Patents Examined by Janet Andres
  • Tri-, tetra-substituted-3-aminopyrrolidine derivative
    Patent number: 8476429
    Abstract: An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: July 2, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
  • Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
    Patent number: 8471029
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: June 25, 2013
    Assignee: Vertex Pharmaceutical Incorporated
    Inventors: Sneha G. Arekar, Steven C. Johnston, Mariusz Krawiec, Ales Medek, Praveen Mudunuri, Mark Jeffrey Sullivan
  • Substituted hydroxamic acids and uses thereof
    Patent number: 8471026
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 25, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Adamantyl compounds
    Patent number: 8471027
    Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: June 25, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Kevin Richard Guertin, Nancy-Ellen Haynes, Eric Mertz, Lida Qi, Yimin Qian, Nathan Robert Scott
  • Optically active cyclic alcohol compound
    Patent number: 8471028
    Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: June 25, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masaki Okamoto, Akira Sakuragi, Yoshikazu Mori, Muneki Kishida, Takanori Higashijima
  • Niacin prodrugs and deuterated versions thereof
    Patent number: 8471034
    Abstract: The invention relates to prodrugs of niacin and their use in pharmaceutical composition and therapeutic treatment of disease.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: June 25, 2013
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators
    Patent number: 8470852
    Abstract: The invention relates to substituted 2-amino-quinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: June 25, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Sven Kühnert, Gregor Bahrenberg, Dagmar Kaulartz, Achim Kless, Wolfgang Schröder
  • 5,6-bisaryl-2-pyridine-carboxamide derivatives, preparation thereof and therapeutic application thereof as urotensin II receptor antagonists
    Patent number: 8466292
    Abstract: The present invention is directed to compounds of the general formula: as well as pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: June 18, 2013
    Assignee: Sanofi
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
  • Process for preparing 2,2-difluoroethylamine derivatives by alkylation with 2,2-difluoroethyl-1-haloethanes
    Patent number: 8466293
    Abstract: Process for preparing 2,2-difluorethylamine derivatives of the general formula (III) in which A is an optionally substituted heterocycle as described in the description, by reacting a 2,2-difluoroethyl-1-haloethane compound of the general formula (I) in which Hal is Cl, Br or iodine, with an amine of the general formula (II) in which A is as defined above, optionally in the presence of a base.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: June 18, 2013
    Assignee: Bayer CropScience AG
    Inventors: Norbert Lui, Jens-Dietmar Heinrich, Wahed Ahmed Moradi, Christian Funke
  • Tricyclic heterocyclic compounds, compositions and methods of use thereof
    Patent number: 8461328
    Abstract: The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: June 11, 2013
    Assignee: Genentech, Inc.
    Inventors: Srinivasan Babu, Phillippe Bergeron, Peter Dragovich, Hazel Joan Dyke, Paul Gibbons, Stefan Gradl, Emily Hanan, Christopher Hurley, Tony Johnson, Michael Koehler, Janusz Kulagowski, Sharada Labadie, Joseph Lyssikatos, Rohan Mendonca, Rebecca Pulk, Stuart Ward, Bohdan Waszkowycz, Mark Zak
  • Resolution of (±)-methyl phenyl[4-[4-[[[4?(trifluoromethyl)-2-biphenylyl]carbonyl]amino]Phenyl]-1-piperidinyl]acetate
    Patent number: 8461341
    Abstract: The present invention relates to a resolution process of (±)-methyl phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate to isolate the MTP (microsomal triglyceride transfer protein) inhibitor methyl (2S)-phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate and an epimerisation procedure for racemizing methyl (2R)-phenyl[4-[4-[[[4?-(trifluoromethyl)-2-biphenylyl]carbonyl]amino]phenyl]-1-piperidinyl]acetate.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: June 11, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Alex Herman Copmans, Jérôme Albert Joseph Hoet, Albert Louis Anna Willemsens, Wouter Louis J Couck, Joannes Petrus Van Dun
  • Fused heterocyclic compound and use thereof
    Patent number: 8461181
    Abstract: A fused heterocyclic compound of formula (1): wherein, A1 and A2 represent a nitrogen atom or the like, R1, R2, R3 and R4 represent a halogen atom or the like, R2 and R3 represent a halogen atom or the like, R5 represents a C1-C6 chain hydrocarbon group optionally substituted with one or more halogen atoms, or the like, R6 and R7 represent a C1-C4 chain hydrocarbon group substituted with one or more halogen atoms, or the like, and n represents 0 or 1, has an excellent noxious arthropod controlling effect.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: June 11, 2013
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Masaki Takahashi, Mitsuhiko Iwakoshi, Hiroshi Ikegami
  • Herbicidal quinoline and 1,8-naphthyridine compounds
    Patent number: 8450243
    Abstract: The present invention relates to novel herbicidal oxopyridine and thionopyridine derivatives of Formula (I), or an agronomically acceptable salt of said compound wherein R1, R5, R6, R7, X1, X2 and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the oxopyridine derivatives, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: May 28, 2013
    Assignee: Syngenta Limited
    Inventors: Roger Salmon, Glynn Mitchell, James Alan Morris
  • Process for the preparation of cis-2-methylspiro (1,3-oxathiolane 5-3?) quinuclidine
    Patent number: 8450487
    Abstract: Methods are provided for making pharmaceutical-grade cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and pharmaceutically acceptable salts thereof by isomerizing racemic 2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine to cis-2-methylspiro(1,3-oxathiolane-5,3?)quinuclidine and subsequent purification of the C-MSOQ by salt formation with inexpensive and commercially available material such as sulfuric acid. Purification methods are disclosed which employ an organic solvent/water system and recrystallization with an organic solvent such as acetone.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: May 28, 2013
    Assignee: Apicore, LLC
    Inventors: Ravishanker Kovi, Jayaraman Kannapan, Talluri Buhshaiah Chowdari, Chirag Vasantlal Shah
  • Process for the preparation of [1-hydroxy-2-(3-pyridinyl)ethylidene] bisphosphonic acid and hemipentahydrate monosodium salt thereof
    Patent number: 8450488
    Abstract: The invention relates to a novel process for the preparation of [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid and hemipentahydrate monosodium salt thereof comprising (a) reacting an aqueous solution of 3-pyridyl acetic acid hydrochloride with phosphorus trichloride; (b) removing unreacted phosphorus trichloride; (c) adding water and hydrolyzing; (d) isolating crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid; (e) suspending said crystalline [1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid in water; (f) adding sodium hydroxide, filtering off, and washing; and (g) drying obtained hemipentahydrate monosodium salt of 1-hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonic acid.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 28, 2013
    Assignee: Zaklady Farmaceutyczne Polpharma S.A.
    Inventors: Leszek Dembkowski, Robert Rynkiewicz, Janusz Rachoń, Slawomir Makowiec, Witold Przychodzeń, Dariusz Witt
  • Process for beta-lactone production
    Patent number: 8445703
    Abstract: The present application provides a method for producing an beta-lactone product. The method includes the steps of: reacting an epoxide, a solvent with a carbonylation catalyst and carbon monoxide to produce a reaction stream comprising a beta-lactone then separating a portion of the beta-lactone in the reaction stream from the solvent and carbonylation catalyst to produce: i) a beta-lactone stream with the beta-lactone, and ii) a catalyst recycling stream including the carbonylation catalyst and the high boiling solvent; and adding the catalyst recycling stream to the feed stream.
    Type: Grant
    Filed: April 7, 2010
    Date of Patent: May 21, 2013
    Assignee: Novomer, Inc.
    Inventors: Scott D. Allen, Ronald R. Valente, Han Lee, Anna E. Cherian, Donald L. Bunning, Nye A. Clinton, Olan Stanley Fruchey, Bernard Duane Dombek
  • Pesticides
    Patent number: 8445689
    Abstract: Compounds having the following generic formula are disclosed.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: May 21, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette Vitale Brown, Ronald Ross, Jr., William C. Lo, Matthias S. Ober
  • Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin-5-HTreceptor
    Patent number: 8440694
    Abstract: The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X?, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: May 14, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean Colm Turner, Wilfried Braje, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer, Andrea Hager-Wernet
  • 4-benzylamino-1-carboxylacyl-piperidine derivatives as CETP inhibitors
    Patent number: 8440682
    Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: May 14, 2013
    Assignee: Novartis AG
    Inventors: Muneto Mogi, Ken Yamada, Kayo Yasoshima, Toshio Kawanami, Ichiro Umemura, Yuki Iwaki, Hongbo Qin, Hidetomo Imase
  • Process and intermediates for preparing integrase inhibitors
    Patent number: 8440831
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: May 14, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Steven Pfeiffer