Patents by Inventor Diane E. Carrera

Diane E. Carrera 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).

  • Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto
    Patent number: 11999749
    Abstract: A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N?,N?-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
    Type: Grant
    Filed: June 28, 2022
    Date of Patent: June 4, 2024
    Assignees: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Francis Gosselin, Stefan G. Koenig, Eduardo V. Mercado-Marin, Andreas Stumpf, Daniel Zell, Haiming Zhang, Stephan Bachmann, Diane E. Carrera, Michael E. Dalziel, Yonghui Ge, Jie Zhang, Raphael Bigler, Laure Elizabeth Simone Finet, Regis Jean Georges Mondiere, Yuki Nakagawa
  • SYNTHESIS OF A BIS-MESYLATE SALT OF 4-AMINO-N-(1-((3-CHLORO-2-FLUOROPHENYL)AMINO)-6-METHYLISOQUINOLIN-5-YL)THIENO[3,2-D]PYRIMIDINE-7-CARBOXAMIDE AND INTERMEDIATES THERETO
    Publication number: 20230028651
    Abstract: A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective PtN/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N?,N?-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
    Type: Application
    Filed: June 28, 2022
    Publication date: January 26, 2023
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Francis GOSSELIN, Stefan G. KOENIG, Eduardo V. MERCADO-MARIN, Andreas STUMPF, Daniel ZELL, Haiming ZHANG, Stephan BACHMANN, Diane E. CARRERA, Michael E. DALZIEL, Yonghui GE, Jie ZHANG, Raphael BIGLER, Laure Elizabeth Simone FINET, Regis Jean Georges MONDIERE, Yuki NAKAGAWA
  • Process for making benzoxazepin compounds
    Patent number: 9303043
    Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 5, 2016
    Assignee: Greentech, Inc.
    Inventors: Remy Angelaud, Danial R. Beaudry, Diane E. Carrera, Sushant Malhotra, Travis Remarchuk, Frederic St-Jean
  • PROCESS FOR MAKING BENZOXAZEPIN COMPOUNDS
    Publication number: 20140275523
    Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Remy Angelaud, Danial R. Beaudry, Diane E. Carrera, Sushant Malhotra, Travis Remarchuk, Frederic St-Jean