发明授权
US06849714B1 Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
失效
通过与血液成分缀合,保护内源性治疗肽免受肽酶活性的影响
- 专利标题: Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components
- 专利标题(中): 通过与血液成分缀合,保护内源性治疗肽免受肽酶活性的影响
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申请号: US09623548申请日: 2000-05-17
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公开(公告)号: US06849714B1公开(公告)日: 2005-02-01
- 发明人: Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
- 申请人: Dominique P. Bridon , Alan M. Ezrin , Peter G. Milner , Darren L. Holmes , Karen Thibaudeau
- 申请人地址: CA Montreal
- 专利权人: ConjuChem, Inc.
- 当前专利权人: ConjuChem, Inc.
- 当前专利权人地址: CA Montreal
- 代理机构: Morrison & Foerster LLP
- 国际申请: PCTUS00/13576 WO 20000517
- 国际公布: WO0069900 WO 20001123
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; C07K1/107 ; C07K17/00
摘要:
A method of synthesizing a modified therapeutic peptide capable of forming a peptidase-stabilized therapeutic peptide conjugate, the peptide having between 3 and 50 amino acids, is k. In a first step of the method, a therapeutic peptide having a carboxy terminal amino acid and amino terminal amino acid is synthesized. In a second step, pairs of cysteine residues present in the therapeutic peptide are sequentially and selectively oxidized to form disulfide bridges in the therapeutic peptide. In a third step, a protecting group is attached to remaining cysteine residues that do not form disulfide bridges in the therapeutic peptide. Finally, the peptide is coupled to a reactive group capable of reacting with amino groups, hydroxyl groups or thiol groups on a blood component to form a covalent bond therewith.
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