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  • Title: Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
    Author: Venkatraman S, Lebsack AD, Alves K, Gardner MF, James J, Lingham RB, Maniar S, Mumford RA, Si Q, Stock N, Treonze KM, Wang B, Zunic J, Munoz B.
    Journal: Bioorg Med Chem Lett; 2009 Oct 01; 19(19):5803-6. PubMed ID: 19713111.
    Abstract:
    A series of prolyl-N-isonicotinoyl-(L)-4-aminophenylalanine derivatives substituted at the proline 4-position with cyclic amines was evaluated as VLA-4 antagonists. The ring size and presence or absence of fluorine affected potency and receptor occupancy. The analog with 3,3-difluoropiperidine at the proline 4-position (13) was the most potent compound and had very good duration of receptor occupancy in vitro. The ethyl ester prodrug of 13 demonstrated excellent receptor occupancy after oral dosing in rats.
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