Preparation of indane derivatives for treating and preventing psychiatric diseases.

Gillen, Kevin James (2010) Preparation of indane derivatives for treating and preventing psychiatric diseases. WO2010115952A1.

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Abstract

The present invention relates to indane deriv. I [L1 = O, (CR5R6)m, OCR7R8, CR9R10O; L2 = NR11SO2 or SO2NR12; X1-X4 = N or CR1 with the proviso that only one of X1-X4 can be N; R1 = H, alkyl, cycloalkyl, etc.; R2 = alkyl, cycloalkyl, alkoxy, CN; R3 = H, alkyl, cycloalkyl, etc.; R4 = H, alkyl, alkenyl, etc.; R5-R12 = H or alkyl; m = 1-2; n = 0-1; Y1-Y3 = N or CR29 with the proviso that only one of Y1-Y3 can be N; R29 = H or (halo)alkyl; with the proviso that when L1 = (CR5R6)m and L2 is a substituent at the 2-position, n cannot be 0], or to a pharmaceutically acceptable salt or solvate thereof. Over sixty compds. I were prepd. E.g., a multi-step synthesis of (S)-II, starting from 2-aminoindane hydrochloride, is given. Compds. I exhibit pos. modulation of the AMPA receptor having EC50 values in the range 0.3 μM to 30 μM. The present invention also relates to a pharmaceutical compn. comprising one or more of indane derivs. I 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.