379692-00-9Relevant academic research and scientific papers
Non-peptidyl inhibitors of VLA-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
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, (2008/06/13)
Compounds of Formula (1.0.0): are described wherein A is for example aryl, heteroaryl or heterocyclyl, Y is preferably —C(═O)—; B is independently selected from a group of moieties, the most preferred of which are those of partial Formulas (1.1.2) and (1.1.6): and E is a single bond; oxygen; 1,1-cyclopropyl; C(CH3)2; CF2; or a bridging moiety of partial Formula (1.9.0): where R1ais hydrogen when R1has the meaning of a mono-valent substituent; and R1ais a single bond when R1has the meaning of a di-valent substituent. Said compounds are useful in methods of treating or preventing an inflammatory, autoimmune or respiratory diseases by inhibiting cell adhesion and consequent or associated pathogenic processes subsequently mediated by VLA-4.
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent α4β1 integrin antagonists
Duplantier, Allen J.,Beckius, Gretchen E.,Chambers, Robert J.,Chupak, Louis S.,Jenkinson, Teresa H.,Klein, Anne S.,Kraus, Kenneth G.,Kudlacz, Elizabeth M.,McKechney, Michael W.,Pettersson, Martin,Whitney, Carrie A.,Milici, Anthony J.
, p. 2593 - 2596 (2007/10/03)
A series of isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives derived from LDV was found to be a potent antagonist of the α4β1 integrin. The synthesis and SAR leading up to 3-[3-(1-{2-[3-methoxy-4-(3-o-tolyl-ureido)-pheny
