Preparation of indane derivatives as AMPA receptor modulators.

Gillespie, Jonathan (2009) Preparation of indane derivatives as AMPA receptor modulators. WO2009147167A1.

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Abstract

Title compds. I [L1 = O, CO or SO2; L2 = NR8SO2 or SO2NR9; R1 = H, (un)substituted alkyl, cycloalkyl, etc.; R2 = (un)substituted alkyl, cycloalkyl, alkyloxy, or CN; R3 = H, (un)substituted alkyl, cycloalkyl, etc.; R4 = H, alkyl, alkenyl, etc.; R8 and R9 independently = H or alkyl; n = 1-3; X1 and X3 independently = O, S, N, etc.], and their pharmaceutically acceptable salts or solvates, are prepd. The invention also relates to a pharmaceutical compn. comprising said heterocyclic derivs. and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease. Thus, e.g., II was prepd. by in 7 steps starting from 2-aminoindane hydrochloride with bromine. The compds. of the invention exhibited pos. modulation of the AMPA receptor having EC50 values in the range 0.3 μM to 30 μM. [on SciFinder(R)]