Patents Assigned to Theravance Biopharma R&D IP, LLC
  • Pyrimidine compound as JAK kinase inhibitor
    Patent number: 12172994
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: October 3, 2023
    Date of Patent: December 24, 2024
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell, Marta Dabros, Jerry Nzerem
  • Crystalline hydrate of a JAK inhibitor compound
    Patent number: 12122773
    Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
    Type: Grant
    Filed: May 31, 2023
    Date of Patent: October 22, 2024
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Gene Timothy Fass
  • Neprilysin inhibitors
    Patent number: 12016835
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z 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: November 18, 2022
    Date of Patent: June 25, 2024
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Neprilysin inhibitors
    Patent number: 11919888
    Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: February 23, 2023
    Date of Patent: March 5, 2024
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes
  • JAK inhibitors containing a 4-membered heterocyclic amide
    Patent number: 11878977
    Abstract: The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: August 10, 2022
    Date of Patent: January 23, 2024
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, Gary E. L. Brandt, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden, Melanie A. Kleinschek, Glenn D. Crater
  • Crystalline freebase forms of a biphenyl compound
    Patent number: 11858898
    Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
    Type: Grant
    Filed: May 19, 2023
    Date of Patent: January 2, 2024
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventor: Grahame Woollam
  • Neprilysin inhibitors
    Patent number: 11851443
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, 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: January 19, 2022
    Date of Patent: December 26, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Ester and carbonate pyrimidine compounds as JAK kinase inhibitors
    Patent number: 11845747
    Abstract: The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases and release an active metabolite in vivo. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory skin diseases and other diseases.
    Type: Grant
    Filed: September 27, 2021
    Date of Patent: December 19, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Philip A. Gerken, Jianhua Chao, Daniel D. Long
  • Pyrimidine compound as JAK kinase inhibitor
    Patent number: 11814377
    Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
    Type: Grant
    Filed: June 30, 2022
    Date of Patent: November 14, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Jennifer Kozak, Ryan Hudson, Marta Dabros, Jerry Nzerem
  • Formulation of a pan-JAK inhibitor
    Patent number: 11795180
    Abstract: The present disclosure relates to pharmaceutical compositions comprising (3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile), methods of use thereof, and methods of preparation.
    Type: Grant
    Filed: October 7, 2021
    Date of Patent: October 24, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Bernardus Joseph Nitert, Yvonne Rosiaux, Marian E. Van Der Veen, Nathan Schulpen, Jens Maes, Guido Verniest, Venkat R. Thalladi, Ai Ling Ching
  • Methods of treatment using a JAK inhibitor compound
    Patent number: 11786517
    Abstract: The invention relates to methods of treating ocular diseases and certain respiratory diseases using the compound 5-ethyl-2-fluoro-4-(3-(5-(1-methylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl)phenol or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: September 28, 2021
    Date of Patent: October 17, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melanie A. Kleinschek, Glenn D. Crater
  • Methods for treating Crohn's disease using 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile
    Patent number: 11780852
    Abstract: Disclosed are methods for treating Crohn's disease using a compound of the formula: or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 2021
    Date of Patent: October 10, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Ryan Hudson, Jennifer Kozak, Dante D. Podesto, Xiaojun Huang, Venkat R. Thalladi
  • ALK5 inhibitors
    Patent number: 11730720
    Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
    Type: Grant
    Filed: December 4, 2020
    Date of Patent: August 22, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Svitlana Kulyk, Christina Owens, Steven D. E. Sullivan, Jennifer Kozak, Adam D. Hughes
  • 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds
    Patent number: 11723900
    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: February 3, 2021
    Date of Patent: August 15, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Eric L. Stangeland
  • Crystalline (2S,4R)-5-(5?-chloro-2?-fluoro-[1,1?-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2- methylpentanoic acid and uses thereof
    Patent number: 11718591
    Abstract: In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I?) forms.
    Type: Grant
    Filed: December 14, 2021
    Date of Patent: August 8, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi, Gene Timothy Fass, Michael Simeone, R. Michael Baldwin, David L. Bourdet
  • JAK kinase inhibitor compounds for treatment of respiratory disease
    Patent number: 11718616
    Abstract: The invention provides compounds of formula (I): wherein X is and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 7, 2022
    Date of Patent: August 8, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, John R. Jacobsen, Anne-Marie Beausoleil, Gary E. L. Brandt, Melissa Fleury, Lan Jiang, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden, Pierre-Jean Colson, Gene Timothy Fass, Miroslav Rapta, Noah Benjamin, Marta Dabros, Venkat R. Thalladi
  • 5 to 7 membered heterocyclic amides as JAK inhibitors
    Patent number: 11713315
    Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.
    Type: Grant
    Filed: October 13, 2020
    Date of Patent: August 1, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, Cameron Smith, Corbin Thompson
  • Crystalline hydrate of a JAK inhibitor compound
    Patent number: 11702415
    Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
    Type: Grant
    Filed: March 1, 2021
    Date of Patent: July 18, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Gene Timothy Fass
  • Fused pyrimidine pyridinone compounds as JAK inhibitors
    Patent number: 11697648
    Abstract: The disclosure provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The disclosure also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat gastrointestinal inflammatory diseases.
    Type: Grant
    Filed: November 24, 2020
    Date of Patent: July 11, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Robert Murray McKinnell, Erik Fenster, Tom M. Lam, Diana Jin Wang, Anthony Francesco Palermo, Luke Boralsky, Breena Fraga
  • Crystalline freebase forms of a biphenyl compound
    Patent number: 11691948
    Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.
    Type: Grant
    Filed: April 15, 2021
    Date of Patent: July 4, 2023
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Grahame Woollam