Cyclopeptide Utilizing Patents (Class 514/21.1)
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Publication number: 20120283196Abstract: ?-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections eases of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.Type: ApplicationFiled: December 4, 2009Publication date: November 8, 2012Applicant: POLYPHOR AGInventors: Sophie Barthélémy, Christian Bisang, Frank Otto Gombert, Alexander Lederer, Daniel Obrecht, Barbara Romagnoli, Jürg Zumbrunn, Tobias Remus, Guillaume Lemercier
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Publication number: 20120277145Abstract: The present invention pertains generally to certain compounds of the deoxyactagardine A and B type. Such compounds are suitable for use in the treatment of microbial infections, for example Clostridium infection, such as C. perfringens, C. difficile, C. tetani, and/or C. botulinum, in particular C. difficile, especially infection of the colon and/or lower intestines and diarrhoea associated with the microbial infection.Type: ApplicationFiled: May 21, 2012Publication date: November 1, 2012Inventor: Sjoerd Nicolaas Wadman
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Publication number: 20120277164Abstract: Compounds based around tetrapeptide, tripeptide and dipeptide moeties and corresponding peptiod moeties. Related methods and pharmaceutical compositions for use in treatment of cancer, inflammatory diseases, and other disorders.Type: ApplicationFiled: October 22, 2010Publication date: November 1, 2012Applicant: Imperial Innovations LimitedInventors: Guido Franzoso, Albert Andrzej Jaxa-Chamiec, Caroline Minli Rachel Low, Simona Maria Monti, Menotti Ruvo, Laura Tornatore, Catherine Jane Tralau-Stewart
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Patent number: 8299030Abstract: The invention relates to new peptide-based compounds for use as diagnostic imaging agents or as therapeutic agents wherein the agents comprise targeting vectors which bind to integrin receptors.Type: GrantFiled: August 8, 2011Date of Patent: October 30, 2012Assignee: GE Healthcare LimitedInventors: Alan Cuthbertson, Bard Indrevoll, Magne Solbakken, Torgrim Engell, Colin Mill Archer, Harry John Wadsworth
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Publication number: 20120270806Abstract: The present invention is concerned with a novel composition of matter—a cyclic peptide derived from computer modeling studies that modulates the structure and function of the HIV main envelope protein gp120. The compound is capable of binding to the CD4-binding region of gp120 (this defines it as a CD4 mimic), and can be used for the purposes of: (1) controlling and preventing HIV infections, (2) detecting, isolating and purifying gp120. Contrary to examples of prior art that involved CD4 mimics being either small molecules or macromolecules, the present invention is concerned with the class of “large small molecules” that may offer a satisfactory balance between the activity and drug-like properties. Modified variants of the prototype compound that can be reasonably considered its derivatives are also claimed.Type: ApplicationFiled: April 20, 2012Publication date: October 25, 2012Inventor: Przemyslaw Czyryca
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Publication number: 20120270807Abstract: The present invention relates to novel macrocyclic compounds and salts thereof that bind to and/or are inhibitors of serine protease enzymes. The present invention also relates to intermediates of these compounds, pharmaceutical compositions containing these compounds and methods of using the compounds. These compounds are useful as therapeutics for treatment and prevention of a range of disease indications including hyperproliferative disorders, in particular those characterized by tumor metastasis, inflammatory disorders, skin and tissue disorders, cardiovascular disorders, respiratory disorders and viral infections.Type: ApplicationFiled: October 22, 2010Publication date: October 25, 2012Inventors: Éric Marsault, Olivier Leogane, Axel Mathieu, Sylvie Beaubien
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Publication number: 20120270774Abstract: The present invention relates to backbone cyclized CD-4 mimetics and to compositions and methods comprising them for preventing and treating viral infection. In particular, the present invention relates to orally bio-available compounds and formulations for prevention and treatment of human HIV-1 infection.Type: ApplicationFiled: August 29, 2010Publication date: October 25, 2012Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem LTdInventors: Chaim Gilon, Amnon Hoffman, Moshe Kotler, Mattan Hurevich, Salim Joubran, Avi Swed
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Publication number: 20120270769Abstract: The present invention relates to novel macrocyclic compounds and salts thereof that bind to and/or are inhibitors of serine protease enzymes and methods of using the compounds. The present invention also relates to intermediates of these compounds, pharmaceutical compositions containing these compounds and methods of using the same. These compounds are useful as therapeutics for treatment and prevention of a range of disease indications including hyperproliferative disorders, in particular those characterized by tumor metastasis, inflammatory disorders, skin and tissue disorders, cardiovascular disorders, respiratory disorders and viral infections.Type: ApplicationFiled: October 22, 2010Publication date: October 25, 2012Inventors: Éric Marsault, Olivier Leogane, Axel Mathieu, Sylvie Beaubien, Richard Leduc
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Patent number: 8293713Abstract: The present invention relates to methods of treating dry eye using ?-turn peptidomimetic cyclic compounds or derivatives thereof. The ?-turn peptidomimetic cyclic compounds can be used alone, in combination and/or in conjunction with one or more other compounds, molecules or drugs that treat dry eye.Type: GrantFiled: April 3, 2009Date of Patent: October 23, 2012Assignee: Mimetogen Pharmaceuticals, Inc.Inventors: Garth Cumberlidge, Karen Meerovitch, Teresa Lama
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Publication number: 20120264693Abstract: Compounds capable of modulating intracellular gap junctional communication, as well as their use in the treatment of diseases associated with impaired gap junction intracellular communication (GJIC) 1 are disclosed.Type: ApplicationFiled: June 11, 2010Publication date: October 18, 2012Applicants: Zealand Pharma A/S, The Regents of the University of Michigan, The Research Foundation of State Univesity of New YorkInventors: Mario Delmar, Steven M. Taffet, Wanda Coombs, Vandana Verma, Bjarne Due Larsen
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Publication number: 20120251581Abstract: There is provided inter alia a compound of formula (I): for use in treatment of viral infection or as an immunosuppressant.Type: ApplicationFiled: March 29, 2012Publication date: October 4, 2012Inventors: Matthew Alan Gregory, Steven James Moss, Barrie Wilkinson
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Publication number: 20120252730Abstract: Peptides and cyclized analogs thereof that are useful as platelet aggregation inhibitors in the treatment of cardiac disease, including acute coronary syndrome are disclosed.Type: ApplicationFiled: September 2, 2010Publication date: October 4, 2012Applicant: UNIVERSITY OF CHICAGOInventors: Milan Mrksich, Juan Sanchez-Cortes
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Publication number: 20120251444Abstract: The present invention relates to the use of receptor-associate protein (RAP) and fragments and variants thereof to improve delivery of therapeutic compounds to the liver and provides methods to treat liver disorders and conditions, such as hepatic carcinoma, by administering RAP or RAP variants conjugated to active agents.Type: ApplicationFiled: September 18, 2007Publication date: October 4, 2012Inventors: Christopher M. Starr, Todd C. Zankel
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Publication number: 20120245081Abstract: Exocyclic peptide mimetics that disable Fas were developed. A three dimensional model of the Fas receptor-ligand complex was constructed and structurally predicted regions of the receptor that were relevant to binding ligand were used to create constrained peptide mimetics. Exocyclic anti-Fas peptide mimetics were identified that block Fas receptor-ligand interactions, and modulate Fas biological activity both in vitro and in vivo. The mimetics are useful, e.g., for treating Fas-related pathologies.Type: ApplicationFiled: August 15, 2011Publication date: September 27, 2012Applicant: Trustees of the University of PennsylvaniaInventors: Mark I. Greene, Ramachandran Murali, Akihiro Hasegawa
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Publication number: 20120238505Abstract: The present invention relates to the use of a peptide, or derivative thereof of general formula X1-X2-X3-ThT-X4-LyS-X5-ATg-X6 for promoting accelerated wound healing with reduced scarring. X1 is Ala or Gly; X2 is Tyr or Phe; X3, X4 and X5 are independently selected from the group comprising Met, He, Leu and Val; and X6 is selected from the group comprising Asp, Gln and Glu.Type: ApplicationFiled: October 7, 2011Publication date: September 20, 2012Applicant: RENOVO LIMITEDInventors: Mark W.J. Ferguson, Nick Occleston, Amanda Deakin, Sharon O'Kane
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Publication number: 20120238507Abstract: Disclosed are short chain peptides that are constrained to adopt an alpha helicial conformation and their use as alpha helical scaffolds for directing amino acid side chains into positions analogous to those found in longer chain alpha helical peptides. Also disclosed is the use of these peptides for attaching peptidic or non-peptidic appendages in order to mimic side chains of longer alpha helical peptides. The peptides find use in mimicking naturally occurring peptides or proteins or in preparing new materials.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: THE UNIVERSITY OF QUEENSLANDInventors: David P. Fairlie, Nicholas E. Shepherd
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Publication number: 20120225830Abstract: Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: ASTELLAS PHARMA INC.Inventors: Satoshi UEDA, Yoko Watamoto, Masaru Tsuboi, Munekazu Kanda, Tomoji Higaki, Mitsunori Matsuda
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Publication number: 20120225828Abstract: Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.Type: ApplicationFiled: May 16, 2012Publication date: September 6, 2012Applicant: PALATIN TECHNOLOGIES, INC.Inventors: Wei Yang, Yi-Qun Shi
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Publication number: 20120225829Abstract: Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: ASTELLAS PHARMA INC.Inventors: Satoshi UEDA, Yoko Watamoto, Masaru Tsuboi, Munekazu Kanda, Tomoji Higaki, Mitsunori Matsuda
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Patent number: 8258101Abstract: This invention relates to new peptide-based compounds and their use in therapeutically effective treatments as well as for diagnostic imaging techniques. More specifically the invention relates to the use of such peptide-based compounds used as targeting vectors that bind to receptors associated with angiogenesis, in particular the ?v?3 integrin receptor. Such contrast agents may thus be used for diagnosis of for example malignant diseases, heart diseases, inflammation-related diseases, rheumatoid arthritis and Kaposi's sarcoma. Moreover such compounds may also be used in therapeutic treatment of these diseases.Type: GrantFiled: June 14, 2010Date of Patent: September 4, 2012Assignee: GE Healthcare ASInventor: Alan Cuthbertson
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Patent number: 8258258Abstract: Disclosed is a polypeptide comprising at least two microproteins, which preferably comprise an amino acid sequence having a specific binding activity to a target protein. Furthermore, disclosed are polynucleotides encoding such a polypeptide as well as pharmaceutical compositions and kits comprising said polypeptide or polynucleotide. Also disclosed herein are methods of treatments and second medical uses applying the disclosed polypeptide or polynucleotide. Additionally, the disclosure of the present application relates to a method for forming a covalent bond in a microprotein which can be used for producing the disclosed polypeptides.Type: GrantFiled: March 9, 2006Date of Patent: September 4, 2012Assignee: BioNTech AGInventors: Harald Kolmar, Ernst Boehnlein, Alexander Wentzel, Hans-Ulrich Schmoldt
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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: 20120214750Abstract: The present invention relates to crystalline forms of linaclotide, as well as to various methods and processes for the preparation and use of the crystalline forms.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Ritesh Sanghvi, Andreas Grill, Rahul Surana, Haijian Zhu
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Publication number: 20120214731Abstract: The present invention relates to a new compound useful as a modulator of melanocortin receptors. In particular, the present invention relates to a compound WS727713, a process for production of the compound by culturing, in a culture medium, a WS727713-producing strain belonging to Pseudonocardia and recovering the compound from a culture broth, a pharmaceutical composition containing the compound, and uses of the compound.Type: ApplicationFiled: January 19, 2012Publication date: August 23, 2012Inventors: Takanao Otsuka, Hirotsugu Ueda, Keiko Fujie, Hideyuki Muramatsu, Michizane Hashimoto, Shigehiro Takase
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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: 20120214749Abstract: Disclosed are microparticles comprising a somatostatin analogue embedded in a biocompatible pharmacologically acceptable polymer matrix for a long acting release and pharmaceutical compositions comprising such microparticles.Type: ApplicationFiled: April 26, 2012Publication date: August 23, 2012Applicant: NOVARTIS AGInventors: Markus Ahlheim, Michael Ausborn, Olivier Lambert, Marc Riemenschnitter
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Publication number: 20120213846Abstract: Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (“linaclotide”) or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.Type: ApplicationFiled: August 14, 2009Publication date: August 23, 2012Applicants: Forest Laboratories Holdings Limited, Ironwood Pharmaceuticals, Inc.Inventors: Angelika Fretzen, Steven Witowski, Alfredo Grossi, Hong Zhao, Mahendra Dedhiya, Yun Mo
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Patent number: 8247372Abstract: Compounds which are Spiruchostatin analogues of the general formula (I) or (I?), isosteres thereof and pharmaceutically acceptable salts thereof are found to inhibit HDAC wherein R1, R2, R3 and R4 are the same or different and represent an amino acid side chain moiety and each R6 is the same or different and represents hydrogen or C1-C4 alkyl.Type: GrantFiled: November 23, 2007Date of Patent: August 21, 2012Assignee: University of SouthamptonInventors: Graham Keith Packham, Arasu Ganesan, Alexander Richard Liam Cecil
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Patent number: 8247613Abstract: The present invention provides methods and compositions useful for the elimination of latent HIV reservoirs that persist despite HAART. The methods and compositions overcome this latent barrier by inducing the replication of HIV in latently infected T cells while preventing the spread of the newly produced virions to uninfected cells by providing HAART simultaneously. Compositions of the invention comprise an activator of latent HIV expression, such as prostratin, and an inhibitor of histone deacetylase, such as TSA. A surprising finding of this invention is that the inhibitor of the histone deacetylase synergizes the effect of prostratin thus, allowing administering to a patient a lower, non-toxic dose of prostratin.Type: GrantFiled: April 17, 2007Date of Patent: August 21, 2012Assignee: The J. David Gladstone InstitutesInventors: Samuel A. F. Williams, Warner C. Greene
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Publication number: 20120202744Abstract: The present invention relates to the field of anatomy, and more particularly to the control of pain and to the prevention and treatment of osteoarthritic cartilage degradation. Described herein are methods for treating pain which comprise administering to a subject in need a combination of (i) an antagonist of the endothelin type A receptor (ETA) and (ii) an antagonist of the bradykinin B1 receptor (BKB1). Also described are methods for preventing osteoarthritic cartilage degradation and pharmaceutical compositions for treating pain, for preventing osteoarthritic cartilage degradation, and/or for preventing osteoarthritic joint inflammation, in subjects.Type: ApplicationFiled: February 3, 2012Publication date: August 9, 2012Inventors: Florina MOLDOVAN, Gabriel Nathan Kaufman, Pierre Sirois
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Publication number: 20120201753Abstract: Disclosed are compositions and methods useful for targeting regenerating tissue, wounds, and tumors. The compositions and methods are based on peptide sequences that selectively bind to and home to regenerating tissue, wound sites, and tumors in animals. The disclosed targeting is useful for delivering therapeutic and detectable agents to regenerating tissue, wound sites, and tumors in animals.Type: ApplicationFiled: April 19, 2012Publication date: August 9, 2012Inventors: Erkki Ruoslahti, Tero Jarvinen
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Publication number: 20120202733Abstract: 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: ApplicationFiled: October 13, 2010Publication date: August 9, 2012Applicant: SIGNABLOK, INC.Inventor: Alexander B. Sigalov
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Publication number: 20120202746Abstract: Compounds and compositions, and methods of use thereof, for treatment and/or prevention of multiple sclerosis, including symptoms associated with multiple sclerosis, and/or treatment and/or prevention of other disease/disorder affecting the nervous system (e.g. central, peripheral) or muscle including symptoms thereof, comprising administering to a subject in need thereof daptomycin and/or daptomycin-related lipopeptide.Type: ApplicationFiled: September 2, 2010Publication date: August 9, 2012Inventor: Joseph B. Guarnaccia
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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: 20120196790Abstract: The present application relates to cyclic depsipeptides, or derivatives thereof, having the structure of formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7 and human neutrophil elastase.Type: ApplicationFiled: February 14, 2012Publication date: August 2, 2012Applicant: NOVARTIS AGInventors: Philipp KRASTEL, Brigitta-Maria LIECHTY, Josef Gottfried MEINGASSNER, Esther SCHMITT, Erwin Paul SCHREINER
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Patent number: 8232245Abstract: The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable salt of caspofungin as active ingredient being useful for the prevention and/or treatment of fungal infections. The compositions additionally comprise specific bulking agents and small amounts or no amounts of an additional pH modifier and may be in a liquid or solid form, e.g. may be lyophilized compositions. The compositions show good stability and reduced amounts of sub-visible particulate matter formed in solutions which are reconstituted from the lyophilized product.Type: GrantFiled: July 24, 2007Date of Patent: July 31, 2012Assignee: Sandoz AGInventors: Christian Welz, Gottfried Stubauer, Andreas Schmarda, Herwig Jennewein, Ingolf Macher, Johannes Ludescher
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Publication number: 20120190613Abstract: The invention features echinocandin class compounds that have been modified to (i) have activity against one or more fungal species or genera; (ii) have increased aqueous solubility; (iii) have an increased therapeutic index; (iv) be suitable for topical administration; and/or (v) be suitable for oral administration. The echinocandin class compounds of the invention include, for example, a PEG, alkyl-PEG, aryl-PEG, alkaryl-PEG, PEG-alkyl, PEG-aryl, or PEG-alkaryl substituent.Type: ApplicationFiled: August 26, 2010Publication date: July 26, 2012Inventors: Kenneth Duke James, JR., Christopher Patrick Laudeman
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Patent number: 8227422Abstract: Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.Type: GrantFiled: December 13, 2006Date of Patent: July 24, 2012Assignee: Glaxosmithkline LLCInventors: William J. Dower, Ronald W. Barrett, Steven E. Cwirla, David J. Duffin, Christian M. Gates, Sherril S. Haselden, Larry C. Mattheakis, Peter J. Schatz, Christopher R. Wagstrom, Nicholas C. Wrighton
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Patent number: 8222217Abstract: An isolated polypeptide comprising any amino acid fragment of unacylated ghrelin or any analog thereof, wherein the polypeptide has an activity selected from the group consisting of a) decreasing blood glucose levels; b) increasing insulin secretion an/or sensitivity; c) binding to insulin-secreting cells; and d) promoting survival of insulin-secreting cells. As well as the use of the polypeptide in the treatment of a disorder associated with impaired glucose metabolism.Type: GrantFiled: May 30, 2008Date of Patent: July 17, 2012Assignee: Alize Pharma SASInventors: Ezio Ghigo, Riccarda Granata, Aart Jan Van Der Lely
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Publication number: 20120178700Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.Type: ApplicationFiled: September 22, 2009Publication date: July 12, 2012Applicant: Aileron Therapeutics, Inc.Inventors: Huw M. Nash, Rosana Kapeller-Libermann, Jiawen Han, Tomi K. Sawyer, Justin Noehre
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Publication number: 20120178694Abstract: Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs having a constrained backbone at position 8 (glycine) and, optionally, specific substitutions for threonine at position 13.Type: ApplicationFiled: May 3, 2010Publication date: July 12, 2012Inventors: John D. Lambris, Hongchang Qu
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Publication number: 20120177692Abstract: A delivery system for water-insoluble pharmaceutical active ingredients is provided. The delivery system includes water-insoluble pharmaceutical active ingredient(s), organic solvent(s) and amphiphilic co-solvent(s), and a mixture of hydrophilic and hydrophobic non-ionic surfactants. Upon dilution in an aqueous medium, this formulation forms spontaneously dispersion of non-ionic surfactant nanoparticles.Type: ApplicationFiled: August 11, 2008Publication date: July 12, 2012Applicant: EMS S/AInventors: Flavia Giuliana Tinti, Marcia Cristina Breitreitz, Vladimir Matha, Carlo Oliani
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Publication number: 20120178701Abstract: Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z 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: December 6, 2011Publication date: July 12, 2012Applicant: PALATIN TECHNOLOGIES, INC.Inventors: Yi-qun Shi, Shubh D. Sharma, John H. Dodd, Wei Yang, Xin Chen
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Patent number: 8216999Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: GrantFiled: December 1, 2008Date of Patent: July 10, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David B. Olsen, Michael T. Rudd, Joseph P. Vacca, Charles J. McIntyre
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Publication number: 20120172294Abstract: The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration. The diketopiperazines have the formula given in the application.Type: ApplicationFiled: September 7, 2011Publication date: July 5, 2012Applicant: DMI ACQUISITION CORP.Inventor: David Bar-Or
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Publication number: 20120172311Abstract: The present invention provides biologically active crosslinked polypeptides with improved properties relative to their corresponding precursor polypeptides, having good cell penetration properties and reduced binding to human proteins. The invention additionally provides methods of identifying and making such improved polypeptides.Type: ApplicationFiled: February 3, 2012Publication date: July 5, 2012Applicant: Aileron Therapeutics, Inc.Inventors: Huw M. Nash, David Allen Annis, Rosana Kapeller-Libermann, Tomi K. Sawyer, Noriyuki Kawahata
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Publication number: 20120172283Abstract: Disclosed are Drug Delivery Molecules (DDMs) which both facilitate functional imaging, as by PET, MRI or SPECT, and create a biological effect and methods of their use. These DDMs which are variously designed to target specific receptors, internalized and then function biologically, as for purposes of cell destruction or therapy.Type: ApplicationFiled: March 11, 2011Publication date: July 5, 2012Inventor: Gerhart Graupner
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Publication number: 20120157392Abstract: Method of treating a patient suffering from apoptosis of tissue by administering to the patient a therapeutically effective amount of one or more ketogenic compounds such that a physiological ketosis is produced which arrests the apoptosis.Type: ApplicationFiled: December 20, 2011Publication date: June 21, 2012Applicant: BTG INTERNATIONAL LIMITEDInventors: KEITH FRANK MARTIN, DAVID JOHN HEAL, ELIZABETH JAGGER
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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: 20120156304Abstract: Disclosed herein are branched polyol polyesters, which are useful in pharmaceutical formulations. Also disclosed are blends, microparticles, and other formulations, comprising the branched polyol polyesters.Type: ApplicationFiled: December 15, 2011Publication date: June 21, 2012Inventor: Thomas Tice