Benzene Ring Bonded Directly To The Five-membered Hetero Ring Patents (Class 548/577)
  • Patent number: 11078186
    Abstract: 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: Grant
    Filed: November 8, 2017
    Date of Patent: August 3, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang, T. G. Murali Dhar, Zhonghui Lu, Arun Kumar Gupta, Ananta Karmakar
  • Patent number: 9359285
    Abstract: 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: Grant
    Filed: October 20, 2014
    Date of Patent: June 7, 2016
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
  • Patent number: 8980937
    Abstract: 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: Grant
    Filed: May 15, 2012
    Date of Patent: March 17, 2015
    Assignee: Bayer CropScience AG
    Inventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Ulrich Görgens
  • Publication number: 20150073139
    Abstract: 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: Application
    Filed: July 21, 2014
    Publication date: March 12, 2015
    Inventors: 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
  • Patent number: 8975345
    Abstract: 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: Grant
    Filed: April 22, 2014
    Date of Patent: March 10, 2015
    Assignee: Plastipak Packaging, Inc.
    Inventor: Girish N. Deshpande
  • Patent number: 8951999
    Abstract: 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: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Publication number: 20150011553
    Abstract: 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: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: 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
  • Publication number: 20140371272
    Abstract: 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: Application
    Filed: January 18, 2013
    Publication date: December 18, 2014
    Inventors: Venkatram R. Mereddy, Lester R. Drewes, Mohammed Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
  • Patent number: 8865918
    Abstract: 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: Grant
    Filed: August 23, 2013
    Date of Patent: October 21, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
  • Publication number: 20140303384
    Abstract: 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: Application
    Filed: October 5, 2012
    Publication date: October 9, 2014
    Inventors: 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
  • Publication number: 20140296527
    Abstract: 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: Application
    Filed: September 28, 2012
    Publication date: October 2, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Tomas Smejkal, Helmars Smits, Sebastian Volker Wendeborn, Guillaume Berthon, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8772313
    Abstract: 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: Grant
    Filed: November 1, 2011
    Date of Patent: July 8, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • Publication number: 20140187556
    Abstract: Anti-amyloid compounds are provided along with methods of use thereof.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Treventis Corporation
    Inventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
  • Patent number: 8754117
    Abstract: 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: Grant
    Filed: January 28, 2013
    Date of Patent: June 17, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Jianguo Ma
  • Patent number: 8748519
    Abstract: 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: Grant
    Filed: November 12, 2010
    Date of Patent: June 10, 2014
    Assignee: Plastipak Packaging, Inc.
    Inventor: Girish N. Deshpande
  • Patent number: 8748633
    Abstract: 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: Grant
    Filed: October 23, 2012
    Date of Patent: June 10, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventor: Lin Zhi
  • Patent number: 8735385
    Abstract: 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: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Publication number: 20140081019
    Abstract: 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: Application
    Filed: May 21, 2012
    Publication date: March 20, 2014
    Applicant: SANOFI
    Inventors: Jens Atzrodt, Volker Derdau, Wolfgang Holla, Matthias Beller, Lorenz Neubert, Dirk Michalik
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20140039181
    Abstract: 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: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8642583
    Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: February 4, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi T. Tran, Victoria D. Wong
  • Patent number: 8642642
    Abstract: 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: Grant
    Filed: April 18, 2007
    Date of Patent: February 4, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
  • Publication number: 20140024839
    Abstract: 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: Application
    Filed: May 31, 2013
    Publication date: January 23, 2014
    Applicant: RICOH COMPANY, LTD.
    Inventor: Yoshiki Yanagawa
  • Publication number: 20130331397
    Abstract: 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: Application
    Filed: February 23, 2012
    Publication date: December 12, 2013
    Applicant: IRM LLC
    Inventors: Valentina Molteni, Yi Fan, Jon Loren, Jeffrey M. Smith, Brenton T. Flatt
  • Publication number: 20130310408
    Abstract: 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: Application
    Filed: March 14, 2013
    Publication date: November 21, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: 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
  • Publication number: 20130281452
    Abstract: 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: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Inventors: Gregor BAHRENBERG, Sven KUEHNERT, Simon LUCAS, Wolfgang SCHROEDER
  • Publication number: 20130274466
    Abstract: 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: Application
    Filed: September 26, 2011
    Publication date: October 17, 2013
    Applicant: Alphora Research Inc.
    Inventors: Boris Gorin, Craig Edward Dixon, Yang Qu
  • Patent number: 8552051
    Abstract: 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: Grant
    Filed: March 16, 2010
    Date of Patent: October 8, 2013
    Assignee: H. L. Hall & Sons Limited
    Inventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
  • Patent number: 8551364
    Abstract: 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: Grant
    Filed: June 20, 2012
    Date of Patent: October 8, 2013
    Assignee: Hakuto Co., Ltd.
    Inventors: Junichi Nakajima, Seiji Tanizaki
  • Patent number: 8519158
    Abstract: 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: Grant
    Filed: March 11, 2005
    Date of Patent: August 27, 2013
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
  • Patent number: 8507537
    Abstract: 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: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: 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
  • Publication number: 20130190288
    Abstract: 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: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130184320
    Abstract: 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: Application
    Filed: September 30, 2011
    Publication date: July 18, 2013
    Applicant: BASF SE
    Inventors: Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertud Bandur
  • Patent number: 8476336
    Abstract: 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: Grant
    Filed: December 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Acri.Tec GmbH
    Inventor: Juergen Nachbaur
  • Publication number: 20130160827
    Abstract: 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: Application
    Filed: December 5, 2012
    Publication date: June 27, 2013
    Applicant: University of Washington Through its Center for Commercialization
    Inventor: University of Washington Through Its Center for Commercialization
  • Patent number: 8450398
    Abstract: 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: Grant
    Filed: November 12, 2010
    Date of Patent: May 28, 2013
    Assignee: Constar International, Inc.
    Inventor: Girish N. Deshpande
  • Patent number: 8383668
    Abstract: 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: Grant
    Filed: September 16, 2011
    Date of Patent: February 26, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Soren Ebdrup, Henrik Sune Andersen
  • Patent number: 8362025
    Abstract: Compounds of formula (I) and compositions comprising a compound of formula (I) for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 29, 2013
    Assignee: Hydra Biosciences, Inc.
    Inventors: Howard Ng, Jianfeng Hang
  • Patent number: 8354446
    Abstract: 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: Grant
    Filed: December 12, 2008
    Date of Patent: January 15, 2013
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventor: Lin Zhi
  • Publication number: 20120322833
    Abstract: 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: Application
    Filed: December 23, 2010
    Publication date: December 20, 2012
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Norio Sasaki, Tetsuya Murata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Hidetoshi Kishikawa, Ulrich Görgens
  • Publication number: 20120270877
    Abstract: 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: Application
    Filed: November 1, 2010
    Publication date: October 25, 2012
    Applicant: MannKind Corporation
    Inventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
  • Publication number: 20120234721
    Abstract: 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: Application
    Filed: September 9, 2011
    Publication date: September 20, 2012
    Applicant: Neurotherapeutics Pharma, Inc.
    Inventors: Daryl W. HOCHMAN, John J. Partridge
  • Publication number: 20120232278
    Abstract: 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: Application
    Filed: May 15, 2012
    Publication date: September 13, 2012
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Katsuhiko SHIBUYA, Eiichi SHIMOJO, Ulrich GÖRGENS
  • Patent number: 8263583
    Abstract: 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: Grant
    Filed: March 6, 2008
    Date of Patent: September 11, 2012
    Assignee: Pfizer Limited
    Inventors: Paul Alan Glossop, Kim James
  • Publication number: 20120190854
    Abstract: 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: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Patent number: 8227623
    Abstract: 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: Grant
    Filed: May 24, 2010
    Date of Patent: July 24, 2012
    Assignee: MSD Oss B.V.
    Inventors: Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
  • Publication number: 20120184735
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: September 30, 2010
    Publication date: July 19, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20120178789
    Abstract: 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: Application
    Filed: September 16, 2010
    Publication date: July 12, 2012
    Inventors: Eric J. Gilbert, Michael W. Miller, Duane Eugene DeMong, Andrew W. Stamford, William J. Greenlee
  • Publication number: 20120142937
    Abstract: 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: Application
    Filed: March 16, 2010
    Publication date: June 7, 2012
    Applicant: Zylum Beteiligungsgesellschaft mbH & Co. Patente II KG
    Inventors: Andreas Kreipl, Nicolas Boege, Werner R. Thiel
  • Patent number: 8188301
    Abstract: 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: Grant
    Filed: June 4, 2008
    Date of Patent: May 29, 2012
    Assignee: NSAB, Filial af NeuroSearch Sweden AB, Sverige
    Inventors: Clas Sonesson, Lars Swanson, Fredrik Pettersson, Nicholas Waters, Susanna Waters