263276-03-5Relevant articles and documents
Squaric acid derivatives as VLA-4 integrin antagonists
Porter, John R.,Archibald, Sarah C.,Childs, Kirstie,Critchley, David,Head, John C.,Linsley, Janeen M.,Parton, Ted A.H.,Robinson, Martyn K.,Shock, Anthony,Taylor, Richard J.,Warrellow, Graham J.,Alexander, Rikki P.,Langham, Barry
, p. 1051 - 1054 (2002)
SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.
VLA-4 ANTAGONISTS
-
, (2008/06/13)
Substituted N-[N-(sulphonylphenyl)sulfonyl-prolyl]-phenylalanine derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds.
PHENYLALANINE ENAMIDE DERIVATIVES CONTAINING A SPIRO`3.5!NON-1-ENE RING FOR USE AS INTEGRIN INHIBITORS
-
Page/Page column 15; 16, (2010/02/06)
Phenylalanine enamide derivatives of formula (1) are described: wherein R1 is a -CH3, -(CH2)3CH3, -CH2CH20H, -CH2CH20CH3, -CH2CH2