Patents Examined by Jason M. Nolan
  • Composition and device structure for iontophoresis
    Patent number: 8155738
    Abstract: Device structure 100 for iontophoresis provides electrode 101 and electrically conductive layer 102. Electrically conductive layer 102 contains active ingredient D and basic water swelling methacrylate copolymer P1 and/or acidic water swelling methacrylate copolymer P2. Electrode 101 and electrically conductive layer 102 are placed into a hollow of backing 103 and electrode terminal 104 is connected to electrode 101 through backing 103. Adhesive layer 105 is set around backing 103, and liner 106 to be removed when using the device, is placed so as to cover the hollow of backing 103.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: April 10, 2012
    Assignee: Hisamitsu Pharmaceutical Co., Inc.
    Inventors: Hirotoshi Adachi, Noriyuki Kuzumaki, Tetsuya Arimoto, Naruhito Higo
  • Metalloproteinase inhibitors
    Patent number: 8153673
    Abstract: Compounds of the formula (I) wherein Z is SO2(N6) or N(R7)SO2 or N(R7)SO2N(R6) useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: April 10, 2012
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • Method for producing crystal polymorphs of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid
    Patent number: 8148542
    Abstract: A method for producing crystal A of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid by dissolving 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxylic acid in methanol or a mixed solvent of methanol and water (the volume ratio of methanol to water is 90/10 or more), then adding water until the ratio of methanol to water becomes 7/3, and further adding a specific amount of a seed crystal at a specific timing during the addition of water.
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: April 3, 2012
    Assignee: Teijin Pharma Limited
    Inventor: Mitsutaka Kitamura
  • Carbazole derivatives as functional 5-HTligands
    Patent number: 8143303
    Abstract: Carbazole derivatives of formula (I), useful in treatment of a CNS disorders related to or affected by the 5-HT6 receptor are described. The pharmacological profile of these compounds includes high affinity binding with 5-HT6 receptor along with good selectivity towards the receptor. Stereoisomers, the salts, methods of preparation and medicines containing the carbazole derivatives are also described.
    Type: Grant
    Filed: June 9, 2006
    Date of Patent: March 27, 2012
    Assignee: Suven Life Sciences Limited
    Inventors: Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Vikas Shreekrishna Shirsath, Jagadish Babu Konda, Santosh Vishwakarma, Venkateswarlu Jasti
  • Process for the preparation of rapamycin derivatives
    Patent number: 8138344
    Abstract: Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32-hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and ?,??-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: March 20, 2012
    Assignee: Novartis AG
    Inventors: Murat Acemoglu, Sabine Pfeffer
  • Polyether carbonate polyols made via double metal cyanide (DMC) catalysis
    Patent number: 8134022
    Abstract: The present invention relates to a polyether carbonate polyol made by copolymerizing a starter molecule with carbon dioxide, at a pressure ranging from about 10 psia to about 2,000 psia, and an alkylene oxide, at a temperature ranging from about 50° C. to about 190° C. and in the presence of from about 0.001 wt. % to about 0.2 wt. % of a substantially non-crystalline double metal cyanide (DMC) catalyst, wherein the polyol has an incorporated carbon dioxide content of from about 1 wt. % to about 40 wt. %, wherein the ratio of cyclic carbonate by-product to total carbonate is less than about 0.3 and wherein the weight percentages are based on the weight of the polyol. The inventive polyether carbonate polyols may find use in producing polyurethane foams, elastomers, coatings, sealants and adhesives with improved properties.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: March 13, 2012
    Assignee: Bayer MaterialScience LLC
    Inventors: Karl W. Haider, Kenneth G. McDaniel, Sr., John E. Hayes, Jianzhong Shen
  • Hydrazide containing taxane conjugates
    Patent number: 8133888
    Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: March 13, 2012
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Trinadha Rao Chitturi, Rajamannar Thennati
  • Hemiasterlin derivatives and uses thereof in the treatment of cancer
    Patent number: 8129407
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: March 6, 2012
    Assignee: Eisai Inc.
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Method of using imidazolothiazole compounds for the treatment of disease
    Patent number: 8129374
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: March 6, 2012
    Assignee: Ambit Bioscience Corporation
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Imidazolidinone derivatives as 11B-HSD1 inhibitors
    Patent number: 8124636
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein A and R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 28, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
  • Process for separating the diastereomers of RSS-and SSS-N- ? [1-carboxy-3-phenylpropyl] lysylproline
    Patent number: 8119817
    Abstract: A process for separating the diastereomers of RSS— and SSS—N-?[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent.
    Type: Grant
    Filed: August 3, 1999
    Date of Patent: February 21, 2012
    Assignee: Degussa-Huels AG
    Inventors: Frédéric Boisivon, Jean Debas, Gérard Richet
  • Macrolide antibiotics and their use for medical purposes
    Patent number: 8114864
    Abstract: The invention provides novel Thuggacin-Type macrolide compounds which form rearrangement products forming a lacton bond to different carbon atoms. The novel compounds can be produced by fermentation of Sorangium cellulosum and Chondromyces crocatus and can be isolated by adsorption and chromoatograhic processing steps. The compounds are found to have antibiotic activity. The invention also relates to Thuggacin A, Thuggacin B, Thuggacin C, 13-Methyl-Thuggacin A, Thuggacin CMC-A, Thuggacin CMC-B and Thuggacin CMC-C AS Antimycobacterial Agents.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: February 14, 2012
    Assignee: Helmholtz-Zentrum Fuer Infektionsforschung
    Inventors: Rolf Jansen, Brigitte Kunze, Herbert Irschik
  • Process for preparing 5-biphenyl-4-amino-2-methyl pentanoic acid
    Patent number: 8115016
    Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: February 14, 2012
    Assignee: Novartis AG
    Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar M Waykole
  • Stabilization of hydroformylation catalysts based on phosphoramide ligands
    Patent number: 8110709
    Abstract: The present invention relates to a process for the hydroformylation of ethylenically unsaturated compounds by reaction with carbon monoxide and hydrogen in the presence of a catalytically active fluid which comprises a dissolved metal complex of a metal of transition group VIII of the Periodic Table of the Elements with at least one phosphoramidite compound as ligand, wherein the fluid is brought into contact with a base.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: February 7, 2012
    Assignee: BASF SE
    Inventors: Rainer Papp, Wolfgang Ahlers, Thomas Mackewitz, Rocco Paciello, Martin Volland
  • Inhibitors of matrix metalloproteinases
    Patent number: 8093287
    Abstract: The present invention provides novel compounds of formulas I-IX, as described herein. Also provided are compositions of compounds of formulas I-IX, methods of making compounds of formulas I-IX, and methods of using compounds of formulas I-IX. The compounds of the invention can be used to inhibit matrix metalloproteinases, and are useful to treat conditions and diseases associated therewith.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: January 10, 2012
    Assignees: University of Notre Dame du Lac, Wayne State University
    Inventors: Mijoon Lee, Masahiro Ikejiri, Mayland Chang, Rafael Fridman, Shahriar Mobashery
  • Rho kinase inhibitors
    Patent number: 8093266
    Abstract: Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
    Type: Grant
    Filed: January 2, 2008
    Date of Patent: January 10, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Dahmann, Eugene Richard Hickey, Xiang Li, Wang Mao, Daniel R. Marshall, Tina M. Morwick, Robert Sibley, Roger John Snow, Ronald J. Sorcek, Frank Wu, Erick Richard Roush Young
  • 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 bis-(monoethanolamine)
    Patent number: 8088813
    Abstract: 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: Grant
    Filed: September 1, 2010
    Date of Patent: January 3, 2012
    Assignee: GlaxoSmithKline LLC
    Inventor: Stephen Moore
  • Solid states of atorvastatin potassium
    Patent number: 8071638
    Abstract: Atorvastatin potassium crystalline Forms A, B, E, F, and G are provided. Also provided are methods of preparing atorvastatin potassium crystalline Forms A, B, E, F, and G. Atorvastatin potassium crystalline Forms A, B, E, F, and G may be used to prepare pharmaceutical compositions useful for the treatment of hypercholesterolemia or hyperlipidemia.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: December 6, 2011
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Yoav Kowalski, Ariel Mittelman, Sigalit Levi
  • 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 bis-(monoethanolamine)
    Patent number: 8071129
    Abstract: Disclosed are novel pharmaceutical compositions containing 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 bis-(monoethanolamine) (eltrombopag olamine) and processes for preparing the same.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: December 6, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Francis X Muller, Shivakumar G Kapsi
  • 3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
    Patent number: 8067452
    Abstract: This invention provides compounds of Formula I which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to the isothiocyanate group to form a thioamide adduct; d) cyclizing the thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to the cyano group to form a carboxamidine group.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: November 29, 2011
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jim Zhen Wu, Huanming Chen