151447-85-7Relevant academic research and scientific papers
MONOACYLGLYCEROL LIPASE INHIBITORS
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Paragraph 0111-0112; 0141; 0153-0154; 0339, (2021/09/09)
Provided are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof: Also provided are compositions comprising compounds of formula (I). The compounds and compositions are also provided for use as medicaments, for example as medicaments useful in the treatment of a condition modulated by monoacylglycerol lipase (MAGL). Also provided are the use of compounds and compositions for the inhibition of monoacylglycerol lipase (MAGL).
PHARMACEUTICAL COMPOSITION COMPRISING A 1-(3-CHLOROPHENYL)-3-ALKYLPIPERAZINE FOR TREATING APETITE DISORDER
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Page/Page column 8-9, (2008/06/13)
Use of a 1- (3-chlorophenyl) -3-alkylpiperazine of formula (I), in racemic (R, S) form or in the form of the (S) enantiomer, in which R is a linear or branched alkyl group having from 1 to 3 carbon atoms, or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, for treating apetite disorder. A pharmaceutical composition that comprises a therapeutically effective amount of a 1-(3-chlorophenyl)-3-alkylpiperazine of formula (I) as previously defined or of an addition salt thereof with a pharmaceutically acceptable organic or inorganic acid, and at least one pharmaceutically acceptable excipient.
Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT(2A) and α1 receptor binding affinity
Giannangeli, Marilena,Cazzolla, Nicola,Luparini, Maria Rita,Magnani, Maurizio,Mabilia, Massimo,Picconi, Giuseppe,Tomaselli, Mauro,Baiocchi, Leandro
, p. 336 - 345 (2007/10/03)
A series of triazolopyridine derivatives (compounds 2a-1) were synthesized in order to explore the effect of modifications of the alkylpiperazine moiety of trazodone (fragment A) on binding affinity for 5HT(2A) and α1 receptors. All of the synthesized compounds show a decrease of affinity for both 5HT(2A) and α1 receptors, as compared to trazodone, with the exception of compounds 2b,c which bear a methyl group in an α position to the aliphatic nitrogen atom N1. These compounds showed a decrease of affinity only for the α1 receptor. The stereochemical influence of the piperazine moiety of compound 2c was also evaluated. Enantiomer (S)- 2c showed the most significant differences between 5HT(2A) and α1 receptor affinity (IC50 values) and among the corresponding functional properties (pA2 values). Since (S)-2c cannot generate the metabolite 4-(3- chlorophenyl)piperazine this product was selected for further pharmacological studies.
