Containing -c(=x)x- Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 536/18.2)
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Publication number: 20120022008Abstract: Compounds extracted from Rhodiola rosea have ability to inhibit gelatinases and collagenases activity. The compounds have the chemical structure as shown below.Type: ApplicationFiled: June 23, 2011Publication date: January 26, 2012Applicants: CHINA MEDICAL UNIVERSITY, TAIPEI MEDICAL UNIVERSITY (TMU)Inventors: Ching-Kuo Lee, Chieh-Chih Hsu, George Hsiao, Shin-Hun Juang
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Publication number: 20120022241Abstract: A composition of matter comprising sophorolipids as antimicrobial agents, antifungal agents, biopesticides, for uses as drugs to treat HIV, septic shock, cancer, asthma, dermatological conditions, as spermicidal agents, as anti-inflammatory drugs, as ingredients in cosmetics and building blocks for monomers and polymers and self-assembled templates for further chemical elaboration.Type: ApplicationFiled: April 5, 2011Publication date: January 26, 2012Inventors: Richard A. Gross, Mark H. Schofield
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Publication number: 20120021046Abstract: Mutual prodrugs of glucosamine, and derivatives and analogs of glucosamine and an anti-inflammatory agent, compositions thereof, and methods for, e.g., treating disorders and conditions by administration of the compositions are provided. Topical compositions of glucosamine, and derivatives and analogs of glucosamine are also provided.Type: ApplicationFiled: September 9, 2011Publication date: January 26, 2012Inventors: Anthony C. Capomacchia, Solomon T. Garner, JR., J. Warren Beach
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Patent number: 8100961Abstract: A method and product are provided for the treatment of connective tissue weakened due to destruction of tissue architecture, and in particular due to elastin degradation. The treatment agents employ certain unique properties of phenolic compounds to develop a protocol for reducing elastin degradation, such as that occurring during aneurysm formation in vasculature. According to the invention, elastin can be stabilized in vivo and destruction of connective tissue, such as that leading to life-threatening aneurysms in vasculature, can be tempered or halted all together. The treatment agents can be delivered or administered acutely or chronically according to various delivery methods, including sustained release methods incorporating perivascular or endovascular patches, use of microsphere carriers, hydrogels, or osmotic pumps.Type: GrantFiled: March 29, 2010Date of Patent: January 24, 2012Assignee: Clemson University Research Foundation (CURF)Inventors: Narendra R. Vyavahare, Jason C. Isenburg, Dan T. Simionescu
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Publication number: 20110306569Abstract: The present disclosure relates to an isolated strain of Pseudomonas aeruginosa strain NY3 and compounds produced by this strain having biosurfactant activity, for instance rhamnolipids Rha-C8-C8:1, Rha-C16, Rha-C16:1, Rha-C17:1, Rha-C24:1, Rha-Rha-C6-C6:1, Rha-Rha-C9:1, Rha-Rha-C10:1-C10:1, Rha-Rha-C24, and Rha-Rha-C24:1, as well as compositions of, derived from, comprising, or consisting of one or more of such compounds isolated from P. aeruginosa. Also provided are methods of treating environmental materials contaminated with hydrocarbons, heavy metals, or pesticides with such compositions and methods of inhibiting microbial growth with such compositions.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Inventors: Xihou Yin, Maiqian Nie, Qirong Shen
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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: 20110300120Abstract: Provided herein are conjugates comprising a protein and an oligosaccharide of one of Formulae I-VI. Also provided herein are pharmaceutical compositions comprising such conjugates. Further provided herein are methods of treating a lysosomal storage disorder in a mammal by administration of an oligosaccharide-glycoprotein conjugate.Type: ApplicationFiled: December 11, 2009Publication date: December 8, 2011Inventors: Luis Z. Avila, Clark Q. Pan, Patrick Finn, John Harrahy, Qun Zhou, Yunxiang Zhu, Paul A. Konowicz, Duncan E. Paterson, Andreas Peer, Joseph P. Kutzko, Michael R. Reardon, James E. Stefano, Xiaoyang Zheng, Robert J. Miller, Lauren Young
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Patent number: 8067625Abstract: The present invention relates to fatty acid esters of polyols or sulfonated fatty acid esters or sulfonated fatty acid amides containing at least one group Y, where Y stands for CF3—(CH2)a—O—, SF5—, CF3—(CH2)a—S—, CF3CF2S—, [CF3—(CH2)a]2N— or [CF3—(CH2)a]NH—, where a stands for an integer selected from the range from 0 to 5, or formula (I), where Rf stands for CF3—(CH2)r—, CF3—(CH2)r—O—, CF3—(CH2)r—S—, CF3CF2—S—, SF5—(CH2)t— or [CF3—(CH2)r]2N—, [CF3—(CH2)r]NH— or (CF3)2N—(CH2)r—, B stands for a single bond, O, NH, NR, CH2, C(O)—O, C(O), S, CH2—O, O—C(O), N—C(O), C(O)—N, O—C(O)—N, N—C(O)—N, O—SO2 or SO2—O, R stands for alkyl having 1 to 4 C atoms, b stands for 0 or 1 and c stands for 0 or 1, q stands for 0 or 1, where at least one radical from b and q stands for 1, and r stands for 0, 1, 2, 3, 4 or 5, to processes for the preparation of these compounds, and to uses of these surface-active compounds.Type: GrantFiled: July 2, 2007Date of Patent: November 29, 2011Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Wolfgang Hierse, Nikolai (Mykola) Ignatyev, Martin Seidel, Elvira Montenegro, Peer Kirsch, Andreas Bathe
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Publication number: 20110288282Abstract: The invention relates to methods for making deoxyribofuranose compounds such as compound (2) which are useful intermediates in the preparation of pharmaceutical compounds such as 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.Type: ApplicationFiled: November 16, 2009Publication date: November 24, 2011Applicant: Anadys Pharmaceuticals, Inc.Inventor: Gregory J. Haley
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Publication number: 20110280893Abstract: The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative.Type: ApplicationFiled: September 5, 2008Publication date: November 17, 2011Applicant: UNIVERSITY OF GEORGIA RESEACH FOUNDATION, INCInventor: Geert-Jan Boons
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Publication number: 20110257114Abstract: The novel crystalline and polymorphic forms of 1,6-Bis [3-(3-carboxymethylphenyl)-4-(2-?-D-mannopyranosyloxy)-phenyl]hexane have advantageous properties and can be used in pharmaceutical and dermatological compositions.Type: ApplicationFiled: June 14, 2011Publication date: October 20, 2011Applicant: Revotar Biopharmaceuticals AGInventors: Ewald M. AYDT, Remo Kranich, Karin Vollhardt, Gerhard Wolff
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Publication number: 20110257380Abstract: Compounds and methods are provided for obtaining oligosaccharide mimics. More specifically, compounds and methods are described wherein oligosaccharide mimics are obtained by incorporating or substituting in a cyclohexane derivative.Type: ApplicationFiled: April 25, 2011Publication date: October 20, 2011Applicant: GlycoMimetics, Inc.Inventors: Beat ERNST, Daniel SCHWIZER, Arun K. SARKAR, John L. MAGNANI
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Publication number: 20110257108Abstract: This disclosure provides for a novel lactose monolaurate (LML) with the structure useful as an antimicrobial agent and as a potential substitute for other sugar esters. Methods of synthesizing LML using immobilize lipases and various solvents are also provided.Type: ApplicationFiled: April 14, 2010Publication date: October 20, 2011Applicant: Utah State UniversityInventor: Marie K. Walsh
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Patent number: 8039601Abstract: The novel crystalline and polymorphic forms of 1,6-Bis [3-(3-carboxymethylphenyl)-4-(2-?-D-mannopyranosyloxy)-phenyl] hexane have advantageous properties and can be used in pharmaceutical and dermatological compositions.Type: GrantFiled: June 14, 2011Date of Patent: October 18, 2011Assignee: Revotar Biopharmaceuticals AGInventors: Ewald M. Aydt, Remo Kranich, Karin Vollhardt, Gerhard Wolff
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Publication number: 20110251378Abstract: The present invention provides a one-pot method of preparing an unprotected ?-O-glycolipid. The first step involves contacting a protected ?-iodo sugar with a catalyst and a lipid comprising a hydroxy group, under conditions sufficient to prepare a protected ?-O-glycolipid. The second step involves deprotecting the protected ?-O-glycolipid under conditions sufficient to prepare the unprotected ?-O-glycolipid, wherein the contacting and deprotecting steps are performed in a single vessel. The present invention also provides a one-pot method of preparing an unprotected ?-O-glycolipid following the steps for the preparation of the unprotected ?-O-glycolipid.Type: ApplicationFiled: April 8, 2008Publication date: October 13, 2011Applicant: The Regents of the University of CaliforniaInventors: Jacquelyn Gervay-Hague, Wenjun Du, Suvarn S. Kulkarni, Matthew Schombs
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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: 20110237531Abstract: The present invention provides a low-cost, efficient method for producing a glycolipid biosurfactant, in particular, lactonic sophorose lipids. This method is characterized by culturing a microorganism capable of producing the biosurfactant under limited oxygen supply. The present invention enables preferential production of lactonic sophorose lipids and facilitates recovery of the lactonic sophorose lipids in a solid form. Further, the present invention enables production of high purity acidic sophorose lipids by hydrolyzing high purity lactonic sophorose lipids produced by the above method. The present invention also provides lactonic sophorose lipids that possess strong antibacterial and antifungal activities, and an antibacterial and/or antifungal agent containing the sophorose lipids.Type: ApplicationFiled: October 23, 2009Publication date: September 29, 2011Applicant: KANEKA CORPORATIONInventors: Satohiro Yanagisawa, Shigeru Kawano, Yoshihiko Yasohara
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Publication number: 20110229565Abstract: This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.Type: ApplicationFiled: September 17, 2009Publication date: September 22, 2011Inventors: Jeffrey M. Karp, Praveen Kumar Vemula, George John, Greg Cruikshank
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Publication number: 20110224158Abstract: The invention provides esterified ?-galactosylceramides effective for cancer treatment and the like, and a medicament containing same. In particular, the invention relates to a compound represented by the formula (I): wherein R1 is a hydrocarbon group having a carbon number of 1 to 30, R2 is a hydrocarbon group having a carbon number of 1 to 20, R3 is a hydrogen atom or hydrocarbon group having a carbon number of 1 to 5, R4 and R5 are the same or different and each is a hydrogen atom or a hydrocarbon group having a carbon number of 1 to 5, or R4 and R5 in combination form a divalent hydrocarbon group having a carbon number of 1 to 5, and optionally form a ring structure together with the adjacent ethylenedioxy, or a salt thereof.Type: ApplicationFiled: September 11, 2009Publication date: September 15, 2011Applicant: RIKENInventors: Masao Shiozaki, Takuya Tashiro, Kenji Mori, Ryusuke Nakagawa, Hiroshi Watarai, Masaru Taniguchi
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Publication number: 20110217344Abstract: Sophorolipid compounds having spermicidal and/or antiviral properties prepared by synthesizing the sophorolipid by fermentation of Candida bombicola in a fermentation media to form a natural mixture of lactonic sophorolipids compounds and non-lactonic sophorolipids compounds and utilizing the natural mixture as a spermicidal and/or antiviral agent, and/or separating the lactonic sophorolipids from the natural mixture to form a lactonic fraction and mixing all remaining fractions to form a non-lactonic fraction and utilizing the lactonic fraction and/or the non-lactonic fraction as an spermicidal and/or antiviral agent, and sophorolipid compounds for use as spermicidal and/or antiviral agents.Type: ApplicationFiled: May 20, 2011Publication date: September 8, 2011Inventors: Richard A. Gross, Vishal Shah, Gustavo F. Doncel
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Publication number: 20110212904Abstract: Pro-drugs of all non-steroidal anti-inflammatories with free acid function derivatized with an ester group, which have the general structural formula given below (I) where A is: aspirin, diflunisal, benorylate, ibufenac, diclofenac, indomethacin, sulindac, ketorolac, ibuprofen, naproxen, ketoprofen, fenoprofen, flurbiprofen, mefenamic acid, meclof enamic acid, flufenamic acid, niflumic acid, and where in the ester group R can be a sugar (amongst which aldose, or ketose pentose, or esose selected from a group of D- and L-enantioiuers of ribose, glucose, galactose, mannose, arabinose, xilose, allose, altrose, gulose, idose and talose and substituted derivatives thereof, such as glucosamine, galactosamine, N-acetyl glucosamine, N-acetyl galactosamine, N-acetyl ribosamine), a disaccharide, a trisaccharide or an oligosaccharide.Type: ApplicationFiled: January 28, 2011Publication date: September 1, 2011Applicants: STEWART ITALIA SRLInventors: Maria Grazia RIMOLI, Antonio CALIGNANO, Rosario CUOMO, Gianpiero BOATTO, Enrico ABIGNENTE, Daniela MELISI, Annalisa CURCIO, Elvira LUONGO, Giovanna LA RANA, Oscar SASSO, Giovanni SARNELLI, Roberto RUSSO, Maria NIEDDU, Carla CIRILLO, Salvatore DE LUCIA
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Publication number: 20110212913Abstract: The invention provides compositions comprising a therapeutically effective amount of a compound of general formula (I): wherein R1, R2 and R3 may be independently selected from H, OH and OMe; wherein X is C1 or C2 and wherein for C2 each carbon is linked by a single or multiple bond (preferably a double bond) and is substituted with one or more H or OH; for use as a medicament for treating or preventing the development of medical conditions characterised by inappropriate platelet aggregation.Type: ApplicationFiled: November 2, 2009Publication date: September 1, 2011Applicant: PROVEXIS NATURAL PRODUCTS LIMITEDInventor: Niamh O'Kennedy
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Publication number: 20110206734Abstract: Described herein are fatty acid carbohydrate-hydroxyl-hybrid compounds and derivatives thereof, and methods of treating or preventing disease and disease symptoms using the compounds and compositions thereof.Type: ApplicationFiled: August 7, 2008Publication date: August 25, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Kevin J. Yarema, Udayanath Aich, Christopher Thomas Campbell, Srinivasa-Gopalan Sampathkumar, Sean S. Choi, Michael Adam Meledeo, Christopher Weier
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Publication number: 20110184159Abstract: The present invention relates to novel processes for the production of F-18 labeled radiotracers for Positron Emission Tomography (PET). The invention also comprises radiopharmaceutical kits using these processes.Type: ApplicationFiled: June 24, 2009Publication date: July 28, 2011Inventors: Matthias Friebe, Keith Graham, Mathias Berndt
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Publication number: 20110160151Abstract: Novel compounds and methods of using the same to inhibit glycolysis and treat cancer and other diseases are provided herein.Type: ApplicationFiled: June 25, 2009Publication date: June 30, 2011Inventors: Waldemar Priebe, Marcin Cybulski, Izabela Fokt, Stanislaw Skora, Charles Conrad, Timothy Madden
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Patent number: 7968522Abstract: A method and composition for the prophylaxis or treatment of humans or animals for septic shock and sepsis using a mixture of sophorolipids.Type: GrantFiled: March 26, 2007Date of Patent: June 28, 2011Assignee: Polytechnic Institute of NYUInventor: Richard A. Gross
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Publication number: 20110136748Abstract: The invention relates to a novel ester, the 3,5-di-tertiobutyl-4-hydroxybenzoate of 3,4,5-trihydroxy-6-methoxytetrahydropyran-2-yl methyl defined by the following formula (I). The invention also relates to the method for preparing the compound of formula (I) and to the use of said compound (I) to prepare a drug for treating and/or preventing enveloped virus infections.Type: ApplicationFiled: July 20, 2009Publication date: June 9, 2011Inventor: Robert Vachy
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Publication number: 20110130473Abstract: Manufactured hyaluronic acid products are used in numerous surgical applications including viscoelastic supplementation for the treatment of osteoarthritis, however, traditional sterilization techniques result in the breakdown of such high molecular weight viscoelastic biopolymers and are thus unsuitable. Disclosed are processes for obtaining concentrated sterile solutions of high molecular weight biopolymers such as hyaluronic acid. The processes include filter sterilization with a dilute preparation of the biopolymer, and concentration of the dilute filter sterilized biopolymer by ultrafiltration to a desired concentration.Type: ApplicationFiled: November 12, 2008Publication date: June 2, 2011Applicant: Bio-Technology General (Israel) Ltd.Inventors: Menakem Fuchs, Dror Eyal, Yehuda Zelig
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Publication number: 20110130553Abstract: Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3?-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.Type: ApplicationFiled: May 18, 2009Publication date: June 2, 2011Inventor: Ulf Nilsson
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Publication number: 20110091726Abstract: The present invention aims to provide a particulate composition containing anhydrous crystalline 2-O-?-D-glucosyl-L-ascorbic acid having a significantly, hardly solidifiable property compared to conventional ones in a grade for use in quasi-drugs; a process for producing the same; and uses thereof. The present invention solves the above object by providing a particulate composition containing anhydrous crystalline 2-O-?-D-glucosyl-L-ascorbic in an amount of over 98.0% by weight but less than 99.9% by weight, on a dry solid basis; or a degree of crystallinity of 90% or higher for anhydrous crystalline 2-O-?-D-glucosyl-L-ascorbic acid, when calculated based on a profile of powder X-ray diffraction analysis of the particulate composition, and a dynamic vapor sorption level of 0.01% by weight or lower, when kept at 25° C.Type: ApplicationFiled: September 3, 2010Publication date: April 21, 2011Applicant: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Takashi Shibuya, Seisuke Izawa, Tomoyuki Nishimoto, Shigeharu Fukuda, Toshio Miyake
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Publication number: 20110070269Abstract: This disclosure provides, in certain embodiments, methods for generating and using extracts of Pyrularia (e.g., Pyrularia pubera) and/or epiphytic/endophytic bacteria associated therewith, either alone or in combination with conventional immunostimulant(s) or anti-inflammatory agents, for modulation of the immune system of a subject. Also provided are compositions that include specific Pyrularia extracts, bacteria isolated from Pyrularia tissue (in particular, Pantoea species), and extracts of from such bacteria. Also provided herein are purified components of Pyrularia extracts and/or extracts from the epiphytic/endophytic bacteria, which extracts exhibit mitogenic or cytotoxic activities. Compositions provided herein can be used for the treatment of neutropenia subsequent to chemotherapy, and for the treatment of immune deficiency (e.g., such as is caused by toxic chemotherapy, disease, or advancing age), as well as in other immune-stimulatory methods.Type: ApplicationFiled: September 24, 2010Publication date: March 24, 2011Inventors: STEVEN G. WOOD, KATIE SOUTHWICK, L. DEE NORD
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Publication number: 20110065662Abstract: Aspects of the invention relate to compounds, extracts and compositions thereof, and methods of using of the same, to treat neurodegenerative disorders and/or improve brain health. In certain embodiments, said compounds are pomegranate flavonoids.Type: ApplicationFiled: July 23, 2010Publication date: March 17, 2011Applicant: Amazentis SAInventors: Christopher L. Rinsch, Philippe V. L. Dupraz
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Publication number: 20110059910Abstract: The invention relates to substituted aromatic fluoroglycoside derivatives, and to the physiologically compatible salts and physiologically functional derivatives thereof. The invention also relates to methods of lowering blood sugar and the treatment of type I and type II diabetes.Type: ApplicationFiled: August 6, 2010Publication date: March 10, 2011Applicant: SANOFI-AVENTISInventors: Wendelin FRICK, Heiner GLOMBIK, Stefan THEIS, Ralf ELVERT
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Publication number: 20110015344Abstract: Degradable complexes comprising a polycation, a polyanion and a polynucleotide are useful for in vivo polynucleotide delivery applications.Type: ApplicationFiled: September 10, 2010Publication date: January 20, 2011Applicant: NITTO DENKO CORPORATIONInventors: Sang Van, Jiadong Zhou, Xiaoli Fu, Lei Yu
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Publication number: 20100297156Abstract: The invention relates to compounds which are immunomodulatory compounds and, in particular, can induce IL-12 secretion. The invention also relates to compositions containing the compounds, precursors, and prodrugs of these compounds, use of these compounds as adjuvants in combination with vaccines, and use of these compounds for treatment of diseases or conditions relating to infection, atopic disorders, or cancer.Type: ApplicationFiled: December 20, 2007Publication date: November 25, 2010Applicant: INDUSTRIAL RESEARCH LIMITEDInventors: Gary David Ainge, Bryce Malcolm Buddle, Michel Denis, Robyn Louise Wright, Darren Gibson, Ahivali Ashwin Gulab, David Samual Larsen, Gavin Frank Painter, Natalie Anne Parlane
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Publication number: 20100298550Abstract: It is an object of the present invention to provide a process for producing 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose in an industrially appropriate manner. The present invention provides a process for producing a 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose which comprises hydrogenating a compound represented by the formula (1) or formula (2) in the presence of a metal catalyst: wherein P1 and P2 independently represent a hydrogen atom or an acyl group, OP1 and OP2 may together form an acetal group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group; wherein X1 represents Br or I, P3 and P4 independently represent a hydrogen atom or an acyl group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group.Type: ApplicationFiled: October 3, 2008Publication date: November 25, 2010Applicant: API CORPORATIONInventors: Tomoko Maeda, Hisatoshi Uehara, Naoki Harada, Manabu Katsurada, Mitsuharu Sano
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Publication number: 20100298246Abstract: Sulfoquinovosylacyl propanediol compounds represented by formula (I): wherein R1 is an acyl residue of a fatty acid, Y is a number of 1, 2 or 3, and M represents a cation having a positive charge equal to Y and pharmaceutically acceptable salts thereof are effective for treating tumors.Type: ApplicationFiled: July 30, 2010Publication date: November 25, 2010Applicant: TOYO SUISAN KAISHA, LTD.Inventors: Keisuke Ohta, Masahiko Miura, Kengo Sakaguchi, Fumio Sugawara, Noriyuki Sato, Hiroeki Sahara, Nobuaki Takahashi, Yoko Mori, Takayuki Yamazaki, Kazuyoshi Masaki, Hiroshi Murata
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Publication number: 20100280232Abstract: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patient who is then diagnosed or treated using the effector molecule.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Applicant: MALLINCKRODT INC.Inventors: Gary L. Cantrell, B. Daniel Burleigh
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Publication number: 20100267940Abstract: There is disclosed a method for producing a 4-deoxy-4-fluoro-D-glucose derivative by reacting a D-galactose derivative with either sulfuryl fluoride (SO2F2), trifluoromethanesulfonyl fluoride (CF3SO2F) or perfluorobutanesulfonyl fluoride (C4F9SO2F) in the presence of an organic base or in the presence of an organic base and a salt or complex of an organic base and hydrogen fluoride.Type: ApplicationFiled: November 26, 2008Publication date: October 21, 2010Inventors: Akihiro Ishii, Manabu Yasumoto, Takashi Ootsuka, Yasuko Nigorikawa
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Publication number: 20100261664Abstract: Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof The invention relates to substituted heterocyclic fluoroglycoside derivatives of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation. The compounds are suitable for example as antidiabetics.Type: ApplicationFiled: May 25, 2010Publication date: October 14, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wendelin FRICK, Heiner GLOMBIK, Werner KRAMER, Hubert HEUER, Harm BRUMMERHOP, Oliver PLETTENBURG
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Publication number: 20100248365Abstract: Provided herein are ganglioside synthesis inhibitors, including modulators of ganglioside glycosylation.Type: ApplicationFiled: March 29, 2010Publication date: September 30, 2010Applicant: ZACHARON PHARMACEUTICALS, INC.Inventors: Brett E. CRAWFORD, Charles A. GLASS, Jillian R. BROWN, Xiaomei BAI
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Publication number: 20100228015Abstract: This invention relates to novel homotopic prodrugs and medicaments and methods for their preparation, testing and use. In one embodiment, the homotopic prodrug has the general formula wherein is a biologically-active moiety comprising a carboxylic acid functional group, and Rb is a homotopically-symmetrical alcohol bonded to the biologically-active moiety through the carboxylic acid functional group to form an ester linkage, as well as optical isomers, enantiomers, pharmaceutically acceptable salts, biohydrolyzable amides, esters, and imides thereof and combinations thereof.Type: ApplicationFiled: April 23, 2010Publication date: September 9, 2010Inventors: Mitchell A. deLong, Jill M. McFadden, Susan M. Royalty, Eric J. Toone, Jeffrey D. Yingling
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Publication number: 20100222549Abstract: A dechalcogenative method for the preparation of an allylic sulfide comprises contacting an activated chalcogenide of Formula (I) with a thiol of Formula (II) for a period of time sufficient to form an intermediate of Formula (III), and supplying sufficient activation energy to the intermediate of Formula (III), in a suitable solvent, preferably in the absence of a phosphine or other thiophile, to induce a [2,3]-sigmatropic rearrangement therein to form an allylic sulfide of Formula (IV), with concomitant loss of chalcogen Z, as set forth in the following reaction scheme, wherein X is an activating group selected from the group consisting of CN, S-pyridyl, S-heteroaryl, SO2-aryl, and SO3Y; Y is an alkali metal ion; Z is Se or S; R1, R2, R3, R4, and R5 are each independently H or a hydrocarbon moiety; and R is an organic moiety.Type: ApplicationFiled: April 29, 2008Publication date: September 2, 2010Inventors: David Crich, Maheswaran Karatholuvhu, Venkataramanan Krishnamurthy, Thomas K. Hutton, Franck Brebion, Venkataraman Subramanian
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Publication number: 20100221269Abstract: The invention provides functionalized monosaccharides and disaccharides suitable for use in synthesizing a lipid A derivative, as well as methods for synthesizing and using a synthetic lipid A derivative.Type: ApplicationFiled: September 5, 2008Publication date: September 2, 2010Applicant: UNIVERSITY OF GEORGIA RESEACH FOUNDATION, INCInventor: Geert-Jan Boons
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Patent number: 7772193Abstract: A method and composition for the prophylaxis or treatment of humans or animals for septic shock and sepsis using a mixture of sophorolipids.Type: GrantFiled: March 26, 2007Date of Patent: August 10, 2010Assignee: Polytechnic University of NYUInventor: Richard A. Gross
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Patent number: 7767798Abstract: The present invention provides novel loganin analogues and a process for the preparation thereof. The present invention further provides the use of Iridoid glycoside loganin isolated from the fruit pulp of Strychnos nux-vomica and its bioactive semi-synthetic analogues against various human cancer cell lines grown in-vitro.Type: GrantFiled: March 2, 2006Date of Patent: August 3, 2010Assignee: Council of Scientific & Industrial ResearchInventors: Suman Preet Singh Khanuja, Santosh Kumar Srivastava, Ankur Garg, Merajuddin Khan, Mahendra Pandurang Dardokar, Anirban Pal
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Publication number: 20100185272Abstract: A method and product are provided for the treatment of connective tissue weakened due to destruction of tissue architecture, and in particular due to elastin degradation. The treatment agents employ certain unique properties of phenolic compounds to develop a protocol for reducing elastin degradation, such as that occurring during aneurysm formation in vasculature. According to the invention, elastin can be stabilized in vivo and destruction of connective tissue, such as that leading to life-threatening aneurysms in vasculature, can be tempered or halted all together. The treatment agents can be delivered or administered acutely or chronically according to various delivery methods, including sustained release methods incorporating perivascular or endovascular patches, use of microsphere carriers, hydrogels, or osmotic pumps.Type: ApplicationFiled: March 29, 2010Publication date: July 22, 2010Inventors: Narendra R. Vyavahare, Jason C. Isenburg, Dan T. Simionescu
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Publication number: 20100168045Abstract: The invention concerns novel polyunsaturated compounds of formula (I) wherein: R1 represents a R?1, -A-R?1 group, R?1 being selected from —COOH, —COOR3, —CONH2, —CONHR3, —CONR3, R4, —CHO, —CH2OH, —CH2OR5, and A represents a C2-C16 alkylene, alkenylene or alkynylene; R2 represents: an optionally substituted aryl group or an optionally substituted heteroaryl group; a sugar residue or, a fatty acid residue optionally branched and/or substituted preferably at the chain terminus and particularly by hydroxy, acetoxy radical or by an optionally protected amino radical; a —OC—(CH2)n CO-tocopheryl (alpha, beta or gamma or delta) group, with 2 $m(F) n $m(F) 10; a —R?2—O—R6 group, wherein R?2 is an optionally substituted arylene group or an optionally substituted heteroarylene group, and R6 represents a hydrogen atom, a straight or branched optionally substituted C1-C16 alkyl, a straight or branched optionally substituted C2-C16 alkenyl, or a straight or branched C2-C16 alkynyl group, an optionally substituted tocopheryType: ApplicationFiled: December 14, 2006Publication date: July 1, 2010Applicant: Pierre Fabre Dermo-CosmetiqueInventors: Pascal Bordat, Roger Tarroux, Jean-Hilaire Saurat, Olivier Sorg, Jean-Louis Brayer, Natacha Frison
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Publication number: 20100166801Abstract: The present invention relates to compounds of the following general formula (I) their process of preparation and their use in the treatment or the prophylaxis of tuberculosis.Type: ApplicationFiled: January 11, 2008Publication date: July 1, 2010Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.)Inventors: Germain Puzo, Jacques Prandi, Martine Gilleron, Gennaro De Libero, Julie Guiard, Lucia Mori, Samantha Paoletti
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Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof to Modulate Lipid Metabolism
Publication number: 20100137194Abstract: The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels.Type: ApplicationFiled: November 23, 2009Publication date: June 3, 2010Applicants: EASTERN MICHIGAN UNIVERSITYInventors: Daniel A. Lawrence, Cory Emal, Jacqueline Cale, Enming J. Su, Mark Warnock, Shih-Hon Li, Jeanne A. Cupp