Patents by Inventor Bradley E. Loe

Bradley E. Loe has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 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
  • 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
  • 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
  • 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
  • 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
  • Publication number: 20120129845
    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: January 26, 2012
    Publication date: May 24, 2012
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • 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
  • Publication number: 20110301171
    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: Application
    Filed: June 2, 2011
    Publication date: December 8, 2011
    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
  • Publication number: 20110105479
    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: January 10, 2011
    Publication date: May 5, 2011
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Publication number: 20110071143
    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: Application
    Filed: September 15, 2010
    Publication date: March 24, 2011
    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
  • 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
  • Patent number: 7902194
    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: June 24, 2009
    Date of Patent: March 8, 2011
    Assignee: Roche Palo Alto
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Publication number: 20100099659
    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: Application
    Filed: December 11, 2009
    Publication date: April 22, 2010
    Inventors: Joshua Kennedy-Smith, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel Mclntosh, Timothy D. Owens, Michael Soth, Zachary Kevin Sweeney, Joshua Paul Gergely Taygerly
  • Publication number: 20090318448
    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: June 24, 2009
    Publication date: December 24, 2009
    Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
  • Patent number: 5716954
    Abstract: Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;R.sup.1 is hydrogen, lower alkyl, aryl, aralkyl, heterocyclo, heterocyclo lower-alkyl, heteroaryl, or heteroaralkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from hydrogen, lower alkyl, halo, carboxy, alkoxycarbonyl, carbamoyl, lower-alkyl carbonyl, halocarbonyl, thiomethyl, trifluoromethyl, cyano or nitro;or a pharmaceutically acceptable ester, ether or salt thereof, have been found to be useful as an anti-inflammatory, antasthmatic, immunosuppressive, anti-allograft rejection, anti-graft-vs-host rejection, autoimmune disease or analgetic agent(s).
    Type: Grant
    Filed: January 5, 1995
    Date of Patent: February 10, 1998
    Assignee: Syntex U.S.A. Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe, Bruce H. Devens, Robert Alvarez, Michael G. Martin
  • Patent number: 5466697
    Abstract: The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; andR.sub.2 is aryl; or a pharmaceutically acceptable salt or N-oxide thereof are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), bronchodilation agents, anti-autoimmune agents or analgetic agents.
    Type: Grant
    Filed: July 13, 1994
    Date of Patent: November 14, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Bradley E. Loe