Consejo Superior De Investigaciones Cientificas

Mercedes Alonso Giner

Esperanza Benito Cano

Bernardo Herradon García

Vicente Jesús Aran Redo

Bernardo Herradon Garcia

Antonio Chana Lopez

Roberto Chicharro Martin

Ana Montero Aguado

The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.

Isoquinoline derivatives as calpain inhibitors

The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2'-disubstituted biphenyl, where the substituents in the 2 and 2&#x2032; positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2&#x2032;-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease. 

Biphenyl derived thiamides as calpain inhibitors

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Juan de la Cierva, Spain

Mercedes Alonso Giner