181519-21-1Relevant academic research and scientific papers
Substituted anilides
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, (2008/06/13)
The invention is directed to physiologically active compounds of formula (I): wherein: R1is hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; X1, X2and X6independently represent N or CR10; and one of X3, X4and X5represents CR11and the others independently represents N or CR10; where R10is hydrogen, amino, halogen, hydroxy, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulphinyl, lower alkylsulphonyl, nitro or trifluoromethyl; and R11represents a group —L1—Ar1—L2—Y; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (α4β1).
Substituted β-alanines
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Page column 99, (2010/01/30)
The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(=O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (à4β1).
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
