Containing Only Normal Peptide Links In The Ring, I.e., Homodetic Cyclic Peptides Patents (Class 530/321)
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Publication number: 20140378390Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.Type: ApplicationFiled: August 15, 2014Publication date: December 25, 2014Inventors: Vincent GUERLAVAIS, Noriyuki KAWAHATA
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Publication number: 20140363376Abstract: In some aspects, the present invention provides novel ligands, which may be used to make novel dual-modality imaging agents, for example, for PET and MRI imaging. In further aspects, by the present disclosure also provides methods of use and methods of preparation of the novel ligands, metal complexes, and imaging agents thereof.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: Board of Regents, The University of Texas SystemInventors: Xiankai SUN, Amit Kumar, Zoltan Kovacs
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Publication number: 20140357569Abstract: 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: February 28, 2014Publication date: December 4, 2014Applicant: UCL Business PLCInventors: David Selwood, Martin Crompton
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Publication number: 20140357575Abstract: Melanocortin receptor-specific cyclic heptapeptides of the formula Z-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Y??(II) or a pharmaceutically acceptable salt thereof, where Z, Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7 and Y are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.Type: ApplicationFiled: July 11, 2014Publication date: December 4, 2014Inventors: Yi-qun Shi, Shubh D. Sharma, John H. Dodd, Wei Yang
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Patent number: 8883718Abstract: Provided is a cyclic peptide which comprises: (i) a CDK4 peptide region; and (ii) a cell-penetrating region; wherein the CDK4 peptide region comprises the amino acid sequence P1R1x1y1R2P2V (SEQ ID NO: 1), in which P1 and P2 are each proline, R1 and R2 are each arginine and each of x1 and y1 are either a linker or proline, wherein if x1 is a linker then y1 is proline or if x1 is proline then y1 is a linker, or wherein x1 and y1 when taken together form a linker, and wherein V may be present or absent; and wherein the cell-penetrating region is capable of enhancing the uptake of the cyclic peptide or a part thereof into cancer cells and comprises an amphiphilic amino acid sequence; and wherein the cyclic peptide or a part thereof is cytotoxic to and/or inhibiting to the growth of a cancer cell.Type: GrantFiled: March 11, 2009Date of Patent: November 11, 2014Assignee: Theryte LimitedInventors: Hilmar Meek Warenius, William Ure Primrose
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Publication number: 20140316104Abstract: The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.Type: ApplicationFiled: August 29, 2012Publication date: October 23, 2014Applicants: LEAD DISCOVER CENTER GMBH, MAX-PLANCK-GUSELLSCHAFT ZUR FÖRDERUNG DER WISSENSCHAFTEN E.V.Inventors: Gunter Fischer, Miroslav Malesevic, Frank Erdmann, Jan Kuhling, Michael Bukrinsky, Stephanie Constant, Gerd Ruhter, Peter Nussbaumer, Klaus Dinkel
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Patent number: 8865648Abstract: Methods are disclosed for determining progression of a condition, onset of a condition, or efficacy of treatment of a condition characterized by an adipocyte imbalance in a patient. In addition, methods are disclosed of treating diabetes, abnormal adipocyte activity, and insulin resistance using monomeric, homodimeric, and heterodimeric forms of certain C-terminal fragments of adiponectin receptor. In addition, methods of treating abnormal adipocyte activity, treating metabolic syndrome, causing insulin secretion, increasing insulin levels, inhibiting insulin degradation enzyme, treating Alzheimer's disease, treating cardiovascular disease associated with adiponectin levels, inhibiting ADAM-17 enzyme, inhibiting a protease, treating a condition associated with TNF-alpha, and treating a condition associated with HER2-neu are disclosed. Compositions, dosage forms, and kits are also disclosed.Type: GrantFiled: April 13, 2010Date of Patent: October 21, 2014Assignee: Siemens Healthcare Diagnostics Inc.Inventors: Michael J. Pugia, Rui Ma
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Publication number: 20140309160Abstract: The present invention relates to a plant disease control agent containing a compound represented by the following formula (1) or salt thereof as an active ingredient (in the formula, R1 and R2 represents a hydrogen atom or methyl group but excepting cases where R1 and R2 are the same), a plant disease controlling method applying the plant disease control agent on plants suffering from diseases, and a novel compound represented by formula (1) or salt thereof.Type: ApplicationFiled: December 22, 2011Publication date: October 16, 2014Applicant: SDS BIOTECH K. K.Inventors: Keijitsu Tanaka, Yusuke Amaki, Motoki Tanaka, Mutsumi Miyazaki
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Patent number: 8859723Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.Type: GrantFiled: August 13, 2011Date of Patent: October 14, 2014Assignee: Aileron Therapeutics, Inc.Inventors: Vincent Guerlavais, Noriyuki Kawahata
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Publication number: 20140303071Abstract: The present invention relates to cyclic cationic peptides and their use in the treatment of microbial infections.Type: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventor: Deborah O'NEIL
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Publication number: 20140303075Abstract: Provided are bioactive compounds and metabolites derived from Chromobacterium species culture responsible for controlling pests, compositions containing these compounds, methods for obtaining these compounds and methods of using these compounds and compositions for controlling pests.Type: ApplicationFiled: June 2, 2014Publication date: October 9, 2014Applicant: Marrone Bio Innovations, Inc.Inventors: Ratnakar Asolkar, Huazhang Huang, Marja Koivunen, Pamela Marrone
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Patent number: 8853151Abstract: The present invention provides methods, compositions and applications for efficient, site-specific drug delivery using pro-drug complexes comprising one or more functional groups (e.g., imaging agents, targeting agents, and trigger agents) 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.))). Trigger agents include an indolequinone; attachment groups include a triazole ring; and therapeutic agents include camptothecin.Type: GrantFiled: June 30, 2010Date of Patent: October 7, 2014Assignee: The Regents of the University of MichiganInventors: James R. Baker, Jr., Baohua M. Huang, Thommey P. Thomas
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Publication number: 20140294865Abstract: The invention relates to tumor therapy. In one aspect, the present invention relates to conjugates of an amatoxin and a target-binding moiety, e.g. an antibody, connected by certain linkages, which are useful in the treatment of cancer. In a further aspect the invention relates to pharmaceutical compositions comprising such conjugates.Type: ApplicationFiled: March 9, 2012Publication date: October 2, 2014Applicant: HEIDELBERG PHARMA GMBHInventors: Werner Simon, Christian Lutz, Christoph Muller, Jan Anderl
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Publication number: 20140296160Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.Type: ApplicationFiled: November 1, 2013Publication date: October 2, 2014Applicants: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Loren D. Walensky, Stanley J. Korsmeyer, Gregory Verdine
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Publication number: 20140296477Abstract: Antagonist peptide of the bond between CD47 and a protein belonging to the thrombospondin family has the sequence S1 R1-R2-R3-S-Q-L-L-K-G-R4-R5-R6 and interacts specifically with the C-terminal end of the TSP, at the site of the bond between the TSP and the CD47 receptor. Interaction between the CD47 receptor and the protein is prevented. The peptide can be used in the context of cancer treatments.Type: ApplicationFiled: July 6, 2012Publication date: October 2, 2014Inventors: Stéphane Dedieu, Nicolas Floquet, Laurent Martiny, Christophe Schneider, Albin Jeanne, Emilie Sick, Manuel Dauchez
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Publication number: 20140294942Abstract: In certain embodiments this invention provides novel antiviral peptide(s) that are effective against positive sense RNA viruses that have an internal ribosome entry site (IRES). The peptide(s) can be used to inhibit propagation of such viruses and thereby provide a effective modality for the treatment of infections such as hepatitis C, and the like.Type: ApplicationFiled: September 6, 2012Publication date: October 2, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Samuel Wheeler French, Ronik Khachatoorian, Piotr Pawel Ruchala
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Publication number: 20140287986Abstract: Novel template-fixed ?-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] wherein the single elements T or P are ?-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: October 2, 2012Publication date: September 25, 2014Applicant: POLYPHOR AGInventors: Françoise Jun, Danie Obrecht, Ralf Löwe, Johann Zimmermann, Guillaume Lemercier, Eric Chevalier
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Publication number: 20140274884Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: Kyla L. Bjornson, Kapil K. Karki, John O. Link, Hyung-jung Pyun, Adam J. Schrier, Kirk L. Stevens, James G. Taylor, Randall W. Vivian, Jeff Zablocki, Sheila Zipfel
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Publication number: 20140256628Abstract: Isolated peptides, compositions and methods of use for treating tumors infiltrated with macrophages, such as glioblastomas.Type: ApplicationFiled: May 16, 2014Publication date: September 11, 2014Applicant: NENCKI INSTITUTE OF EXPERIMENTAL BIOLOGYInventors: Bozena Kaminska-Kaczmarek, Malgorzata Sielska, Pawel Wisniewski, Aleksandra Ellert-Miklaszewska
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Publication number: 20140256651Abstract: The present invention describes Cyclosporine A/steroid hybrid analogs. These single drug entities are formed by connecting a steroid with Cyclosporine A. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256615Abstract: Compounds that affect quorum sensing (QS) in Staphylococcus aureus and related Staphylococcus species (e.g., S. epidermidis). Compounds which modulate one or more of the four AgrC receptors of Staphylococcus species, particularly of Staphylococcus aureus. Modulation includes inhibition or activation of one or more of these four AgrC receptors. These compounds are useful for bacterial interference and are useful for treating bacterial infections, particularly staphylococcal infection. Treatment can include combination of one or more of the compounds of the invention in combination with one or more antibiotics.Type: ApplicationFiled: December 17, 2013Publication date: September 11, 2014Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Helen BLACKWELL, Yftah TAL-GAN, Danielle STACY
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Patent number: 8829157Abstract: The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.Type: GrantFiled: January 17, 2011Date of Patent: September 9, 2014Assignee: USV, Ltd.Inventors: Divya Lal Saksena, Chandrakesan Muralidharan, Lester Lobo, Digamber Shripati Pawar, Nikhil Umesh Mohe, Radhakishnan Venkatasubramanian Tarur
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Publication number: 20140243258Abstract: Methods and compositions are presented for use in diagnostic, imaging or targeting of therapeutic agents to treat obesity/adiposity-associated disorders, where such as compositions and methods identify and use peptides to selectively target adipose tissue stromal cells in mammals, both in vitro and in vivo.Type: ApplicationFiled: March 30, 2012Publication date: August 28, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Mikhail G. Kolonin, Alexes Daquinag, Yan Zhang
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Publication number: 20140243501Abstract: The invention provides histone deacetylase (HDAC) inhibitors shown as Formula I, where R1 to R8 are as defined in the specification. The invention also provides methods for synthesis of these compounds and applications of these compounds in preparing pharmaceuticals for preventing or treating mammal diseases related to the dysregulation of HDAC.Type: ApplicationFiled: February 23, 2012Publication date: August 28, 2014Applicants: NANJING YOKO BIOMEDICAL R & D LTD. [CN/CN], NANJING XINGANG MEDICAL CO., LTD. [CN/CN], NANJING YOKO PHARMACEUTICAL CO., LTD. [CN/CN]Inventors: Sheng Jiang, Shang Li, Zhiyi Yao, Yiwu Yao, Feng Zhang, Yang Chao, Hai Ye, Min Chen
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Publication number: 20140235819Abstract: Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins 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 metabo-lism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and methods of producing immunosuppression with reduced toxicity using the disclosed cyclosporine derivatives.Type: ApplicationFiled: February 17, 2014Publication date: August 21, 2014Applicant: Aurinia Pharmaceuticals, Inc.Inventors: Selvaraj A. Naicker, Randall W. Yatscoff, Robert T. Foster
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Publication number: 20140235820Abstract: 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: April 29, 2014Publication date: August 21, 2014Applicant: GENENTECH, INC.Inventors: Eric Bourhis, Andrea Cochran, Yingnan Zhang
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Publication number: 20140235821Abstract: A substance contains a phosphatidylinositol-3-kinase (PI3K) inhibitor including a depsipeptide-class compound represented by formula (1), or a physiologically acceptable salt thereof that combines a PI3K inhibitory effect and an HDAC inhibitory effect to provide an anti-cancer pharmaceutical composition for the treatment of an intractable cancer.Type: ApplicationFiled: September 25, 2012Publication date: August 21, 2014Applicant: TOHOKU UNIVERSITYInventors: Ken Saijo, Chikashi Ishioka, Tadashi Katoh
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Patent number: 8809278Abstract: 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: GrantFiled: July 10, 2009Date of Patent: August 19, 2014Assignee: University of KansasInventors: Jane V. Aldrich, Nicolette C. Ross, Santosh Kulkarni
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Publication number: 20140228281Abstract: The invention concerns the use of cyclophilin inhibitors in the treatment of Hepatitis C virus infection.Type: ApplicationFiled: September 25, 2012Publication date: August 14, 2014Inventor: Claudio Avila
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Patent number: 8796221Abstract: Disclosed herein are methods of making cyclosporin A Form 2.Type: GrantFiled: November 14, 2012Date of Patent: August 5, 2014Assignee: Allergan, Inc.Inventors: Ke Wu, Scott W. Smith
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Publication number: 20140212381Abstract: Cyclosporin derivatives, methods of manufacturing the cyclosporin derivatives and methods for treating subjects infected with certain viruses, including hepatitis virus or HIV by administering the cyclosporin derivatives are described.Type: ApplicationFiled: October 21, 2013Publication date: July 31, 2014Applicant: Scynexis, Inc.Inventors: Keqiang Li, Michael Robert Peel
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Publication number: 20140213508Abstract: Cyclosporin derivatives, methods of manufacturing the cyclosporin derivatives and methods for treating subjects infected with certain viruses, including hepatitis virus or HIV by administering the cyclosporin derivatives are described.Type: ApplicationFiled: October 21, 2013Publication date: July 31, 2014Applicant: Scynexis, Inc.Inventors: Keqiang Li, Michael Robert PEEL
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Patent number: 8790691Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: GrantFiled: May 26, 2009Date of Patent: July 29, 2014Assignee: The University of British ColumbiaInventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20140206602Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase having the general structural formula (I): X-?-Y (I) wherein X is an moiety that binds to the rifamycin binding site of a bacterial RNA polymerase, Y is a moiety that binds to the GE23077 binding site of a bacterial RNA polymerase, and is a linker. The invention also provides compositions comprising such compounds, methods of making such compounds, and methods of using said compounds. The invention has applications in control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, and antibacterial therapy.Type: ApplicationFiled: June 20, 2012Publication date: July 24, 2014Inventors: Richard H. Ebright, David Degen, Yu Zhang, Yon Ebright
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Patent number: 8785394Abstract: Disclosed herein are methods of treating diseases of the eye by administering to the subconjunctival space a formulation comprising cyclosporin A form 2 and a hydrogel.Type: GrantFiled: November 14, 2012Date of Patent: July 22, 2014Assignee: Allergan, Inc.Inventors: Wendy M. Blanda, Mayssa Attar
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Patent number: 8778881Abstract: 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: GrantFiled: March 1, 2012Date of Patent: July 15, 2014Assignee: Ferring B.V.Inventors: Kazimierz Wisniewski, Claudio Schteingart, Regent LaPorte, Robert Felix Galyean, Pierre J.M. Riviere
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Publication number: 20140194369Abstract: Provided herein is a new class of cyclic lactadherin peptides (cLac) that mimic the natural phosphatidylserine (PS)-binding activity of the parent lactadherin protein. These cLacs are useful as small molecule indicators of early stage of apoptosis and of treatment efficacy evaluation.Type: ApplicationFiled: May 24, 2012Publication date: July 10, 2014Applicant: TRUSTEES OF BOSTON COLLEGEInventors: Jianmin Gao, Hong Zheng
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Patent number: 8772245Abstract: The present invention relates generally to crystalline forms of cyclosporine A and particularly to a newly identified form of cyclosporine A. The invention further relates to methods for its preparation and to methods for treating certain ocular disorders.Type: GrantFiled: May 25, 2012Date of Patent: July 8, 2014Assignee: Allergan, Inc.Inventors: Anuradha V. Gore, Kiomars Karami, Ke Wu, Richard S. Graham, Scott W. Smith
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Publication number: 20140187501Abstract: Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.Type: ApplicationFiled: December 30, 2013Publication date: July 3, 2014Applicant: Blend Therapeutics, Inc.Inventors: Mark T. Bilodeau, Sudhakar Kadiyala, Rajesh Shinde, Brian White, Richard Wooster, Timothy Edward Barder
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Publication number: 20140187471Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 ?-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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: February 7, 2014Publication date: July 3, 2014Applicants: UNIVERSITAET ZUERICH, POLYPHOR LTD.Inventors: Steven J. DEMARCO, Wim Vrijbloed, Ricardo Dias, John Anthony Robinson, Nityakalyani Srinivas, Frank Gombert, Daniel Obrecht
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Publication number: 20140187472Abstract: Template-fixed ?-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 ?-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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These ?-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.Type: ApplicationFiled: February 7, 2014Publication date: July 3, 2014Applicants: Universitaet Zuerich, Polyphor Ltd.Inventors: Steven J. DEMARCO, Wim Vrijbloed, Ricardo Dias, John Anthony Robinson, Nityakalyani Srinivas, Frank Gombert, Daniel Obrecht
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Patent number: 8765684Abstract: 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: GrantFiled: September 16, 2013Date of Patent: July 1, 2014Assignee: 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: 20140178302Abstract: The present invention relates to a novel class of diagnostically or therapeutically effective compounds comprising novel aza-bicycloalkane based cyclic peptides, acting as a targeting moiety towards integrin receptors.Type: ApplicationFiled: January 13, 2014Publication date: June 26, 2014Applicant: BRACCO IMAGING S.P.A.Inventors: Luciano LATTUADA, Pierfrancesco Morosini, Fulvio Uggeri, Silvio Aime, Enzo Terreno, Daniela Delli Castelli, Carlo Scolastico, Leonardo Manzoni, Daniela Arosio
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Patent number: 8759259Abstract: 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: GrantFiled: October 15, 2010Date of Patent: June 24, 2014Assignee: The Board of Regents of the University of Texas SystemInventors: Yong-Uk Kwon, Thomas Kodadek
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Publication number: 20140161719Abstract: The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics.Type: ApplicationFiled: March 14, 2013Publication date: June 12, 2014Applicant: The Regents of the University of CaliforniaInventors: Kit S. Lam, Yuanpei Li, ChongXian Pan, Tzu-yin Lin
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Publication number: 20140154208Abstract: The present invention relates to novel cyclosporine analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yat Sun Or, In Jong Kim, Jiang Long, Lijuan Jiang, Sheng Sean Liu, Guoqiang Wang
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Publication number: 20140155575Abstract: The invention provides processes of preparing a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-249 described herein.Type: ApplicationFiled: March 1, 2012Publication date: June 5, 2014Applicant: SYNERGY PHARMACEUTICALS INC.Inventors: Juncai Bai, Ruoping Zhang, Jun Jian, Junfeng Zhou, Qiao Zhao, Guoquing Zhang, Kunwar Shailubhai, Stephen Comiskey, Rong Feng
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Publication number: 20140154181Abstract: The invention provides RGD-containing cyclic peptidomimetics; conjugates of said peptidomimetics and a moiety of a payload selected from fluorescent probes, photosensitizers, chelating agents, or cytotoxic agents; and pharmaceutical compositions comprising these conjugates. The conjugates of the invention are useful both for diagnostic purposes and treatment of various diseases, disorders and conditions. More specifically, conjugates comprising fluorescent probes can be used for diagnostic purposes, e.g., visualization of organs and tissues, and diagnosis of tumors; conjugates comprising photosensitizers can be used for photodynamic therapy of both tumors and nonneoplastic tissues; conjugates comprising chelating agents can be used in radioimaging or radiotherapy; and conjugates comprising cytotoxic agents can be used for targeted chemotherapy.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: STEBA BIOTECH S.A.Inventors: Doron EREN, Tamar YECHEZKEL, Yoseph SALITRA, Natalia KOUDINOVA
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Publication number: 20140147416Abstract: Occidiofungin is a cyclic nonribosomally synthesized antifungal peptide with submicromolar activity. This invention is directed to compositions enriched for particular occidiofungin diastereomers/conformers, methods of making compositions enriched for particular diastereomers/conformers and microorganisms suitable for producing enriched compositions of particular diastereomers/conformers. Methods of treating fungal infections or plants infected by fungi are also provided.Type: ApplicationFiled: November 26, 2013Publication date: May 29, 2014Inventors: JAMES LEIF SMITH, AKSHAYA RAVICHANDRAN, SHIEN LU, GANYU GU
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Publication number: 20140147385Abstract: The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma.Type: ApplicationFiled: October 30, 2013Publication date: May 29, 2014Inventors: Yubin Miao, Haixun Guo