Affiliation: F. Hoffmann-La Roche Ltd
- Minor structural modifications convert a selective PPARalpha agonist into a potent, highly selective PPARdelta agonistStefan Weigand
Bayer Health Care AG, Pharma Research, D 42096 Wuppertal, Germany
Bioorg Med Chem Lett 15:4619-23. 2005..Compound 33 showed good pharmacokinetics...
- Global quantitative phosphoproteome analysis of human tumor xenografts treated with a CD44 antagonistStefan Weigand
Discovery Oncology, Pharma Research and Early Development, Roche Diagnostics GmbH, Penzberg, Germany
Cancer Res 72:4329-39. 2012..Taken together, our approach augments the value of other high throughput techniques to identify biomarkers for clinical development of targeted agents...
- Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesisMichael Brands
Bayer HealthCare AG, Business Group Pharma, Research and Development, D 42096 Wuppertal, Germany
Bioorg Med Chem Lett 15:4201-5. 2005..We report systematic optimization of this compound class by means of classical and solid-phase chemistry. Optimized compounds with a bisarylamide side chain at the 2-position of the indole skeleton exhibit low-nanomolar activity on ECE...
- Selective indole-based ECE inhibitors: synthesis and pharmacological evaluationMichael Brands
Bayer HealthCare AG, Business Group Pharma, Research and Development, Aprather Weg 18a, 42096 Wuppertal, Germany
ChemMedChem 1:96-105. 2006..All ECE inhibitors of the indole class showed high selectivity for ECE over related metalloproteases such as NEP and ACE. Therefore, these compounds might have further potential as drugs for the treatment of coronary heart diseases...