Osanetant

Osanetant (developmental code name SR-142,801) is a neurokinin 3 receptor antagonist which was developed by Sanofi-Synthélabo and was being researched for the treatment of schizophrenia but was discontinued.

[3][4] Professor David J. Anderson, Director and Leadership Chair of the Tianqiao and Chrissy Chen Institute for Neuroscience at California Institute of Technology, has advocated that osanetant be explored as a treatment for pain, anxiety, and aggression in humans and companion animals experiencing bereavement or social isolation, citing research suggesting that osanetant has an excellent safety profile and suppresses negative effects of social isolation in mice through an evolutionarily-conserved mechanism and without acting as a depressant.

[5][6][7] Another potential application for osanetant is in the treatment of drug addiction, as it has been found to block the effects of cocaine in animal models.

[8][9] Osanetant is being investigated by Acer Therapeutics as a treatment for severe vasomotor symptoms such as a hot flashes and flushes among people experiencing menopause.

Catalytic hydrogenation removal of the benzyl protecting group gave N-Methyl-N-(4-phenylpiperidin-4-yl)acetamide [172733-87-8] (5).

Synthesis (Glaxo): [ 11 ]
Synthesis (Warner Lambert): [ 14 ]
Osanetant precursor: [ 15 ]