申请人:TAKEDA CHEMICAL INDUSTRIES, LTD.
公开号:EP0547317A1
公开(公告)日:1993-06-23
Disclosed are a peptide represented by formula (I) or a pharmaceutically acceptable salt thereof:
wherein M represents a mercaptoacyl group; P, Q, R, S, T, U, V, W, X, Y and Z each represent amino acid residues, wherein an amino acid side chain of Y is either a substituted saturated aliphatic hydrocarbon group having 1 to 15 carbon atoms or an unsubstituted saturated aliphatic hydrocarbon group having 4 to 15 carbon atoms other than (1S)-1-methylpropyl; (2) a method for producing the above-mentioned peptide or the salt thereof, which comprises subjecting a peptide represented by formula (II) or a salt thereof to an oxidation reaction:
wherein M, P, Q, R, S, T, U, V, W, X, Y and Z are as diefined above; and (3) use of the above-mentioned peptide or the pharmaceutically acceptable salt thereof as an anti-endothelin agent.
本发明公开了一种由式(I)代表的
多肽或其药学上可接受的盐:
其中M代表巯基;P、Q、R、S、T、U、V、W、X、Y和Z各自代表
氨基酸残基,其中Y的
氨基酸侧链是除(1S)-1-甲基丙基以外的具有1至15个碳原子的取代饱和脂肪族烃基或具有4至15个碳原子的未取代饱和脂肪族烃基;(2) 生产上述
多肽或其盐的方法,包括将式(II)代表的
多肽或其盐进行氧化反应:
其中 M、P、Q、R、S、T、U、V、W、X、Y 和 Z 如上定义;以及 (3) 将上述
多肽或其药学上可接受的盐用作抗内皮素制剂。