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Use of biphenyl-derived thiamides as calpain inhibitors

Authors: Herradón García, Bernardo; Alonso Giner, Mercedes; Benito Cano, Esperanza; Chana López, Antonio; Montero, Ana;

Use of biphenyl-derived thiamides as calpain inhibitors

Abstract

[ES] La presente invención se refiere a compuestos derivados de bifenilo con actividad como inhibidores de calpaina. Un compuesto de la presente invención es un bifenilo 2,2'-disustituido, siendo los sustituyentes en las posiciones 2 y 2' del esqueleto de bifenilo cadenas conteniendo estructuras relacionados con los aminoácidos, incluyendo fragmentos de compuestos aminocar bonílicos, dónde al menos uno de los sustituyentes en dichas posiciones 2- ó 2'- está unido al esqueleto de bifenilo por un grupo tiocarbonilo, siendo compuestos con funcionalidad de tioamida. La presente invención también engloba cualquiera de los isómeros conformacionales (atropisómeros) de dicho compuesto de fórmula (1). Los compuestos de fórmula (1) tienen aplicación en el trata miento preventivo o terapéutico de una enfermedad degenerativa.

[EN] The invention relates to biphenyl-derived compounds having a calpain inhibitor activity. One of the inventive compounds is a 2,2'-disubstituted biphenyl, with the substituents at positions 2 and 2' of the biphenyl skeleton being chains containing structures that are associated with amino acids, including fragments of aminocarbonyl compounds, whereby at least one of the substituents at positions 2 or 2' is attached to the biphenyl skeleton by a thiocarbonyl group, said compounds having a thioamide functionality. The invention also relates to all of the conformational isomers (atropisomers) of the aforementioned compound having formula (I). Compounds having formula (I) can be used for the preventive or therapeutic treatment of a degenerative disease.

Fecha de presentación internacional: 06.05.2005. - Titular: Consejo Superior de Investigaciones Científicas (CSIC)

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This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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impulse
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