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:
April 30, 2008
Date of Patent:
June 21, 2011
Assignee:
Theravance, Inc.
Inventors:
Martin S. Linsell, John R. Jacobsen, Daisuke Roland Saito
Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
September 5, 2008
Date of Patent:
June 14, 2011
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
July 2, 2010
Date of Patent:
June 7, 2011
Assignee:
Theravance, Inc.
Inventors:
Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt 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:
August 26, 2008
Date of Patent:
May 24, 2011
Assignee:
Theravance, Inc.
Inventors:
Daisuke Roland Saito, Daniel D. Long, John R. Jacobsen
Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamideor a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
Type:
Grant
Filed:
February 27, 2008
Date of Patent:
May 17, 2011
Assignee:
Theravance, Inc.
Inventors:
Sean Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
Abstract: The invention provides an efficient method for preparing 3-endo-(8-azabicyclo[3.2.1]oct-3-yl)benzamide by hydrogenation, under controlled conditions, of an amino-protected 3-(8-azabicyclo[3.2.1]oct-2-en-3-yl)benzamide intermediate in which the amino-protecting group is removable by catalytic hydrogenation.
Type:
Grant
Filed:
July 15, 2008
Date of Patent:
April 26, 2011
Assignee:
Theravance, Inc.
Inventors:
Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
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:
March 22, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: This invention is directed to methods of administering an echinocandin antifungal agent in combination with a glycopeptide antibacterial agent having a substituent comprising at least about 8 carbon atoms. The invention is also directed to methods of using an echinocandin antifungal agent in combination with a specified glycopeptide antibacterial agent to treat fungal infections; and to compositions, kits and systems comprising an echinocandin antifungal agent and a specified glycopeptide antibacterial agent.
Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m are defined in the specification, or a pharmaceutically -acceptable salt 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:
August 26, 2008
Date of Patent:
March 8, 2011
Assignee:
Theravance, Inc,
Inventors:
Daisuke Roland Saito, Daniel D. Long, Priscilla Van Dyke, Timothy J. Church, Lan Jiang, Bryan Frieman
Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, and a are defined in the specification, or a pharmaceutically-acceptable salt 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:
August 26, 2008
Date of Patent:
March 8, 2011
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Daisuke Roland Saito, Priscilla Van Dyke, Lan Jiang, Tmothy J. Church, John R. Jacobsen
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:
October 13, 2009
Date of Patent:
March 1, 2011
Assignee:
Theravance, Inc.
Inventors:
Sean M. Dalziel, Kirsten M. Phizackerley
Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 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. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
July 23, 2009
Date of Patent:
February 15, 2011
Assignee:
Theravance, Inc.
Inventors:
Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
April 23, 2008
Date of Patent:
February 1, 2011
Assignee:
Theravance, Inc.
Inventors:
Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
Abstract: The invention relates to crystalline free base forms of biphenyl-2-ylcarbamic acid 1-[2-(4-{[(R)-2-(3-formylamino-4-hydroxyphenyl)-2-hydroxyethylamino]methyl}-2,5-dimethylphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also relates to pharmaceutical compositions containing or prepared from such crystalline forms; processes and intermediates useful for preparing such crystalline forms; and methods of using such crystalline forms to, for example, treat a pulmonary disorder.
Type:
Grant
Filed:
April 24, 2007
Date of Patent:
February 1, 2011
Assignee:
Theravance, Inc.
Inventors:
Jennifer Bolton, Robert S. Chao, Miroslav Rapta, Lisa Williams, Richard D. Wilson
Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
June 7, 2006
Date of Patent:
February 1, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Sarah Dunham, Adam Hughes, Craig Husfeld, Eric Stangeland, Yan Chen
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:
September 22, 2008
Date of Patent:
January 25, 2011
Assignee:
Theravance, Inc.
Inventors:
Adam A. Goldblum, Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Lan Jiang, Daniel D. Long, Daniel Marquess, S. Derek Turner
Abstract: This invention provides cephalosporin compounds and salts thereof. Such compounds are useful for preparing cross-linked glycopeptide-cephalosporin antibiotics.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
January 18, 2011
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, Daniel D. Long, Jason P. Chinn, Matthew B. Nodwell, Edmund J. Moran, James B. Aggen
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:
October 21, 2009
Date of Patent:
January 11, 2011
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, Li Li, Mathai Mammen, YongQi Mu, Eric L. Stangeland
Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
July 23, 2009
Date of Patent:
January 4, 2011
Assignee:
Theravance, Inc.
Inventors:
Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair