Benzene Ring Containing Patents (Class 564/251)
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Patent number: 8987335Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: August 15, 2012Date of Patent: March 24, 2015Assignee: University of Utah Research FoundationInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Patent number: 8981152Abstract: A microwave-induced process for the preparation of 2-aryl and 2,2-diaryl aldehydes and analogs wherein halohydrin formation and subsequent rearrangement to 2-aryl aldehydes from corresponding aryl alkanols occurs without formation of an intermediate epoxide or use of transition metal catalysts or lewis acids/bases.Type: GrantFiled: January 16, 2014Date of Patent: March 17, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Arun Kumar Sinha, Abhishek Sharma, Rakesh Kumar, Naina Sharma
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Publication number: 20150010469Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer, stereoisomer or deuterated analogue thereof, wherein X, R, R1, R2, R3, R4, M1, M2, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicants: British Columbia Cancer Agency Branch, University of British ColumbiaInventors: Raymond John Andersen, Javier Garcia Fernandez, Marianne Dorothy Sadar
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Patent number: 8916183Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: GrantFiled: January 22, 2013Date of Patent: December 23, 2014Assignee: Dow AgroSciences, LLC.Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
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Publication number: 20140275558Abstract: This document is related to the field of preparation of haloalkoxyarylhydrazines and certain intermediates derived therefrom, where said intermediates are useful in the preparation of certain pesticides disclosed in U.S. Pat. No. 8,178,658.Type: ApplicationFiled: February 27, 2014Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Ronald ROSS, JR., Peter BORROMEO
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Patent number: 8779200Abstract: The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used.Type: GrantFiled: February 25, 2010Date of Patent: July 15, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Arun Kumar Sinha, Abhishek Sharma, Rakesh Kumar, Naina Sharma
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Patent number: 8765810Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.Type: GrantFiled: October 18, 2012Date of Patent: July 1, 2014Assignees: The Trustees Of The University Of Pennsylvania, Cephalon, Inc.Inventors: Mark I. Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiaio
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Publication number: 20140163017Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 19, 2013Publication date: June 12, 2014Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
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Patent number: 8742173Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: GrantFiled: March 13, 2012Date of Patent: June 3, 2014Assignee: The Feinstein Institute for Medical ResearchInventor: Yousef Al-Abed
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Publication number: 20140116292Abstract: The present invention relates to a cellulose acetate film used for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).Type: ApplicationFiled: June 20, 2012Publication date: May 1, 2014Applicant: SK INNOVATION CO., LTD.Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Myoung Lae Kim, Yong Gyun Cho, Sang Yeup Lee, Ki Yup Kim
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Publication number: 20140107348Abstract: The present invention relates to methods of initiating a reaction represented by scheme 1 wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.Type: ApplicationFiled: December 17, 2013Publication date: April 17, 2014Applicant: SYNGENTA LIMITEDInventors: George Robert HODGES, Lisa MITCHELL, Alan James ROBINSON
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Patent number: 8642761Abstract: The present invention describes a method for the synthesis of enantiomerically pure 3-amidinophenylalanine derivatives, which are used as pharmaceutically effective urokinase inhibitors, by starting from 3-cyanophenylalanine derivatives. The methods of manufacture comprising only one synthesis step lead to new intermediates, namely 3-hydroxyamidino- and 3-amidrazonophenylalanine derivatives. These intermediates or their acetyl derivatives can be reduced into the desired 3-amidino-phenylalanine derivatives under gentle conditions (H2 or ammonium formiate, Pd/C (approx. 10%), ethanol/water, room temperature, normal pressure or also H2, Pd/C, AcOH or HCl/ethanol, 1-3 bar) in excellent yields and in an enantiomeric excess of up to 99.9%.Type: GrantFiled: November 18, 2011Date of Patent: February 4, 2014Assignee: Wilex AGInventors: Hugo Ziegler, Peter Wikstroem
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Patent number: 8637678Abstract: The present invention relates to methods of initiating a reaction represented by scheme (1), wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.Type: GrantFiled: December 16, 2009Date of Patent: January 28, 2014Assignee: Syngenta LimitedInventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
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Patent number: 8519003Abstract: The present invention relates to phenoxyphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyphenylamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.Type: GrantFiled: March 8, 2008Date of Patent: August 27, 2013Assignee: Bayer Cropscience AGInventors: Klaus Kunz, Ralf Dunkel, Jörg Nico Greul, Kerstin Ilg, Darren James Mansfield, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Ulrike Wachendorff-Neumann, Arnd Voerste
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Patent number: 8501995Abstract: The present invention provides new ?-phenylethylidenehydrazine derivatives, processes for preparing them and their use as pharmaceutical compostions.Type: GrantFiled: July 9, 2010Date of Patent: August 6, 2013Assignee: The Governors of the University of AlbertaInventors: Glen Baker, Edward Knaus
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Publication number: 20130172556Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.Type: ApplicationFiled: September 7, 2011Publication date: July 4, 2013Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
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Publication number: 20130072562Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.Type: ApplicationFiled: October 18, 2012Publication date: March 21, 2013Applicants: CEPHALON, INC., THE TRUSTEES OF THE UNIVERSITY OF PENNSYVANIAInventors: The Trustees Of The University Of Pennsyvania, Cephalon, Inc.
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Patent number: 8318699Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.Type: GrantFiled: January 31, 2006Date of Patent: November 27, 2012Assignees: The Trustees Of The University Of Pennsylvania, Cephalon, Inc.Inventors: Mark I Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiao
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Patent number: 8314132Abstract: Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).Type: GrantFiled: June 18, 2008Date of Patent: November 20, 2012Assignee: Biotechnologijos InstitutasInventors: Daumantas Matulis, Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene
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Publication number: 20120252839Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: FRED HUTCHINSON CANCER RESEARCH CENTERInventors: David HOCKENBERY, Julian SIMON
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Patent number: 8252958Abstract: The invention concerns the use of guanabenz and its derivatives for making drugs for treating cystic fibrosis and diseases related to a protein addressing deficiency in the cells, said derivatives corresponding to formula (I), wherein: R?H or C1 and the phenyl group comprises two substituents, or a pharmaceutically acceptable salt of said derivatives.Type: GrantFiled: November 28, 2006Date of Patent: August 28, 2012Assignees: Centre National de la Recherche Scientifique (CNRS), Universite de PoitiersInventors: Frederic Becq, Deborah Triboullard, Marc Blondel
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Publication number: 20120178805Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.Type: ApplicationFiled: March 13, 2012Publication date: July 12, 2012Inventor: Yousef Al-Abed
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Publication number: 20120148682Abstract: The present invention relates to the use of hydrazone compounds and copper for controlling the growth of fungi.Type: ApplicationFiled: January 14, 2010Publication date: June 14, 2012Applicant: DOW AGROSCIENCES LLCInventors: David H. Young, Steven Howard Shaber, Gerald Shaber, Cruz Avila-Adame, Nneka T. Breaux, James M. Ruiz, Thomas L. Siddall, Jeffery D. Webster
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Publication number: 20120129894Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: May 19, 2011Publication date: May 24, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
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Publication number: 20120041234Abstract: The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N-iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1 min-30 min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55%, depending upon the solvent and substrate used.Type: ApplicationFiled: February 25, 2010Publication date: February 16, 2012Inventors: Arun Kumar Sinha, Abhishek Sharma, Rakesh Kumar, Naina Sharma
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Patent number: 8101804Abstract: A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.Type: GrantFiled: July 25, 2007Date of Patent: January 24, 2012Assignee: Clariant Specialty Fine Chemicals (France)Inventors: Alain Schouteeten, Sébastien Jus, Jean-Claude Vallejos
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Publication number: 20110263869Abstract: The present invention relates to methods of initiating a reaction represented by scheme (1), wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.Type: ApplicationFiled: December 16, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, LLCInventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
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Publication number: 20110172436Abstract: The invention provides an Ethernet bridge or router comprising a network fabric adapted to provide interconnectivity to a plurality of Ethernet ports, each of the Ethernet ports being adapted to receive and/or transmit Ethernet frames, and wherein the Ethernet bridge or router further comprises an encapsulator connected to receive Ethernet Protocol Data Units from the Ethernet ports, wherein the encapsulator is operable to generate a Fabric Protocol Data Unit from a received Ethernet Protocol Data Unit, the Fabric Protocol Data Unit comprising a header portion, and a payload portion which comprises the Ethernet Protocol Data Unit concerned, and wherein the encapsulator is operable to transform Ethernet destination address information from the Ethernet Protocol Data Unit into a routing definition for the network fabric, and to include this routing definition in the header portion of the Fabric Protocol Data Unit. Also provided is a method of data delivery across a network.Type: ApplicationFiled: May 4, 2009Publication date: July 14, 2011Applicant: BASF SEInventors: Bernd Wolf, Volker Maywald, Michael Keil, Christopher Koradin, Michael Rack, Thomas Zierke, Martin Sukopp
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Patent number: 7932422Abstract: The invention relates to chlorine Guanabenz derivatives for treating Huntington's disease and other polyglutamine expansion associated diseases. More specifically, it relates to the use of the molecule of formula (I) wherein R?H or Cl and the phenyl group is at least substituted twice, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for treating polyglutamine expansion associated diseases.Type: GrantFiled: October 3, 2007Date of Patent: April 26, 2011Inventors: Anne Bertolotti, Marc Blondel
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Publication number: 20110046387Abstract: Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).Type: ApplicationFiled: June 18, 2008Publication date: February 24, 2011Inventors: Daumantas Matulis, Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene
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Patent number: 7884245Abstract: The present invention provides a process for producing a hydrazone compound represented by the general formula (5): which comprises a step of condensing a hydrazine compound represented by the general formula (3): with a carbonyl compound represented by the general formula (4): without taking the hydrazine compound out of a reactor. According to the invention, the target hydrazone compound can be obtained in high quality and in a high yield without taking the hydrazine compound out of the reactor at all, the hydrazine compound being a reaction intermediate which is structurally unstable and has a fear of influencing safety of workers owing to its toxicity (mutagenicity).Type: GrantFiled: June 28, 2005Date of Patent: February 8, 2011Assignee: Hodogaya Chemical Co., Ltd.Inventors: Kiyokazu Takaso, Katsumi Abe, Atsushi Takesue
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Patent number: 7875748Abstract: Disclosed are compounds represented by formula (1), wherein m, X, R1, R2, R3, R1?, R2?, R3?, and Ar are described herein. The inventive cyclopentadienone compounds can be used as core materials for an organic electroluminescence element or other optical devices. The invention also describes methods for preparing compounds of formula (1).Type: GrantFiled: April 6, 2009Date of Patent: January 25, 2011Assignee: Korea Institute of Science and TechnologyInventors: Hyun-Nam Cho, Sung Hyun Jung, Seok-Jin Park, Seung-Eun Lee
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Publication number: 20110009492Abstract: The present invention provides new ?-phenylethylidenehydrazine derivatives, processes for preparing them and their use as pharmaceutical compostions.Type: ApplicationFiled: July 9, 2010Publication date: January 13, 2011Applicant: The Governors of the University of AlbertaInventors: Glen Baker, Edward Knaus
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Patent number: 7794907Abstract: A hydrazone compound capable of realizing an electrophotographic photoreceptor having good electric properties such as good sensitivity and light responsibility, good electric and mechanical durability and good environment stability, is provided. The hydrazone compound is represented by the following general formula (1). The compound is contained in the charge transporting layer of the electrophotographic photoreceptor.Type: GrantFiled: September 7, 2005Date of Patent: September 14, 2010Assignee: Sharp Kabushiki KaishaInventors: Akihiro Kondoh, Takatsugu Obata
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Publication number: 20100152125Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: ApplicationFiled: March 20, 2008Publication date: June 17, 2010Applicant: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R.P. Novak
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Publication number: 20090306430Abstract: The invention concerns the use of guanabenz and its derivatives for making drugs for treating cystic fibrosis and diseases related to a protein addressing deficiency in the cells, said derivatives corresponding to formula (I), wherein: R?H or C1 and the phenyl group comprises two substituents, or a pharmaceutically acceptable salt of said derivatives.Type: ApplicationFiled: November 28, 2006Publication date: December 10, 2009Inventors: Frederic Becq, Deborah Triboullard, Marc Blondel
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Publication number: 20090221527Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.Type: ApplicationFiled: January 31, 2006Publication date: September 3, 2009Applicants: CEPTION THERAPEUTICS, INC., TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Mark I. Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiao
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Patent number: 7557248Abstract: The present invention relates to a method of creating a carbon-heteroatom bond, and preferably a carbon-nitrogen bond, by reacting a leaving group-bearing unsaturated compound and a nucleophilic compound. In particular, the invention relates to the creation of a carbon-nitrogen bond, using a method involving the arylation of nitrogenous organic derivatives; the inventive method consists in creating a carbon-heteroatom bond by reacting a leaving group-bearing unsaturated compound and a nucleophilic compound introducing a heteroatom which can be substituted for the leaving group, thereby creating a carbon-heteroatom bond, in the presence of a palladium-based catalyst, optionally a ligand. The invention is characterized in that the reaction takes place in the presence of an effective quantity of a metal hydroxide or ammonium hydroxide which is associated with an alcohol-type solvent.Type: GrantFiled: May 12, 2004Date of Patent: July 7, 2009Assignee: Rhodia ChimieInventors: Christelle Mauger, Gérard Mignani
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Patent number: 7547719Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.Type: GrantFiled: May 21, 2003Date of Patent: June 16, 2009Assignee: SmithKline Beecham Corp.Inventor: Stephen Moore
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Patent number: 7534540Abstract: An improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where X and X? are, each independently, a linking group; Ar comprises an aromatic group; R1, R2, and R3 comprise, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, or a heterocyclic group; and E1 and E2 are, each independently, a reactive ring group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses, imaging methods, and a polymeric charge transport material prepared from the charge transport material above are described.Type: GrantFiled: April 29, 2004Date of Patent: May 19, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Vygintas Jankauskas, Tadas Malinauskas, Edmundas Montrimas
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Patent number: 7531695Abstract: The present invention is directed to compounds having the structure (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.Type: GrantFiled: June 3, 2004Date of Patent: May 12, 2009Assignee: Auspex Pharmaceutical, IncInventors: Borcherng Hong, Sepehr Sarshar, Bruno Tse
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Publication number: 20090054629Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.Type: ApplicationFiled: February 8, 2006Publication date: February 26, 2009Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Jeffery W. Kelly, Steven M. Johnson, H. Michael Petrassi
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Patent number: 7479357Abstract: An organophotoreceptor that includes: (a) a charge transport material having the formula wherein A is selected from heterocyclic groups, naphthyl group, alkylsulfonylphenyl, stilbenyl or the group X, wherein X is represented by the formula B is selected from hydrogen, alkyl group, and an aryl group, with the proviso that when A is naphthyl, B is naphthyl; or where R1 is selected from the group consisting of N-pyrrolyl, N-pyrazolyl, N-tetrazolyl, N-indolyl, N-carbazolyl, N-triazolyl, N-imidazolyl, N-benzimidazolyl, N-indazolyl, and N-benzotriazolyl group, and R3 is a 9-fluorenone group. (b) a charge generating compound; and (c) an electrically conductive substrate.Type: GrantFiled: September 13, 2002Date of Patent: January 20, 2009Assignee: Samsung Electronics Co., Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katritzky, Ritu Jain, Rexiat Maimait, Anatoliy V. Vakulenko
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Patent number: 7427460Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where Ar is an aryl group; X comprises a bond or a linking group; R1, R2, and R3 each comprise H, a carboxyl, an amino group, a halogen, an alkyl group, an acyl group, an alkoxy group, an alkylsulfanyl group, an alkenyl group, an alkynyl group, a heterocyclic group, an aromatic group, or a part of a ring group; R4 comprises H, an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, or a heterocyclic group; and R5, R6, R7, and R8 each comprise an alkyl group, an alkenyl group, an alkynyl group, an aromatic group, a heterocyclic group, or a part of a ring group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: July 30, 2004Date of Patent: September 23, 2008Assignee: Samsung Electronics Co., Ltd.Inventors: Ruta Budreckiene, Gintaras Buika, Vygintas Jankauskas, Juozas V. Grazulevicius, Jonas Sidaravicius, Nusrallah Jubran, Zbigniew Tokarski
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Publication number: 20080221343Abstract: Conjugationally extended hydrazine compositions of the formula (RR2)N(H)n(NH2)n, fluorescent hydrazone compositions of the formula (RR2)NN?C(R1R2), methods of the formation of hydrazones from the reaction of conjugationally extended hydrazines with conjugationally extended carbonyls and methods of their use in assays systems are described. Use of these conjugationally extended hydrazine and oxime compositions for direct calorimetric and fluorometric assays wherein a chromophore or the fluorophore is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule.Type: ApplicationFiled: April 18, 2007Publication date: September 11, 2008Inventors: David A. Schwartz, Leopoldo Mendoza
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Publication number: 20080171793Abstract: Provided herein are bioactive agents comprising a compound that inhibits the ion transport activity of a cystic fibrosis transmembrane conductance regulator (CFTR) and that is linked to a macromolecule that interacts with a cell that expresses CFTR. The bioactive agents described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, secretory diarrhea.Type: ApplicationFiled: December 19, 2007Publication date: July 17, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Nitin D. Sonawane
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Patent number: 7326506Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where Z1 and Z2 comprise, each independently, a bond, a vinyl group, a —CR1?N—NR2— group, or a —CR3?N—N?CR4— group; Y1 and Y2 comprise, each independently, an aromatic group; X1 and X2 are, each independently, a linking group; W1 and W2 are, each independently, a —(CH2)n— group or a —(CH2)n-1—C(?O)— group, where n is an integer between 1 and 10, inclusive; Q1 and Q2 are, each independently, O, S, or NR; and R1, R2, R3, R4, R, R?, and R? comprise, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an acyl group, a heterocyclic group, or an aromatic group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: May 28, 2004Date of Patent: February 5, 2008Assignee: Samsung Electronics Co., Ltd.Inventors: Nusrallah Jubran, Zbigniew Tokarski, Vytautas Getautis, Juozas V. Grazulevicius, Vygintas Jankauskas, Ingrida Paulauskaite, Jurate Simokaitiene, Albina Stanisauskaite, Valentas Gaidelis
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Patent number: 7312361Abstract: Bisaryloxime ethers and bisarylhydroazones are shown to be effective for inhibiting formation of amyloid fibrils of transthyretin.Type: GrantFiled: February 8, 2006Date of Patent: December 25, 2007Assignee: The Scripps Research InstituteInventors: Jeffery W. Kelly, Steven M. Johnson, H. Michael Petrassi
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Patent number: 7144665Abstract: Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where R1, R2, R3, R4, R5, R6, R7, and R8 are, each independently, an alkyl group, an alkaryl group, an aryl group, or heterocyclic group, X and X? are, each independently, aromatic groups, and Z is a divalent linking group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.Type: GrantFiled: December 30, 2003Date of Patent: December 5, 2006Assignee: Samsung Electronics Co., Ltd.Inventors: Zbigniew Tokarski, Nusrallah Jubran, Vytautas Getautis, Ingrida Paulauskaite, Valentas Gaidelis, Edmundas Montrimas
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Patent number: 7138548Abstract: A process for the preparation of a compound of formula (I): wherein Ar represents an optionally substituted aromatic carbocycle or heterocycle, and R1 and R2 independently represent hydrogen, C1-10 alkyl, C(O)C1-10 alkyl or optionally substituted aryl provided that R1 and R2 are not both hydrogen which process comprises reacting together a compound of formula (II): Ar—X??(II) wherein Ar is as defined in relation to formula (I) and X represents a leaving group with a a compound of formula (III) wherein R1 and R2 are as defined in relation to formula (I) under aqueous conditions in the presence of a Pd (II) salt, a ligand and a Group I or Group II metal hydroxide base at a pH greater than 7. Compounds of formula (I) may be hydrolysed to the corresponding hydrazine.Type: GrantFiled: October 2, 2002Date of Patent: November 21, 2006Assignee: Avecia LimitedInventors: Andrew John Blacker, David Dodman, David Anthony Jackson, Jan Michael Fielden, John Heathcote Atherton