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
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.
Venkatraman, Shankar,Lebsack, Alec D.,Alves, Kenneth,Gardner, Michael F.,James, Joyce,Lingham, Russell B.,Maniar, Salony,Mumford, Richard A.,Si, Qian,Stock, Nicholas,Treonze, Kelly M.,Wang, Bowei,Zunic, Jasmine,Munoz, Benito
scheme or table
p. 5803 - 5806
(2010/04/25)
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