Benzene Ring Bonded Directly To The Five-membered Hetero Ring Patents (Class 548/577)
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Patent number: 11078186Abstract: There are described ROR? modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.Type: GrantFiled: November 8, 2017Date of Patent: August 3, 2021Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang, T. G. Murali Dhar, Zhonghui Lu, Arun Kumar Gupta, Ananta Karmakar
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Patent number: 9359285Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.Type: GrantFiled: October 20, 2014Date of Patent: June 7, 2016Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
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Patent number: 8980937Abstract: The present invention provides novel aryl pyrrolidines having an excellent insecticidal action as insecticides. Aryl pyrrolidines represented by the formula (I) and use thereof as insecticide.Type: GrantFiled: May 15, 2012Date of Patent: March 17, 2015Assignee: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Ulrich Görgens
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Publication number: 20150073139Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: July 21, 2014Publication date: March 12, 2015Inventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
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Patent number: 8975345Abstract: The disclosure relates to oxygen scavenging polymer compositions, methods of making the compositions, articles prepared from the compositions, and methods of making the articles. 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: April 22, 2014Date of Patent: March 10, 2015Assignee: Plastipak Packaging, Inc.Inventor: Girish N. Deshpande
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Patent number: 8951999Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: GrantFiled: October 20, 2010Date of Patent: February 10, 2015Assignee: Orexo ABInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
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Publication number: 20150011553Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20140371272Abstract: The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula (I).Type: ApplicationFiled: January 18, 2013Publication date: December 18, 2014Inventors: Venkatram R. Mereddy, Lester R. Drewes, Mohammed Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
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Patent number: 8865918Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.Type: GrantFiled: August 23, 2013Date of Patent: October 21, 2014Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
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Publication number: 20140303384Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical compositions containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: October 5, 2012Publication date: October 9, 2014Inventors: Brian A. Duclos, Richard Andrew Ewin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Derek James Sheehan, Susan Mary Kult Sheehan, Donald James Skalitzky, Rajendran Vairagoundar
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Publication number: 20140296527Abstract: The present invention relates to processes for the enantio-selective preparation of spyrrolidine derivatives useful in the manufacture of pesticidally active compounds, as well as to intermediates in the processes. The processes include those comprising (a-i) reacting a compound of formula Ia wherein P is alkyl, aryl or heteroaryl, each optionally substituted, wherein the heteroaryl is connected at P via a ring carbon atom; R1 is chlorodifluoromethyl or trifluoromethyl; R2 is aryl or heteroaryl, each optionally substituted; with a source of cyanide in the presence a chiral catalyst to give a compound of formula IIa wherein P, R1 and R2 are as defined for the compound of formula Ia; and (a-ii) oxidising the compound of formula IIa with a peroxy acid, or peroxide in the presence of an acid to give a compound of formula VI wherein R1 and R2 are as defined for the compound of formula Ia.Type: ApplicationFiled: September 28, 2012Publication date: October 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkal, Helmars Smits, Sebastian Volker Wendeborn, Guillaume Berthon, Jerome Yves Cassayre, Myriem El Qacemi
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Patent number: 8772313Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.Type: GrantFiled: November 1, 2011Date of Patent: July 8, 2014Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KGInventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
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Publication number: 20140187556Abstract: Anti-amyloid compounds are provided along with methods of use thereof.Type: ApplicationFiled: March 2, 2012Publication date: July 3, 2014Applicant: Treventis CorporationInventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
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Patent number: 8754117Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.Type: GrantFiled: January 28, 2013Date of Patent: June 17, 2014Assignee: Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, Jianguo Ma
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Patent number: 8748519Abstract: The disclosure relates to oxygen scavenging polymer compositions, methods of making the compositions, articles prepared from the compositions, and methods of making the articles. 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: November 12, 2010Date of Patent: June 10, 2014Assignee: Plastipak Packaging, Inc.Inventor: Girish N. Deshpande
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Patent number: 8748633Abstract: Provided herein are compounds, such as compounds of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: GrantFiled: October 23, 2012Date of Patent: June 10, 2014Assignee: Ligand Pharmaceuticals IncorporatedInventor: Lin Zhi
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Patent number: 8735385Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: GrantFiled: November 6, 2012Date of Patent: May 27, 2014Assignee: SanofiInventor: Zhongli Gao
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Publication number: 20140081019Abstract: The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Applicant: SANOFIInventors: Jens Atzrodt, Volker Derdau, Wolfgang Holla, Matthias Beller, Lorenz Neubert, Dirk Michalik
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Patent number: 8653304Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: GrantFiled: September 30, 2010Date of Patent: February 18, 2014Assignee: Toray Industries, Inc.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
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Publication number: 20140039181Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.Type: ApplicationFiled: December 28, 2012Publication date: February 6, 2014Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of SciencesInventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
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Patent number: 8642642Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.Type: GrantFiled: April 18, 2007Date of Patent: February 4, 2014Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KGInventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
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Patent number: 8642583Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: GrantFiled: October 29, 2009Date of Patent: February 4, 2014Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi T. Tran, Victoria D. Wong
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Publication number: 20140024839Abstract: A fullerene derivative having 60 or more carbon atoms includes at least one structure having the following formula (I): wherein R1, R2 and R3 independently represent a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted aryl group and a substituted or unsubstituted monofunctional heterocyclic group; and at least one of R1, R2 and R3 comprises the following formula (II): wherein R4 represents a substituted or unsubstituted alkyl group having 4 to 30 carbon atoms, a substituted or unsubstituted alkenyl group having 4 to 30 carbon atoms, a substituted or unsubstituted alkynyl group having 4 to 30 carbon atoms or a substituted or unsubstituted aralkyl group having 4 to 30 carbon atoms.Type: ApplicationFiled: May 31, 2013Publication date: January 23, 2014Applicant: RICOH COMPANY, LTD.Inventor: Yoshiki Yanagawa
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Publication number: 20130331397Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.Type: ApplicationFiled: February 23, 2012Publication date: December 12, 2013Applicant: IRM LLCInventors: Valentina Molteni, Yi Fan, Jon Loren, Jeffrey M. Smith, Brenton T. Flatt
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Publication number: 20130310408Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Applicant: Bayer Intellectual Property GmbHInventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
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Publication number: 20130281452Abstract: Substituted 4-aminobenzamides, pharmaceutical compositions containing these compounds and also methods of using these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
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PROCESS FOR THE PREPARATION OF TETRACYCLIC DERIVATIVES AND INTERMEDIATE PRODUCTS USED IN THE PROCESS
Publication number: 20130274466Abstract: A process for preparation of a compound of formula I or a pharmaceutically acceptable salt thereof, is disclosed. The process involves subjecting a compound of formula II to Ullmann-type conditions to effect an intra-molecular ring closure reaction to form the compound of formula I. The different substituents are as described in the specification. Further, the process can provide an alternate route for the synthesis of asenapine from starting materials that can be readily available.Type: ApplicationFiled: September 26, 2011Publication date: October 17, 2013Applicant: Alphora Research Inc.Inventors: Boris Gorin, Craig Edward Dixon, Yang Qu -
Patent number: 8551364Abstract: A process for inhibiting polymerization of an aromatic vinyl compound during the stage of producing, purifying, storing or transporting the aromatic vinyl compound which not only inhibits an initial polymerization but also inhibits polymerization efficiently over a long period of time and which is excellent in handleability. The process involves the step of adding a nitrogenous aromatic compound in combination with a sulfonic acid compound to the aromatic vinyl compound during the production, purification, storage of transportation thereof.Type: GrantFiled: June 20, 2012Date of Patent: October 8, 2013Assignee: Hakuto Co., Ltd.Inventors: Junichi Nakajima, Seiji Tanizaki
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Patent number: 8552051Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryanthemaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.Type: GrantFiled: March 16, 2010Date of Patent: October 8, 2013Assignee: H. L. Hall & Sons LimitedInventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
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Patent number: 8519158Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.Type: GrantFiled: March 11, 2005Date of Patent: August 27, 2013Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
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Patent number: 8507537Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.Type: GrantFiled: October 13, 2007Date of Patent: August 13, 2013Assignee: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130184320Abstract: The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: ApplicationFiled: September 30, 2011Publication date: July 18, 2013Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertud Bandur
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Patent number: 8476336Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.Type: GrantFiled: December 17, 2009Date of Patent: July 2, 2013Assignee: Acri.Tec GmbHInventor: Juergen Nachbaur
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Publication number: 20130160827Abstract: Fullerene surfactant compounds useful as interfacial layer in polymer solar cells to enhance solar cell efficiency. Polymer solar cell including a fullerene surfactant-containing interfacial layer intermediate cathode and active layer.Type: ApplicationFiled: December 5, 2012Publication date: June 27, 2013Applicant: University of Washington Through its Center for CommercializationInventor: University of Washington Through Its Center for Commercialization
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Patent number: 8450398Abstract: The disclosure relates to oxygen scavenging molecules, compositions, methods of making the compositions, articles prepared from the compositions, and methods of making the articles. 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: November 12, 2010Date of Patent: May 28, 2013Assignee: Constar International, Inc.Inventor: Girish N. Deshpande
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Patent number: 8383668Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: September 16, 2011Date of Patent: February 26, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Patent number: 8362025Abstract: Compounds of formula (I) and compositions comprising a compound of formula (I) for treating disorders related to TRPA1 are described herein.Type: GrantFiled: December 22, 2009Date of Patent: January 29, 2013Assignee: Hydra Biosciences, Inc.Inventors: Howard Ng, Jianfeng Hang
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Patent number: 8354446Abstract: Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: GrantFiled: December 12, 2008Date of Patent: January 15, 2013Assignee: Ligand Pharmaceuticals IncorporatedInventor: Lin Zhi
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Publication number: 20120322833Abstract: The present invention relates to novel pesticidal arylpyrrolidine compounds (arylpyrrolidines) having the general formula (I) wherein A, X1, X2, X3, X4, R1, R2, R3, R4, and G are as defined in the application and their use as pesticide, in particular for combating animal pests which occur in the agricultural and/or the veterinary field, as well as to a preparation methods for preparing such compounds.Type: ApplicationFiled: December 23, 2010Publication date: December 20, 2012Applicant: Bayer Intellectual Property GmbHInventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Norio Sasaki, Tetsuya Murata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Hidetoshi Kishikawa, Ulrich Görgens
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Publication number: 20120270877Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.Type: ApplicationFiled: November 1, 2010Publication date: October 25, 2012Applicant: MannKind CorporationInventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
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Publication number: 20120234721Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.Type: ApplicationFiled: September 9, 2011Publication date: September 20, 2012Applicant: Neurotherapeutics Pharma, Inc.Inventors: Daryl W. HOCHMAN, John J. Partridge
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Publication number: 20120232278Abstract: The present invention provides novel aryl pyrrolidines having an excellent insecticidal action as insecticides. Aryl pyrrolidines represented by the formula (I) and use thereof as insecticide.Type: ApplicationFiled: May 15, 2012Publication date: September 13, 2012Applicant: Bayer Intellectual Property GmbHInventors: Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Katsuhiko SHIBUYA, Eiichi SHIMOJO, Ulrich GÖRGENS
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Patent number: 8263583Abstract: This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament.Type: GrantFiled: March 6, 2008Date of Patent: September 11, 2012Assignee: Pfizer LimitedInventors: Paul Alan Glossop, Kim James
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Publication number: 20120190854Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.Type: ApplicationFiled: April 5, 2012Publication date: July 26, 2012Applicant: The Board of Trustees of the University of IllinoisInventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
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Patent number: 8227623Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.Type: GrantFiled: May 24, 2010Date of Patent: July 24, 2012Assignee: MSD Oss B.V.Inventors: Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
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Publication number: 20120184735Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: September 30, 2010Publication date: July 19, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
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Publication number: 20120178789Abstract: The present invention relates to compounds of the general formula: (I) wherein ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: September 16, 2010Publication date: July 12, 2012Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
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Publication number: 20120142937Abstract: A process is provided for the preparation of aryl-heteroatom-bridged compounds by reacting a halogen-substituted aromatic compound with a trialkylsilyl-substituted heteroatom-containing organic compound.Type: ApplicationFiled: March 16, 2010Publication date: June 7, 2012Applicant: Zylum Beteiligungsgesellschaft mbH & Co. Patente II KGInventors: Andreas Kreipl, Nicolas Boege, Werner R. Thiel
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Patent number: 8188301Abstract: The present invention relates to the use of compounds which increase extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically to the use of 3-disubstituted phenyl-1-pyrrolidinols for the treatment of central nervous system disorders.Type: GrantFiled: June 4, 2008Date of Patent: May 29, 2012Assignee: NSAB, Filial af NeuroSearch Sweden AB, SverigeInventors: Clas Sonesson, Lars Swanson, Fredrik Pettersson, Nicholas Waters, Susanna Waters