- MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2
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The present application provides a compound of Formula: or a pharmaceutically acceptable salt thereof, wherein ring B, L1, ring A, L2, n, R1, R2, R3, R4, and X1 are as described herein. Pharmaceutical compositions comprising the compound, as well as the methods of making and using the compound, are also provided.
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- 2-Substituted-oxy-5-methylsulfonyl pyridine piperazine acidamide analogue and preparation method and application thereof
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The invention discloses 2-substituted-oxy-5-methylsulfonyl pyridine piperazine acidamide analogue and a preparation method and application thereof, and particularly, relates to 2-substituted-oxy-5-methylsulfonyl pyridine piperazine acidamide analogue with
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Paragraph 0094; 0095; 0096
(2016/10/08)
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- 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
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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.
- 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
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experimental part
p. 4603 - 4614
(2010/09/17)
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- SYNTHESIS OF GLYT-1 INHIBITORS
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The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
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Page/Page column 10
(2008/12/08)
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- CAMPHOR-DERIVED CXCR3 ANTAGONISTS
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The instant invention related to camphor derivatives of which are useful in treating diseases wherein inhibition of the exzyme CXCR3 results in beneficial therapy in a mammal.
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Page/Page column 18
(2008/06/13)
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- Sulfanyl substituted phenyl methanones
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The present invention relates to compounds of formula I wherein R1, R2, R3, X, X1, and n are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. These compounds are good inhibitors of the glycine transporter 1 (GlyT-1) for the treatment CNS disorders, such as schizophrenia, cognitive impairment, and Alzheimer's disease.
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Page/Page column 7
(2008/06/13)
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