SYNTHESIS OF A KIF18A INHIBITOR
    6.
    发明申请

    公开(公告)号:US20250129050A1

    公开(公告)日:2025-04-24

    申请号:US18832887

    申请日:2023-01-26

    Applicant: Amgen Inc.

    Abstract: The present invention relates to improved preparation of a KIF18A inhibitor having the chemical structure Compound (1), or a salt thereof Compound (la); wherein HA is as defined herein; and key intermediates thereof, i.e., Compound (2a), Compound (3a), Compound (5) or a salt thereof, and Compound (6a) or a hydrate thereof, of the formulae: Compound (2a); Compound (3a); Compound (5) or a salt thereof; and Compound (6a) or a hydrate thereof, preferably Compound (6a-1). The present invention further relates to solid form of Compound (6a), preferably the crystalline hydrate form of Compound (6a-1).

    METHOD FOR PRODUCING AN ANTIBODY PEPTIDE CONJUGATE

    公开(公告)号:US20250108121A1

    公开(公告)日:2025-04-03

    申请号:US18708513

    申请日:2022-11-08

    Applicant: AMGEN INC.

    Inventor: Jonathan DIEP

    Abstract: The present invention relates to mammalian cells modified to provide for reduced cleavage of peptides that will be conjugated to polypeptides expressed by the cells. In particular, the invention relates to a method of producing an antibody peptide conjugate, the method comprising: a) expressing the antibody in a mammalian cell wherein the mammalian cell is a cathepsin D knock out cell, and wherein the antibody comprises a cysteine or non-canonical amino acid amino acid substitution at one or more conjugation site(s); b) purifying the antibody; and c) conjugating a peptide to the antibody at the conjugation site(s).

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