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)benzamide or 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:
April 6, 2011
Date of Patent:
August 21, 2012
Assignee:
Theravance, Inc.
Inventors:
Sean M. Dalziel, Leticia M. Preza, Miroslav Rapta, Pierre-Jean Colson
Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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:
January 4, 2011
Date of Patent:
August 14, 2012
Assignee:
Theravance, Inc.
Inventors:
Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
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.
Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to 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:
August 5, 2011
Date of Patent:
August 14, 2012
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu
Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.
Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, 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. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
August 7, 2012
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Vivek Sasikumar
Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, 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:
July 26, 2011
Date of Patent:
August 7, 2012
Assignee:
Theravance, Inc.
Inventors:
Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.
Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar 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:
June 22, 2011
Date of Patent:
July 24, 2012
Assignee:
Theravance, Inc.
Inventors:
Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W 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.
Abstract: The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2?, 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. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
Type:
Grant
Filed:
December 8, 2008
Date of Patent:
July 3, 2012
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
Abstract: The invention provides heteroarylene substituted 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, A, 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:
February 11, 2010
Date of Patent:
July 3, 2012
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Lan Jiang, Daisuke Roland Saito, Priscilla Van Dyke
Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q 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:
April 23, 2008
Date of Patent:
June 19, 2012
Assignee:
Theravance, Inc.
Inventors:
Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
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 9, 2011
Date of Patent:
June 12, 2012
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.
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:
September 7, 2011
Date of Patent:
May 8, 2012
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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 15, 2010
Date of Patent:
April 24, 2012
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Adam A. Goldblum, Daniel Genov
Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
Abstract: Disclosed are pharmaceutical compositions containing a cyclodextrin and a therapeutically effective amount of a glycopeptide antibiotic or a salt thereof. Also disclosed are methods of treating a bacterial disease in a mammal by administering such pharmaceutical compositions.
Type:
Grant
Filed:
April 29, 2009
Date of Patent:
April 17, 2012
Assignee:
Theravance, Inc.
Inventors:
J. Kevin Judice, Jeng-Pyng Shaw, YongQi Mu, Michael W. Conner, John L. Pace