Patents Examined by Yong Chu
  • Patent number: 8217052
    Abstract: The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p 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, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: July 10, 2012
    Assignee: Sanofi
    Inventors: Zhongli Gao, Ryan Hartung, David Stefany
  • Patent number: 8217051
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt or ester thereof wherein X, Y, R1, R2 are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: July 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jing Zhang, Zhuming Zhang
  • Patent number: 8211925
    Abstract: The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.
    Type: Grant
    Filed: April 27, 2007
    Date of Patent: July 3, 2012
    Assignee: TransTech Pharma, Inc.
    Inventors: Anthony Murray, Jesper Lau, Lone Jeppsen, Per Vedsø, Dharma Rao Polisetti, Bapu Reddy Gaddam, Daniel P. Christen, Kalpathy Chidambareswaran Santhosh, Jeremy T. Cooper, Robert Carl Andrews
  • Patent number: 8211862
    Abstract: The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: July 3, 2012
    Assignee: Pharmion LLC
    Inventors: Dumitru Ionescu, Peter Blumbergs, Gary L. Silvey
  • Patent number: 8207196
    Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
    Type: Grant
    Filed: February 1, 2008
    Date of Patent: June 26, 2012
    Assignee: Baylor College of Medicine
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
  • Patent number: 8207207
    Abstract: The invention relates to a fungicidally active compound of formula (I): as defined in claim 1; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: June 26, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi
  • Patent number: 8207368
    Abstract: By using phosphorus compounds, diesters of dicarbonic acid may be stabilized against thermal and chemical decomposition over a relatively long period. Mixtures of diesters of dicarbonic acid and phosphorus compounds are outstandingly suitable for preserving foods.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: June 26, 2012
    Assignee: LANXESS Deutschland GmbH
    Inventors: Steffen Kahlert, Johannes Kaulen, Erasmus Vogl
  • Patent number: 8207349
    Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 26, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bodo Betzemeier, Trixi Brandl, Steffen Breitfelder, Ralph Brueckner, Thomas Gerstberger, Michael Gmachl, Matthias Grauert, Frank Hilberg, Christoph Hoenke, Matthias Hoffmann, Maria Impagnatiello, Dirk Kessler, Christian Klein, Bernd Krist, Udo Maier, Darryl McConnell, Charlotte Reither, Stefan Scheuerer, Andreas Schoop, Norbert Schweifer, Oliver Simon, Martin Steegmaier, Steffen Steurer, Irene Waizenegger, Ulrike Weyer-Czernilofsky, Andreas Zoephel
  • Patent number: 8203003
    Abstract: Novel 4-fluoropyrrolidine-2-carbonyl fluoride compounds as useful fluorinated intermediates are disclosed. Their preparative methods are also disclosed. Useful applications of the 4-fluoropyrrolidine-2-carbonyl fluorides are shown.
    Type: Grant
    Filed: January 8, 2010
    Date of Patent: June 19, 2012
    Assignee: UBE Industries, Ltd.
    Inventors: Teruo Umemoto, Rajendra P. Singh
  • Patent number: 8202894
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: June 19, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Harald Walter, Daniel Stierli, Hans Tobler
  • Patent number: 8202895
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: June 19, 2012
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiβ, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Patent number: 8193701
    Abstract: The present invention provides a novel substance having an excellent color purity of blue, a light-emitting element and a light-emitting device using the novel substance. A stilbene derivative has a structure shown by the general formula (1). In the general formula (1), R1 is hydrogen, an alkyl group having 1 to 4 carbon atoms, or an aryl group having 6 to 25 carbon atoms. R2 is an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 25 carbon atoms. Each of R3 to R5 is hydrogen or an alkyl group having 1 to 4 carbon atoms. Ar1 is an aryl group having 6 to 25 carbon atoms.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: June 5, 2012
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Masakazu Egawa, Harue Nakashima, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo, Ryoji Nomura
  • Patent number: 8193350
    Abstract: A novel fluorescent compound having a high light fastness, high fluorescence quantum yield and sharp absorption spectrum, which emits fluorescence having a wavelength in long wavelength region, as well as its use as a labeling agent, is disclosed. In Formula [I] below, by forming a specific hetero ring(s) with R1 and R2, and/or R6 and R7, shift of the wavelength of the fluorescence to longer wavelength and increase in molar extinction coefficient are attained maintaining the high light fastness, high fluorescence quantum yield and sharp absorption spectrum which the fluorescent dyes having the boron dipyrromethene skeleton have.
    Type: Grant
    Filed: April 27, 2007
    Date of Patent: June 5, 2012
    Assignee: Keio University
    Inventors: Koji Suzuki, Keitaro Umezawa, Hiroshi Makino, Daniel Citterio
  • Patent number: 8193195
    Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: June 5, 2012
    Assignee: Merck Patentgesellschaft
    Inventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
  • Patent number: 8188128
    Abstract: Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: May 29, 2012
    Assignee: The University of Medicine and Dentistry of New Jersey
    Inventors: William J. Welsh, Youyi Peng, Qiang Zhang, Susan M. Keenan, Sonia Arora
  • Patent number: 8183404
    Abstract: The present invention is to provide a process for producing dicyanonorbornane characterized by causing hydrogen cyanide to undergo addition reaction with cyanonorbornene (bicyclo[2.2.1]-5-heptene-2-carbonitrile) in the presence of a zerovalent nickel complex catalyst which is produced by using a phosphite represented by P(x)(y)(z) (wherein P is a phosphorus atom, and x, y and z are each OR, where R represents an aryl group having not more than 18 carbon atoms) as a ligand to reduce a nickel halide with at least one metal selected among zinc, cadmium, beryllium, aluminum, iron and cobalt, wherein the phosphite is one which has a phosphate content of 1.0 weight % or lower based on the whole phosphite.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: May 22, 2012
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Norihiko Fukatsu, Hiroyuki Morijiri, Chitoshi Shimakawa, Koichi Tokunaga, Seiichi Kobayashi
  • Patent number: 8183274
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: May 22, 2012
    Assignee: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
  • Patent number: 8183416
    Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4alkoxy, C1-4haloalkoxy, CH2C?CR9, CH2CR10?CHR11, CH?C?CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4haloalkoxy(C1-4)alkyl or C1-4haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen,
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: May 22, 2012
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi
  • Patent number: 8183389
    Abstract: The invention relates to a process for the treatment of an aqueous mixture comprising a dipolar aprotic compound, comprising: a) an adsorption step, in which the aqueous mixture is brought into contact with a porous adsorbent, whereby the porous adsorbent is chosen such that the dipolar aprotic compound adsorbs to it more readily than water; b) a desorption step, in which the porous adsorbent is brought into contact with a desorbing agent, whereby a recovery solution is formed comprising the desorbing agent and the dipolar aprotic compound.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: May 22, 2012
    Assignee: DSM IP Assets B.V.
    Inventor: Jochen Stangl
  • Patent number: 8178568
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: May 15, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John Regan, Doris Riether