Abstract: The invention provides novel benzoimidazolone-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:
November 20, 2007
Date of Patent:
August 10, 2010
Assignee:
Theravance, Inc.
Inventors:
Roland Gendron, Seok-ki Choi, Paul R. Fatheree, Adam A. Goldblum, Daniel D. Long, Daniel Marquess, S. Derek Turner
Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
Type:
Grant
Filed:
May 13, 2009
Date of Patent:
August 10, 2010
Assignee:
Theravance, Inc.
Inventors:
Ioanna Stergiades, Edward Yost, Cristin Hubbard, Weijiang Zhang
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:
March 13, 2008
Date of Patent:
July 27, 2010
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 benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to 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:
May 24, 2006
Date of Patent:
July 20, 2010
Assignee:
Theravance, Inc.
Inventors:
Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
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: Disclosed are processes for preparing glycopeptide phosphonate derivatives having an amino-containing side chain. Several of the process steps are conducted in a single reaction vessel without isolation of intermediate reaction products, thereby generating less waste and improving the overall efficiency and yield of the process.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
June 1, 2010
Assignee:
Theravance, Inc.
Inventors:
Michael R. Leadbetter, Martin S. Linsell, Junning Lee, Jyanwei Liu
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:
June 12, 2006
Date of Patent:
June 1, 2010
Assignee:
Theravance, Inc
Inventors:
Yu-Hua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
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:
June 1, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide 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 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
Type:
Grant
Filed:
April 5, 2006
Date of Patent:
June 1, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
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, hadroxy, C1-4 alkyl, or C1-4 alkoxy; R2 is C3-4 alkyl, or C3-6cycloakyl; R3 is hydrogen or C1-3 alkyl: R4 is —S(O)2 R6 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:
April 6, 2005
Date of Patent:
June 1, 2010
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long
Abstract: Disclosed are compounds of the formula: or a trifluoroacetic acid salt thereof, wherein A, B and Fmoc are as defined herein. Such compounds are useful as synthetic intermediates for preparing glycopeptides antibiotics.
Type:
Grant
Filed:
October 24, 2007
Date of Patent:
May 25, 2010
Assignee:
Theravance, Inc.
Inventors:
J. Kevin Judice, Paul Ross Fatheree, Bernice M. T. Lam, Michael R. Leadbetter, Martin S. Linsell, YongQi Mu, Sean Gary Trapp, Guang Yang, Yan Zhu
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:
May 11, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, S. Derek Turner
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: Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
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:
August 26, 2008
Date of Patent:
April 6, 2010
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Lan Jiang, Daisuke Roland Saito, Priscilla Van Dyke
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:
March 30, 2010
Assignee:
Theravance, Inc.
Inventors:
YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
Abstract: This invention relates to compounds of formula I: wherein R1 and R2 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions and combinations comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compound to, for example, treat pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
March 18, 2009
Date of Patent:
March 30, 2010
Assignee:
Theravance, Inc.
Inventors:
Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
Abstract: The invention provides compounds of formula I: wherein a, b, c, d, f, W, Q, 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:
November 5, 2008
Date of Patent:
March 23, 2010
Assignee:
Theravance, Inc.
Inventors:
Yu-Hua Ji, Craig Husfeld, Mathai Mammen, YongQi Mu, Eric L. Stangeland
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:
February 4, 2008
Date of Patent:
March 9, 2010
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Adam A. Goldblum, Daniel D. Long
Abstract: The invention provides 8-azabicyclo[3.2.1 ]octyl intermediates useful for the preparation of 5-HT4 receptor agonist compounds. The invention also provides processes for the preparation of such useful intermediates.