Non-glycosidic and non-peptidic inhibitors of selectin, and...

Details Non-glycosidic and non-peptidic inhibitors of selectin, and... Non-glycosidic and non-peptidic inhibitors of selectin, and...

2005-07-26

2009-02-03

Puttlitz, Karl J (Department: 1621)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

C560S021000, C560S043000, C560S044000, C562S433000, C562S440000, C562S442000, C562S443000, C562S453000

Reexamination Certificate

active

07485742

ABSTRACT:
A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.

REFERENCES:
patent: 0 671 407 (1995-09-01), None
patent: 11 140038 (1999-05-01), None
Helvetica Chimica Acta (1987), 70(1), 153-7.
Ulbrich, Holger, Einar E. Eriksson and Lennart Lindbom “Leukocyte and endothelial cell adhesion molecules as targets for therapeutic interventions in inflammatory disease”Trends in Pharmacological Sciences,Dec. 2003, vol. 24(12):640-647.
Wong, Chi-Huey et al., “Small Molecules as Structural and Functional Mimics of Sialyl Lewis X Tetrasaccharide in Selectin Inhibition: A Remarkable Enhancement of Inhibition by Additional Negative Charge and/or Hydrophobic Group”J. Am. Chem. Soc.,1997, vol. 119:8152-8158.

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