186183-13-1Relevant academic research and scientific papers
Salts of ethyl 3-(2-(4-(4-amino-imino-methyl)phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl)acetylamino)-3-phenylpropionate
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, (2008/06/13)
The present invention relates to ethyl 3-(2-(4-(4-(amino-imino-methyl)-phenyl)-4-methyl-2,5-dioxoimidazolidin-1-yl)acetylamino)-3-phenylpropionate salts of the formula I, in which HM is maleic acid, and to their physiologically tolerated salts, thereof, to processes for their preparation and to their use in pharmaceuticals.
From Peptides to Heterocyclic Peptide Mimetics - Design and Synthesis of an Orally Active Fibrinogen Receptor Antagonist for the Prevention of Thrombosis
Stilz, H. U.,Beck, G.,Jablonka, B.,Just, M.
, p. 711 - 720 (2007/10/03)
The binding of fibrinogen to the platelet fibrinogen receptor (GP IIb/IIIa receptor) depends on an Arg-Gly-Asp-Ser (RGDS) tetrapeptide recognition motif.Structural modifications of the RGDS tetrapeptide lead structure has led to the discovery of a non-peptide RGD mimetic GP IIb/IIIa antagonist 1 (S 1197).Compound 1 inhibited dose-dependently and reversibly human platelet aggregation.In conscious dogs the ethyl ester prodrug 2 (S 5740) showed a high plasma availability of the active moiety of 42+/-8percent (n=4) and a plasma half life of 9.9 hours after oral administration as measured by bioassay.Compound 2 may potentially be used for chronic treatment and prophylaxis of thrombotic diseases in humans.A pilot plant synthesis of compound 2 was developed.
