| 摘要 |
<p>PURPOSE:To provide a novel benzodiazepine derivative having cholecystokinin-B antagonism, which is useful as a prophylactic or therapeutic agent for the appestat disorder, intestine smooth muscle hyperergasia related disease, anxiety, neuropathy, etc. CONSTITUTION:A compound of the formula I, for example (3R)-1, 3-dihydro-5-(2- fluorophenyl)-3-[3-(3-methylphenyl) ureido]-1-(4-imidazolyl) methyl-2H-1,4- benzodiazepine-2-one, and its hydrochloric salt are included. The compound of the formula I is obtained first by reacting a compound of the formula II (where, R<1> is an imino protecting group) with a compound of the formula III in a solvent (for example; chloroform), under cooling to heating conditions to give a compound of the formula IV, and then by removing the protecting group from the compound IV by hydrolysis or reduction. The compound of the formula I is useful also as an analgesic.</p> |
