CAS: 147611-81-2; 7-Isothiocyanato-N,N-Dimethylbenzo[c][1,2,5]Oxadiazol-4-Sulfonamide

专利信息

专利号:US-10858414-B2
优先权日:2018-03-09
标 题:Chemo-enzymatic synthesis of semaglutide, liraglutide and GLP-1
发明人：NUIJENS TIMO; TOPLAK ANA; QUAEDFLIEG PETER JAN LEONARD MARIO
权利人:ENZYPEP B V
摘要:The invention relates to a method for preparing a coupling product having the sequence P q -W v -His-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Gly. The method includes enzymatically couplingn (a) a peptide C-terminal ester or thioester having a first peptide fragment represented by the formula P q -W v -His-X-Glu-(thio)ester; and (b) a peptide nucleophile having an N-terminally unprotected amine having a second peptide fragment with the sequence H-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Glyn whereinn P represents a protective group at the N-terminal α-amino function of the peptide C-terminal ester or thioester and q is an integer having a value of 1 or 0; W represents one or more amino acid residues, which may be the same or different and v is an integer having a value of 1 or more representing the number of amino acid residues W; X is Ala or an α-amino-isobutyric acid unit (Aib); Y is Lys, which Lys has a free side-chain ε-amino group or a side-chain ε-amino group that is protected with a protective group or a side-chain ε-amino group that is functionalized with an amino acid or another functional group; and n Z is Arg or Lys.

专利号:US-10920258-B2
优先权日:2018-03-09
标题 :Chemo-enzymatic synthesis of semaglutide, liraglutide and GLP-1
发明人：NUIJENS TIMO; TOPLAK ANA; QUAEDFLIEG PETER JAN LEONARD MARIO
权利人:ENZYPEP B V
摘要:A method for synthesizing a peptide having the sequence His-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Gly is disclosed. The method includes enzymatically coupling:n (a) a peptide C-terminal ester or thioester having a first peptide fragment with the sequence His-X-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-(thio)ester; and (b) a peptide nucleophile having an N-terminally unprotected amine having a second peptide fragment with the sequence H-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Y-Glu-Phe-Ile-Ala-Trp-Leu-Val-Z-Gly-Arg-Gly; wherein:n X is Ala or an α-amino-isobutyric acid (Aib) residue; Y is Lys, which Lys has a free side-chain ε-amino group or of which Lys the side-chain ε-amino group is protected with a protective group or of which Lys the side-chain ε-amino group is functionalized with an amino acid or another functional group; and Z is Arg or Lys.

专利号:US-2020262886-A1
优先权日:2018-03-09
标 题 :Chemo-enzymatic synthesis of semaglutide, liraglutide and glp-1

专利号:EP-3704143-A1
优先权日:2018-03-09
标 题:Chemo-enzymatic synthesis of liraglutide, semaglutide and glp-1

专利号:CN-111757891-A
优先权日:2018-03-09
标题 :Chemo-enzymatic synthesis of semaglutide, liraglutide and GLP-1

专利号:WO-2019170918-A1
优先权日:2018-03-09
标 题:Chemo-enzymatic synthesis of liraglutide, semaglutide and glp-1