Treatment or prevention of sexual dysfunction, e.g. lack of sexual desire or erectile dysfunction, uses neurokinin A NK2 receptor antagonist, e.g. sareductant

摘要

The use of neurokinin A NK 2receptor antagonists (I), i.e. saredutant (Ia), (+)-N-(1-(2-(2-(3,4-dichlorophenyl)-5-oxo-4-phenyl-morpholin-2-yl)-ethyl)-4-(3-fluorophenyl)-piperidin-4-yl)-acetamide (Ib), (+)-1'-(2-(4-benzoyl-3,4-dichlorophenyl)-morpholin-2-yl)-ethyl)-N,N-dimethyl-1,4'-bipiperidine-4'-carboxamide (Ic) and their salts, is claimed in production of medicaments for treating or preventing sexual dysfunction. Independent claims are included for: (1) combinations of (I) with other active agents (II) for treating sexual dysfunction, selected from sildenafil, vardenafil, tardalafil, alprostadil, apomorphine, midrodrine, moxisylite, phentolamine, aviptadil, testosterone, dapoxetine, flibanserine and tobolone; and (2) kits containing (I) and (II) in separate compartments and the same or different packaging, for simultaneous, separate or sequential administration. ACTIVITY : Vasotropic; Aphrodisiac. In double-blind clinical trials in male and female patients with major depression, oral administration of saredutant (Ia) at 100 mg per day for 8 weeks increased the average 'Changes in Sexual Functioning Questionnaire' score from 1.36 (average of 551 patients) in an untreated control group to 2.23 (average of 553 patients). MECHANISM OF ACTION : Neurokinin A NK 2receptor antagonist.