Affiliation: Schering AG
- GR ligands: can we improve the established drugs?Hartmut Rehwinkel
Schering AG, Corporate Research, Medicinal Chemistry, 13342 Berlin, Germany
ChemMedChem 1:803-5. 2006
- Insight into the molecular mechanisms of glucocorticoid receptor action promotes identification of novel ligands with an improved therapeutic indexHeike Schäcke
CRBA Inflammation, Corporate Research, Schering AG, Berlin, Germany
Exp Dermatol 15:565-73. 2006..Nevertheless, considerable improvement in the therapeutic action of glucocorticoid receptor ligands is being achieved through the use of key molecular targets for screening novel glucocorticoid receptor ligands...
- Selective glucocorticoid receptor agonists (SEGRAs): novel ligands with an improved therapeutic indexHeike Schäcke
Bayer Schering Pharma AG, Global Drug Discovery, TRG Inflammation Immunology, Müllerstr 178, 13342 Berlin, Germany
Mol Cell Endocrinol 275:109-17. 2007..Such selective GR agonists (SEGRAs) are likely to enter clinical testing soon...
- Dissociated glucocorticoid receptor ligandsHeike Schäcke
Schering AG, Corporate Research, Mullerstrasse 178, 13342 Berlin, Germany
Curr Opin Investig Drugs 5:524-8. 2004..Several pharmaceutical companies are currently pursuing this goal...
- Dissociated glucocorticoid receptor ligands: compounds with an improved therapeutic indexHeike Schäcke
Schering AG, RBA Dermatology Europe, 13342 Berlin, Germany
Curr Opin Investig Drugs 6:503-7. 2005..Compounds that preferentially induce transrepression rather than transactivation should be superior to classical glucocorticoids. Indeed, proof of concept has been recently achieved with such selective glucocorticoid receptor agonists...
- Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effectsHeike Schäcke
Corporate Research Business Area Dermatology, Corporate Project Management Strategic Business Unit Specialized Therapeutics, and Medicinal Chemistry, Schering AG, Berlin, D 13342 Berlin, Germany
Proc Natl Acad Sci U S A 101:227-32. 2004..Moreover, they are useful tool compounds for further investigating the mechanisms of GR-mediated effects...
- Fluorinated dihydroquinolines as potent n-NOS inhibitorsStefan Jaroch
Medicinal Chemistry, Corporate Research, Research Center Europe, Schering AG, D 13342 Berlin, Germany
Bioorg Med Chem Lett 14:743-6. 2004..Fluorinated dihydroquinolines showed reduced basicity of the amidine function. Their syntheses and potencies as neuronal nitric oxide synthase (n-NOS) inhibitors are reported...
- Dihydroquinolines as novel n-NOS inhibitorsStefan Jaroch
Department of Medicinal Chemistry, Corporate Research, Schering AG, D 13342 Berlin, Germany
Bioorg Med Chem Lett 12:2561-4. 2002..Dihydroquinolines have been synthesized and have been shown to be potent n-NOS inhibitors. Selectivity versus e-NOS was increased to approximately 100-fold through appropriate substitution at the benzene ring...
- Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitorsStefan Jaroch
Department of Medicinal Chemistry, Research Center Europe, Corporate Research, Schering AG, D 13342, Berlin, Germany
Bioorg Med Chem Lett 13:1981-4. 2003..Dihydroquinolines with aminoalkyl side chains have been synthesized and have been shown to be potent n-NOS inhibitors. A marked selectivity versus e-NOS of up to approximately 300-fold was observed, whereas i-NOS was moderately inhibited...