 24, 2009Publication date: March 29, 2012Applicant: SYDNEY WEST AREA HEALTH SERVICEInventors: Nicholas Manolios, Veronika Judit Bender, Marina Ali
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Publication number: 20120065142Abstract: The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-Benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.Type: ApplicationFiled: May 20, 2010Publication date: March 15, 2012Applicant: Merck Patent GmbHInventors: Alfred Jonczyk, Clemens Kuehn, Kerstin Seemann, Christoph Saal, Gerald Scholz, Soenke Petersen, Harald Untenecker, Michael Lange
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Publication number: 20120065367Abstract: Provided are: a radiolabeled drug, which is efficiently accumulated in a target and has high in vivo stability; and diagnosis and treatment each using the radiolabeled drug. Specifically provided are: a radiolabeled drug showing increased accumulation in a target site, which comprises a complex composed of a ligand that is bound to a compound capable of binding to a target molecule and forms a polycoordinated complex with a metal (e.g., technetium or rhenium) and a radionuclide of the metal; the radiolabeled drug for diagnosis or treatment; a ligand for preparing the radiolabeled drug; a kit that comprises a drug comprising the ligand and a drug comprising a radionuclide of a metal, as separate package units; and a method of increasing accumulation of a radiolabeled drug in a target site, comprising using the above-mentioned radiolabeled drug.Type: ApplicationFiled: April 28, 2009Publication date: March 15, 2012Applicant: NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITYInventors: Yasushi Arano, Tomoya Uehara
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Publication number: 20120058905Abstract: Naturally-occurring and modified recombinant nucleic acid molecules have been isolated that encode linear pre-cursors of cyclopeptides of the Caryophyllaceae (Ccps) and Caryophyllaceae-like (Clcps) type V1 class of cyclopeptides. Such nucleic acid molecules are useful for producing cyclopeptides and their linear precursors by recombinant methods.Type: ApplicationFiled: May 10, 2010Publication date: March 8, 2012Inventors: Patrick S. Covello, Raju S.S. Datla, Sandra Lee Stone, J. John Balsevich, Martin John Reaney, Paul Grenville Arnison, Janet Anne Condie
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Publication number: 20120045411Abstract: The invention is directed to beta-defensin-derived peptides and their use in modulating the activity of hematopoietic cells and other CXCR4-expressing cells. Specifically, the invention provides compositions and methods useful in the treatment of cancer. The invention further provides compositions and methods useful for promoting mobilization and transplantation of hematopoietic stem cells and progenitor cells.Type: ApplicationFiled: February 10, 2010Publication date: February 23, 2012Applicant: Yeda Research and Development Co., Ltd.Inventors: Tsvee Lapidot, Alexander Kalinkovich, Matityahu Fridkin
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Patent number: 8114831Abstract: A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis.Type: GrantFiled: April 20, 2010Date of Patent: February 14, 2012Assignee: Synergy Pharmaceuticals Inc.Inventors: Kunwar Shailubhai, Gregory Nikiforovich, Gary S. Jacob
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Publication number: 20120034593Abstract: The present invention relates to a method for preparing a cyclic peptide with antiparasite activity and anticancer activity. The invention also relates to this peptide as an antiparasite agent, for example in the treatment of toxoplasmosis and as an anticancer agent. The invention also relates to the use of this cyclic peptide for treating organs ex vivo before transplantation.Type: ApplicationFiled: April 6, 2010Publication date: February 9, 2012Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE JOSEPH FOURIER (GRENOBLE 1)Inventors: Yung-Sing Wong, Mohamed-Ali Hakimi, Alexandre Bougdour, Hervé Pelloux, Danièle Maubon
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Publication number: 20120027778Abstract: Novel anti-cancer agents, including, but not limited to, antibodies and other polypeptides, that bind to human frizzled receptors are provided. Novel epitopes within the human frizzled receptors which are suitable as targets for anti-cancer agents are also identified. Methods of using the agents or antibodies, such as methods of using the agents or antibodies to inhibit Wnt signaling and/or inhibit tumor growth are further provided. Screening methods are also provided.Type: ApplicationFiled: April 1, 2011Publication date: February 2, 2012Applicant: OncoMed Pharmaceuticals, Inc.Inventor: Austin L. GURNEY
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Publication number: 20120028880Abstract: The present invention concerns the fields of molecular medicine and targeted delivery of therapeutic agents. More specifically, the present invention relates to the identification of novel peptide sequences that incorporate the amino acids Leu-Pro-Arg (LPR), and particularly D(LPR), that selectively target VEGFR-I and NRP-I expressing cells. Targeted molecules in accor-dance with the invention are useful in the treatment and detection of neovascular or angiogenic VEGF associated disorders, including but not limited to cancer, obesity, diabetes, asthma, arthritis, cirrhosis and ocular diseases.Type: ApplicationFiled: August 8, 2008Publication date: February 2, 2012Inventors: Renata Pasqualini, Wadih Arap, Ricardo Giordano, Marina Cardó-Vila, Ana Paula Valente, Fabio Ceneviva Lacerda De Almeida
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Publication number: 20120028904Abstract: Methods, systems and compositions comprising novel peptidomimetics are disclosed that can be used to inhibit calpain and, more specifically, to treat tissue damage caused by pathologic activation of calpains.Type: ApplicationFiled: September 21, 2009Publication date: February 2, 2012Applicant: HENRY FORD HEALTH SYSTEMInventors: John Anagli, Donald Seyfried
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Publication number: 20120010154Abstract: There is provided a series of novel neuropeptide Y-cytotoxic conjugates, compositions comprising the same, and methods relating to their therapeutic use for the treatment of disease or condition states associated with aberrant or undesirable proliferation of cells that express NPY-Y1 receptors.Type: ApplicationFiled: August 18, 2011Publication date: January 12, 2012Inventors: Zheng Xin Dong, Kevin Zhou, Daniel B. Deoliveira
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Publication number: 20120010131Abstract: The invention relates to the use of cyclic compounds of general formula (I): wherein A, B, R1 and R2 are as defined in the specification, and their use as pharmaceuticals.Type: ApplicationFiled: December 30, 2010Publication date: January 12, 2012Applicant: Scynexis, Inc.Inventors: Cyprian Okwara Ogbu, Thomas Edward Richardson
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Publication number: 20110294724Abstract: 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: ApplicationFiled: March 29, 2011Publication date: December 1, 2011Inventors: Jya-Wei CHENG, Kuo-Chun HUANG, His-Tsu CHENG, Hui-Yuan YU
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Publication number: 20110293517Abstract: The present invention relates to compounds that are useful as metal ligands and which either contain a molecular recognition moiety or can be bound to a molecular recognition moiety and methods of making these compounds. Once the compounds that contain a molecular recognition moiety are coordinated with a suitable metallic radionuclide, the coordinated compounds are useful as radiopharmaceuticals in the areas of radiotherapy and diagnostic imaging. The invention therefore also relates to methods of diagnosis and therapy utilising the radiolabelled compounds of the invention.Type: ApplicationFiled: December 2, 2009Publication date: December 1, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Michelle Therese Ma, Denis Bernard Scanlon
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Publication number: 20110286923Abstract: Conjugates of a polymer having attached thereto an angiogenesis targeting moiety and a therapeutically active agent such as an anti-cancer agent or anti-angiogenesis agent, and processes of preparing same are disclosed. Pharmaceutical compositions containing these conjugates and uses thereof in the treatment of angiogenesis-related medical conditions such as cancer and cancer metastases are also disclosed.Type: ApplicationFiled: May 21, 2009Publication date: November 24, 2011Applicant: Fundacion de la Communidad Valenciana Centro de Investigacion principe felipeInventors: Ronit Satchi-Fainaro, Maria Jesus Vincent Docon
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Publication number: 20110275784Abstract: 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: ApplicationFiled: July 20, 2011Publication date: November 10, 2011Inventors: Laurence M. Harwood, Ran Yan
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Publication number: 20110256058Abstract: The invention relates to a peptide of 8-50 amino acids comprising the sequence of KAHKKRAD or KARKKHAD, or a cyclic peptide of 8-50 amino acids comprising the sequence of HKKR or RKKH. Also disclosed are methods of using the peptide for detecting, monitoring, or treating cancer.Type: ApplicationFiled: October 17, 2008Publication date: October 20, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventor: Mehran Neshat
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Publication number: 20110256567Abstract: The invention pertains to a cyclic peptide comprising the following sequence: -S1-X1-S2-X2- wherein S1 is a first target peptide sequence of a protease enzyme E1, S2 is a second target peptide sequence of a protease enzyme E2, S1 and S2 possibly being the same or different, said first peptide sequence S1 and said second peptide sequence S2 comprising 4 to 14 amino acids, E1 and E2 possibly corresponding to the same protease enzyme or to two different protease enzymes, X1 is a probe carrying a fluorescent donor group and X2 is a probe carrying a fluorescent or non-fluorescent acceptor group. Application of these peptides to determination of the activity of protease enzymes.Type: ApplicationFiled: June 10, 2009Publication date: October 20, 2011Inventors: Thomas Berthelot, Gérard Deleris
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Publication number: 20110251138Abstract: The present invention is a design and synthesis of a series of therapeutic conjugates which consists of tautomers of lipoic acid metabolites, with small molecule, vitamin, carbohydrates, peptides, chemotherapeutic agent wherein or not the conjugate possesses dual binding ability. The present invention can be used to therapeutics and diagnostics in vitro for cancer and other diseases associated with altered metabolic enzymes. The invention can also be used for the controlled release of more stable form of lipoic acid in its salt form with the minerals or vitamins.Type: ApplicationFiled: June 8, 2010Publication date: October 13, 2011Inventor: Ravikumar Kabyadi Seetharama
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Patent number: 8034747Abstract: A photolabile compound, an oligomer probe array, and a substrate for oligomer probe array comprising the same, and a manufacturing method of the same are disclosed.Type: GrantFiled: January 25, 2008Date of Patent: October 11, 2011Assignee: Samsung Electronics Co., Ltd.Inventors: Sung-min Chi, Jung-hwan Hah, Kyoung-seon Kim, Won-sun Kim, Man-hyoung Ryoo
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Publication number: 20110243981Abstract: A first aspect of the invention relates to a conjugate comprising: (i) mannan; and (ii) at least one epitope comprising a peptide fragment of a protein selected from myelin basic protein (MBP), myelin oligodentrocyte glycoprotein (MOG) and proteolipid protein (PLP), said peptide fragment being in linear or cyclic form; wherein said epitope is linked to mannan via a [(LyS-GIy)n] bridge, where n is an integer from 1 to 10. Further aspects of the invention relate to pharmaceutical compositions comprising said conjugates, and their use in the preparation of a medicament for treating an immune disorder.Type: ApplicationFiled: January 22, 2009Publication date: October 6, 2011Applicant: Eldrug S.A.Inventors: John Matsoukas, Theodoros Tselios, Vasso Apostolopoulos, Vivian Tseveleki, Maria Katsara, Lesley Probert
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Publication number: 20110230638Abstract: Methods and reagents are disclosed for determining the presence and/or amount of cyclosporin A in a medium suspected of containing cyclosporin A. In the method a combination is provided in a medium. The combination comprises (i) the sample, (ii) a first member of a signal producing system (sps) associated with a first support wherein the first sps member is capable of activating a second member of the sps and wherein the first support is associated with a first member of a specific binding pair, and (iii) the second sps member associated with a second support wherein the second sps member is activatable by the first sps member. The second support comprises either (I) cyclosporin C or cyclosporin A and the combination further comprises a conjugate of an antibody for cyclosporin A and a second member of the specific binding pair or (II) antibody for cyclosporin A and the combination further comprises a conjugate of cyclosporin A and a second member of the specific binding pair.Type: ApplicationFiled: April 27, 2011Publication date: September 22, 2011Applicant: SIEMENS HEALTHCARE DIAGNOSTICS INC.Inventors: Yi Feng Zheng, Deb K. Vickery, Susan C. Swann
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Publication number: 20110230426Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 8 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly or Pro or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: August 8, 2008Publication date: September 22, 2011Applicants: POLYPHOR AG, UNIVERSITAT ZURICHInventors: Daniel Obrecht, Frank Gombert, Markus Seitz, Ludovic T. Maillard, Roba Mounme, Kerstin Moehle, John Anthony Robinson, Odile Sellier-Kessler, Heiko Henze, Christian Bisang, Alexander Lederer
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Patent number: 8008440Abstract: 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 the preparation of these compounds in a combinatorial manner, is also disclosed.Type: GrantFiled: December 22, 2006Date of Patent: August 30, 2011Assignee: Tranzyme Pharma Inc.Inventors: Pierre Deslongchamps, Yves Dory, Gilles Berthiaume, Luc Ouellet, Ruoxi Lan
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Publication number: 20110206637Abstract: The present invention provides antiviral compounds of formula (I), as well as pharmaceutical compositions comprising these compounds, methods for synthesizing these compounds and methods of using these compounds for treating a viral infection.Type: ApplicationFiled: February 23, 2011Publication date: August 25, 2011Inventors: Yat Sun Or, In Jong Kim, Guoqiang Wang, Jiang Long
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Publication number: 20110200528Abstract: Cyclized peptide compounds containing the NGR motif of formula (I) or a pharmaceutically-acceptable salt thereof are disclosed. Compositions comprising the cyclized peptide compounds and methods of their use are also disclosed.Type: ApplicationFiled: June 15, 2009Publication date: August 18, 2011Inventors: Bradford J. Wood, Matthew Dreher, Ayele H. Negussie
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Publication number: 20110195914Abstract: The instant invention describes macrocyclic compounds having antiproliferation activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders.Type: ApplicationFiled: January 15, 2009Publication date: August 11, 2011Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATIONInventors: Hendrik Luesch, Valerie J. Paul, Jason C. Kwan
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Publication number: 20110195861Abstract: A liposomal composition, preferably a vaccine, comprising liposomes formed of liposome forming compounds, containing coentrapped polysaccharide antigen and T-cell dependent protein carrier, such as tetanus toxoid or diphtheria toxin modified to render it non-toxic. The invention is of use in the production of vaccines against Haemophilus influenzae, Streptococcus pneumoniae or Neisseria meningitidis.Type: ApplicationFiled: January 24, 2011Publication date: August 11, 2011Applicant: Stichting voor de technische wetenschappenInventors: Waltherus Jacobus Wilhelmus VAN VENROOIJ, Jan Wouter Drijfhout, Martinus Adrianus Maria Van Boekel, Gerardus Jozef Maria Pruijn
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Publication number: 20110190212Abstract: Cyclic tetrapeptides that are kappa opioid receptor (KOR) antagonists can be used in therapeutic applications for treating, inhibiting, and/or preventing drug addiction, drug use, or drug seeking behavior in a subject. This can include subjects that have a history of drug addiction. The drug can be selected from cocaine, alcohol, amphetamines, methamphetamines, nicotine, opiate, or combinations thereof. These cyclic tetrapeptides can also be useful for treating, inhibiting, and/or preventing stress-induced drug seeking behavior.Type: ApplicationFiled: July 10, 2009Publication date: August 4, 2011Applicant: UNIVERSITY OF KANSASInventors: Jane V. Aldrich, Nicolette C. Ross, Santosh Kulkarni