Patents Examined by Patricia Morris
  • Patent number: 8440701
    Abstract: The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: May 14, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
  • Patent number: 8404723
    Abstract: The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
    Type: Grant
    Filed: September 8, 2007
    Date of Patent: March 26, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lars Barfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche
  • Patent number: 8394837
    Abstract: The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 12, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, James C. Barrow, Shaun R. Stauffer, Joseph P. Vacca, Keith P. Moore, Shawn J. Stachel, Mattahew G. Stanton
  • Patent number: 8389714
    Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt thereof, may be made by a process including a triflating step by which a ketone of formula (II) is converted into a triflate of formula (III) in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: March 5, 2013
    Assignee: BTG International Limited
    Inventor: Paul S Bury
  • Patent number: 8389550
    Abstract: The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceutical agents.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: March 5, 2013
    Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8378109
    Abstract: Contemplated compositions and methods are employed to bind in vitro and in vivo to an ?4?2 nicotinic acetylcholine receptor in a highly selective manner. Where such compounds are labeled, compositions and methods employing such compounds can be used for PET and SPECT analysis. Alternatively, and/or additionally contemplated compounds can be used as antagonists, partial agonists or agonists in the treatment of diseases or conditions associated with ?4??2 dysfunction.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: February 19, 2013
    Assignee: The Regents of the University of California
    Inventors: Jogeshwar Mukherjee, Ramaiah Pichika, Steven Potkin, Frances Leslie, Sankha Chattopadhyay
  • Patent number: 8378103
    Abstract: The invention is directed to improved processes for preparing Tiotropium bromide.
    Type: Grant
    Filed: January 4, 2010
    Date of Patent: February 19, 2013
    Assignee: Sicor, Inc.
    Inventors: Jonathan Busolli, Nicola Diulgheroff, Francesca Scarpitta, Roberta Volonte, Alessandro Pontiroli
  • Patent number: 8367832
    Abstract: The present invention provides novel crystalline forms of Nelfinavir mesylate, Form-A, Form-B, Form-C, Form-D and the process for their preparation without the use of any special equipment such as a spray drier, avoiding the use of highly flammable solvents such as ethers. The crystalline form can be tailored with the selection of the ante solvent and appropriate conditions for the process.
    Type: Grant
    Filed: August 23, 2004
    Date of Patent: February 5, 2013
    Assignee: Mylan Laboratories Limited
    Inventors: Chava Satyanarayana, Vasireddy Umamaheswara-Rao, Vellanki Siva Ram Prasad, Balusu Rajababu
  • Patent number: 8367706
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Altman, Matthew Christopher, Jonathan B. Grimm, Andrew Haidle, Kaleen Konrad, Jongwon Lim, Rachel N. MacCoss, Michelle Machacek, Ekundayo Osimboni, Ryan D. Otte, Tony Siu, Kerrie Spencer, Brandon Taoka, Paul Tempest, Kevin Wilson, Hyun Chong Woo, Jonathan Young, Anna Zabierek
  • Patent number: 8362259
    Abstract: There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: January 29, 2013
    Assignee: Lek Pharmaceuticals, D.D.
    Inventor: Renata Toplak Casar
  • Patent number: 8362260
    Abstract: The present invention relates to novel crystalline forms of Dexlansoprazole and a process for the preparation of amorphous Dexlansoprazole.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: January 29, 2013
    Assignee: Dipharma Francis S.r.l.
    Inventors: Chiara Vladiskovic, Gabriele Razzetti
  • Patent number: 8362258
    Abstract: The present invention is directed to a process for the catalytic oxidation of the thioether 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)methylthio)-1H-benzimidazole to its sulfoxide: 5-methoxy-2-((4-methoxy-3,5-dimethyl-2-pyridinyl) methyl)methylsulfinyl)-1H-benzimidazole comprising: reacting the thioether with: 1) a transition metal catalyst; and, 2) an oxygen source; wherein the thioether is oxidized to a sulfoxide and wherein one of either the R and S enantiomers is formed to an enantiomeric excess.
    Type: Grant
    Filed: July 7, 2009
    Date of Patent: January 29, 2013
    Assignee: Praktikatalyst Pharma LLC
    Inventors: Kenneth S. Wheelock, Louis A. Piccone
  • Patent number: 8362043
    Abstract: The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
    Type: Grant
    Filed: November 21, 2005
    Date of Patent: January 29, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Ronald Knegtel, Michael Mortimore, John R. Studley
  • Patent number: 8362261
    Abstract: The present invention relates to a process for preparing 1-pyridyl-substituted pyrazoles, comprising the reaction of acetyleneketones with pyridylhydrazine derivatives to give 1-pyridyl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-pyridyl-substituted trihalomethylpyrazoles, and the further processing thereof.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: January 29, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Sergii Pazenok, Norbert Lui, Harry Blaschke
  • Patent number: 8350045
    Abstract: A process for preparation of E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula-I, and acid addition salts thereof, said process comprising; dehydrating 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinopropan-1-ol of Formula III followed by adding a base solution to obtain a mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene, and washing said mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene with water to dissolve Z isomer and to obtain E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula I, which is substantially free from Z isomer.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: January 8, 2013
    Assignee: Hikal Limited
    Inventors: Rajender Pershad Gupta, Veerabhadra Swamy Hiremath, Raghavendra Arekal Vasanna, Vasantha Gowda Nekkilar
  • Patent number: 8349872
    Abstract: The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: January 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
  • Patent number: 8344143
    Abstract: The invention is directed to improved processes for preparing Tiotropium bromide.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: January 1, 2013
    Assignee: Sicor, Inc.
    Inventors: Jonathan Busolli, Nicola Diulgheroff, Francesca Scarpitta, Roberta Volonte, Alessandro Pontiroli
  • Patent number: 8344005
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.
    Type: Grant
    Filed: May 12, 2009
    Date of Patent: January 1, 2013
    Assignee: Glaxo Wellcome Manufacturing Pte Ltd
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 8344003
    Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 23, 2009
    Date of Patent: January 1, 2013
    Assignee: MSD K. K.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
  • Patent number: 8338588
    Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: December 25, 2012
    Assignee: BTG International Limited
    Inventor: Neil John Hunt