专利号:US-8227571-B2 优先权日:2007-12-11 标题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R; ROCHE PALO ALTO LLC 摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid†) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counteparts.
专利号:WO-2025042853-A1 优先权日:2023-08-18 标 题 :Compositions and methods for prophylaxis and/or treatment of alpha synuclein proteinopenia in parkinson's and other diseases 发明人:LEE JIN HYUNG; AHMED KARIEM E 权利人:LVIS REGAIN LP 摘要:Material compositions and/or methods useful for the prophylaxis and/or treatment of a-syn protein depletion (proteinopenia) are provided, including material compositions that retain native function of a-syn protein while limiting and/or preventing amyloid formation and/or aggregation of said protein. Material compositions and formulations for enhancing protein solubility, stability, circulation time, receptor interaction, brain penetrance, CSF halflife, and for facilitating peptide/protein synthesis and purification are also provided.
专利号:US-2010292435-A1 优先权日:2009-05-01 标题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybrid†) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to couple the second fragment and the first fragment. Alternatively, a different second fragment is coupled to a first fragment in the solid phase. Then, solution phase chemistry is then used to add the third fragment, whereby the third fragment is coupled to the coupled first and second fragments in the solution phase. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counterparts.
专利号:CN-103613642-A 优先权日:2013-11-20 标题:A liquid phase segmented synthesis method of hexapeptide
参考文献:10.1007/s00706-017-2074-x 摘要:Müller BJ, Mistlberger G, Klimant I. Insights in the determination of saxitoxin with fluorogenic crown ethers in water. Monatshefte für Chemie - Chemical Monthly. 2018 Jan 11;149(3):493–7. doi: 10.1007/s00706-017-2074-x.