Patents Examined by Joseph K. McKane
  • Patent number: 8389720
    Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: March 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
  • Patent number: 8383643
    Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: February 26, 2013
    Assignee: Merck Canada Inc.
    Inventors: Jean-Philippe Leclerc, Chun-Sing Li, Oscar Miguel Moradei
  • Patent number: 8383650
    Abstract: The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.
    Type: Grant
    Filed: June 25, 2008
    Date of Patent: February 26, 2013
    Assignee: Novartis AG
    Inventors: Fumiaki Yokokawa, Takeru Ehara, Shimpei Kawakami, Osamu Irie, Masaki Suzuki, Yuko Hitomi, Atsushi Toyao
  • Patent number: 8383619
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopro
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: February 26, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Martyn Frederickson, Marian Williams
  • Patent number: 8383659
    Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: February 26, 2013
    Assignee: Novartis AG
    Inventors: Steve Nanchen, Noëlle Gauvry, Thomas Goebel
  • Patent number: 8377942
    Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: February 19, 2013
    Assignee: Novartis AG
    Inventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
  • Patent number: 8372874
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse 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: September 22, 2009
    Date of Patent: February 12, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Monika Ermann
  • Patent number: 8367863
    Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: February 5, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Gideon Shapiro, Richard Chesworth
  • Patent number: 8367836
    Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: February 5, 2013
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Ying-zi Xu, Shendong Yuan, David Wone, Andrei Konradi
  • Patent number: 8367665
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 5, 2013
    Assignee: Karo Bio AB
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Patent number: 8362039
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse 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: August 25, 2011
    Date of Patent: January 29, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • Patent number: 8362057
    Abstract: The invention relates to the compounds of the general formula (I): in which A, D, R, R1 and X are as defined in the description, to a process for the preparation thereof and to the therapeutic use thereof in the treatment of pathologies associated with insulin resistance syndrome.
    Type: Grant
    Filed: July 7, 2006
    Date of Patent: January 29, 2013
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Gérard Moinet, Gérard Botton, Annick Arbellot de Vacqueur
  • Patent number: 8362066
    Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.
    Type: Grant
    Filed: November 19, 2007
    Date of Patent: January 29, 2013
    Assignee: Treventis Corporation
    Inventors: Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
  • Patent number: 8362002
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Grant
    Filed: March 15, 2011
    Date of Patent: January 29, 2013
    Assignee: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 8362279
    Abstract: A process for the preparation of pure Duloxetine hydrochloride comprises the steps of: a) reacting 1-(thiophen-2-yl)ethanone with dimethylamine hydrochloride, b) purifying the component in a solvent, c) reducing the component with an alkali metal borohydride, d) resolving the compound with a chiral acid, and treating the obtained compound with weak inorganic base, e) reacting the compound to give Duloxetine oxalate salt and f) converting the Duloxetine salt into its hydrochloride salt. Further the purifications of the obtained compound and of two intermediate products are described.
    Type: Grant
    Filed: January 4, 2007
    Date of Patent: January 29, 2013
    Assignee: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Muppa Kishore Kumar, Srinivasan Thirumalai Rajan, Durgadas Shyla Prasad
  • Patent number: 8357684
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 22, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
  • Patent number: 8354400
    Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: January 15, 2013
    Assignee: Eisai R&D Co., Ltd.
    Inventors: Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
  • Patent number: 8354436
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: January 15, 2013
    Assignee: 4SC Discovery GmbH
    Inventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
  • Patent number: 8349899
    Abstract: Embodiments of the present invention comprises a compound of formula I or its enantiomer, diastereomer, stereoisomer or its pharmaceutically acceptable salt, methods of use and methods of synthesis.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: January 8, 2013
    Assignee: Arrowhead Center, Inc.
    Inventors: Jeffrey Arterburn, Charles Shuster
  • Patent number: 8349871
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse 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: September 21, 2011
    Date of Patent: January 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi