Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
November 19, 2007
Date of Patent:
February 16, 2010
Assignee:
Theravance, Inc.
Inventors:
Robert Murray McKinnell, Edmund J. Moran
Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
February 9, 2010
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
August 24, 2007
Date of Patent:
February 2, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
August 24, 2007
Date of Patent:
January 19, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
January 5, 2010
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, Yu-Hua Ji, Mathai Mammen, Eric L. Stangeland
Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.
Type:
Grant
Filed:
January 30, 2008
Date of Patent:
December 29, 2009
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
December 15, 2009
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
Abstract: The invention provides compounds of formula I: wherein a, b, c, d, n, R1, R2, R3, R6, R7, W, and A are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
December 8, 2009
Assignee:
Theravance, Inc.
Inventors:
Yu-Hua Ji, Craig Husfeld, Li Li, Mathai Mammen, YongQi Mu, Eric L. Stangeland
Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
February 28, 2007
Date of Patent:
November 24, 2009
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Timothy J. Church, John R. Jacobsen, Lan Jiang, Daisuke Roland Saito, Ioanna Stergiades, Priscilla M. Van Dyke, Sean Dalziel, Leticia Maria Preza
Abstract: The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention also provides pharmaceutical compositions comprising the crystalline compound, methods of using the compound to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing crystalline forms of the compound.
Type:
Grant
Filed:
May 30, 2007
Date of Patent:
November 24, 2009
Assignee:
Theravance, Inc.
Inventors:
Sean M. Dalziel, Kirsten M. Phizackerley
Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
January 11, 2005
Date of Patent:
November 24, 2009
Assignee:
Theravance, Inc.
Inventors:
Robert M. McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke R. Saito
Abstract: This invention is directed to compounds of formula I: wherein R1-R5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.
Type:
Grant
Filed:
January 30, 2008
Date of Patent:
November 10, 2009
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Adam Hughes, Yu-hua Ji, Li Li, Weijiang Zhang
Abstract: Oncokinase fusion polypeptides associated with hyperproliferative disorders and the polynucleotides encoding for such fusion polypeptides are provided. The fusion polypeptides have a C-terminal tyrosine kinase domain fused to an N-terminal domain that is not normally fused to the C-terminal tyrosine kinase domain and they possess constitutively activated tyrosine kinase activity. Also provided are methods for detecting and identifying the fusion polypeptides and polynucleotides and methods of diagnosing disease conditions associated with the fusion polypeptides and polynucleotides. In addition, screening assays for identifying agents useful for treating disease conditions associated with such fusion polypeptides and polynucleotides are provided. Furthermore, methods of treating disease conditions associated with the presence of the fusion polypeptides are provided.
Abstract: This invention provides cross-linked glycopeptides—cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
August 24, 2007
Date of Patent:
October 13, 2009
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
June 29, 2007
Date of Patent:
September 22, 2009
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
July 19, 2007
Date of Patent:
September 8, 2009
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: Oncokinase fusion polypeptides associated with hyperproliferative disorders and the polynucleotides encoding for such fusion polypeptides are provided. The fusion polypeptides have a C-terminal tyrosine kinase domain fused to an N-terminal domain that is not normally fused to the C-terminal tyrosine kinase domain and they possess constitutively activated tyrosine kinase activity. Also provided are methods for detecting and identifying the fusion polypeptides and polynucleotides and methods of diagnosing disease conditions associated with the fusion polypeptides and polynucleotides. In addition, screening assays for identifying agents useful for treating disease conditions associated with such fusion polypeptides and polynucleotides are provided. Furthermore, methods of treating disease conditions associated with the presence of the fusion polypeptides are provided.
Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides combinations of such compounds and other therapeutic agents, pharmaceutical compositions comprising such compounds and combinations, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
May 22, 2007
Date of Patent:
September 1, 2009
Assignee:
Theravance, Inc.
Inventors:
Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
Abstract: Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)-piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.
Type:
Grant
Filed:
October 27, 2005
Date of Patent:
August 11, 2009
Assignee:
Theravance, Inc.
Inventors:
Matthew J Peterson, Junning Lee, Richard J Lee, Weijiang Zhang
Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4,R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
August 15, 2005
Date of Patent:
August 4, 2009
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji