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 18, 2010
Date of Patent:
December 20, 2011
Assignee:
Theravance, Inc.
Inventors:
Seok-ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.
Type:
Grant
Filed:
March 6, 2008
Date of Patent:
December 20, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Richard Wilson, Sarah Dunham, Adam Hughes, Craig Husfeld, Yu-Hua Ji, Li Li, Trevor Mischki, Ioanna Stergiades, David Oare
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, 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.
Type:
Grant
Filed:
November 3, 2010
Date of Patent:
November 29, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Eric L. Stangeland, Aaron Kushner, Craig Husfeld
Abstract: This invention provides methods of using compounds of formula Ib below to treat pulmonary disorders. wherein: R4 is hydrogen or (1-4C)alkyl; q is 0, 1, or 2; R5 is independently selected from halo, (1-4C)alkyl, and (1-4C)alkoxy, wherein each alkyl and alkoxy group is optionally substituted with from 1 to 3 fluoro substituents; R7 is hydrogen or (1-4C)alkyl; or a pharmaceuticallly acceptable salt thereof.
Type:
Grant
Filed:
February 10, 2011
Date of Patent:
November 8, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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 indazole-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:
January 19, 2010
Date of Patent:
October 25, 2011
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Adam A. Goldblum, Daniel D. Long, S. Derek Turner, Jyanwei Liu
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:
June 14, 2010
Date of Patent:
October 11, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula: —Ra—Y—Rb—(Z)x where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Abstract: This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.
Type:
Grant
Filed:
October 17, 2007
Date of Patent:
October 4, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, David Oare, Junning Lee, Weijiang Zhang
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 5, 2007
Date of Patent:
September 13, 2011
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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:
December 12, 2008
Date of Patent:
September 13, 2011
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu
Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 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 14, 2010
Date of Patent:
September 6, 2011
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
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:
April 23, 2008
Date of Patent:
September 6, 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: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z 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 and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Abstract: The invention provides novel indazole-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:
July 23, 2010
Date of Patent:
August 23, 2011
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Roland Gendron, Adam A. Goldblum, Daniel D. Long, Daniel Marquess, S. Derek Turner, Seok-Ki Choi
Abstract: Disclosed are hydrochloride salts of telavancin having a chloride ion content of from about 2.4 wt. % to about 4.8 wt. %. The disclosed salts have improved stability during storage at ambient temperatures compared to other hydrochloride salts. Also disclosed are processes for preparing such salts.
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 12, 2010
Date of Patent:
August 9, 2011
Assignee:
Theravance, Inc.
Inventors:
Eric Strangeland, Daisuke Roland Saito, Adam Hughes, Jane Schmidt, Priscilla Van Dyke, Lori Jean Patterson
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:
October 6, 2009
Date of Patent:
August 9, 2011
Assignee:
Theravance, Inc.
Inventors:
Robert Murray McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke Roland Saito
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:
April 28, 2009
Date of Patent:
August 2, 2011
Assignee:
Theravance, Inc.
Inventors:
Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-[2-({3-[2-(4-hydroxybenzylamino)ethylcarbamoyl]benzoyl}methylamino)ethyl]piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase (Form I or II), a salt such as a hemiedisylate salt or a heminapadisylate salt, or a solvate of a salt such as a heminapadisylate methanolate or a heminapadisylate ethanolate. 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.
Type:
Grant
Filed:
March 8, 2007
Date of Patent:
July 5, 2011
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, Yu-Hua Ji, Leticia Maria Preza