Patents Examined by Andrew D. Kosar
  • Process for the preparation of sulfamide derivatives
    Patent number: 8895762
    Abstract: The present invention is directed to an improved process for the preparation of sulfamide derivatives.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Stefan Horns, Roger Faessler
  • Methods of use of cyclopamine analogs
    Patent number: 8895576
    Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: November 25, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Michael J. Grogan, Karen J. McGovern, Martin R. Tremblay
  • Methods for the preparation of HIV attachment inhibitor piperazine prodrug compound
    Patent number: 8889869
    Abstract: A method for making the compound is set forth utilizing the starting material
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: November 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin D. Eastgate, Michael S. Bultman, Ke Chen, Dayne Dustan Fanfair, Richard J. Fox, Thomas E. La Cruz, Boguslaw M. Mudryk, Christina Ann Risatti, James H. Simpson, Maxime C. Soumeillant, Jonathan Clive Tripp, Yi Xiao
  • Fibrosis inhibitor
    Patent number: 8889693
    Abstract: The main object of the present invention is to provide a fibrosis inhibitor. The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient: In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: November 18, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Koji Murakami, Takuya Toramoto
  • Treatment of hyperproliferative diseases with vinca alkaloid N-oxide analogs
    Patent number: 8883775
    Abstract: The present invention relates to vinca alkaloid and analog N-oxides having activity for treating hyperproliferative disorders. Further, the invention relates to pharmaceutical compositions and methods of using vinca alkaloid and analog N-oxides, alone or in combination with one or more other active agents or treatments, to treat hyperproliferative disorders.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: November 11, 2014
    Assignee: Cascade Prodrug Inc.
    Inventors: John G. Curd, John F. W. Keana, Alshad S. Lalani, Paul B. Westberg, Bradford Goodwin, W. David Henner
  • Trioxane monomers and dimers
    Patent number: 8884032
    Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: November 11, 2014
    Assignee: The Johns Hopkins University
    Inventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
  • Process for preparing aminobenzoylbenzofuran derivatives
    Patent number: 8884033
    Abstract: The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which R1 and R2 are as defined in the disclosure; by reduction of a 5-nitrobenzofuran derivative of formula II: using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: November 11, 2014
    Assignee: Sanofi
    Inventors: Xavier Bon, Christine Biencourt, Corinne Leroy, Julia Mateos-Caro, Philippe Vayron
  • 3-(4-aminophenyl)-2-furancarboxylic acid derivative and pharmaceutically acceptable salt thereof
    Patent number: 8883824
    Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five-to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: November 11, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
  • Process for the preparation of a mono-N-alkypiperazine
    Patent number: 8884015
    Abstract: Process for the preparation of a mono-N-alkylpiperazine of the formula I in which R1 is C1- to C5-alkyl or 2-(2-hydroxyethoxy)ethyl, by reacting diethanolamine (DEOA) of the formula II with a primary amine of the formula H2N—R1 (III) in the presence of hydrogen and a supported, metal-containing catalyst, where the catalytically active mass of the catalyst, prior to its reduction with hydrogen, comprises oxygen-containing compounds of aluminum, copper, nickel and cobalt and, in the range from 0.2 to 5.0% by weight, oxygen-containing compounds of tin, calculated as SnO, and the reaction is carried out in the liquid phase at an absolute pressure in the range from 95 to 145 bar.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: November 11, 2014
    Assignee: BASF SE
    Inventors: Roland Bou Chedid, Johann-Peter Melder, Ulrich Abel, Roman Dostalek, Bernd Stein
  • Method for purifying a fused pyrrolocarbazole derivative
    Patent number: 8884014
    Abstract: The present invention relates a method for purifying a fused pyrrolocarbazole compound known as 11-isobutyl-2-methyl-8-(2-pyrimidinylamino)-2,5,6,11,12,13-hexahydro-4Hindazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one using an acid complex thereof. The present invention also relates to a crystalline form of the acid complex.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: November 11, 2014
    Assignees: Cephalon, Inc., Teva Sante
    Inventors: Shawn P. Allwein, Arnaud Grandeury, Guy Piacenza, Sebastien Rose
  • 2,6-dihalo-5-alkoxy-4-substituted-pyrimidines, pyrimidine-carbaldehydes, and methods of formation and use
    Patent number: 8877925
    Abstract: 2,6-Dihalo-5-alkoxy-4-substituted-pyrimidines, 2,6-dihalo-5-alkoxy-4-pyrimdine carbaldehydes, and derivatives of each are useful intermediates in forming potent herbicides that demonstrate a broad spectrum of weed control. These compounds are disclosed, as are methods of forming and using these compounds.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 4, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Thomas Lyman Siddall, Joshua John Roth
  • Process for in-situ electrochemical oxidative generation and conversion of organosulfur compounds
    Patent number: 8871951
    Abstract: Hydrocarbon feedstocks are desulfurized by conversion of organosulfur compounds in a mixture of hydrocarbons into sulfoxides and/or sulfones. The oxidant used to promote oxidation of organosulfur-compounds is electrosynthesized in-situ.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: October 28, 2014
    Assignee: Saudi Arabian Oil Company
    Inventor: Emad Naji Al-Shafei
  • Process for the preparation of alditol acetals
    Patent number: 8871954
    Abstract: The present invention is directed to a process for the preparation of 1,3:2,4-bis (4-methylbenzylidene) sorbitol (MDBS) and 1,3:2,4-bis (4-dimethylbenzylidene) sorbitol (DMDBS) by dehydrocondensating an aldehyde and an alditol using a hydrophobic ionic liquid as an acid catalyst. The ionic liquid used in the accordance with the process of the present invention is a phosphonium ion based ionic liquid.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: October 28, 2014
    Assignee: Reliance Industries Limited
    Inventors: Pavankumar Aduri, Parasu Veera Uppara
  • Method for preparing adenine compound
    Patent number: 8865896
    Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: October 21, 2014
    Assignees: Astrazeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
  • Crystalline (6R,7R)-7-{2-(5-amino-[1,2,4] thiadiazol-3-yl)-2-[(Z)-trityloxyimino]-acetylamino}-3-[(R)-1?-tert-butoxycarbonyl-2-oxo-[1,3?]bipyrrolidinyl-(3E)-ylidenemethyl]-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid benzhydryl ester; its manufacture and use
    Patent number: 8865697
    Abstract: A solid DMSO solvate of a compound of formula (I) is described, which is a useful intermediate for preparing the broad spectrum antibiotics Ceftobiprole and Ceftobiprole Medocaril.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: October 21, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Marco Alpegiani, Walter Cabri, Markus Heubes, Davide Longoni, Michael Schleimer
  • Method for producing optically active fluorine-containing oxeten
    Patent number: 8859789
    Abstract: A method for producing an optically active fluorine-containing oxeten, the method being provided to include the steps of causing a fluorine-containing ?-ketoester and an internal alkyne to react with each other in the presence of a transition metal complex that has an optically active ligand.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: October 14, 2014
    Assignee: Tokyo Institute of Technology
    Inventors: Koichi Mikami, Kohsuke Aikawa, Yuta Hioki
  • Process for the manufacture of a 1,2-epoxide and a device for carrying out said process
    Patent number: 8859790
    Abstract: Apparatus and processes are provided for forming epoxide compounds. In one embodiment, a process for the manufacture of an epoxide is provided including adding an oxidant, a water-soluble manganese complex and a terminal olefin to form a multiphasic reaction mixture, reacting the terminal olefin with the oxidant in the multiphasic reaction mixture having at least one organic phase in the presence of the water-soluble manganese complex, separating the reaction mixture into the at least one organic phase and an aqueous phase, and reusing at least part of the aqueous phase. The invention is also related to a device for performing the above process.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: October 14, 2014
    Assignee: Momentive Specialty Chemicals Inc.
    Inventors: Prasad Muppa, Ron Postma, Bart Van Den Berg, Juergen Stock, Holger Wiederhold, Hans Rausch, Jorg Schallenberg, Stefan Bernhardt
  • Derivatives of N-acyl-N?-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes
    Patent number: 8853215
    Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: October 7, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Kevin Francis McGee, Jr.
  • Methods for the preparation of lapatinib and the salts thereof
    Patent number: 8853396
    Abstract: Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: October 7, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventor: Francesco Fontana
  • Phosphonates with reduced toxicity for treatment of viral infections
    Patent number: 8846643
    Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: September 30, 2014
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva