Patents Assigned to Theravance, Inc.
  • Publication number: 20140329845
    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: March 4, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Publication number: 20140288112
    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: January 15, 2014
    Publication date: September 25, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20140288033
    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: March 19, 2014
    Publication date: September 25, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Sabine Axt, Timothy J. Church
  • Publication number: 20140274877
    Abstract: The present invention relates to a compound of formula I: wherein x is in the range of from about 1 to about 2. 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 a bacterial infection.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 18, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Weijiang Zhang, Ronnie Cheung, Dimitar Filipov, Jack Green, Junning Lee
  • Publication number: 20140275554
    Abstract: The invention relates to a crystalline form of a triethylamine salt of (2Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(3-N-tert-butoxycarbonylaminopropoxyimino)acetic acid. The invention also relates to processes and intermediates for preparing the crystalline form. The crystalline form is useful as an intermediate for preparing cross-linked glycopeptide-cephalosporin antibiotics.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 18, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Weijiang Zhang, Michael R. Tracey, Junning Lee
  • Publication number: 20140256702
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R5 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: Application
    Filed: March 4, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
  • Publication number: 20140256769
    Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide 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 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: January 8, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
  • Publication number: 20140243536
    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: Application
    Filed: November 26, 2013
    Publication date: August 28, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20140235864
    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 asthma.
    Type: Application
    Filed: November 22, 2013
    Publication date: August 21, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Mathai Mammen, Adam Hughes, Yan Chen
  • Publication number: 20140194426
    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: October 24, 2013
    Publication date: July 10, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • Publication number: 20140171397
    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: September 11, 2013
    Publication date: June 19, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Patent number: 8754225
    Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: June 17, 2014
    Assignee: Theravance, Inc.
    Inventor: Pierre-Jean Colson
  • Patent number: 8754223
    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: June 5, 2013
    Date of Patent: June 17, 2014
    Assignee: Theravance, Inc.
    Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
  • Publication number: 20140163063
    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: October 1, 2013
    Publication date: June 12, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Patent number: 8735625
    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 31, 2013
    Date of Patent: May 27, 2014
    Assignee: Theravance, Inc.
    Inventors: Seok-ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
  • Patent number: 8729119
    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: May 22, 2013
    Date of Patent: May 20, 2014
    Assignee: Theravance, Inc.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20140135333
    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 16, 2014
    Publication date: May 15, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8716313
    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: January 14, 2013
    Date of Patent: May 6, 2014
    Assignee: Theravance, Inc.
    Inventors: Sabine Axt, Timothy J Church
  • Publication number: 20140121385
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Application
    Filed: January 7, 2014
    Publication date: May 1, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Publication number: 20140121378
    Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.
    Type: Application
    Filed: November 26, 2013
    Publication date: May 1, 2014
    Applicant: THERAVANCE, INC.
    Inventor: Pierre-Jean Colson