发明名称 TYROSINE DERIVATIVE AND USE THEREOF
摘要 NEW MATERIAL:A compound shown by the formula [R<1> is (alkyloxy-substituted) lower alkyl; X is CO or SO2; -Y- is direct bond, lower alkylene or (substituted) vinylene; R<2> is (substituted)phenyl or naphthyl], an ester and a salt thereof. EXAMPLE:O-Methyl-N-(4-methylcinnamoyl)-L-tyrosine. USE:An agent for providing a drug such as insulin with absorption characteristics or enhancing absorption capacity. When the titled derivative is administered together with a drug activator, the activity is increased and oral or parenteral absorption is helped. PREPARATION:A compound shown by the formula is obtained by N-acylation reaction and salt-forming process according to a conventional procedure. The compound shown by the formula exhibits not only effects as an absorption imparter or an absorption enhancer but also inhibitory effects on trypsin and/or chymotrypsin, enzyme to hydrolyze insulin. The compound is expected to be an absorption imparter having high safety even in long-term continuous insulin therapy in diabetes.
申请公布号 JPS63258841(A) 申请公布日期 1988.10.26
申请号 JP19870092894 申请日期 1987.04.15
申请人 AJINOMOTO CO INC 发明人 FUKUSHIMA KOJI;SETO YOSHIKO;AMINO YUUSUKE;ETOU HIROZUMI;EGUCHI ARAHIKO;TOI KOJI
分类号 A61K47/00;A61K47/16;A61K47/42;C07C67/00;C07C233/51;C07C233/83;C07C235/20;C07C237/20;C07C237/22;C07C301/00;C07C311/00;C07C311/17;C07D307/85;C07K5/06 主分类号 A61K47/00
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