Patents Assigned to Roche Palo Alto LLC
  • [1,2,4]triazolo[3,4-C][1,4]oxazines as P2X7 modulators
    Patent number: 8871760
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 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: September 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
  • Isoxazolo-pyridine derivatives
    Patent number: 8846719
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: September 30, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Diaminopyrimidines as P2Xand P2Xantagonists
    Patent number: 8846705
    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: December 8, 2010
    Date of Patent: September 30, 2014
    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
  • Tetrazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 8841336
    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: September 22, 2011
    Date of Patent: September 23, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8822457
    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: September 11, 2013
    Date of Patent: September 2, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Oxazolone and pyrrolidinone-substituted biphenyls as P2Xand P2Xantagonists
    Patent number: 8809402
    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: December 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20140194413
    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: Application
    Filed: September 11, 2013
    Publication date: July 10, 2014
    Applicant: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • 1,2-pyridazines, 1,6-pyridazines and pyrimidines
    Patent number: 8748434
    Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: June 10, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Henrietta Dehmlow, Shawn David Erickson, Patrizio Mattei, Hans Richter
  • Heterocyclic antiviral compounds
    Patent number: 8734777
    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: August 10, 2011
    Date of Patent: May 27, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Francisco Xavier Talamas
  • Therapeutic composition
    Patent number: 8735345
    Abstract: Embodiments disclosed in the present application relate to a composition that can include a hepatitis C viral polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof and a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof. Additional embodiments disclosed relate to methods for treating a disease condition such as a hepatitis C virus infection, liver fibrosis and/or impaired liver function with a hepatitis C viral polymerase inhibitor, or pharmaceutically acceptable salt or prodrug thereof and a hepatitis C viral protease inhibitor, or pharmaceutically acceptable salt or prodrug thereof.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: May 27, 2014
    Assignees: Hoffmann la Roche Inc., Pharmasset, Inc., Roche Palo Alto LLC
    Inventors: Steven B. Porter, Williamson Ziegler Bradford, Patrick F. Smith, Ellen S. Yetzer, Abel De La Rosa, Michael D. Rogers, William T. Symonds
  • Liquid pharmaceutical formulations of palonosetron
    Patent number: 8729094
    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.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: May 20, 2014
    Assignees: Helsinn Healthcare SA, Roche Palo Alto LLC
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee
  • Triazole compounds II
    Patent number: 8697696
    Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 15, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Stephen Deems Gabriel, Andrew Thomas
  • LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON
    Publication number: 20140097114
    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.
    Type: Application
    Filed: November 4, 2013
    Publication date: April 10, 2014
    Applicants: Roche Palo Alto LLC, Helsinn Healthcare S.A.
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee, Carmine Panuccio
  • PROCESS FOR SYNTHESIS OF PHENOXY DIAMINOPYRIMIDINE DERIVATIVES
    Publication number: 20140045871
    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: Application
    Filed: October 14, 2013
    Publication date: February 13, 2014
    Applicant: Roche Palo Alto LLC
    Inventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
  • 4?-substituted nucleoside derivatives as inhibitors of HCV RNA replication
    Patent number: 8648054
    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: April 12, 2013
    Date of Patent: February 11, 2014
    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
  • LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON
    Publication number: 20140039000
    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.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 6, 2014
    Applicants: Roche Palo Alto LLC, Helsinn Healthcare S.A.
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M. Lee
  • Inhibitors of JNK
    Patent number: 8642601
    Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof, wherein R5 is a group of formula (a) or (b): and wherein m, n, p, q, X, Y, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: February 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Humberto Bartolome Arzeno, Lubov K. Filonova, David Michael Goldstein, Leyi Gong, Bradley E. Loe, Erin M. O'Brien, Wylie Solang Palmer, David Mark Rotstein, Tania M. Silva, Yun-Chou Tan
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8618098
    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 26, 2012
    Date of Patent: December 31, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Liquid pharmaceutical formulations of palonosetron
    Patent number: 8598219
    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.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: December 3, 2013
    Assignees: Helsinn Healthcare SA, Roche Palo Alto LLC
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee, Carmine Panuccio
  • Liquid pharmaceutical formulations of palonosetron
    Patent number: 8598218
    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.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: December 3, 2013
    Assignees: Helsinn Healthcare SA, Roche Palo Alto LLC
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee