Antidepressant patents: 1995 - 1997

Abstract

Whilst considerable advances have been made in the treatment of depression, particularly with the advent of the selective serotonin re-uptake inhibitors (SSRIs), current drug treatments are unsatisfactory for several reasons. In particular, they fail to treat approximately 30% of patients, and they are slow in onset, requiring 3 - 8 weeks for efficacy. Consequently, the search for new antidepressants is now focussed on providing solutions to these problems. This review surveys the antidepressant patent literature for the years 1995 - 1997 in the context of these issues. Progress has been made, particularly with combinations of SSRIs and 5-HT autoreceptor ligands. Initially this has been achieved by combining individual drugs with single modes of action, but single compounds with multiple activities have also been patented. There has also been extensive patent activity suggesting that agonists at postsynaptic 5-HT_1A and 5-HT_2C receptors and antagonists at presynaptic 5-HT_1B autoreceptors possess antidepressant potential. While the major focus of research has been the enhancement of serotonergic neurotransmission, attention is now turning to other mechanisms of action. In particular, growing interest in the role of corticotrophin-releasing factor (CRF) in stress-related disorders, and recent clinical trials with the substance P antagonist, MK-869, has seen a rapid expansion in patent activity around CRF and tachykinin receptor antagonists for the treatment of depression.

• 5-HT autoreceptor
• 5-HT1A
• 5-HT1B
• 5-HT2C
• α-adrenoceptor
• antidepressant
• BIMT-17
• corticotrophin
• CP 93393
• CRF
• depression
• desensitisation
• EMD 68843
• GABA
• hypericum
• inositol monophosphatase
• MAO inhibitor
• MK-869
• neurosteroid
• onset of activity
• pindolol
• re-uptake inhibition
• RIMA
• SB 224289
• SNRI
• SSRI
• substance P
• tachykinin
• treatment resistance