Synese Jolidon

Summary

Affiliation: F. Hoffmann-La Roche Ltd

Publications

  1. doi request reprint Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1
    Synese Jolidon
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 18:5533-6. 2008
  2. ncbi request reprint Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Switzerland
    Bioorg Med Chem Lett 16:4305-10. 2006
  3. ncbi request reprint 4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Basel, Switzerland
    Bioorg Med Chem Lett 16:4321-5. 2006
  4. doi request reprint Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Division, CH 4070 Basel, Switzerland
    J Med Chem 53:4603-14. 2010
  5. ncbi request reprint Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Basel, Switzerland
    Bioorg Med Chem Lett 16:4311-5. 2006
  6. doi request reprint Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers
    Eric Vieira
    Pharma Division, Discovery Research, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 19:1666-9. 2009
  7. doi request reprint Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 18:5134-9. 2008
  8. doi request reprint Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Basel, Switzerland
    Bioorg Med Chem Lett 20:6960-5. 2010
  9. ncbi request reprint Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors
    Henrietta Dehmlow
    Pharmaceuticals Division, Preclinical Research, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, CH 4070 Basel, Switzerland
    J Med Chem 46:3354-70. 2003

Collaborators

Detail Information

Publications9

  1. doi request reprint Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1
    Synese Jolidon
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 18:5533-6. 2008
    ..The most potent compounds of these structurally simple classes show low nanomolar inhibition at the GlyT1 target...
  2. ncbi request reprint Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Switzerland
    Bioorg Med Chem Lett 16:4305-10. 2006
    ..A novel, straightforward and efficient synthetic strategy for the assembly of the target molecules is also presented...
  3. ncbi request reprint 4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Basel, Switzerland
    Bioorg Med Chem Lett 16:4321-5. 2006
    ..In addition, a straightforward two-step procedure for the assembly of the target molecules is also presented...
  4. doi request reprint Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Division, CH 4070 Basel, Switzerland
    J Med Chem 53:4603-14. 2010
    ..This effort culminated in the discovery of compound 10a (RG1678), the first potent and selective GlyT1 inhibitor to have a beneficial effect in schizophrenic patients in a phase II clinical trial...
  5. ncbi request reprint Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability
    Daniela Alberati
    Discovery Biology, F Hoffmann La Roche Ltd, Pharmaceuticals Division, Basel, Switzerland
    Bioorg Med Chem Lett 16:4311-5. 2006
    ..We have also identified within these diazaspiropiperidine series a key relationship between reducing basicity of the piperidine nitrogen and reducing hERG affinity...
  6. doi request reprint Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers
    Eric Vieira
    Pharma Division, Discovery Research, F Hoffmann La Roche Ltd, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 19:1666-9. 2009
    ..The synthesis and the structure-activity relationship of this class of positive allosteric modulators of mGlu1 receptors will be discussed in detail...
  7. doi request reprint Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Discovery Chemistry, CH 4070 Basel, Switzerland
    Bioorg Med Chem Lett 18:5134-9. 2008
    ..The SAR which was developed in this series resulted in the discovery of highly potent compounds displaying excellent selectivity against the GlyT2 isoform, drug-like properties, and in vivo efficacy after oral administration...
  8. doi request reprint Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors
    Emmanuel Pinard
    F Hoffmann La Roche Ltd, Pharmaceutical Research Basel, Basel, Switzerland
    Bioorg Med Chem Lett 20:6960-5. 2010
    ....
  9. ncbi request reprint Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors
    Henrietta Dehmlow
    Pharmaceuticals Division, Preclinical Research, F Hoffmann La Roche Ltd, Grenzacherstrasse 124, CH 4070 Basel, Switzerland
    J Med Chem 46:3354-70. 2003
    ..In this respect, the most promising compounds are the benzophenone derivative 1.fumarate and the benzo[d]isothiazol 24.fumarate, which lowered TC by 40% and 33%, respectively...