Patents Assigned to Roche Palo Alto LLC
  • 4?-substituted nucleoside derivatives as inhibitors of HCV RNA replication
    Patent number: 7915232
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof which inhibit HCV polymerase and are useful for treating a patient suffering from a HCV infection and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: March 29, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Nobuo Shimma, Takuo Tsukuda
  • HETEROCYCLIC ANTIVIRAL COMPOUNDS
    Publication number: 20110070190
    Abstract: The invention discloses 1-N-substituted-6-(hetero)aryl-1H-thieno[3,2-d]pyrimidin-4-one derivatives of formula wherein R1, R2, R3 and R4 are as defined herein that inhibit Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: September 24, 2010
    Publication date: March 24, 2011
    Applicant: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Robert Than Hendricks, Hans Maag, David Bernard Smith, Jutta Wanner
  • Process for the preparation of a macrocycle
    Patent number: 7910728
    Abstract: The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: March 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Stefan Hildbrand, Kurt Puentener, Michelangelo Scalone
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 7906540
    Abstract: Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: March 15, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Zachary Kevin Sweeney, Michael Welch
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 7906509
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-III: wherein, variables 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 containing compounds of Formulae I-III and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: March 15, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
  • Assays for measuring phosphate modification enzyme activity
    Patent number: 7901901
    Abstract: The present invention relates to assays that can measure the activity of enzymes that catalyze phosphate modifications, such as kinases, phosphatases, cyclases and phosphodiesterases. The assays can also be used to identify and screen for substances that modulate the activity of kinases, phosphatases, cyclases and phosphodiesterases.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: March 8, 2011
    Assignee: Roche Palo Alto LLC
    Inventor: Qing-Fen Gan
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 7902197
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: March 8, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Todd Richard Elworthy, Robert Than Hendricks, Rama K. Kondru, Yan Lou, Timothy D. Owens, Michael Soth, Hanbiao Yang
  • Pharmaceutical composition and process
    Patent number: 7893037
    Abstract: The present invention relates to a method of forming granules of (2R,3S,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-2-azido-3,4-bis-iso-butyryloxy-tetrahydro-furan-2-ylmethyl isobutyrate; hydrochloride salt (I), comprising mixing I, with a granulating amount of a granulating liquid, and a polyethylene glycol (PEG)/polypropylene glycol (PPG) block copolymer as a binder and solubility enhancer to form wet granules which are then dried to remove the granulating liquid.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: February 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Kondamraj Birudaraj, Michael Thomas Brandl, Shridhar Hegde, Felix Sana, Dimitrios Stefanidis
  • Process for preparing triazolones
    Patent number: 7893276
    Abstract: The present process provides a improved method for the preparation of alkylsulfanyl substituted triazoles 2 which are useful intermediates in a new process for the preparation of triazolones 20.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: February 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Gary M. Lee, Jiang Zhu
  • Anti-OX40L antibodies
    Patent number: 7868141
    Abstract: This invention relates to anti-OX40L antibodies and, in particular, to anti-OX40L antibodies and variants thereof that contain a Fc part derived from human origin and do not bind complement factor C1q. These antibodies have new and inventive properties causing a benefit for a patient suffering from inflammatory diseases.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: January 11, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joseph Endl, Elsie M. Eugui, Maria Elena Fuentes, Yvo Graus, Aran Frank Labrijn, Martin Lanzendoerfer, Paul Parren, Frank Rebers, Ralf Schumacher, Stefan Seeber, Jan Van De Winkel, Martine Van Vugt
  • Propionamide compounds as antiinflammatory agents
    Patent number: 7868031
    Abstract: The present invention relates to propionamide compounds of formula I for use as antiinflammatory agents: wherein R1, R2 and R3 are as defined herein and pharmaceutically acceptable salts thereof. The invention also relates to methods of using the compounds of formula I and pharmaceutical compositions comprising the compounds of formula I.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: January 11, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Leyi Gong, Counde O'Yang, Yun-chou Tan
  • 3-amino-1-arylpropyl indoles as monoamine reuptake inhibitors
    Patent number: 7863305
    Abstract: Compounds of formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: January 4, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova, Deborah Carol Reuter, Karin Ann Stein, Robert Weikert
  • Diaminopyrimidines as P2Xand P2Xantagonists
    Patent number: 7858632
    Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
    Type: Grant
    Filed: March 3, 2005
    Date of Patent: December 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
  • Imidazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 7858654
    Abstract: Compounds of the formula I: wherein R1 is optionally substituted imidazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: December 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Scintillation proximity assay for measuring polymerase activity
    Patent number: 7851156
    Abstract: The present invention provides for methods of assaying the activity of a polymerase enzyme by using a Scintillation Proximity Assay (SPA) without the need of primers modified with affinity tags. The methods of the present invention can be practiced with any number of RNA and DNA polymerase enzymes.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: December 14, 2010
    Assignee: Roche Palo Alto LLC
    Inventor: Qing-Fen Gan
  • Process for the preparation of macrocyclic compounds
    Patent number: 7847106
    Abstract: The present invention relates to a new process for the preparation of tripeptides of formula I wherein R1 is an amino protecting group and X is a halogen atom and wherein the tipeptide contains two olefinic moieties suitably disposed to undergo an intramolecular olefin metathesis reaction and produce macrocyclic tripeptides useful for the manufacture of macrocyclic HCV protease inhibitors.
    Type: Grant
    Filed: April 24, 2008
    Date of Patent: December 7, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Francois Gantz, Helmut Stahr
  • Method for the recombinant expression of a polypeptide
    Patent number: 7807409
    Abstract: A method for the recombinant production of a heterologous polypeptide in a eukaryotic host cell is described. The host cell comprises an expression plasmid, whereby the expression plasmid comprises in a 5? to 3? direction a) a promoter, b) a nucleic acid encoding a first polypeptide, whose amino acid sequence is selected from Table 1 depending on the first two amino acids of the second polypeptide, c) a nucleic acid encoding a second polypeptide comprising a nucleic acid encoding a heterologous polypeptide, a nucleic acid encoding a linker, and a nucleic acid encoding an immunoglobulin fragment, and d) a 3? untranslated region comprising a polyadenylation signal. Further a plasmid and a kit are described.
    Type: Grant
    Filed: October 19, 2006
    Date of Patent: October 5, 2010
    Assignee: Roche Palo Alto LLC
    Inventor: Erhard Kopetzki
  • Antibodies against IL-13 receptor alpha1 and uses thereof
    Patent number: 7807158
    Abstract: The instant specification discloses an antibody binding to IL-13R?1, inhibiting IL-13 bioactivity and comprising a variable heavy and a variable light chain, characterized in that the variable heavy chain amino acid sequence CDR3 of this antibody is selected from the group consisting of the heavy chain CDR3 sequences of SEQ ID NO: 1, 3, 5, 7 or 9, and this antibody is useful in the treatment of asthma and allergic diseases.
    Type: Grant
    Filed: January 3, 2006
    Date of Patent: October 5, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Josef Endl, Maria Elena Fuentes, Yvo Graus, Adelbert Grossmann, Sebastian Neumann, Paul Parren, Frank Rebers, Joerg Thomas Regula, Ralf Schumacher, Stefan Seeber, Jan Olaf Stracke, Kay-Gunnar Stubenrauch, Jan Van De Winkel, Martine Van Vugt, Sandra Vereecken-Verploegen
  • Method for screening human intestinal Npt2B modulatory agents
    Patent number: 7803562
    Abstract: A novel human sodium phosphate cotransporter expressed on the apical surface of intestinal epithelial cells (huNpt2B) and polypeptides related thereto, as well as nucleic acid compositions encoding the same, are provided. The subject polypeptides and nucleic acid compositions find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications. Also provided are methods of inhibiting Npt2B activity in a host and methods of treating disease conditions associated with Npt2B activity.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: September 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Paul David Cannon, Suryanarayana Sankuratri
  • 3-amino-1-arylpropyl indoles and AZA-substituted indoles and uses thereof
    Patent number: 7803830
    Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: October 8, 2008
    Date of Patent: September 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert