发明授权
EP2632935B1 PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES
有权
VERFAHREN ZUR HERSTELLUNG VON DEGARELIX UND SEINEN ZWISCHENPRODUKTEN
- 专利标题： PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES
- 专利标题（中）： VERFAHREN ZUR HERSTELLUNG VON DEGARELIX UND SEINEN ZWISCHENPRODUKTEN
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申请号： EP11776745.9申请日： 2011-10-26
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公开(公告)号： EP2632935B1公开(公告)日： 2016-09-21
- 发明人: RASMUSSEN, Jon Holbech , FOMSGAARD, Jens , HANSEN, Stefan , RASMUSSEN, Palle Hedengran , WACHS, Wolfgang Oliver
- 申请人： Ferring B.V.
- 申请人地址： Polaris Avenue 144 2132 JX Hoofddorp NL
- 专利权人： Ferring B.V.
- 当前专利权人： Ferring B.V.
- 当前专利权人地址： Polaris Avenue 144 2132 JX Hoofddorp NL
- 代理机构： Hoffmann Eitle
- 优先权： EP10189032 20101027
- 国际公布： WO2012055905 20120503
- 主分类号： C07K5/083
- IPC分类号： C07K5/083 ; C07K5/087 ; C07K5/09 ; C07K7/23 ; C07K1/02
摘要：
The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ (P 1 )AA 1 -AA 2 -AA 3 -AA 4 (P 4 )-AA 5 -AA 6 (P 6 )-AA 7 -AA 8 (P 8 )-AA 9 -AA 10 -NH 2 €ƒ€ƒ€ƒ€ƒ€ƒ(II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P 1 is an amino protecting groups; preferably acetyl; P 4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P 6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P 8 is an amino protecting group.
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