发明授权
- 专利标题: Process for the preparation of insulin derivatives, the B chain of which is lengthened c-terminally
- 专利标题(中): 胰岛素衍生物的制备方法,其B链延长c末端
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申请号: US172236申请日: 1988-03-23
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公开(公告)号: US5015728A公开(公告)日: 1991-05-14
- 发明人: Rainer Obermeier , Rolf Geiger , Ulrich Grau
- 申请人: Rainer Obermeier , Rolf Geiger , Ulrich Grau
- 申请人地址: DEX Frankfurt am Main
- 专利权人: Hoechst Aktiengesellschaft
- 当前专利权人: Hoechst Aktiengesellschaft
- 当前专利权人地址: DEX Frankfurt am Main
- 优先权: DEX3333640 19830917
- 主分类号: C07K14/575
- IPC分类号: C07K14/575 ; A61K38/00 ; A61K38/28 ; A61P5/00 ; C07K14/62 ; C12P21/02
摘要:
The invention relates to a process for the preparation of an insulin derivative of the formula I ##STR1## in which R.sup.1 denotes H or H-Phe, R.sup.30 represents the radical of a naturally occurring L-aminoacid and R.sup.31 represents a physiologically acceptable organic group of neutral or basic character consisting of 1 to 3 .alpha.-aminoacids in which the terminal carboxyl function is present in the free form and which insulin derivative has an isoelectric point above 5.8, which comprises reacting an insulin of the formula I in which R.sup.30 denotes the radical of a genetically codable L-aminoacid and R.sup.31 represents OH or a protective group of the carboxyl function, with a peptide or aminoacid derivatives of the formula R-R.sup.30 -R.sup.31 consisting of 2 to 4 .alpha.-aminocacids, in which the terminal carboxyl function is in free form, in the presence of a trypsin-like endopeptidase at a pH value below the isoelectric point of the starting insulin.