1020724-07-5Relevant articles and documents
EST64454: A Highly Soluble σ1Receptor Antagonist Clinical Candidate for Pain Management
Díaz, José Luis,García, Mónica,Torrens, Antoni,Caama?o, Ana María,Enjo, Juan,Sicre, Cristina,Lorente, Adriana,Port, Adriana,Montero, Ana,Yeste, Sandra,álvarez, Inés,Martín, Miquel,Maldonado, Rafael,De Lapuente, Beatriz,Vidal-Torres, Alba,Cendán, Cruz Miguel,Vela, José Miguel,Almansa, Carmen
, p. 14979 - 14988 (2020/12/23)
The synthesis and pharmacological activity of a new series of pyrazoles that led to the identification of 1-(4-(2-((1-(3,4-difluorophenyl)-1H-pyrazol-3-yl)methoxy)ethyl)piperazin-1-yl)ethanone (9k, EST64454) as a σ1 receptor (σ1R) antagonist clinical candidate for the treatment of pain are reported. The compound 9k is easily obtained through a five-step synthesis suitable for the production scale and shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability in all species, linked to an adequate pharmacokinetic profile in rodents, and antinociceptive properties in the capsaicin and partial sciatic nerve ligation models in mice.
Pyrazole compounds as sigma receptor inhibitors
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Page/Page column 10-11; 14-15, (2012/01/03)
The invention refers to compounds of general formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.