摘要 |
<p>Azepine derivatives of the general formula (I) or salts thereof, and drugs containing the derivatives or the salts as the active ingredient. In said Formula, R1 is hydrogen, alkyl, aryl, or the like; R2 is hydrogen or a carboxyl-protecting group; R3 is alkylene, a divalent aromatic hydrocarbon group, or the like; R4 is hydrogen, alkyl, or the like; X is an aromatic carbocycle or a heterocycle; m is an integer of 1 to 3; Y is nitrogen, oxygen, or the like; and Z is a group of the general formula (II): R?8 - R7 - R6 - A1¿ -, (wherein A1 is methylene, sulfonyl, or the like; R6 is alkylene, a divalent group derived from an arylalkane, or the like; R7 is methylene, carbonyl, or the like; and R8 is alkyl, arylalkyl, or the like). The drugs are excellent in peroral absorbability and in vivo fate and exhibit VLA-4 antagonism.</p> |