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:
January 9, 2012
Date of Patent:
January 8, 2013
Assignee:
Theravance, Inc.
Inventors:
Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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:
June 22, 2012
Date of Patent:
January 8, 2013
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 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:
March 6, 2012
Date of Patent:
January 1, 2013
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 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:
May 10, 2012
Date of Patent:
December 25, 2012
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, 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:
November 17, 2011
Date of Patent:
December 25, 2012
Assignee:
Theravance, Inc.
Inventors:
Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
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:
November 12, 2009
Date of Patent:
December 11, 2012
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, YuHua Ji, Mathai Mammen, Eric L. Stangeland
Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.
Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 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:
December 19, 2011
Date of Patent:
November 27, 2012
Assignee:
Theravance, Inc.
Inventors:
Sean Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke
Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, 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:
December 19, 2011
Date of Patent:
November 20, 2012
Assignee:
Theravance, Inc.
Inventors:
Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
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.
Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds of Formula (I). The invention also provides pharmaceutical compositions comprising such compounds, the use such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. Wherein; R1 is hydrogen, halo, hydroxy, C1-4 alkyl, or C1-4 alkoxy; R2 is C3-4 alkyl, or C3-6cycloalkyl; R3 is hydrogen or C1-3 alkyl: R4 is S(O)2R6 or C(O)R7; R5 is hydrogen, C1-3alkyl, C2-3 alkyl substituted with —OH or C1-3 alkoxy, or —CH2-pyrydyl; R6 is C1-3 alkyl; or R5 and R6 taken together from C3-4 alkylenyl; and R7 is hydrogen, C1-3alkyl, or pyrydyl; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
Type:
Grant
Filed:
May 19, 2010
Date of Patent:
November 13, 2012
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-ki Choi, Adam A. Goldblum, Daniel Genov
Abstract: The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. 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:
November 13, 2009
Date of Patent:
November 6, 2012
Assignee:
Theravance, Inc.
Inventors:
Lori Jean Patterson, Eric L. Stangeland, Sheila Zipfel, Daniel D. Long
Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. 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.
Type:
Grant
Filed:
November 13, 2009
Date of Patent:
November 6, 2012
Assignee:
Theravance, Inc.
Inventors:
Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
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:
November 17, 2010
Date of Patent:
October 16, 2012
Assignee:
Theravance, Inc.
Inventors:
Sean M. Dalziel, Kirsten M. Phizackerley
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:
April 3, 2012
Date of Patent:
September 25, 2012
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: In one aspect, the invention relates to compounds of formula I: where 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 14, 2010
Date of Patent:
September 25, 2012
Assignee:
Theravance, Inc.
Inventors:
Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
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:
February 22, 2011
Date of Patent:
September 18, 2012
Assignee:
Theravance, Inc.
Inventors:
Daisuke Roland Saito, Daniel D. Long, John R. Jacobsen
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:
October 14, 2009
Date of Patent:
September 11, 2012
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Timothy J. Church, John R. Jacobsen, Lan Jiang, Daisuke Roland Saito, Ioanna Stergiades, Priscilla M. Van Dyke
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:
March 14, 2011
Date of Patent:
August 21, 2012
Assignee:
Theravance, Inc.
Inventors:
Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
Abstract: The invention relates to processes and intermediates for preparing compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors.