Patents by Inventor Miroslav Rapta

Miroslav Rapta has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 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
  • CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
    Publication number: 20230201181
    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: February 28, 2023
    Publication date: June 29, 2023
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • (2R,4R)-5-(5?-chloro-2?-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid
    Patent number: 11642332
    Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
    Type: Grant
    Filed: May 14, 2021
    Date of Patent: May 9, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
  • Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
    Patent number: 11596624
    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: Grant
    Filed: February 5, 2021
    Date of Patent: March 7, 2023
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • JAK KINASE INHIBITOR COMPOUNDS FOR TREATMENT OF RESPIRATORY DISEASE
    Publication number: 20220306624
    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: Application
    Filed: March 7, 2022
    Publication date: September 29, 2022
    Applicant: 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
  • 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
    Publication number: 20220242836
    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: Application
    Filed: December 14, 2021
    Publication date: August 4, 2022
    Applicant: 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
  • PYRAZOLO AND TRIAZOLO BICYCLIC COMPOUNDS AS JAK KINASE INHIBITORS
    Publication number: 20220119369
    Abstract: The invention 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 invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: February 22, 2021
    Publication date: April 21, 2022
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Robert Murray McKinnell, Erik Fenster, Tom M. Lam, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
  • 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: 11230536
    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: July 14, 2020
    Date of Patent: January 25, 2022
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi
  • (2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID
    Publication number: 20210401808
    Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
    Type: Application
    Filed: May 14, 2021
    Publication date: December 30, 2021
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
  • CRYSTALLINE ALK5 INHIBITORS AND USES THEREOF
    Publication number: 20210387983
    Abstract: The present disclosure provides crystalline forms of activin receptor-like kinase 5 (ALK5) inhibitors. Also disclosed are pharmaceutical compositions comprising the crystalline forms, methods of using the crystalline forms to modulate the activity of ALK5 and methods of treating disorders mediated by ALK5 using the crystalline forms.
    Type: Application
    Filed: June 9, 2021
    Publication date: December 16, 2021
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Alec Brozell, Marta Dabros, Jing Fu, Miroslav Rapta
  • CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
    Publication number: 20210290608
    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: February 5, 2021
    Publication date: September 23, 2021
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • (2R,4R)-5-(5?-chloro-2?-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid
    Patent number: 11033533
    Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
    Type: Grant
    Filed: December 16, 2019
    Date of Patent: June 15, 2021
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
  • Pyrazolo and triazolo bicyclic compounds as JAK kinase inhibitors
    Patent number: 10968205
    Abstract: The invention 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 invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 19, 2019
    Date of Patent: April 6, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Robert Murray McKinnell, Erik Fenster, Tom M. Lam, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
  • Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
    Patent number: 10946006
    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: Grant
    Filed: January 16, 2020
    Date of Patent: March 16, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • 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
    Publication number: 20210061776
    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: Application
    Filed: July 14, 2020
    Publication date: March 4, 2021
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi
  • CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND
    Publication number: 20200316047
    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: January 16, 2020
    Publication date: October 8, 2020
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • (2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID
    Publication number: 20200281900
    Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
    Type: Application
    Filed: December 16, 2019
    Publication date: September 10, 2020
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
  • 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: 10752599
    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: September 25, 2019
    Date of Patent: August 25, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury, Miroslav Rapta, Venkat R. Thalladi, Gene Timothy Fass, Michael Simeone
  • PYRAZOLO AND TRIAZOLO BICYCLIC COMPOUNDS AS JAK KINASE INHIBITORS
    Publication number: 20200216423
    Abstract: The invention 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 invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 19, 2019
    Publication date: July 9, 2020
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: ROBERT MURRAY MCKINNELL, ERIK FENSTER, TOM M. LAM, JERRY NZEREM, MARTA DABROS, VENKAT R. THALLADI, MIROSLAV RAPTA