The present invention provides novel tricyclic diazepine compounds and methods and pharmaceutical compositions utilizing them for the treating or preventing disorders including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, congestive heart failure or for inducing temporary delay of urination, and in conditions with increased vascular resistance and coronary vasoconstriction; and for the treating or preventing disorders remedied or alleviated by oxytocin antagonist activity, including suppression of preterm labor, dysmenorrhea, endometritis, and for suppressing labor at term prior to caesarean delivery. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.