The invention relates to a carbohydrate derivative having formula I ##STR1##wherein R.sup.1 is (1-4C)alkoxy; R.sup.2, R.sup.3 and R.sup.4 are independently (1-4C)alkoxy or OSO.sub.3.sup.-, the total number of sulfate groups is 4, 5, or 6; and the twisted lines represent bonds either above or below the plane of the six-membered ring to which they are attached; or a pharmaceutically acceptable salt thereof.The compounds of the invention have antithrombotic activity and may be used for treating or preventing thrombosis and for inhibiting smooth muscle cell proliferation.

Akzo Nobel N.V.

Carbohydrate derivatives

N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.

Hoffmann-La Roche Inc.

N-(4-carb-amimidophenyl)glycineamide derivatives

Reagents that specifically bind a carbohydrate target wherein sialic acid is linked at the nonreducing terminus of a glycoside to a galactose or galactosamine residue through an .alpha.2-6 linkage are able to inhibit the conversion of human Factor X to human Factor Xa. These reagents (SA/Gal/GalNAc binding reagents) as well as other strategies for inhibiting the conversion of Factor X to Factor Xa are useful in treating thrombosis, inflammation and other conditions associated with excess thrombin activity.

thrombosis/carbohydrate

Carbohydrate derivatives

N-(4-carb-amimidophenyl)glycineamide derivatives

Glycosylation-mediated inhibition of factor X

Glycosylation-mediated inhibition of factor X

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