Patents Assigned to Theravance, Inc.
  • Amidoalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
    Patent number: 8518966
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula 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: January 31, 2011
    Date of Patent: August 27, 2013
    Assignee: Theravance, Inc.
    Inventors: Daniel D. Long, Daisuke Roland Saito, Priscilla M. Van Dyke, Lan Jiang, Timothy J. Church, John R. Jacobsen
  • Neprilysin inhibitors
    Patent number: 8513244
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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: May 18, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Adam D. Hughes
  • Dual-acting benzoimidazole antihypertensive agents
    Patent number: 8513432
    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: May 30, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • DUAL-ACTING ANTIHYPERTENSIVE AGENTS
    Publication number: 20130210874
    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: Application
    Filed: November 20, 2012
    Publication date: August 15, 2013
    Applicant: THERAVANCE, INC.
    Inventor: THERAVANCE, INC.
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8501776
    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: November 30, 2010
    Date of Patent: August 6, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Li Li, Mathai Mammen, YongQi Mu, Eric L. Stangeland
  • Dual-acting antihypertensive agents
    Patent number: 8501798
    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 19, 2012
    Date of Patent: August 6, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Serotonin reuptake inhibitors
    Patent number: 8501964
    Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: August 6, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric L. Stangeland, Lori Jean Van Orden, Daisuke Roland Saito
  • Aminotetralin compounds as mu opioid receptor antagonists
    Patent number: 8497287
    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: October 17, 2012
    Date of Patent: July 30, 2013
    Assignee: Theravance, Inc.
    Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
  • Quaternary ammonium compounds useful as muscarinic receptor antagonists
    Patent number: 8492407
    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: May 17, 2012
    Date of Patent: July 23, 2013
    Assignee: Theravance, Inc.
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
    Patent number: 8492399
    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: October 16, 2012
    Date of Patent: July 23, 2013
    Assignee: Theravance, Inc.
    Inventors: Michael R. Leadbetter, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Crystalline forms of a 3-carboxypropyl-aminotetralin compound
    Patent number: 8486958
    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.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: July 16, 2013
    Assignee: Theravance, Inc.
    Inventors: Sean M. Dalziel, Miroslav Rapta
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8487107
    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: January 25, 2010
    Date of Patent: July 16, 2013
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
  • 3-(PHENOXYPHENYLMETHYL)PYRROLIDINE COMPOUNDS
    Publication number: 20130178509
    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: Application
    Filed: June 27, 2012
    Publication date: July 11, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
  • Neprilysin inhibitors
    Patent number: 8481044
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: July 9, 2013
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
    Patent number: 8481549
    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 18, 2011
    Date of Patent: July 9, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds as mu opioid receptor antagonists
    Patent number: 8481563
    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: January 26, 2011
    Date of Patent: July 9, 2013
    Assignee: Theravance, Inc.
    Inventors: Daisuke Roland Saito, Daniel D. Long, Priscilla Van Dyke, Timothy J. Church, Lan Jiang, Bryan Frieman
  • BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20130172301
    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: Application
    Filed: August 23, 2012
    Publication date: July 4, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Crystalline form of a biphenyl compound
    Patent number: 8476299
    Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: July 2, 2013
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • Process for preparing an intermediate to mu opioid receptor antagonists
    Patent number: 8476440
    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 18, 2012
    Date of Patent: July 2, 2013
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
  • Serotonin reuptake inhibitors
    Patent number: 8471040
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin 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: October 10, 2011
    Date of Patent: June 25, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito