Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra 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:
December 15, 2009
Date of Patent:
October 16, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Dov Nitzan, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 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:
October 9, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Chris Allen Broka, Ronald Charles Hawley
Abstract: The application discloses compounds of Formula I: wherein Q1, Q2, R1, R2, R3, and n are defined as described herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.
Abstract: This application discloses compounds of generic Formula I: or pharmaceutically acceptable salts thereof, wherein A, R1, R2, R3, R4, Q, X, Y, m, p, and q 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:
July 15, 2009
Date of Patent:
June 12, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Eun Kyung Lee, Ryan Craig Schoenfeld, Robert James Weikert
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 and R6 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:
August 18, 2009
Date of Patent:
June 5, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, R1, R2, R3, R4, R5 and R6 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:
December 15, 2009
Date of Patent:
April 24, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Jacob Berger, Christine E. Brotherton-Pleiss, Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 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:
December 14, 2009
Date of Patent:
April 10, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 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:
December 15, 2009
Date of Patent:
April 10, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Christine E. Brotherton-Pleiss, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Dov Nitzan, Keith Adrian Murray Walker
Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, 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 12, 2009
Date of Patent:
February 21, 2012
Assignee:
Roche Palo Alto LLP
Inventors:
Li Chen, Lichun Feng, Minmin Yang, Michael Patrick Dillon, Yingjie Lai
Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1 E, E?, D, Z and L are as defined herein.
Type:
Grant
Filed:
December 14, 2009
Date of Patent:
February 21, 2012
Assignee:
Roche Palo Alto LLP
Inventors:
Kieran Durkin, Lawrence Emerson Fisher, Arthur Meili, Michaelangelo Scalone, Xianqing Shi, Justin Vitale
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
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
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
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
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
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
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