Nitrogen In Aglycone Moiety Patents (Class 536/17.8)
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Publication number: 20150140573Abstract: The present invention relates to a method of detecting ?-(1?6)-glucosidase activity in a sample. The method is for example useful for determining the limit dextrinase activity in a sample. The method involves use of an oligosaccharide substrate of the formula X-(glucoside)n-*(glucoside)m-Z—Y, where X is a blocking group, -* is a ?-(1?6)-glucosidic linkage and Y is a detectable label. Upon cleavage of the ?-(1?6)-glucosidic linkage, the detectable label is released and thus the ?-(1?6)-glucosidase activity can be determined. The invention also relates to the oligosaccharide substrate per se.Type: ApplicationFiled: June 7, 2013Publication date: May 21, 2015Inventors: Marie Bøjstrup, Caspar Elo Christensen, Ole Hindsgaul
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Publication number: 20140336137Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
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Publication number: 20140274930Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Evelyne Dietrich, Carl Poisson, Michel Gallant, Stephanie Lessard, Bingcan Liu, Sanjoy Kumar Das, Yeeman Ramtohul, Thumkunta Jagadeeswar Reddy, Julien Martel, Frederic Vallee, Jean-Francois Lévesque
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Publication number: 20130310331Abstract: There is provided an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pre-diabetic or have diabetes, obesity and/or syndrome X. Hence the compounds of the present invention help to manage blood sugar levels, i.e. helping the body by balancing the blood sugar levels; helping to keep balanced blood glucose levels, particularly in humans with diabetes; aiding by enhancing the glucose uptake by the cells and by reducing sugar levels, thus improving or restoring the glucose tolerance; optimizing the glycemic response; normalizing the glucose tolerance.Type: ApplicationFiled: October 7, 2010Publication date: November 21, 2013Applicant: ZADEC APSInventors: Elizabeth Joubert, Stephen John Fey, Johan Louw, Trond Ulven, Rahul Tyagi
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Patent number: 8309526Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.Type: GrantFiled: June 9, 2010Date of Patent: November 13, 2012Assignees: The UAB Research Foundation, University College Cardiff Consultants Ltd, Morehouse School of Medicine, University of OregonInventors: Bruce A. Freeman, Francisco Schopfer, Valerie O'Donnell, Paul Baker, Yuqing E. Chen, Bruce Branchaud
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Publication number: 20120178705Abstract: Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of ?-galactosyl ceramide, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells.Type: ApplicationFiled: January 5, 2012Publication date: July 12, 2012Applicant: NATIONAL TAIWAN UNIVERSITYInventor: Pi-Hui LIANG
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Publication number: 20120053330Abstract: Disclosed herein are processes for preparing glucopyranosyloxypyrazole derivatives. In particular, the present invention relates to glucopyranosyloxypyrazole derivatives having SGLT2 inhibitory activity and processes and intermediates for preparing the same.Type: ApplicationFiled: April 29, 2010Publication date: March 1, 2012Inventors: Daniel Edward Patterson, Michael S. McClure, Jeremiah David Powers, Claire Frances Crawford, Malcolm Brian Berry
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Patent number: 8076466Abstract: The present invention relates to fluorescent enzymatic substrates of saccharidic nature having a self-cleavable spacer arm functionalized by a fluorophore F and by at least one inhibitor of the fluorescence of F, to the use thereof for preparation of a diagnostic reagent for functional imaging in vivo, and to the diagnostic reagent for functional imaging containing at least one such enzymatic substrate.Type: GrantFiled: September 8, 2008Date of Patent: December 13, 2011Assignee: Commissariat a l'Energie AtomiqueInventors: François Durrat, Isabelle Texier-Nogues, Véronique Robert
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Publication number: 20110251068Abstract: Disclosed is a parasitic plant control agent which can control a parasitic plant effectively. Also disclosed is a parasitic plant control method. A parasitic plant can be controlled by inhibiting the metabolism of gentianose in the parasitic plant to inhibit the germination of the parasitic plant.Type: ApplicationFiled: October 5, 2009Publication date: October 13, 2011Applicant: OSAKA UNIVERSITYInventors: Atsushi Okazawa, Joseph Benesh
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Publication number: 20100331268Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.Type: ApplicationFiled: June 9, 2010Publication date: December 30, 2010Applicants: THE UAB RESEARCH FOUNDATION, State of Oregon Acting By and Through the Board of Education on behalf of the University of OregonInventors: Bruce A. Freeman, Francisco Schopfer, Valerie O'Donnell, Paul Baker, Yuqing E. Chen, Bruce Branchaud
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Patent number: 7820627Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.Type: GrantFiled: May 9, 2003Date of Patent: October 26, 2010Assignee: Oncothyreon Inc.Inventors: Zi-Hua Jiang, R. Rao Koganty, Wladyslaw Budzynski
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Publication number: 20080188380Abstract: A photolabile compound, an oligomer probe array, and a substrate for oligomer probe array comprising the same, and a manufacturing method of the same are disclosed.Type: ApplicationFiled: January 25, 2008Publication date: August 7, 2008Inventors: SUNG-MIN CHI, Jung-hwan Hah, Kyoung-seon Kim, Won-sun Kim, Man-hyoung Ryoo
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Patent number: 6887854Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.Type: GrantFiled: May 13, 2003Date of Patent: May 3, 2005Assignee: Mallinckrodt Inc.Inventors: Samuel Achilefu, Hermo N. Jimenez, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugai
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Patent number: 6844346Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. These compounds are based upon N-acetylneuraminic acid glycosides. In particular, this invention provides a novel class of these compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: December 24, 2002Date of Patent: January 18, 2005Assignees: IBBEX, Inc., Univ. of Alabama at BirminghamInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
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Patent number: 6812332Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: January 21, 2003Date of Patent: November 2, 2004Assignees: IBBEX, Inc., UAB Research FoundationInventors: Stephen C. Johnson, Ashraf Saeed, Ming Luo
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Publication number: 20040186061Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compouds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.Type: ApplicationFiled: January 27, 2004Publication date: September 23, 2004Applicant: Schwarz Pharma AGInventors: Claus Meese, Bengt Sparf
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Patent number: 6512100Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.Type: GrantFiled: August 30, 2000Date of Patent: January 28, 2003Assignees: Ibbex, Inc., UAB Research FoundationInventors: Stephen C Johnson, Ashraf Saeed, Ming Luo