Cyclopeptide Utilizing Patents (Class 514/21.1)
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Patent number: 8993581Abstract: Disclosed are methods of treating viral disorders via the administration of an inducing agent and an anti-viral agent. In one embodiment, the inducing agent and the anti-viral agent are administered for about five days, and the anti-viral agent is subsequently administered without the inducing agent for an additional period of about sixteen days for a total cycle of about 21 days.Type: GrantFiled: June 11, 2013Date of Patent: March 31, 2015Assignee: Trustees of Boston UniversityInventors: Susan Perrine, Douglas Faller
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Patent number: 8992940Abstract: The use of an agent in the manufacture of a medicament to affect an allergic condition and/or a hypersensitivity condition is described. The agent is capable of modulating a ganglioside associated activity. The agent is not coupled to an antigen. The modulation of the ganglioside associated activity affects an allergic condition and/or a hypersensitivity condition.Type: GrantFiled: January 18, 2013Date of Patent: March 31, 2015Assignee: Trident Pharmaceuticals, Inc.Inventors: Neil Andrew Williams, Timothy Raymond Hirst, John Bienenstock
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Publication number: 20150087597Abstract: Described herein are fragments of fibronectin and vitronectin and variants thereof that have certain activities, including growth factor-binding activity. Also described are fragments of growth factors that bind to fibronectin and inhibit binding of full-length growth factors to fibronectin. Compositions containing such fragments are useful in cosmetic treatments (e.g., the treatment of wrinkles or UV photodamage of skin), and the treatment of wounds and cancer.Type: ApplicationFiled: May 1, 2014Publication date: March 26, 2015Applicant: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORKInventor: Richard A. Clark
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Publication number: 20150080319Abstract: A method is provided for inhibiting TACE activity in a human subject, through the administration of a ?-defensin, analog, or derivative. Such a ?-defensin, analog, or derivative can be effectively administered parenterally, topically, or orally. The ?-defensin, analog, or derivative can be selected to additionally inhibit ADAM-10 activity.Type: ApplicationFiled: September 19, 2014Publication date: March 19, 2015Inventors: Michael E. Selsted, Dat Q. Tran
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Publication number: 20150078999Abstract: Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R1, L1, L2, G, M, Y1 Y2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.Type: ApplicationFiled: June 20, 2014Publication date: March 19, 2015Inventors: James R. Heath, Rosemary Dyane Rohde, Arundhati Nag, Samir Das, Aiko Umeda
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Publication number: 20150080312Abstract: This invention relates to an isolated, compound of Formula (1) or derivatives or pharmaceutically acceptable salts thereof. The invention also includes all isomeric and tautomeric forms of the compound of Formula (1) or the derivatives thereof. The present invention further relates to processes for the production of the compound of Formula (1) by fermentation of the fungal strain of Actinomycetes (PM0895172/MTCC 684), pharmaceutical compositions comprising the compound of Formula (1) as the active ingredient; and use of the compounds or composition containing them in the treatment of cancer.Type: ApplicationFiled: May 6, 2013Publication date: March 19, 2015Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Prabhu Dutt Mishra, Sreekumar Sankaranarayanan Eyyammadichiyl, Saji David George, Shailendra Sonawane, Narayan Subhash Chakor, Abhijit Roychowdhury, Rajiv Sharma
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Patent number: 8980827Abstract: The present invention provides a medicinal composition containing micafungin or a pharmaceutically acceptable salt thereof and trehalose as a stabilizing agent.Type: GrantFiled: January 31, 2012Date of Patent: March 17, 2015Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd.Inventors: Yunhai Hong, Ying Xue, Xiaoming Ji
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Patent number: 8981048Abstract: Disclosed are a caspofungin analog, and a preparation method and applications thereof. The caspofungin analog has a structure as represented in Formula 3.Type: GrantFiled: November 10, 2011Date of Patent: March 17, 2015Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd.Inventors: Bingming He, Ming Li, Zhijun Tang, Xiaoming Ji
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Publication number: 20150072939Abstract: The present invention relates to the use of 5-HT2 receptor antagonists and in particular of 8-?-ergolines such as lisuride, terguride and the derivatives thereof as 5-HT2B and 5-HT2A receptor antagonists and antioxidants in preferably higher-dosed and preferably continuous use for the treatment, progression prophylaxis and general prophylaxis of organ fibroses and other pathological organ remodeling caused by mesenchymal proliferationType: ApplicationFiled: September 22, 2014Publication date: March 12, 2015Applicant: SINOXA PHARMA GMBHInventors: Reinhard HOROWSKI, Heinz PALLA, Johannes TACK
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Publication number: 20150071918Abstract: The invention relates to novel cyclic compounds (cyclic peptides), linkers useful as beta-turn promoters in cyclic peptides, and methods for treatment of malignant cells in vitro or in vivo using one or more linear and cyclic peptides. The peptides can act as integrin interaction inhibitors and may be used in the treatment of cancers as monotherapies or in combination with other anti-cancer agents, such as proteasome inhibitors, inhibitors of autophagy, alkylating agents, MEK inhibitors, FAK/PYK2 inhibitors, and EGFR inhibitors. The invention further concerns a method of predicting the binding of a cyclic or linear HYD1 peptide to a cancer cell by assessing overexpression of biomarkers such as CD44, VLA-4 integrin, basigin, CD138 (syndecan 1), NCAM, ICAM1, ICAM3, and CD59.Type: ApplicationFiled: May 9, 2013Publication date: March 12, 2015Inventors: Mark McLaughlin, Lori Hazlehurst, Priyesh Jain, Michael F. Emmons, Anthony W. Gebhard, Rajesh R. Nair
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Patent number: 8975368Abstract: Peptide nanotube polymers and methods of making such are disclosed. The peptide nanotube polymers are comprised of alternating monomers of the first peptide ring and monomers of the second peptide ring covalently bonded to one another via a linker, and can be functionalized. The described peptide nanotube polymers can enjoy the combined properties of healing and toughness, self-reporting, and tunability and actuation.Type: GrantFiled: August 12, 2010Date of Patent: March 10, 2015Assignee: The United States of America, as represented by the Secretary of the NavyInventors: John L. Kulp, III, Manoj K. Kolel-Veetil, Thomas D. Clark
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Publication number: 20150065434Abstract: Provided herein are cyclic peptide inhibitors of lysine-specific demethylase 1. These cyclic peptides have the potential to treat cancer, diabetes, cardiovascular disease, and neurological disorders.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Patrick M. WOSTER, Isuru R. KUMARASINGHE
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Patent number: 8969513Abstract: Disclosed are a caspofungin analog and applications thereof. The caspofungin analog is a compound having a structure as indicated in Formula (4), or pharmaceutically acceptable salts thereof. R1 can be chosen from hydroxyl, benzyloxy, phenoxy, substituted phenoxy, or substituted benzyloxy. R2, R3, R4, R5 can be chosen from hydrogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, benzyloxyphenyl, substituted benzyloxyphenyl, nitro, fluorine, chlorine, bromine, or iodine. Also disclosed are a preparation method for and applications of the compound.Type: GrantFiled: November 10, 2011Date of Patent: March 3, 2015Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd.Inventors: Bingming He, Ming Li, Zhijun Tang, Xiaoming Ji
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Patent number: 8969307Abstract: A composition comprising from about 0.001% to about 0.4% cyclosporin A, a surfactant, and an oil having a specific gravity from 0.8 to 0.95 is disclosed herein.Type: GrantFiled: November 4, 2013Date of Patent: March 3, 2015Assignee: Allergan, Inc.Inventors: James N. Chang, Orest Olejnik, Bruce A. Firestone
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Patent number: 8969306Abstract: A composition comprising a therapeutically effective amount of cyclosporin A, a blend of oils having a specific gravity of from 0.90 to 1.07, and a surfactant is disclosed herein.Type: GrantFiled: September 13, 2013Date of Patent: March 3, 2015Assignee: Allergan, Inc.Inventors: James N. Chang, Orest Olejnik, Bruce A. Firestone
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Patent number: 8969309Abstract: The present invention discloses a crystal of a peptide substance and the preparation method as well as the use thereof. Said crystal B possesses peaks at the following 2? angles in the X-ray diffraction pattern (XRPD): 3.2±0.2°, 5.4±0.2°, 6.2±0.2°, and 9.3±0.2°.Type: GrantFiled: July 20, 2011Date of Patent: March 3, 2015Assignee: Shanghai Techwell Biopharmaceutical Co., Ltd.Inventors: Shidong Liu, Zhaoli Zhang, Zhonghao Zhuo, Xiaoming Ji, Xiaoliang Gao
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Patent number: 8969308Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.Type: GrantFiled: November 14, 2012Date of Patent: March 3, 2015Assignee: Ampio Pharmaceuticals, Inc.Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
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Publication number: 20150057235Abstract: 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: ApplicationFiled: October 30, 2014Publication date: February 26, 2015Inventors: Kunwar SHAILUBHAI, Gary S. JACOB
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Publication number: 20150056217Abstract: The present invention relates to the use of a TLR9 agonist and/or a TLR4 antagonist and/or a NOD2 agonist for treatment or prevention of disorders involving TLR4 activation, such as systemic sepsis and necrotizing enterocolitis.Type: ApplicationFiled: August 26, 2013Publication date: February 26, 2015Applicant: University of Pittsburgh - of the Commonwealth System of Highter EducationInventor: DAVID J. HACKAM
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Publication number: 20150057234Abstract: Disclosed is a hydrate of a compound as shown in Formula I. In formula I, R represents H or a cation capable of forming a pharmaceutically acceptable salt. The mass percentage of water in the hydrate is more than 8%. The hydrate has good stability. Moreover, disclosed are a preparation method and a use thereof.Type: ApplicationFiled: March 29, 2013Publication date: February 26, 2015Inventors: Shidong Liu, Zhaoli Zhang, Xiusheng Wang, Xiao Zhang, Zhijun Tang, Xiaoming Ji
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Patent number: 8962795Abstract: Factor H-binding peptides that binds to a region of factor H that does not impede the complement-inhibitory activity of factor H are disclosed. When immobilized onto the surface of a biomaterial, these peptides recruit factor H, resulting in a substantial inhibition of biomaterial-induced complement activation in a biological substance exposed to the biomaterial.Type: GrantFiled: December 19, 2011Date of Patent: February 24, 2015Assignee: The Trustees of the University of PennsylvaniaInventor: John D. Lambris
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Patent number: 8962568Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.Type: GrantFiled: November 14, 2012Date of Patent: February 24, 2015Assignee: Ampio Pharmaceuticals, Inc.Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
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Publication number: 20150051157Abstract: Provided herein are formulations of romidepsin. Also provided are methods for producing these formulations and uses thereof. In one embodiment, the formulation is a combination of romidepsin and mannitol.Type: ApplicationFiled: October 17, 2014Publication date: February 19, 2015Inventors: Lianfeng HUANG, Ho-Wah HUI, Victor PEYKOV, Willard R. FOSS, Vijay NARINGREKAR, Mei LAI
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Publication number: 20150050240Abstract: This invention is in the field of treatment of fibrosis. In particular, it relates to the treatment of IPF using N-Cadherin antibodies. The antibody may be any antagonising or neutralizing N-Cadherin antibody suitable for therapeutic use.Type: ApplicationFiled: March 13, 2013Publication date: February 19, 2015Applicant: NOVARTIS AGInventors: Irena Rumenova Konstantinova, Andrew Christopher Pearce
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Publication number: 20150050237Abstract: The present invention relates to the field of anti-mycobacterial therapeutics, in particular the treatment of tuberculosis, especially including pulmonary multidrug-resistant tuberculosis (MDR-TB), with applications in extensively drug-resistant tuberculosis (XDR-TB) and extremely drug-resistant tuberculosis (XXDR-TB), preferably in combination therapy.Type: ApplicationFiled: March 13, 2013Publication date: February 19, 2015Inventors: Vasu Nair, Maurice O. Okello, Machhindra G. Gund, Byung I. Seo, Pankajkumar R. Singh, Naveen K. Mangu
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Publication number: 20150051155Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.Type: ApplicationFiled: September 26, 2014Publication date: February 19, 2015Inventors: Vincent GUERLAVAIS, Carl ELKIN, Huw M. NASH, Tomi K. SAWYER, Bradford J. GRAVES, Eric FEYFANT
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Patent number: 8957027Abstract: The present invention relates to deacetylase inhibitor (e.g., histone deacetylase inhibitor) therapies and demonstrates that individuals with low electrolyte levels may have increased susceptibility to certain unwanted side effects such as cardiac side effects. In some embodiments, the invention provides methods of administering DAC or DAC inhibitor therapy that includes electrolyte supplementation.Type: GrantFiled: June 7, 2007Date of Patent: February 17, 2015Assignee: Celgene CorporationInventors: William McCulloch, Richard L. Piekarz, Susan E. Bates
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Publication number: 20150045310Abstract: Compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. Pharmaceutical compositions comprising peptide sequences with high cytotoxicity to cancer cell lines are provided. A method for treating cancer is provided.Type: ApplicationFiled: February 4, 2013Publication date: February 12, 2015Inventors: A. James Link, Siyan Zhang
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Publication number: 20150045302Abstract: A product comprising a peptide that comprises a motif selected from a group consisting of isoDGR, NGR and DGR, wherein the peptide cyclised by joining the N- and C-termini of its main chain and wherein the cyclic peptide is joined to albumin.Type: ApplicationFiled: March 14, 2013Publication date: February 12, 2015Inventors: Angelo Corti, Flavio Curnis
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Patent number: 8952128Abstract: 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: GrantFiled: October 31, 2013Date of Patent: February 10, 2015Assignee: Ipsen Pharma S.A.S.Inventors: Zheng Xin Dong, Yeelana Shen, Sun Hyuk Kim
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Publication number: 20150037376Abstract: Methods and compositions for oral administration of melanocortin receptor agonist compounds are disclosed herein. Methods and compositions for oral administration of melanocortin receptor agonist compounds are provided for treatment of sexual dysfunction, including male sexual dysfunction and female sexual dysfunction. Methods and compositions for oral administration of melanocortin receptor agonist compounds are provided for treatment of metabolic syndrome, obesity and/or diabetes. In some embodiments, a pharmaceutical composition comprising a peptide-based melanocortin receptor agonist, a protease inhibitor, an absorption enhancer is administered orally.Type: ApplicationFiled: November 2, 2012Publication date: February 5, 2015Inventors: Gaurav Seth, Natan Bar-Chama
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Publication number: 20150038434Abstract: 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: October 15, 2014Publication date: February 5, 2015Inventors: Wei Yang, Yi-Qun Shi
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Publication number: 20150031632Abstract: The present invention relates to orally disintegrating or dissolving pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions.Type: ApplicationFiled: October 9, 2014Publication date: January 29, 2015Inventors: YUN MO, MAHENDRA DEDHIYA, ANIL CHHETTRY, ANGELIKA FRETZEN, STEVEN WITOWSKI, ALFREDO GROSSI, HONG ZHAO
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Publication number: 20150030669Abstract: The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.Type: ApplicationFiled: March 11, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GMBHInventors: Michael Wilhelm Platscher, Raymond Behrendt, Viola Groehn, Simone Rachel Hoertner, Marco Silvio Passafaro, Finn Bauer
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Publication number: 20150031631Abstract: The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.Type: ApplicationFiled: February 24, 2014Publication date: January 29, 2015Applicant: CHIASMA INC.Inventors: Roni Mamluk, Moshe Tzabari, Karen Marom, Paul Salama, Irina Weinstein
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Publication number: 20150031604Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13??I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor.Type: ApplicationFiled: July 21, 2014Publication date: January 29, 2015Applicant: NOVARTIS AGInventors: Frederic ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun Yuan, Aimee Richardson USERA, Changgang LOU, Aaron KANTER, Alexandra Marshall BRUCE, Carla Giumaraes
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Patent number: 8940281Abstract: Disclosed are compositions comprising crosslinked hyaluronic acid gels, preferably vinyl sulfone cross-linked hyaluronic acid known as hylan B gel, for use in topical cosmetic and dermatological formulations. The hylan B gel in these formulations provides prolonged delivery of incorporated substances to the surface of the skin, to provide a hydrated film on the surface of the skin, and to provide a substantive and compatible film on the skin.Type: GrantFiled: March 18, 2014Date of Patent: January 27, 2015Assignee: LuroMed LLCInventors: Adelya K. Leshchiner, Nancy E. Larsen, Edward G. Parent
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Patent number: 8937040Abstract: Provided herein is an antibacterial compound of the following formula: or a pharmaceutically acceptable salt thereof. The antibacterial compound has antibacterial properties against a diverse range of gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin B. Also provided are antibacterial pharmaceutical compositions containing the antibacterial compound, as well as methods for preparing the antibacterial compound.Type: GrantFiled: December 21, 2012Date of Patent: January 20, 2015Assignee: BioSource Pharm, Inc.Inventor: Richard A. Leese
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Publication number: 20150017148Abstract: In certain embodiments compositions are provided that comprise a pentapeptide comprising the formula: C1-X2-X3-X4-C5 where C1 and C5 are independently selected cysteines or cysteine analogues, or other amino acids with sidechains suitable for cyclization, where the cysteines or cysteine analogs are attached to each other by a linkage that does not comprise X2, X3, and X4; where X2, X3, and X4 are independently selected amino acids; and the peptide, when administered to a cell alters APP signaling and/or switches APP processing from aberrant to normal. The compositions mitigate amyloid plaque formation.Type: ApplicationFiled: November 27, 2012Publication date: January 15, 2015Inventors: Varghese John, Clare Peters-Libeu, Dale E. Bredesen
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Patent number: 8933030Abstract: The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein, using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.Type: GrantFiled: February 17, 2011Date of Patent: January 13, 2015Assignee: Ironwwod Pharmaceuticals, Inc.Inventors: Angelika Fretzen, Hong Zhao, Marco Kessler
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Publication number: 20150011481Abstract: The present invention features interferon-free therapies for treating HCV genotype 1b, 2, 3 or 4. In one aspect, the therapies comprise administering Compound 1, ritonavir, and Compound 2 to a subject infected with HCV genotype 1b or 4, wherein the therapies do not include administration of any interferon, and the therapies last for 12 weeks. Preferably, the therapies do not include administration of any ribavirin.Type: ApplicationFiled: July 1, 2014Publication date: January 8, 2015Inventors: Regis A. Vilchez, Lino X. Rodrigues, JR., Barry M. Bernstein, Thomas J. Podsadecki, Scott C. Brun, Daniel E. Cohen, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Tolga Baykal
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Publication number: 20150010541Abstract: The present invention provides a novel macrocyclic compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: May 29, 2014Publication date: January 8, 2015Applicant: The Regents of the University of Colorado, A Body CorporateInventors: Xuedong Liu, Andrew J. Phillips, Dana Ungermannova, Christopher G. Nasveschuk, Gan Zhang
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Patent number: 8927500Abstract: Provided herein are peptidomimetic macrocycles containing amino acid sequences with at least two modified amino acids that form an intramolecular cross-link that can help to stabilize a secondary structure of the amino acid sequence. Suitable sequences for stabilization include those with homology to the p53 protein. These sequences can bind to the MDM2 and/or MDMX proteins. Also provided herein are methods of using such macrocycles for the treatment of diseases and disorders, such as cancers or other disorders characterized by a low level or low activity of a p53 protein or high level of activity of a MDM2 and/or MDMX protein.Type: GrantFiled: February 14, 2013Date of Patent: January 6, 2015Assignee: Aileron Therapeutics, Inc.Inventors: Vincent Guerlavais, Carl Elkin, Huw M. Nash, Tomi K. Sawyer, Bradford J. Graves, Eric Feyfant
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Publication number: 20150005241Abstract: The present invention is directed to stable linaclotide compositions and methods of treating gastrointestinal disorders in patients in need thereof by providing the stable linaclotide compositions.Type: ApplicationFiled: September 18, 2014Publication date: January 1, 2015Inventors: Ritesh Sanghvi, Matthew Miller, Andreas Grill, Yun Mo, Mohammad Mafruhul Bari, Matthew Ronsheim, Joseph Stainkamp
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Patent number: 8921325Abstract: The template-fixed ?-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties 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 immuno suppression; or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These ?-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.Type: GrantFiled: February 11, 2013Date of Patent: December 30, 2014Assignees: Polyphor Ltd., Universität ZürichInventors: Daniel Obrecht, Frank Gombert, Steven J. Demarco, Christian Ludin, Jan Wim Vrijbloed, Kerstin Moehle, John-Anthony Robinson, Reshmi Mukherjee, Heiko Henze, Barbara Romagnoli
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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: 20140378392Abstract: Use of a subcutaneously administered dose of between about 1.0 mg and 1.75 mg of bremelanotide or a pharmaceutically acceptable salt of bremelanotide for the treatment of female sexual dysfunction in women while reducing or minimizing undesirable side effects.Type: ApplicationFiled: June 24, 2014Publication date: December 25, 2014Inventors: Carl Spana, Robert Jordan, Jeffrey D. Edelson
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Publication number: 20140378393Abstract: The present invention relates to stable pharmaceutical compositions comprising linaclotide or pharmaceutically acceptable salts thereof, as well as to various methods and processes for the preparation and use of the compositions.Type: ApplicationFiled: September 12, 2014Publication date: December 25, 2014Inventors: Yun Mo, Angelika Fretzen, Brian Cali, Mahendra Dedhiya
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Patent number: 8916161Abstract: The present invention provides a method of treating BPH using modified pore-forming proteins (MPPs). These MPPs are derived from naturally occurring cytotoxic proteins (nPPs) that kill cells by forming pores or channels in the cell membrane, resulting in cell death. The MPPs are generated by modification of the nPPs such that they are capable of being selectively activated at normal prostate cells. Such modification may include the addition of a prostate-specific protease cleavage site to the activation sequence, and/or the addition of a prostate-specific targeting domain to allow selective targeting of prostate cells. These MPPs are capable of selectively targeting and killing normal prostate cells in vivo. The MPPs may be used either alone or in combination with other therapies for the treatment of BPH.Type: GrantFiled: June 14, 2006Date of Patent: December 23, 2014Assignee: Sophiris Bio Inc.Inventor: James Thomas Buckley
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Publication number: 20140370072Abstract: Provided herein is a prohealing piezoelectric coating and the method of making and using the same.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Syed Faiyaz Ahmed Hossainy, Mikael Trollsas, Lothar Walter Kleiner