845616-57-1Relevant articles and documents
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
Pinard, Emmanuel,Alanine, Alexander,Alberati, Daniela,Bender, Markus,Borroni, Edilio,Bourdeaux, Patrick,Brom, Virginie,Burner, Serge,Fischer, Holger,Hainzl, Dominik,Halm, Remy,Hauser, Nicole,Jolidon, Synese,Lengyel, Judith,Marty, Hans-Peter,Meyer, Thierry,Moreau, Jean-Luc,Mory, Roland,Narquizian, Robert,Nettekoven, Mathias,Norcross, Roger D.,Puellmann, Bernd,Schmid, Philipp,Schmitt, Sebastien,Stalder, Henri,Wermuth, Roger,Wettstein, Joseph G.,Zimmerli, Daniel
supporting information; experimental part, p. 4603 - 4614 (2010/09/17)
The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia. Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine class of GlyT1 inhibitors to improve hERG channel selectivity and brain penetration. 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.
Substituted acylpiperazine derivatives
-
Page/Page column 22, (2008/06/13)
The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
BENZOYL-PIPERAZINE DERIVATIVES
-
Page/Page column 28, (2008/06/13)
The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.