Patents Assigned to Werthenstein BioPharma GmbH
  • Synthetic pathway to belzutifan and crystalline phases of synthetic intermediates
    Patent number: 11827614
    Abstract: The disclosure provides crystalline forms for certain synthetic intermediates for making belzutifan, a HIF-2? inhibitor, useful for the treatment of cancer. The disclosure also provides processes for isolating the crystalline forms.
    Type: Grant
    Filed: May 20, 2022
    Date of Patent: November 28, 2023
    Assignees: Merck Sharp & Dohme LLC, Werthenstein Biopharma GMBH
    Inventors: Stephen M. Dalby, Clinton Scott Shultz, Chintal Desai, Joshua Lee, Zhiwei Chen, Jungchul Kim, Nastaran Salehi Marzijarani, Tao Wang, Eric M. Phillips, Patrick Larpent, Het P. Patel, Haiheng Guo, Xin Wang, Kangze Dai, Lu Chen, Teng Li, Taotao Lu, Jianjun Duan
  • PROCESS FOR PREPARING SUGAMMADEX
    Publication number: 20230312887
    Abstract: The present invention relates to a process for drying crystalline sugammadex to meet solvent specifications that is independent of API crystallinity or crystalline form generated. It further relates to use of sugammadex in the reversal of neuromuscular blockade induced by recuronium bromide or by vecuronium bromide in adults undergoing surgery.
    Type: Application
    Filed: September 8, 2021
    Publication date: October 5, 2023
    Applicants: Merck Sharp & Dohme LLC, Werthenstein BioPharma GMBH
    Inventors: David J. Lamberto, Paolo Avalle, Lorenzo Codan, Patrick Larpent, Jochen Schoell, Jeffrey S. Neuhaus
  • Process for synthesis of a phenoxy diaminopyrimidine compound
    Patent number: 11584724
    Abstract: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
    Type: Grant
    Filed: April 18, 2019
    Date of Patent: February 21, 2023
    Assignees: Merck Sharp & Dohme LLC, Werthenstein BioPharma GmbH
    Inventors: Kevin M. Maloney, Kallol Basu, Michael James Di Maso, Guy R. Humphrey, Alfred Y. Lee, Feng Peng, Hong Ren, Siwei Zhang
  • NOVEL CRYSTALLINE FORMS OF SUGAMMADEX
    Publication number: 20220049023
    Abstract: The present invention provides a novel crystalline forms of sugammadex, designated herein as crystalline form Type 1 of sugammadex, crystalline form Type 2 of sugammadex, crystalline form Type 3 of sugammadex, crystalline form Type 8 of sugammadex, and crystalline form Type 9 of sugammadex, pharmaceutical compositions thereof, and methods for their use in the reversal of neuromuscular blockade induced by recuronium bromide or by vecuronium bromide in adults undergoing surgery.
    Type: Application
    Filed: September 25, 2019
    Publication date: February 17, 2022
    Applicant: Werthenstein Biopharma GMBH
    Inventors: Paolo Avalle, Lorenzo Codan, Patrick Larpent, Jochen Scholl
  • NOVEL PROCESS FOR SYNTHESIS OF A PHENOXY DIAMINOPYRIMIDINE COMPOUND
    Publication number: 20210122717
    Abstract: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
    Type: Application
    Filed: April 18, 2019
    Publication date: April 29, 2021
    Applicants: Merck Sharp & Dohme Corp., Werthenstein BioPharma GmbH
    Inventors: Kevin M. Maloney, Kallol Basu, John Y.L. Chung, Richard Desmond, Michael James Di Maso, Guy R. Humphrey, Alfred Y. Lee, Dan Lehnherr, Feng Peng, Hong Ren, Mark Weisel, Siwei Zhang, Patrick Larpent