Matthew C Lucas
Affiliation: F. Hoffmann-La Roche Ltd
- Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitorsMatthew C Lucas
Roche Palo Alto LLC, Palo Alto, CA 94304, USA
Bioorg Med Chem Lett 19:4630-3. 2009..A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibition were identified...
- Design, synthesis, and biological evaluation of new monoamine reuptake inhibitors with potential therapeutic utility in depression and painMatthew C Lucas
Roche Palo Alto LLC, Department of Medicinal Chemistry, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
Bioorg Med Chem Lett 20:5559-66. 2010..Representative compounds from these series displayed good in vivo pharmacokinetics and high monoamine receptor occupancies which are indicators of good brain penetration...
- 2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depressionDavid S Carter
Department of Medicinal Chemistry, Roche Palo Alto LLC, CA 94304, USA
Bioorg Med Chem Lett 20:3941-5. 2010..In this Letter we describe the optimization of a novel series of 2-substituted N-aryl piperazine based triple reuptake inhibitors...
- Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitorsLinda M Bannwart
Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA
Bioorg Med Chem Lett 18:6062-6. 2008..One example showed in vivo anti-depressant-like effects in the mouse tail suspension assay with a minimum effective dose of 30 mg/kg i.p...
- Cyclic amide bioisosterism: strategic application to the design and synthesis of HCV NS5B polymerase inhibitorsHanbiao Yang
Medicinal Chemistry Department, Roche Palo Alto, LLC, Palo Alto, CA 94304, USA
Bioorg Med Chem Lett 20:4614-9. 2010..Inhibitor binding at the Thumb-II site was ultimately confirmed by solving a crystal structure of 8b complexed with NS5B...