Patents Assigned to Theravance, Inc.
  • 8-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20130158060
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: June 20, 2012
    Publication date: June 20, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • BIPHENYL DERIVATIVES
    Publication number: 20130150404
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthmas.
    Type: Application
    Filed: July 10, 2012
    Publication date: June 13, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Mathai Mammen, Sarah Dunham, Adam Hughes, Craig Husfeld, Eric Stangeland
  • 3-phenoxymethylpyrrolidine compounds
    Patent number: 8455665
    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: August 17, 2012
    Date of Patent: June 4, 2013
    Assignee: 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
    Patent number: 8455530
    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: Grant
    Filed: March 2, 2012
    Date of Patent: June 4, 2013
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Weijiang Zhang
  • DIAMIDE COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
    Publication number: 20130137665
    Abstract: This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and ?2 adrenergic receptor agonist activities. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compounds as bronchodilating agents to treat pulmonary disorders.
    Type: Application
    Filed: February 8, 2012
    Publication date: May 30, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Adam Hughes, Daniel Byun, Yan Chen, Melissa Fleury, John R. Jacobsen, Eric L. Stangeland, Richard D. Wilson, Rose Yen
  • Amidine-containing compounds useful as muscarinic receptor antagonists
    Patent number: 8450362
    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: July 11, 2012
    Date of Patent: May 28, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Cameron Smith
  • Neprilysin inhibitors
    Patent number: 8449890
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-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: May 28, 2013
    Assignee: Theravance, Inc.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • CRYSTALLINE FORMS OF A BIPHENYL COMPOUND
    Publication number: 20130125887
    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.
    Type: Application
    Filed: January 14, 2013
    Publication date: May 23, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Sabine Axt, Timothy J Church, Viengkham Malathong
  • METHODS FOR DETECTING SULFHYDRYL-CONTAINING COMPOUNDS IN A BIOLOGICAL TEST SAMPLE
    Publication number: 20130109046
    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: December 17, 2012
    Publication date: May 2, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Yuqin Dai, Donavon McConn, Huiyu Zhao
  • PROCESS FOR PREPARING AN INTERMEDIATE TO MU OPIOID RECEPTOR ANTAGONISTS
    Publication number: 20130079523
    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: Application
    Filed: July 18, 2012
    Publication date: March 28, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Pierre-Jean Colson, Ying Yu, Daniel D. Long, Ioanna Stergiades
  • 5-HTreceptor agonist compounds for treatment of cognitive disorders
    Patent number: 8404711
    Abstract: The invention provides methods for the treatment of cognitive disorders utilizing specific 5-HT4 receptor agonist compounds, in particular, methods utilizing these compounds in combination with other agents, specifically acetylcholinesterase inhibitors, for the treatment of Alzheimer's disease and other cognitive disorders.
    Type: Grant
    Filed: April 12, 2010
    Date of Patent: March 26, 2013
    Assignee: Theravance, Inc.
    Inventors: David Beattie, Fei Shen, Jacqueline A. M. Smith
  • CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND
    Publication number: 20130072515
    Abstract: The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionypamino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl) benzamide 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 mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: July 17, 2012
    Publication date: March 21, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Sean M. DALZIEL, Leticia M. PREZA, Miroslav RAPTA, Pierre-Jean COLSON
  • Crystalline alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid and methods for preparing thereof
    Patent number: 8399501
    Abstract: The invention provides a micronized 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.
    Type: Grant
    Filed: March 3, 2011
    Date of Patent: March 19, 2013
    Assignee: Theravance, Inc.
    Inventor: Paul R. Fatheree
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8399488
    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: January 11, 2012
    Date of Patent: March 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • CRYSTALLINE FORMS OF A 3-CARBOXYPROPYL-AMINOTETRALIN COMPOUND
    Publication number: 20130065916
    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: Application
    Filed: October 29, 2012
    Publication date: March 14, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Sean M. Dalziel, Miroslav Rapta
  • Dual-acting antihypertensive agents
    Patent number: 8394846
    Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I 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 a process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 12, 2013
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
  • Crystalline form of a 3-phenoxymethylpyrrolidine compound
    Patent number: 8383669
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. 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: March 20, 2012
    Date of Patent: February 26, 2013
    Assignee: Theravance, Inc.
    Inventor: Daisuke Roland Saito
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8377966
    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, 2012
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
  • Benzimidazole-carboxamide compounds as 5-HTreceptor agonists
    Patent number: 8377964
    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: June 9, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Roland Gendron, Lan Jiang, Seok-ki Choi, Daniel D. Long, Paul R. Fatheree, Daniel Marquess
  • Crystalline forms of a biphenyl compound
    Patent number: 8377965
    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.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J. Church