Patents Represented by Attorney Jeffrey A. Hagenah

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  • Dual-acting imidazole antihypertensive agents
    Patent number: 8158659
    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: December 21, 2010
    Date of Patent: April 17, 2012
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Crystalline form of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid
    Patent number: 8153675
    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: November 11, 2010
    Date of Patent: April 10, 2012
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Weijiang Zhang
  • Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
    Patent number: 8153686
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n 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: March 31, 2009
    Date of Patent: April 10, 2012
    Assignee: Theravance, Inc.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Benzimidazole-carboxamide compounds as 5-HTreceptor agonists
    Patent number: 8143279
    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. The invention further relates to crystalline forms of a compound of formula (I).
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: March 27, 2012
    Assignee: Theravance, Inc.
    Inventors: Robert Murray McKinnell, Daniel D. Long, Sean Dalziel, Kirsten M. Phizackerley
  • Method of using compounds having ?adrenergic receptor agonist and muscarinic receptor antagonist activity
    Patent number: 8143277
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m 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. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: March 27, 2012
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, YuHua Ji
  • Dual-acting antihypertensive agents
    Patent number: 8143298
    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: June 30, 2010
    Date of Patent: March 27, 2012
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
  • Diamide compounds having muscarinic receptor antagonist and ?adrenergic receptor agonist activity
    Patent number: 8138345
    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: Grant
    Filed: April 16, 2010
    Date of Patent: March 20, 2012
    Assignee: Theravance, Inc.
    Inventors: Adam Hughes, Daniel Byun, Yan Chen, Melissa Fleury, John R. Jacobsen, Eric L. Stangeland, Richard D. Wilson, Rose Yen
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8133905
    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: December 17, 2009
    Date of Patent: March 13, 2012
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
  • Dialkylphenyl compounds having ?adrenergic receptor agonist and muscarinic receptor antagonist activity
    Patent number: 8134006
    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: February 5, 2010
    Date of Patent: March 13, 2012
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Adam D. Hughes, Craig Husfeld, Mathai Mammen, Miroslav Rapta
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8124627
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, 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: October 26, 2009
    Date of Patent: February 28, 2012
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Viengkham Malathong
  • Biphenyl compounds useful as muscarinic receptor antagonists
    Patent number: 8119796
    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: July 29, 2011
    Date of Patent: February 21, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Mathai Mammen, Craig Husfeld, Li Li, YongQi Mu, Aaron Kushner, Eric Stangeland, Trevor Mischki, Adam Hughes, Sarah Dunham
  • Dual-acting pyrazole antihypertensive agents
    Patent number: 8119634
    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 4, 2011
    Date of Patent: February 21, 2012
    Assignee: Theravance, Inc.
    Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
  • Dual-acting antihypertensive agents
    Patent number: 8106082
    Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, 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 process and intermediates for preparing such compounds.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: January 31, 2012
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Vivek Sasikumar
  • 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
    Patent number: 8106232
    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 10, 2008
    Date of Patent: January 31, 2012
    Assignee: Theravance, Inc.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Crystalline forms of a 3-carboxypropyl-aminotetralin compound
    Patent number: 8101794
    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 9, 2009
    Date of Patent: January 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Sean M. Dalziel, Miroslav Rapta
  • Crystalline form of a biphenyl compound
    Patent number: 8101766
    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: February 11, 2009
    Date of Patent: January 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • Glycopeptide phosphonate derivatives
    Patent number: 8101575
    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: Grant
    Filed: March 2, 2010
    Date of Patent: January 24, 2012
    Assignee: Theravance, Inc.
    Inventor: Michael R. Leadbetter
  • Aminotetralin compounds as mu opioid receptor antagonists
    Patent number: 8101791
    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 10, 2008
    Date of Patent: January 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
  • Process for preparing glycopeptide phosphonate derivatives
    Patent number: 8093354
    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: April 13, 2010
    Date of Patent: January 10, 2012
    Assignee: Theravance, Inc.
    Inventors: Michael R. Leadbetter, Martin S. Linsell, Junning Lee, Jyanwei Liu
  • Cross-linked glycopeptide-cephalosporin antibiotics
    Patent number: 8084417
    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: June 19, 2008
    Date of Patent: December 27, 2011
    Assignee: Theravance, Inc.
    Inventors: Daniel Marquess, Martin S. Linsell, S. Derek Turner, Sean G. Trapp, Daniel D. Long, Paul R. Fatheree