Cyclic Peptides Patents (Class 530/317)
  • Patent number: 8772446
    Abstract: A bifunctional chelating agent of the formula (I): wherein the variables R1, R1?, Q1, Q2 and M are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a stable or radioactive metal; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: July 8, 2014
    Assignee: Nordion (Canada) Inc.
    Inventors: Mike Adam, Eszter Boros, Cara L. Ferreira, Chris Orvig, Eric William Price
  • Patent number: 8765684
    Abstract: 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: Grant
    Filed: September 16, 2013
    Date of Patent: July 1, 2014
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Clemens Kuehn, Kerstin Seemann, Christoph Saal, Gerald Scholz, Soenke Petersen, Harald Untenecker, Michael Lange
  • Patent number: 8764733
    Abstract: Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: July 1, 2014
    Assignee: Rani Therapeutics, LLC
    Inventor: Mir Imran
  • Patent number: 8765907
    Abstract: The invention relates to a compound of the general structure (I), where R is a hydrogen atom (II) or an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, wherein the alkyl is straight, branched, cyclic and/or partially unsaturated, or an unsubstituted, monosubstituted or polysubstituted phenyl group.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: July 1, 2014
    Assignee: Geomar Helmholtz-Zentrum fur Ozeanforschung Kiel
    Inventors: Johannes Imhoff, Inga Knopf-Kajahn, Gerhard Lang, Jutta Wiese, Arne Peters
  • Publication number: 20140179897
    Abstract: The present invention relates to the crystal structures of dolastatin 16, dolamethylleuine and dolaphenvaline. The present invention also relates to processes for preparing dolamethylleuine and dolaphenvaline. The present invention further relates to computer readable medium with crystal structural data and/or information stored thereon.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 26, 2014
    Inventors: George R. Pettit, Thomas Smith, Jun-Ping Xu, Delbert Herald
  • Patent number: 8759259
    Abstract: Embodiments of the invention are directed to a one-bead-two-compound method for the creation of encoded cyclic peptoid libraries. This scheme is useful for the creation of cyclic peptoid microarrays since only the cyclic peptoid, not the linear encoding molecule, contains an attachment residue and thus can be spotted onto an activated substrate.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: June 24, 2014
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Yong-Uk Kwon, Thomas Kodadek
  • Patent number: 8759114
    Abstract: Peptides useful in determining the presence of autoantibodies in patients suffering from rheumatoid arthritis are disclosed.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: June 24, 2014
    Assignee: Stichting Voor de Technische Wetenschappen
    Inventors: Waltherus Jacobus Wilhelmus Van Venrooij, Jan Wouter Drijfhout, Martinus Adrianus Maria Van Boekel, Gerardus Jozef Maria Pruijn
  • Patent number: 8759480
    Abstract: According to the present invention, there is provided a range of new conotoxin derivatives and methods for synthesizing these analogues and other intramolecular dicarba bridge-containing peptides, including dicarba-disulfide bridge-containing peptides.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: June 24, 2014
    Assignee: Syngene Limited
    Inventors: Andrea Robinson, Jomana Elaridi
  • Patent number: 8759296
    Abstract: A cyclized peptide designated BMP Binding Peptide (BBP) is a synthetic peptide that avidly binds rhBMP-2. BBP increases the overall osteogenic activity of rhBMP-2, increases the rate at which rhBMP-2 induces bone formation, and BBP induces calcification alone. Compositions and substrates including BBP, and methods of using BBP are useful in therapeutic, diagnostic and clinical applications requiring calcification and osteogenesis.
    Type: Grant
    Filed: May 25, 2012
    Date of Patent: June 24, 2014
    Assignees: The Regents of The University of California, The United States of America as Represented by The Department of Veterans Affairs
    Inventors: Samuel S. Murray, Keyvan Behnam, Elsa J. Brochmann-Murray
  • Publication number: 20140170064
    Abstract: Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [125I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Charles Andrew Boswell, Leslie A. Khawli, Jan Marik, Simon Williams
  • Patent number: 8754049
    Abstract: A cyclic organic compound which comprises 16 amino acids or 17 amino acids and has no carboxyl group C-terminally and/or no amino group N-terminally. Optionally, one of the amino acids is a nonnatural amino acid. The ring closure is formed between a side chain of one amino acid and the C-terminus of another amino acid, or the ring closure is effected with the aid of a nonnatural amino acid. A process for producing and using the compound for regulating vectorial ion channels, for treating diseases associated with the lung function and for treating oedemas is provided.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: June 17, 2014
    Assignee: APEPTICO Forschung und Entwicklung GmbH
    Inventors: Bernhard Fischer, Rudolf Lucas, Susan Tzotzos
  • Publication number: 20140162939
    Abstract: The invention provides compounds of formula (I): and salts thereof, wherein X and Y have any of the values defined herein. The compounds inhibit bacterial RNA polymerase, inhibit bacterial growth, and have applications in, analysis of RNA polymerase structure and function, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, antibacterial therapy, and drug discovery.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 12, 2014
    Inventors: Richard H. Ebright, Yon W. Ebright, Yu Feng, David Degen
  • Publication number: 20140162940
    Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase that contain: (i) a first moiety that binds to the salinamide binding site of a bacterial RNA polymerase; (ii) a second moiety comprising a nucleoside analog; and (iii) a linker connecting said first and second moieties.
    Type: Application
    Filed: December 12, 2013
    Publication date: June 12, 2014
    Inventors: Richard H. Ebright, Yu Feng, Yu Zhang
  • Patent number: 8748388
    Abstract: Antitumoral compounds of Formula I, and pharmaceutically acceptable salts, derivatives, tautomers, prodrugs or stereoisomers thereof useful as antitumour agents.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: June 10, 2014
    Assignee: Pharma Mar, S.A.
    Inventors: Judit Tulla-Puche, Eleonora Marcucci, Núria Bayó-Puxan, Fernando Albericio, Maria del Carmen Cuevas Marchante
  • Patent number: 8748105
    Abstract: The invention relates to the field of candidate drug testing and drug development. A method is provided for providing a compound composed of at least one molecule attached via at least two linkages to a molecular scaffold, the method comprising providing a scaffold comprising at least a first and a second reactive group; providing at least one molecule capable of reacting with the at least first and second reactive group; contacting the scaffold with at least one molecule to form at least two linkages between the scaffold and the at least one molecule in a coupling reaction, wherein the formation of a linkage accelerates the formation of a consecutive linkage, preferably wherein the coupling reaction is performed in solution, more preferably in an aqueous solution. Furthermore, a method is provided for selecting a candidate drug compound comprising providing a library of compounds according to the invention and determining the binding of a target molecule to the compounds.
    Type: Grant
    Filed: August 26, 2005
    Date of Patent: June 10, 2014
    Assignee: Pepscan Systems B.V.
    Inventors: Peter Timmerman, Joris Beld, Robbert Hans Meloen, Wouter Cornelis Puijk
  • Patent number: 8748570
    Abstract: A dicarba analogue of insulin comprising an A-chain and a B-chain or fragments, salts, solvates, derivatives, isomers or tautomers of the A-chain, the B-chain or both, provided that the dicarba analogue is not [A7,B7-(2,7-diaminosuberoyl]-des-(B26-B30)-insulin B25-amide.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Syngene Limited
    Inventors: Andrea Robinson, Bianca Van Lierop
  • Publication number: 20140154291
    Abstract: Peptides are provided consisting of L- and/or D-amino acids and combinations thereof, which affect myeloid cells by action on the triggering receptors expressed on myeloid cells (TREMs), including TREM-1 and TREM-2. The peptides act on the TREM/DAP-12 signaling complex. Also provided are lipid and sugar conjugated peptides comprising L- or D-amino acids. A method is provided of designing the peptides and lipid- and/or sugar-conjugated peptides comprising L- or D-amino acids. The disclosure relates to the therapy of various myeloid cell-related disease states involving the use of these peptides and compounds. The peptides and compounds are useful in the treatment and/or prevention of a disease or condition where myeloid cells are involved or recruited. The peptides of the present invention also are useful in the production of medical devices comprising peptide matrices (for example, medical implants and implantable devices).
    Type: Application
    Filed: July 12, 2013
    Publication date: June 5, 2014
    Applicant: SIGNABLOK, INC.
    Inventor: Alexander B. Sigalov
  • Patent number: 8741842
    Abstract: This document provides natriuretic polypeptides. For example, this document provides polypeptides having a natriuretic activity. In some cases, a polypeptide provided herein can have natriuretic activities without inducing excessive hypotension. This document also provides methods and materials for inducing natriuretic activities within a mammal.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: June 3, 2014
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: John C. Burnett, Jr., Candace Y. W. Lee
  • Publication number: 20140148573
    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: January 31, 2014
    Publication date: May 29, 2014
    Applicants: Enanta Pharmaceuticals, Inc., AbbVie, Inc.
    Inventors: Yiyin Ku, Keith F. McDaniel, Hui-Ju Chen, Jason P. Shanley, Dale J. Kempf, David J. Grampovnik, Ying Sun, Dong Liu, Yonghua Gai, Yat Sun Or, Seble H. Wagaw, Kenneth Engstrom, Tim Grieme, Ahmad Sheikh, Jianzhang Mei
  • Publication number: 20140147455
    Abstract: 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 comcomitant removal of T-cells associated with autoimmune disorders.
    Type: Application
    Filed: October 24, 2013
    Publication date: May 29, 2014
    Applicant: OPKO Pharmaceuticals, LLC
    Inventors: Phillip FROST, Thomas Kodadek
  • Publication number: 20140142277
    Abstract: The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
    Type: Application
    Filed: September 30, 2013
    Publication date: May 22, 2014
    Applicant: Aurinia Pharmaceuticals Inc.
    Inventors: Selvaraj A. Naicker, Randall W. Yatscoff, Robert T. Foster
  • Publication number: 20140142031
    Abstract: The present invention relates to novel anti-TB cyclic peptides from Nonomuraea sp. MJM5123, a process for the production of the anti-Tuberculosis peptide and a pharmaceutical composition for the prevention and treatment of mycobacterial infection comprising the same. The composition of the present invention is highly active against replicating/non-replicating M. tuberculosis, including MDR and XDR strains, so that it can be effectively used as a therapeutic agent for tuberculosis.
    Type: Application
    Filed: April 18, 2012
    Publication date: May 22, 2014
    Inventors: Jong Woo Kim, Sang Wook Lee, Sang jin Park, Joo Won Suh, In Ae Lee, Tae Mi Yoon, Jong Keun Choi, Ji Ean Lee, Jin Yong Kim, Ying Yu Jin, Scott Franzblau, Sanghyum Cho, Wei Gao, Guido Pauli, James McAlpine, Jose Napolitano, Birgit Jaki, Brent Friesen, Maria Florencia Rodriguez Brasco, David Lankin
  • Patent number: 8729224
    Abstract: Methods for use of a melanocortin receptor agonist cyclic peptide of the formula where R, x and y are as defined in the specification, and compositions and formulations including the peptide of the foregoing formula, for preventing, ameliorating or treating female sexual dysfunction.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: May 20, 2014
    Assignee: Palatin Technologies, Inc.
    Inventors: Yi-Qun Shi, Shubh D. Sharma, Wei Yang, Xin Chen
  • Patent number: 8729031
    Abstract: Compounds of formula (IV) and pharmaceutical compositions comprising the same are described, wherein X1 and X2, R3, L, Ar1, p and Z have the values disclosed herein.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: May 20, 2014
    Assignee: Novacta Biosystems Limited
    Inventor: Sjoerd Nicolaas Wadman
  • Patent number: 8729029
    Abstract: The invention relates to peptide derivatives (peptides and pseudo-peptides) and use thereof as vectors for molecules of interest. The invention also relates to conjugates containing a peptide derivative of the invention bound to a molecule of interest. The peptides and prodrug conjugates of the invention can be used to vectorise molecules of pharmaceutical or diagnostic interest, such as, for example, therapeutic molecules, imaging or diagnostic agents, or molecular probes, across cell membranes, and notably to promote their transport across the blood-brain barrier (BBB).
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: May 20, 2014
    Assignees: Vect-Horus, Centre National de la Recherche Scientifique, Universite d'Aix-Marseille
    Inventors: Michel Khrestchatisky, Marion David, Yves Molino, Patrick Vlieghe
  • Publication number: 20140135274
    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: Application
    Filed: January 21, 2014
    Publication date: May 15, 2014
    Inventor: Kunwar Shailubhai
  • Patent number: 8722628
    Abstract: An autophagy-inducing compound comprises an autophagy-inducing peptide comprising beclin-1 residues 269-283 and a heterologous moiety that promotes therapeutic stability or delivery of the compound. The compound may be used to induce autophagy and in assays with beclin-1 binding partners.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: May 13, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Beth C. Levine, Sanae Shoji-Kawata, Olivier Lichtarge, Angela D. Wilkins
  • Publication number: 20140128544
    Abstract: The present invention relates to immobilized biologically active entities that retain a significant biological activity following manipulation. The invention also comprises a medical substrate comprising a heparin entity bound onto a substrate via at least one heparin molecule, wherein said bound heparin entity is heparinase-1 sensitive.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: W. L. Gore & Associates, Inc.
    Inventors: Roy Biran, Charles D. Claude, Robert L. Cleek, Paul D. Drumheller
  • Patent number: 8716436
    Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 6, 2014
    Assignees: The Administrators of the Tulane Educational Fund, U.S. Department of Veterans Affairs
    Inventors: James E. Zadina, Laszlo Hackler
  • Publication number: 20140121354
    Abstract: The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 1, 2014
    Applicant: IPSEN PHARMA S.A.S.
    Inventors: ZHENG XIN DONG, YEELANA SHEN, SUN HYUK KIM
  • Publication number: 20140121169
    Abstract: 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: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Inventors: Kunwar Shailubhai, Gregory Nikiforovich, Gary S. Jacob
  • Publication number: 20140121168
    Abstract: TRPV1 antagonists and associated methods are provided. A TRPV1 channel antagonist can have the structure: Formula (I) wherein R1 can be —CH3, —(CH2)X(CH)YCH3 where x+y=1-20, an aromatic, a (CH2)n aromatic where n can be less than or equal to 6, a lipid, or a linker, and wherein R2 can be either Formula (II) or Formula (III) Additionally, R3 can be —O—R4 or —NH—R4 and R4 can be —H, —CH3, an ester, a cyclic ester, or an amide.
    Type: Application
    Filed: April 26, 2012
    Publication date: May 1, 2014
    Applicant: ANTAGONISTS OF TRPV1 RECEPTOR
    Inventors: Eric Schmidt, Alan R. Light, Baldomero M. Olivera, Christopher A. Reilly, Zhejian Lin, Gisela P. Concepcion
  • Patent number: 8710180
    Abstract: The present application provides biligand and triligand protein-catalyzed capture (PCC) agents that specifically bind VEGF, as well as the use of these capture agents as detection, diagnosis, and treatment agents.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: April 29, 2014
    Assignee: Indi Molecular, Inc.
    Inventors: Suresh Mark Pitram, Heather Dawn Agnew, Tsun Yin Lai, Rosemary Dyane Rohde, Paul Edward Kearney
  • Publication number: 20140114049
    Abstract: The method of the preparation of micafungin sodium comprises the step of mixing the weak base and the aqueous solution containing micafungin acid (the structure is illustrated by formula I) or the mixed aqueous solution containing the compound of formula I and organic solvent in order to obtain the sodium salt of micafungin (the structure is illustrated by formula II).
    Type: Application
    Filed: May 11, 2012
    Publication date: April 24, 2014
    Applicant: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.
    Inventors: Guangjun Jiao, Shidong Liu, Bingming He, Zhijun Tang, Xiaoming Ji
  • Publication number: 20140113348
    Abstract: Antibodies and meditopes that bind to the antibodies are provided, as well as complexes, compositions and combinations containing the meditopes and antibodies, and methods of producing, using, testing, and screening the same, including therapeutic and diagnostic methods and uses.
    Type: Application
    Filed: February 11, 2013
    Publication date: April 24, 2014
    Applicant: City of Hope
    Inventors: John C. Williams, Cindy Zer, Krzysztof Bzymek, Kendra Nicole Avery
  • Publication number: 20140107031
    Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 4 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, 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 the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: POLYPHOR LTD.
    Inventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Alexander Lederer, Christian Bisang, Odile Sellier-Kessler, Francoise Jung, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
  • Patent number: 8697638
    Abstract: The present invention relates to crystalline and crystal-like forms of lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention relates to methods of purifying lipopeptides, including daptomycin, a lipopeptide antibiotic with potent bactericidal activity against gram-positive bacteria, including strains that are resistant to conventional antibiotics. The present invention also relates to pharmaceutical compositions comprising the purified form of the lipopeptide and methods of using these compositions.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: April 15, 2014
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Dennis Keith, Jan-Ji Lai, Chandrika Govardhan, Nazer Khalaf
  • Publication number: 20140100353
    Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I employing an aldehyde acetal intermediate, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: NOVARTIS AG
    Inventors: Murat ACEMOGLU, Heribert HELLSTERN, Bernard RISS, Christian SPRECHER
  • Patent number: 8691756
    Abstract: The present application describes a method of treating a bacterial infection comprising administering to a subject in need thereof a pharmaceutically acceptable amount of a defined macrocycle compound.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: April 8, 2014
    Assignee: Novartis AG
    Inventors: Roger Aki Fujimoto, Philipp Krastel, Matthew J. LaMarche
  • Publication number: 20140094402
    Abstract: The present invention concerns novel lantibiotic compounds, processes for the isolation and preparation thereof, pharmaceutical compositions containing the same, pharmaceutical acceptable salts thereof, and methods of use of the lantibiotics as antibacterial agents.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 3, 2014
    Applicant: SENTINELLA PHARMACEUTICALS, INC.
    Inventors: Sonia Ilaria Maffioli, Matteo Simone, Paolo Monciardini, Eleonora Gaspari
  • Publication number: 20140094400
    Abstract: The invention relates to novel pharmaceutically-useful peptides, in particular cyclic peptides that are agonists of the AngII type 2 receptor (AT2 receptor). The invention further relates to the use of such peptides as medicaments, to pharmaceutical compositions containing them, and to their production.
    Type: Application
    Filed: November 22, 2011
    Publication date: April 3, 2014
    Applicant: LANTHIOPEP B.V.
    Inventors: Louwe De Vries, Sieger Adriaan Nelemans, Rick Rink, Antonius Jacobus Marinus Roks, Gert Nikolaas Moll
  • Publication number: 20140087997
    Abstract: A method of treating a bacterial infection in a subject is disclosed. The method comprises administering to the subject a therapeutically effective amount of a peptide being between 3 and 5 amino acids, wherein at least one amino acid of said 3 and 5 amino acids is selected from the group consisting of tryptophan, cysteine, proline and methionine.
    Type: Application
    Filed: May 10, 2012
    Publication date: March 27, 2014
    Inventors: Noam Adir, Sharon Navon, Tali Swartzmann
  • Publication number: 20140073761
    Abstract: Described herein are compositions and methods for use in targeted drug delivery using cell receptor binding drug delivery conjugates containing hydrophilic spacer linkers for use in imaging, diagnosing, and/or treating diseases and disease states caused by pathogenic cell populations.
    Type: Application
    Filed: March 5, 2013
    Publication date: March 13, 2014
    Applicant: ENDOCYTE, INC.
    Inventor: ENDOCYTE, INC.
  • Publication number: 20140073762
    Abstract: The present invention generally provides a separation matrix comprising at least two stationary phases and a stationary phase comprising at least one chiral modality and at least one achiral modality. Also provided are methods of using the separation matrix or the stationary phase to separate enantiomers of one or more chiral molecules.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Applicant: Board of Trustees of the University of Arkansas
    Inventors: Grover Miller, Drew R. Jones, Gunnar Boysen
  • Publication number: 20140066382
    Abstract: An autophagy-inducing compound comprises an autophagy-inducing peptide comprising beclin-1 residues 269-283 and a heterologous moiety that promotes therapeutic stability or delivery of the compound. The compound may be used to induce autophagy and in assays with beclin-1 binding partners.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 6, 2014
    Applicants: Baylor College of Medicine, Board of Regents, The University of Texas System
    Inventors: Beth C. Levine, Sanae Shoji-Kawata, Olivier Lichtarge, Angela D. Wilkins
  • Patent number: 8664181
    Abstract: A prodrug comprising at least two different pharmaceutically and/or diagnostically active compounds independently bound by cleavable linkers and a protein-binding moiety which is capable of binding to carrier a molecule is described.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: March 4, 2014
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: Felix Kratz, Irmgard Merfort
  • Publication number: 20140057857
    Abstract: Cross-linked proteins and peptides, and methods of making and uses of such cross-linked proteins and peptides. The cross-linked proteins and peptides have rigid, distance-matching bismethylene aryl cross-linking moieties. Compositions comprising the cross-linked proteins and peptides can be used as pharmaceutical delivery formulations. The cross-linked proteins and peptides can have improved properties, such as cell permeability, as compared to the parent protein or peptide.
    Type: Application
    Filed: December 15, 2011
    Publication date: February 27, 2014
    Applicant: The Research Foundation for the State University of New York
    Inventors: Qing Lin, Avinash Muppidi
  • Publication number: 20140056811
    Abstract: The present invention is related to peptides, which are suitable for use as cell-penetrating peptides (CPPs), variants thereof and/or complexes, fusion molecules and/or conjugates comprising same, use thereof for manufacture of compositions for diagnosing, treating and/or preventing of medical conditions.
    Type: Application
    Filed: December 26, 2011
    Publication date: February 27, 2014
    Applicant: COMPUGEN LTD.
    Inventors: Etai Jacob, Amir Toporik, Ronen Shemesh, Ofer Levy
  • Patent number: 8658604
    Abstract: Template-fixed ?-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 ?-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or Pro(4NHCOPhe), 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 the property to inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: February 25, 2014
    Assignees: Polyphor Ltd, Universitat Zurich
    Inventors: Steven J. DeMarco, Kerstin Moehle, Heiko Henze, Odile Sellier, Françoise Jung, Frank Gombert, Daniel Obrecht, Christian Ludin
  • Publication number: 20140050728
    Abstract: Methods and compositions for modulating cyclophilin D, e.g., at least one cyclophilin D biological activity, are provided. Modulation of cyclophilin D is useful in preventing or treating obesity, an overweight condition, or in accommodating a desire to lose weight as well as being useful in treating a variety of kidney diseases.
    Type: Application
    Filed: January 27, 2012
    Publication date: February 20, 2014
    Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventor: Babu Padanilam