Abstract: Compounds having the formula I wherein wherein R1, R2, R3, R4, X1, X2, X3 and X4 and 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:
June 9, 2010
Date of Patent:
September 27, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
Abstract: The present invention relates to the use of novel pyrrolopyrazinyl urea derivatives of Formula I, wherein the variables R1, R2, R3, R4, and R5 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
Type:
Grant
Filed:
December 3, 2009
Date of Patent:
September 6, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Joe Timothy Bamberg, Johannes Cornelius Hermann, Remy Lemoine, Michael Soth
Abstract: Methods for treating respiratory and gastrointestinal 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 thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
Type:
Grant
Filed:
August 25, 2006
Date of Patent:
August 30, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Anthony P. D. W. Ford, Ronald Charles Hawley, Alam Jahangir, Amy Geraldine Moore, Daniel Warren Parish
Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.
Type:
Grant
Filed:
October 4, 2007
Date of Patent:
August 23, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
Abstract: An antibody binding to IL-17 characterized by binding to the same IL-17 epitope to which monoclonal antibody 3C1 binds, and being of human IgG1 isotype modified in the hinge region at amino acid position 216-240, preferably at amino acid position 220-240, between CH1 and CH2 and/or in the second inter-domain region at amino acid position 327-331 between CH2 and CH3 has advantageous properties for the treatment of inflammatory diseases.
Type:
Grant
Filed:
September 29, 2009
Date of Patent:
August 23, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Johannes Auer, Nikolaos Dimoudis, Guy Georges, Petra Hanke, Hendrik Knoetgen, Ekkehard Moessner, Claire Louise Langrish
Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein Ar is indolyl, indazolyl or dihydroindolyl, and R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using the compounds in the treatment of depressive, anxiolytic and other disorders associated with inhibition of the reuptake of norepinephrine, serotonin, and dopamine, and methods of preparing the compounds.
Type:
Grant
Filed:
February 12, 2009
Date of Patent:
August 16, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
David Scott Carter, Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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 R1, R2, R3, R4, R5a, R5b, R6a, R6b and X 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:
December 13, 2007
Date of Patent:
August 16, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Denis John Kestesz, Christine E. Brotherton-Pleiss, Minmin Yang
Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 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:
December 17, 2008
Date of Patent:
August 2, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
Type:
Grant
Filed:
January 26, 2010
Date of Patent:
July 19, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
Abstract: Compounds of the formula: wherein R1, R2, Ar1, Ar2, and n are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.
Type:
Grant
Filed:
October 1, 2008
Date of Patent:
July 19, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Daisy Joe Du Bois, Todd Richard Elworthy, Hans Maag, Sunil Sahdeo
Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
Abstract: The current invention is related to a conjugate comprising one or more antifusogenic peptides and an anti-CCR5 antibody (mAb CCR5) characterized in that one to eight antifusogenic peptides are each conjugated to one terminus of the heavy and/or light chains of the anti-CCR5 antibody and to the pharmaceutical use of the conjugate.
Type:
Grant
Filed:
August 17, 2007
Date of Patent:
May 31, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Michael Brandt, Stephan Fischer, Erhard Kopetzki, Suryanarayana Sankuratri, Ralf Schumacher
Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd and n 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:
December 14, 2010
Publication date:
May 26, 2011
Applicant:
Roche Palo Alto LLC
Inventors:
RYAN CRAIG SCHOENFELD, Leanna Renee Staben, Francisco Xavier Talamas
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.
Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
Abstract: Compounds of formula I, wherein R1, R2, R3, X 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:
June 20, 2008
Date of Patent:
May 24, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.
Abstract: This application discloses pyridine and pyrimidine compounds according to formula I wherein R1, R2, R3, R4, R5, X1 and A are 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 and at least one carrier, diluent or excipient.
Type:
Grant
Filed:
October 23, 2008
Date of Patent:
May 17, 2011
Assignee:
Roche Palo Alto LLC
Inventors:
Nolan James Dewdney, Rama K. Kondru, Yan Lou, Michael Soth, Tobias Gabriel
Abstract: The invention relates to novel metathesis catalysts of the formula a process for making the same and their use in metathesis reactions such as ring closing or cross metathesis. The invention further relates to a process for the manufacture of a macrocyclic compound of formula VII which have the potential to be useful as HCV protease inhibitors.