Customized proteases
    6.
    发明授权
    Customized proteases 失效
    定制蛋白酶

    公开(公告)号:US06187579B1

    公开(公告)日:2001-02-13

    申请号:US08329892

    申请日:1994-10-27

    IPC分类号: C12N960

    摘要: The invention provides customized proteases (i.e., mutant enzymes), methods of making customized proteases, as well as methods of using customized proteases. The customized proteases of the invention are derived from the known proteases. Altered transacylation reactions include the capability to perform transacylation reactions not substantially catalyzed by the known protease or the capability to perform transacylation reactions with improved yields, or both. The methods of the invention provide for customized proteases through site specific or random mutagenesis of the active site amino acids of the known proteases. The invention also provides for methods of using the customized proteases to prepare a preselected transacylation products. The preselected transacylation products produced can be modified by substitution at the N-or C-terminal with nucleophiles such as L-amino acids, D-amino acids, amino acid amides, and radioactive amino acids.

    摘要翻译: 本发明提供定制的蛋白酶(即突变酶),制备定制蛋白酶的方法以及使用定制的蛋白酶的方法。 本发明的定制的蛋白酶来自已知的蛋白酶。 改变的转酰基反应包括执行基本上不被已知蛋白酶催化的转酰基化反应的能力或者以提高的产量进行转酰化反应的能力,或两者都有。 本发明的方法通过已知蛋白酶的活性位点氨基酸的位点特异性或随机诱变提供定制的蛋白酶。 本发明还提供使用定制的蛋白酶制备预选的转酰胺产物的方法。 所产生的预选择的转酰胺化产物可以通过用亲核试剂如L-氨基酸,D-氨基酸,氨基酸酰胺和放射性氨基酸在N-或C-末端取代来修饰。

    Customized proteases
    8.
    发明授权
    Customized proteases 失效
    定制蛋白酶

    公开(公告)号:US5945329A

    公开(公告)日:1999-08-31

    申请号:US899324

    申请日:1997-07-23

    摘要: The invention provides customized proteases (i.e., mutant enzymes), methods of making customized proteases, as well as methods of using customized proteases. The customized proteases of the invention are derived from the known proteases. Altered transacylation reactions include the capability to perform transacylation reactions not substantially catalyzed by the known protease or the capability to perform transacylation reactions with improved yields, or both. The methods of the invention provide for customized proteases through site specific or random mutagenesis of the active site amino acids of the known proteases. The invention also provides for methods of using the customized proteases to prepare a preselected transacylation products. The preselected transacylation products produced can be modified by substitution at the N- or C-terminal with nucleophiles such as L-amino acids, D-amino acids, amino acid amides, and radioactive amino acids.

    摘要翻译: 本发明提供定制的蛋白酶(即突变酶),制备定制蛋白酶的方法以及使用定制的蛋白酶的方法。 本发明的定制的蛋白酶来自已知的蛋白酶。 改变的转酰基反应包括执行基本上不被已知蛋白酶催化的转酰基化反应的能力或者以提高的产量进行转酰化反应的能力,或两者都有。 本发明的方法通过已知蛋白酶的活性位点氨基酸的位点特异性或随机诱变提供定制的蛋白酶。 本发明还提供使用定制的蛋白酶制备预选的转酰胺产物的方法。 产生的预选择的转酰胺产物可以通过用亲核试剂例如L-氨基酸,D-氨基酸,氨基酸酰胺和放射性氨基酸在N-或C-末端取代来修饰。

    Stabilisation of Liquid-Formulated Factor VII(A) Polypeptides by Aldehyde-Containing Compounds
    10.
    发明申请
    Stabilisation of Liquid-Formulated Factor VII(A) Polypeptides by Aldehyde-Containing Compounds 审中-公开
    通过含醛化合物稳定液体配制因子VII(A)多肽

    公开(公告)号:US20100303786A1

    公开(公告)日:2010-12-02

    申请号:US12743612

    申请日:2008-11-21

    IPC分类号: A61K38/48 A61P7/04

    摘要: The present invention is directed to liquid, aqueous pharmaceutical compositions stabilised against chemical and/or physical degradation containing Factor VII polypeptides, and methods for preparing and using such compositions, as well as vials containing such compositions, and the use of such compositions in the treatment of a Factor VII-responsive syndrome. The main embodiment is represented by a liquid, aqueous pharmaceutical composition comprising at least 0.01 mg/mL of a Factor VII polypeptide (i); a buffering agent (ii) suitable for keeping pH in the range of from about 4.0 to about 9.0; and at least one stabilising agent (iii) comprising a R—CHO motif, e.g. Benzaldehyde, 3-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, or 5-formyl-4-methylimidazole.

    摘要翻译: 本发明涉及针对含有因子VII多肽的化学和/或物理降解稳定的液体水性药物组合物,以及用于制备和使用这些组合物的方法以及含有该组合物的小瓶,以及这些组合物在治疗中的用途 的因子VII反应综合征。 主要实施方案由包含至少0.01mg / mL的因子VII多肽(i)的液体含水药物组合物表示; 适于将pH保持在约4.0至约9.0范围内的缓冲剂(ii); 和至少一种包含R-CHO基序的稳定剂(iii),例如 苯甲醛,3-羟基苯甲醛,4-羟基苯甲醛或5-甲酰基-4-甲基咪唑。