Patents Assigned to Roche Palo Alto LLC
  • Process for synthesis of phenoxy diaminopyrimidine derivatives
    Patent number: 8580960
    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: July 12, 2011
    Date of Patent: November 12, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
  • LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON
    Publication number: 20130261592
    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: May 23, 2013
    Publication date: October 3, 2013
    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
  • LIQUID PHARMACEUTICAL FORMULATIONS OF PALONOSETRON
    Publication number: 20130261149
    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: May 24, 2013
    Publication date: October 3, 2013
    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 Burton's tyrosine kinase
    Patent number: 8536166
    Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, 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-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 17, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
  • Inhibitors of JNK
    Patent number: 8536172
    Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y?, r, R1, R2, X, X1, X2, X3, and X4 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. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: September 17, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Leyi Gong, Xiaochun Han, Ferenc Makra, Wylie Solang Palmer, Lubica Raptova
  • 4'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF HCV RNA REPLICATION
    Publication number: 20130237491
    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: Application
    Filed: April 12, 2013
    Publication date: September 12, 2013
    Applicant: 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
  • Methods of using diaminopyrimidine as P2Xand P2X? receptor modulators for treatment of respiratory and gastrointestinal diseases
    Patent number: 8524725
    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: July 19, 2011
    Date of Patent: September 3, 2013
    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
  • METHODS OF USING DIAMINOPYRIMIDINE P2X3 AND P2X2/3 RECEPTOR MODULATORS FOR TREATMENT OF RESPIRATORY AND GASTROINTESTINAL DISEASES
    Publication number: 20130225570
    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: Application
    Filed: April 19, 2013
    Publication date: August 29, 2013
    Applicant: Roche Palo Alto LLC
    Inventor: Roche Palo Alto LLC
  • Liquid pharmaceutical formulations of palonosetron
    Patent number: 8518981
    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: April 14, 2011
    Date of Patent: August 27, 2013
    Assignees: Helsinn Healthcare SA, Roche Palo Alto LLC
    Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Andrew Miksztal, Thomas Malefyt, Kathleen Lee
  • Heteroaryl pyrrolidinyl and piperidinyl ketone derivatives and uses thereof
    Patent number: 8513425
    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: November 21, 2011
    Date of Patent: August 20, 2013
    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: 20130209397
    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: August 10, 2011
    Publication date: August 15, 2013
    Applicant: Roche Palo Alto LLC
    Inventors: Jim Li, Francisco Xavier Talamas
  • Thiazole and oxazole-substituted arylamides as P2Xand P2Xantagonists
    Patent number: 8501933
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb 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: July 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Quinoline inhibitors of hepatitis C virus polymerase
    Patent number: 8487103
    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: Grant
    Filed: August 18, 2011
    Date of Patent: July 16, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
  • Indole, indazole and benzimidazole arylamides as P2Xand P2Xantagonists
    Patent number: 8476457
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, Z, R1, R2, R3, R4 and R5 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: July 2, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Michael Patrick Dillon, Nancy Elisabeth Krauss
  • BENZOXAZINE DERIVATIVES AND USES THEREOF
    Publication number: 20130123251
    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: Application
    Filed: December 13, 2012
    Publication date: May 16, 2013
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
  • Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists
    Patent number: 8440708
    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: June 16, 2011
    Date of Patent: May 14, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists
    Patent number: 8440673
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, 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: May 14, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Dihydropyrimidone amides as P2X7 modulators
    Patent number: 8435990
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5, Ra and Rb 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: July 30, 2010
    Date of Patent: May 7, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 8426409
    Abstract: This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: wherein, variables Q, R, 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 17, 2009
    Date of Patent: April 23, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Rama K. Kondru, Yan Lou, Eric Brian Sjogren, Michael Soth
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 8426441
    Abstract: This application discloses novel imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives according to Formulae I-VI: wherein R, R?, R?, Q, X, and Y 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-VI and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: April 23, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Michael Soth