N.v. Organon

Mohammad Shahid

Simon James Anthony Grove

Mingqiang Zhang

The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO; R, R, Rand Rare independently selected from H, (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, halogen, nitro, cyano, NRR, NRCOR, and CONRR, R, Rand Rare independently H or (C)alkyl; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system. 

Benzoxazepine derivatives and their use as AMPA receptor stimulators

The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO; R, R, Rand Rare independently selected from H, (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, halogen, nitro, cyano, NRR, NRCOR, and CONRR, R, Rand Rare independently H or (C)alkyl; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system 

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Newhouse, United Kingdom

Mohammad Shahid