457059-32-4Relevant academic research and scientific papers
Trifluoromethyl-substituted hydantoins, versatile building blocks for rational drug design
Wehner, Volkmar,Stilz, Hans-Ulrich,Osipov, Sergej N.,Golubev, Alexander S.,Sieler, Joachim,Burger, Klaus
, p. 4295 - 4302 (2007/10/03)
Preparatively simple, one-pot syntheses of trifluoromethyl-substituted hydantoins starting from Boc-protected imines of hexafluoroacetone and trifluoropyruvate are described. They represent valuable building blocks for the construction of constrained pept
Novel imidazolidine derivatives, their preparation, their use and pharmaceutical preparations comprising them
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, (2008/06/13)
The present invention relates to novel imidazolidine derivatives of formula I, wherein A, E, Z, R1, R2, R3, R4 and R5 have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutical active compounds which are suitable, for example, for the treatment of inflammatory diseases, including rheumatoid arthritis, or allergic diseases. The compounds of formula I are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4 belonging to the integrins group. They are generally suitable for the treatment of diseases which are caused by an undesired extent of leukocyte adhesion and/or leukocyte migration or are associated therewith or in which cell-cell or cell-matrix interactions which are based on the interactions of VLA-4 receptors with their ligands play a role. The invention furthermore relates to processes for the preparation of the compounds of formula I, their use and pharmaceutical preparations which contain compounds of formula I.
Bis(trifluoromethyl)hydantoins as intermediates for pharmaceutically active ingredients
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, (2008/06/13)
The present invention relates to hydantoins of formula I, in which R is the residue of an amino carboxylic acid or of an amino carboxylic acid derivative, which is obtained formally by removing an NH2 group from an amino carboxylic acid or an amino carboxylic acid derivative, to the preparation thereof and to the use thereof as intermediates, in particular for preparing pharmaceutically active ingredients.
