Reaction behaviour of monomeric β-ketoesters, 4. Polymer network formation by Michael reaction of multifunctional acetoacetates with multifunctional acrylates

Based on the Michael reaction of multifunctional acetoacetates with multiacrylates, in the presence or absence of dimethacrylates, tailor made matrix materials can be prepared. This can be achieved in a one- or two-step process. The Michael addition (first step) can be followed by radiation curing of excessive acrylate (second step).     

Limiting the Number of Potential Binding Modes by Introducing Symmetry into Ligands: Structure‐Based Design of Inhibitors for Trypsin‐Like Serine Proteases

In the absence of X‐ray data, the exploration of compound binding modes continues to be a challenging task. For structure‐based design, specific features of active sites in different targets play a major role in rationalizing ligand binding characteristics. For example, dibasic compounds have been reported as potent inhibitors of various trypsin‐like serine proteases, the active sites of which contain several binding pockets that can be targeted by cationic moieties. This results in several possible orientations within the active site, complicating the binding mode prediction of such compounds by docking tools. Therefore, we introduced symmetry in bi‐ and tribasic compounds to reduce conformational space in docking calculations and to simplify binding mode selection by limiting the number of possible pocket occupations. Asymmetric bisbenzamidines were used as starting points for a multistage and structure‐guided optimization. A series of 24 final compounds with either two or three benzamidine substructures was ultimately synthesized and evaluated as inhibitors of five serine proteases, leading to potent symmetric inhibitors for the pharmaceutical drug targets matriptase, matriptase‐2, thrombin and factor Xa. This study underlines the relevance of ligand symmetry for chemical biology.     

A system for automatic measurement of circadian activity deviations in telemedicine

A system for the automatic measurement of the circadian activity deviations in telemedicine has been developed within the framework of a "Health Integrated Smart Home Information System" (HIS2). HIS2 is an experimental platform for the evaluation and the development of technologies in order to ensure the security and quality of life for patients who need home based medical monitoring. Location sensors are placed in each room of the HIS2, allowing the monitoring of patient's successive activity phases within the patient's home environment. We proceeded with a sampling in an hourly schedule to detect weak rhythmic variations. Based on numerous measurements, we established a mean value with confidence limits. These also allowed us to define a zone within which the patient's activity is qualified to be "predictable." Alerts are set off if the patient's activity deviates from this zone.     

Der Schlanke mit der gro?en Bildfl?che

Firmen&;ProdukteNeuer 16-ZOLL-LCD-Monitor

Der Schlanke mit der gro?en Bildfl?che     

Integrated Density of States for Ergodic Random Schrödinger Operators on Manifolds

We consider the Riemannian universal covering of a compact manifold M = X/ and assume that is amenable. We show the existence of a (nonrandom) integrated density of states for an ergodic random family of Schrödinger operators on X.