Patents Assigned to Theravance, Inc.
  • 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
    Patent number: 8318765
    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
  • Aminotetralin compounds as mu opioid receptor antagonists
    Patent number: 8314128
    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
  • Cross-linked glycopeptide-cephalosporin antibiotics
    Patent number: 8314217
    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: December 8, 2010
    Date of Patent: November 20, 2012
    Assignee: Theravance, Inc.
    Inventor: Martin S. Linsell
  • Quinolinone-carboxamide compounds as 5-HTreceptor agonists
    Patent number: 8309575
    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
  • GLYCOPEPTIDE PHOSPHONATE DERIVATIVES
    Publication number: 20120283195
    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.
    Type: Application
    Filed: December 16, 2011
    Publication date: November 8, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Michael R. Leadbetter, Martin S. Linsell
  • CRYSTALLINE FORM OF A BIPHENYL COMPOUND
    Publication number: 20120283289
    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: Application
    Filed: December 16, 2011
    Publication date: November 8, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds
    Patent number: 8304432
    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
  • Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
    Patent number: 8304433
    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
  • AMIDINE-CONTAINING COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
    Publication number: 20120277250
    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: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
  • PROCESS FOR PREPARING 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS
    Publication number: 20120277438
    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.
    Type: Application
    Filed: July 10, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Miroslav Rapta
  • DUAL-ACTING ANTIHYPERTENSIVE AGENTS
    Publication number: 20120264752
    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: Application
    Filed: June 22, 2012
    Publication date: October 18, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • METHODS FOR DETECTING SULFHYDRYL-CONTAINING COMPOUNDS IN A BIOLOGICAL TEST SAMPLE
    Publication number: 20120264223
    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.
    Type: Application
    Filed: June 27, 2012
    Publication date: October 18, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
  • QUINOLINONE-CARBOXAMIDE COMPOUNDS AS 5-HT4 RECEPTOR AGONISTS
    Publication number: 20120264779
    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: Application
    Filed: March 1, 2012
    Publication date: October 18, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Crystalline form of a benzimidazole-carboxamide medicinal compound
    Patent number: 8288550
    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
  • DUAL-ACTING ANTIHYPERTENSIVE AGENTS
    Publication number: 20120258992
    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: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • DUAL-ACTING PYRAZOLE ANTIHYPERTENSIVE AGENTS
    Publication number: 20120259113
    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: Application
    Filed: January 9, 2012
    Publication date: October 11, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
  • 3-phenoxymethylpyrrolidine compounds
    Patent number: 8273786
    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
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8273894
    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
  • DUAL-ACTING BENZOIMIDAZOLE ANTIHYPERTENSIVE AGENTS
    Publication number: 20120238611
    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: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Disubstituted alkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists
    Patent number: 8268863
    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