Patents Assigned to Roche Palo Alto LLC
  • FRET-based binding assay
    Patent number: 8153390
    Abstract: The present invention provides for an assay that identifies kinase inhibitors by employing fluorescence resonance energy transfer in a competition binding approach.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: April 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: James Michael Bradshaw, Joyce Karen Kwan, Alden Er Hong Ling, David Shaw
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8124604
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, 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-IV and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: February 28, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Pyrrolopyrazine kinase inhibitors
    Patent number: 8119636
    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: February 21, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, David Bernard Smith
  • Process for the preparation of a macrocycle
    Patent number: 8106187
    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: August 7, 2009
    Date of Patent: January 31, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Michelangelo Scalone, Helmut Stahr
  • Process for synthesis of tritiated and deuterated thiorphan and acetorphan
    Patent number: 8101665
    Abstract: Methods for preparing tritium or deuterium labeled thiorphan comprising reacting a compound of formula j wherein m is from 1 to 5 and X is halo, with Z2 wherein Z is tritium or deuterium, in the presence of a catalyst, to form a compound of formula k wherein n is from 1 to 5, provided that n is less than or equal to m.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: January 24, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Mohammand R. Masjedizadeh, Shao-Yong Wu
  • HETEROCYCLIC ANTIVIRAL COMPOUNDS
    Publication number: 20120009144
    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: Application
    Filed: July 6, 2011
    Publication date: January 12, 2012
    Applicant: Roche Palo Alto LLC
    Inventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
  • Tetralin and indane derivatives and uses thereof
    Patent number: 8093424
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: January 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Aminopiperidinyl derivatives and uses thereof
    Patent number: 8093285
    Abstract: This application discloses aminopiperidinyl compounds of generic Formulae I-II: or pharmaceutically acceptable salts thereof, wherein m, r, Q1, Q2, Q3, R, Ra, R1, R2a, R2b, and R3 are defined as described herein, useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: January 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Oxazolone and pyrrolidinone-substituted pryidine amides as P2Xand P2Xantagonists
    Patent number: 8093275
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: January 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Pyrrolidinyl and piperidinyl ketone derivatives and uses thereof
    Patent number: 8084623
    Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: December 27, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
  • HETEROCYCLIC ANTIVIRAL COMPOUNDS
    Publication number: 20110300103
    Abstract: Method for treating an HCV infection and inhibiting HCV replication with a compound of formula I wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined herein
    Type: Application
    Filed: August 18, 2011
    Publication date: December 8, 2011
    Applicant: Roche Palo Alto LLC
    Inventors: Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
  • 4?-substituted nucleoside derivatives as inhibitors of HCV RNA replication
    Patent number: 8071567
    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 and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: December 6, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Heterocyclic antiviral compounds
    Patent number: 8071797
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 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: February 12, 2009
    Date of Patent: December 6, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Sharada Shenvi Labadie, Clara Jeou Jen Lin, Francisco Xavier Talamas, Robert James Weikert
  • Heterocyclic antiviral compounds
    Patent number: 8067442
    Abstract: Compounds having the formula I wherein R1, R2a, R2b, R2c, R3, Y and p are as defined herein and C2-C3 is a single or double bond 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: September 25, 2009
    Date of Patent: November 29, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Elbert Chin, Jim Li, Francisco Xavier Talamas, Beihan Wang
  • Heterocyclic antiviral compounds
    Patent number: 8063072
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 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: September 21, 2010
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Javier de Vincente Fidalgo, Ryan Craig Schoenfeld, Francisco Xavier Talamas
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 8063064
    Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A2 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Wylie Solang Palmer, Zachary Kevin Sweeney
  • Polymorphs of acyl sulfonamides
    Patent number: 8063103
    Abstract: The application discloses novel polymorphic crystalline forms of 2-[4-Bromo-3-(3-chloro-5-cyano-phenoxy)-2-fluoro-phenyl]-N-(2-chloro-4-propionylsulfamoyl-phenyl)-acetamide, sodium salt (Ib) with improved stability and physical properties which facilitate manufacturing, handling and formulating for treatment or prophylaxis of HIV mediated diseases, AIDS or ARC, in monotherapy or in combination therapy.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: James Prentice Davidson, Fei Pang, Margaret Wong, Michael Martin
  • Heterocyclic antiviral compounds
    Patent number: 8063028
    Abstract: Compounds of formula I, wherein R1, R2, R3, X1, X2 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: December 22, 2008
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Roland Joseph Billedeau, Zachary Kevin Sweeney
  • Tetrazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 8048905
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: November 1, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Non-nucleoside reverse transcriptase inhibitors
    Patent number: 8026362
    Abstract: Compounds of formula I, wherein R1, X1, X2 and A, 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: May 30, 2008
    Date of Patent: September 27, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joshua Kennedy-Smith, Zachary Kevin Sweeney, Jeffrey Wu