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    • 3. 发明申请
    • SIDE-CHAIN EXTENDED LIGATION
    • 侧链延长码
    • WO2006133962A1
    • 2006-12-21
    • PCT/EP2006/005815
    • 2006-06-16
    • GENEPROT INC.BOTTI, PaoloTCHERTCHIAN, Sylvie
    • BOTTI, PaoloTCHERTCHIAN, Sylvie
    • C07K1/04
    • C07K1/04C07K1/026
    • The invention is directed to methods and compositions for chemical ligation of a first component that includes a carboxythioester and a second component that includes an amino-functionalized compound bearing a branched side chain that includes a removable thiol auxiliary, to give a ligation product having an amide bond at the ligation site. The reactants of the invention are chemoselective and the thiol moiety is removable from the ligation product. Removal of the thiol can be exploited to generate a native side chain at the ligation site. The methods and compositions of the invention are particularly useful for ligation of peptides and polypeptides. The ligation system of the invention is applicable to a wide variety of molecules, and thus can be exploited to generate peptides, polypeptides and other amino acid containing polymers.
    • 本发明涉及用于化学连接第一组分的方法和组合物,所述第一组分包括羧基硫酯和第二组分,所述第二组分包括带有支链侧链的氨基官能化化合物,其包含可除去的硫醇辅助剂,得到具有酰胺的连接产物 结扎部位的结合。 本发明的反应物是化学选择性的,硫醇部分可从连接产物中除去。 可以利用硫醇的去除在结合位点产生天然侧链。 本发明的方法和组合物特别适用于肽和多肽的连接。 本发明的连接系统可应用于各种各样的分子,因此可用于产生肽,多肽和其它含氨基酸的聚合物。
    • 5. 发明申请
    • MUCOSAL DELIVERY OF PEPTIDES
    • 胶原蛋白交付
    • WO2011064316A2
    • 2011-06-03
    • PCT/EP2010/068257
    • 2010-11-25
    • BOTTI, PaoloTCHERTCHIAN, Sylvie
    • BOTTI, PaoloTCHERTCHIAN, Sylvie
    • A61K9/006A61K9/12A61K38/02A61K38/26A61K47/22A61K47/545
    • Compositions and methods are provided for mucosal delivery of peptides. The compositions include a stably hydrated peptide active agent complexed with a crown compound and/or a counter ion solubilized in a nonaqueous hydrophobic vehicle at a pH different from the pI of the peptide active agent. The methods include administering to a subject an effective amount of a composition of the disclosure. Other aspects include methods for the manufacture of the compositions of the disclosure. Also provided are compositions and kits that find use in practicing embodiments of the disclosure. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.
    • 提供组合物和方法用于肽的粘膜递送。 组合物包括与不同于肽活性剂的pI的pH的与非水性疏水载体溶解的冠状化合物和/或抗衡离子配合的稳定水合的肽活性剂。 所述方法包括向受试者施用有效量的本发明的组合物。 其它方面包括制造本公开的组合物的方法。 还提供了在实践本公开的实施方案中使用的组合物和试剂盒。 所述方法和组合物可用于各种应用,包括治疗各种不同疾病状况。