Derivatives of piperidine, tetrahidroquinolina, tetrahidroisoquinolina as caspase inhibitors

摘要

Refers to Derivatives of piperidine, tetrahidroquinolina tetrahidroisoquinolina formula I, where a is a piperidine ring, tetrahidroquinolina or tetrahidroisoquinolina; r1 is H, CN, chn2, r,Ch2y; R is an aliphatic Group, an aryl Group, and is a aralquilo; outgoing Group; R2 is CO2H, ch2co2h, esters, amides, isosteres; R3 is H, aryl, aralquilo,A C1 - C6 aliphatic Group; R is aryl, heterociclilo; R3 and R4 form a Ring with N monocicliclo, bicyclic, tricyclic.Preferred compounds are (3S / R, (2S) - 3 - [1 - (2-chlorophenothiazine - 10 - carbonyl) - piperidine carbonyl] amino} - 2 - 4 - fluoro - 4 - oxo acid, pentanoic acid, [(3S / R,(2S) - 3 - [1 - (3 - clorofenotiazina - 10 - carbonyl) - piperidine carbonyl] amino} - 2 - 4 - fluoro - 4 - oxo acid, pentanoic acid, [(3S / R, (2S) - 3 - [1 - (3,Diclorofenotiazina - 10 - 4 - piperidine carbonyl) carbonyl] amino} - 2 - 4 - 4 - fluoro - oxo acid, pentanoic acid, among others.These compounds are inhibitors of the activity of Caspases involved in Apoptosis and inflammation