Patents Assigned to Theravance, Inc.
  • Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists
    Patent number: 8378121
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e 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: October 6, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • AMINOTETRALIN COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20130040965
    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: Application
    Filed: October 17, 2012
    Publication date: February 14, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
  • Dual-acting oxazole antihypertensive agents
    Patent number: 8372984
    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: July 14, 2010
    Date of Patent: February 12, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • 3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20130035510
    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: Application
    Filed: October 16, 2012
    Publication date: February 7, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Michael R. Leadbetter, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
    Publication number: 20130030185
    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: Application
    Filed: October 1, 2012
    Publication date: January 31, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS
    Publication number: 20130030020
    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: Application
    Filed: September 28, 2012
    Publication date: January 31, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Lori Jean Patterson, Eric L. Stangeland, Sheila Zipfel, Daniel D. Long
  • Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid
    Patent number: 8362060
    Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: January 29, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul R. Fatheree, Venkat R. Thalladi
  • Methods for detecting sulfhydryl-containing compounds in a biological test sample
    Patent number: 8362061
    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: Grant
    Filed: June 27, 2012
    Date of Patent: January 29, 2013
    Assignee: Theravance, Inc.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhou
  • Dual-acting antihypertensive agents
    Patent number: 8349875
    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
  • Dual-acting pyrazole antihypertensive agents
    Patent number: 8350027
    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
  • Dual-acting imidazole antihypertensive agents
    Patent number: 8344013
    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
  • Guanidine-containing compounds useful as muscarinic receptor antagonists
    Patent number: 8338424
    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
  • Dual-acting antihypertensive agents
    Patent number: 8338418
    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
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8329911
    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
  • NEPRILYSIN INHIBITORS
    Publication number: 20120309724
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 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: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • NEPRILYSIN INHIBITORS
    Publication number: 20120308587
    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: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Adam D. Hughes
  • NEPRILYSIN INHIBITORS
    Publication number: 20120308588
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 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: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • 3-PHENOXYMETHYLPYRROLIDINE COMPOUNDS
    Publication number: 20120309985
    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: Application
    Filed: August 17, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric STANGELAND, Jane SCHMIDT, Daisuke Roland SAITO, Adam HUGHES, Lori Jean PATTERSON
  • CRYSTALLINE FORM OF AN ALKOXYIMIDAZOL-1-YLMETHYL BIPHENYL CARBOXYLIC ACID
    Publication number: 20120309805
    Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.
    Type: Application
    Filed: March 2, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Robert S. Chao, Weijiang Zhang
  • Crystalline forms of a 3-carboxypropyl-aminotetralin compound
    Patent number: 8324236
    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: December 19, 2011
    Date of Patent: December 4, 2012
    Assignee: Theravance, Inc.
    Inventors: Sean M. Dalziel, Miroslav Rapta