Patents Assigned to Roche Palo Alto LLC
  • Pyridines
    Patent number: 8415379
    Abstract: The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: April 9, 2013
    Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLC
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Pyridazines
    Patent number: 8410104
    Abstract: The present invention is concerned with isoxazole-pyridazines of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: April 2, 2013
    Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLC
    Inventors: Matthew C. Lucas, Andrew Thomas
  • Pyrimidinyl pyridone inhibitors of JNK
    Patent number: 8404695
    Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, wherein R1, R2, and R3 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: March 26, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Genevieve N. Boice, Leyi Gong, Kristen Lynn McCaleb, Wylie Solang Palmer
  • JNK modulators
    Patent number: 8399462
    Abstract: Compounds of formula I modulate JNK: wherein the variables are as defined herein.
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: March 19, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Leyi Gong, David Michael Goldstein, Xiaochun Han, Joan Heather Hogg, Wylie Solang Palmer, Lubica Raptova, Tania Silva, Parcharee Tivitmahaisoon, Teresa Alejandra Trejo-Martin, Christophe Michoud, Achyutharao Sidduri
  • Isoxazoles / O-pyridines with ethyl and ethenyl linker
    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
  • Heterocyclic antiviral compounds
    Patent number: 8383824
    Abstract: Compounds having the formula I wherein wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors with improved bioavailability. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: February 26, 2013
    Assignee: Roche Palo Alto LLC
    Inventor: Joshua Paul Gergely Taygerly
  • Benzoxazine derivatives and uses thereof
    Patent number: 8377931
    Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, Y, Z1, m, n, and p are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: February 19, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
  • Dihydropyridone amides as P2Xmodulators
    Patent number: 8372865
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: February 12, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Jacob Berger, Joan Marie Caroon, Nancy Elisabeth Krauss, Keith Adrian Murray Walker, Shu-Hai Zhao, Francisco Javier Lopez-Tapia
  • Tricyclic inhibitors of JAK
    Patent number: 8361962
    Abstract: The present invention relates to the use of novel compounds of Formulae I-II, wherein the variables R, X1, X2, X3, Y1, Y2, Y3, Z1, and Z2 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: January 29, 2013
    Assignee: Roche Palo Alto LLC
    Inventor: Roland Joseph Billedeau
  • Stable cell lines expressing hERG
    Patent number: 8349572
    Abstract: A stable eukaryotic cell line that expresses hERG and exhibits a stable current under electrophysiological test conditions is provided.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: January 8, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Paul Shartzer Dietrich, Bruce Koch, Heather Guthrie, Ulrich Andreas Gubler
  • Polymorphic forms of oseltamivir phosphate
    Patent number: 8334319
    Abstract: The present invention relates to polymorphic forms of (3R,4R,5S)-5-amino-4-acetylamino-3-(1-ethyl-propoxy)-cyclohex-1-ene-carboxylic acid ethyl ester phosphate, which is a potent inhibitor of viral neuraminidase.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: December 18, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Pierre Goldbach, Olaf Grassmann, Ines Sauer
  • Methods for treating retroviral infections
    Patent number: 8329755
    Abstract: The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein with at least one carrier, excipient or diluent.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: December 11, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Donald Roy Hirschfeld, Tania Silva, Zachary Kevin Sweeney, Harit Vora
  • Heterocyclic antiviral compounds
    Patent number: 8329712
    Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: December 11, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8324211
    Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: wherein, variables Q, R, X, Y1, Y2, Y3, Y4, n, and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: December 4, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth
  • Macrocyclic inhibitors of JAK
    Patent number: 8318764
    Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Alam Jahangir, Stephen M Lynch, Michael Soth, Hanbiao Yang
  • Tetrahydroquinoline indole derivatives and uses thereof
    Patent number: 8318770
    Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventor: Ryan Craig Schoenfeld
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8318719
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8299077
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: October 30, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Steven Berthel, Fariborz Firooznia, Daniel Fishlock, Jun-Bae Hong, Yan Lou, Matthew Lucas, Timothy D. Owens, Keshab Sarma, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
  • Heterocyclic antiviral compounds
    Patent number: 8293778
    Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
    Type: Grant
    Filed: February 20, 2010
    Date of Patent: October 23, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
  • Dihydropyridone amidesas P2Xmodulators
    Patent number: 8288552
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: October 16, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Dov Nitzan, Keith Adrian Murray Walker, Shu-Hai Zhao