abstract |
THE DERIVATIVES (I) OF MORPHINAN, WHERE NOT EXCLUSIVELY, X AND Y ARE HYDROGEN AND TOGETHER UN -O-, R1 ALLYL SUBSTITUATED OR NOT, R2, R3, C1-10 ALKYL, R4 HYDROGEN OR HYDROXYLOY R5 HYDROGEN OR METHYL; THEY ARE OBTAINED BY SUBJECTING A COMPOUND (II) TO AN ELIMINATION OF ETHER PREFERABLY BY HEATING AT ELEVATED TEMPERATURE BETWEEN 30 AND 300JC WITH HBR AND BBR3 OR PYRIDINE HYDROCHLORIDE. BECAUSE OF THEIR ACTIVITY ANTAGONIST OF MORPHINE AND STIMULATION OF THE SECRETION OF LUTEINIZING HORMONE (LH), THEY ARE APPLICABLE IN THE TREATMENT OF HYPOTHALMIC LHRM INSUFFICIENCY, SUCH AS ANOVULATORY SYNDROME, AMENORRHEA, INFERTILITY, HYPOGONADISM, IDIOPATIC HYPOGONADOTROPIC; THE KALLMAN SYNDROME AND OTHERS. |