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, R<1> is hydrogen, alkyl, aryl, or the like; R<2> is hydrogen or a carboxyl-protecting group; R<3> is alkylene, a divalent aromatic hydrocarbon group, or the like; R<4> 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> - R<7> - R<6> - A<1> -, (wherein A<1> is methylene, sulfonyl, or the like; R<6> is alkylene, a divalent group derived from an arylalkane, or the like; R<7> is methylene, carbonyl, or the like; and R<8> is alkyl, arylalkyl, or the like). The drugs are excellent in peroral absorbability and in vivo fate and exhibit VLA-4 antagonism.</p> |
申请人 |
KAKEN PHARMACEUTICAL CO., LTD.;IKEGAMI, SATORU;INOGUCHI, KIYOSHI;FUKUI, HIDETO;SUMITA, YUJI;MARUYAMA, TATSUYA;WATANUKI, MITSURU |
发明人 |
IKEGAMI, SATORU;INOGUCHI, KIYOSHI;FUKUI, HIDETO;SUMITA, YUJI;MARUYAMA, TATSUYA;WATANUKI, MITSURU |