Patents by Inventor Diane Elizabeth CARRERA

Diane Elizabeth 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).

  • 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
  • Publication number: 20230312473
    Abstract: Processes for preparing biheteroaryl compounds are provided, including the biheteroaryl compound 3-(difluoromethoxy)-5-[2-(3,3-difluoropyrrolidin-1-yl)-6-[(1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl]pyrimidin-4-yl]pyridin-2-amine. Among other advantages, the processes provide for: the use of solvents that are relatively non-toxic and inexpensive; reduced usage of expensive precious metal catalysts; reaction temperature reduction in certain steps; the use of relatively non-toxic oxidation agents; the use of inexpensive transition metal catalysts; a reduction of molar ratios of certain reactants thereby improving process efficiency while reducing cost and waste; significantly higher reactant concentrations in certain steps; elimination of the need for multiple chromatographic purification steps; elimination of the need for certain extraction steps using organic solvent; and provide for higher yield and improved purity.
    Type: Application
    Filed: March 31, 2023
    Publication date: October 5, 2023
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Fabienne HOFFMANN-EMERY, Manuel KONRATH, Christian LAUTZ, Katrin Monika NIEDERMANN, Jonathan Ugo ORCEL, Diane Elizabeth CARRERA