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1. 发明授权

US08377891B2 Process for synthesis of cyclic octapeptide 有权
标题翻译：合成八肽的方法
公开(公告)号：US08377891B2
公开(公告)日：2013-02-19
申请号：US13123623
申请日：2009-05-04
申请人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
发明人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
IPC分类号： A61K38/08
CPC分类号： C07K14/6555 , A61K38/00
摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide. Alternatively threoninol is coupled to the heptapeptide of formula (3) to yield protected octapeptide of formula (4) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-Thr-OL which is subsequently deprotected to yield linear octapeptide of formula (5) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL and cyclized with hydrogen peroxide to yield cyclic octreotide with a yield of >95%.
摘要翻译：本发明涉及制备奥曲肽及其衍生物的方法。将起始物质Cys（Trt）-2-氯三苯甲基树脂与各种氨基酸偶联得到式（2）的保护的七肽：Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc ）-Thr（OBut）-Cys（Trt）-2-氯三苯甲基树脂。使用TFA5TIS和水从支持物上切割式（2）的线性保护肽，得到式（3）的线性保护肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc） - Thr（OBut）-Cys（Trt）-OH将式（3）的线性保护的七肽脱保护得到式（6）的七肽：D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; 其使用过氧化氢和式（7）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH的环肽环化; 苏氨酚在C末端偶联以产生奥曲肽。或者，苏糖醇与式（3）的七肽偶联以得到式（4）的保护的八肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc）-Thr（OBut）-Cys Trt）-Thr-OL，随后脱保护得到式（5）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL的直链八肽，并用过氧化氢环化，得到环状奥曲肽，产量> 95％。

2. 发明申请

US20120035117A1 Process for Synthesis of Cyclic Octapeptide 有权
标题翻译：环十八肽合成方法
公开(公告)号：US20120035117A1
公开(公告)日：2012-02-09
申请号：US13123623
申请日：2009-05-04
申请人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
发明人： Divya Lal Saksena , Digamber Shripati Pawar , Nikhil Umesh Mohe , Nilesh Dagdu Patil , Chandrakesan Muralidharan , Lester Lobo , Radhakrishnan Venkatasubramanian Tarur
IPC分类号： A61K38/08 , C07K7/06 , C07K1/10
CPC分类号： C07K14/6555 , A61K38/00
摘要： This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Cys(Trt)-2-Chlorotrityl resin is coupled with various amino acids to obtain a protected heptapeptide of formula (2): Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-2-Chlorotrityl resin. The linear protected peptide of formula (2) is cleaved from the support using TFA5TIS and water to yield linear protected peptide of formula (3) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-OH Linear protected heptapeptide of formula (3) is deprotected to yield heptapeptide of formula (6): D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; which is cyclized using hydrogen peroxide and to the cyclic peptide of formula (7) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH; threoninol is coupled at C terminal to yield octreotide. Alternatively threoninol is coupled to the heptapeptide of formula (3) to yield protected octapeptide of formula (4) Boc-D-Phe-Cys(Trt)-Phe-D-Trp-Lys(Boc)-Thr(OBut)-Cys(Trt)-Thr-OL which is subsequently deprotected to yield linear octapeptide of formula (5) D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL and cyclized with hydrogen peroxide to yield cyclic octreotide with a yield of >95%.
摘要翻译：本发明涉及制备奥曲肽及其衍生物的方法。将起始物质Cys（Trt）-2-氯三苯甲基树脂与各种氨基酸偶联得到式（2）的保护的七肽：Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc ）-Thr（OBut）-Cys（Trt）-2-氯三苯甲基树脂。使用TFA5TIS和水从支持物上切割式（2）的线性保护肽，得到式（3）的线性保护肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc） - Thr（OBut）-Cys（Trt）-OH将式（3）的线性保护的七肽脱保护得到式（6）的七肽：D-Phe-Cys-Phe-D-Tip-Lys-Thr-Cys-OH; 其使用过氧化氢和式（7）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-OH的环肽环化; 苏氨酚在C末端偶联以产生奥曲肽。或者，苏糖醇与式（3）的七肽偶联以得到式（4）的保护的八肽Boc-D-Phe-Cys（Trt）-Phe-D-Trp-Lys（Boc）-Thr（OBut）-Cys Trt）-Thr-OL，随后脱保护得到式（5）D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-OL的直链八肽，并用过氧化氢环化，得到环状奥曲肽，产量> 95％。

3. 发明授权

US08829157B2 Process for the synthesis of cyclic heptapeptide 有权
标题翻译：用于合成环七肽的方法
公开(公告)号：US08829157B2
公开(公告)日：2014-09-09
申请号：US13007736
申请日：2011-01-17
申请人： Divya Lal Saksena , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , Nikhil Umesh Mohe , Radhakishnan Venkatasubramanian Tarur
发明人： Divya Lal Saksena , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , Nikhil Umesh Mohe , Radhakishnan Venkatasubramanian Tarur
IPC分类号： A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/75 , C07K14/78 , C07K7/06 , A61K38/00
CPC分类号： C07K14/75 , A61K38/00 , C07K7/06 , C07K14/78
摘要： The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
摘要翻译：本发明涉及使用Fmoc固相合成技术大规模合成环七肽的改进方法。所描述的方法通过肽键彼此偶联在固体支持树脂上组装肽，以获得肽，其中半胱氨酸与树脂的偶联采用溶剂的组合以减少半胱氨酸外消旋化。所描述的方法涉及使用C1-C4醇作为有机腈的总替代物，从而使该方法成本有效，无毒和环保。

4. 发明申请

US20110118437A1 Process for the Synthesis of Cyclic Heptapeptide 有权
标题翻译：环肽肽合成方法
公开(公告)号：US20110118437A1
公开(公告)日：2011-05-19
申请号：US13007736
申请日：2011-01-17
申请人： DIVYA LAL SAKSENA , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , NIKHIL UMESH MOHE , Radhakishnan Venkatasubramania Tarur
发明人： DIVYA LAL SAKSENA , Chandrakesan Muralidharan , Lester Lobo , Digamber Shripati Pawar , NIKHIL UMESH MOHE , Radhakishnan Venkatasubramania Tarur
IPC分类号： C07K7/64
CPC分类号： C07K14/75 , A61K38/00 , C07K7/06 , C07K14/78
摘要： The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
摘要翻译：本发明涉及使用Fmoc固相合成技术大规模合成环七肽的改进方法。所描述的方法通过肽键彼此偶联在固体支持树脂上组装肽，以获得肽，其中半胱氨酸与树脂的偶联采用溶剂的组合以减少半胱氨酸外消旋化。所描述的方法涉及使用C1-C4醇作为有机腈的总替代物，从而使该方法成本有效，无毒和环保。

5. 发明申请

US20110196134A1 Process for PEGylation of Proteins 有权
标题翻译：蛋白质聚乙二醇化方法
公开(公告)号：US20110196134A1
公开(公告)日：2011-08-11
申请号：US13123558
申请日：2009-05-04
申请人： Nikhil Umesh Mohe , Radhakrishnan Venkatsubramanian Tarur , Dinesh Kumar Paliwal , Divya Lal Saksena , Nilesh Dagdu Patil , Muralidharan Chandrakesan , Digamber Shripati Pawar , Rakesh Shekhawat , Aruna Khare , Sagar Satyanarayan Zawar , Pankaj Prabhakar Malpure , Dilip Kumar Rana
发明人： Nikhil Umesh Mohe , Radhakrishnan Venkatsubramanian Tarur , Dinesh Kumar Paliwal , Divya Lal Saksena , Nilesh Dagdu Patil , Muralidharan Chandrakesan , Digamber Shripati Pawar , Rakesh Shekhawat , Aruna Khare , Sagar Satyanarayan Zawar , Pankaj Prabhakar Malpure , Dilip Kumar Rana
IPC分类号： C07K14/575
CPC分类号： C07K14/535 , A61K47/60
摘要： The present invention relates to a process for improving pegylation reaction yield of r-metHuG-CSF comprising conjugating r-metHuG-CSF to a PEG aldehyde at a free amine moiety at the N terminal end on the G-CSF in presence of a reducing agent in a pegylation buffer solution comprising a polyol having the formula CnH2n+2On where n is from 3 to 6, or a carbohydrate, or a derivative thereof wherein the concentration of said polyol or carbohydrate or derivative thereof is in the range of 0.1% to 10% w/w.
摘要翻译：本发明涉及一种改善r-metHuG-CSF的聚乙二醇化反应产率的方法，其包括将r-metHuG-CSF与G-CSF上N-末端的游离胺部分的PEG醛在还原剂在包含式C n H 2n + 20n的多元醇（其中n为3至6）的聚乙二醇化缓冲溶液中，或其中所述多元醇或碳水化合物或其衍生物的浓度在0.1至10的范围内的碳水化合物或其衍生物％w / w。

6. 发明授权

US08846614B2 Process for the synthesis of 37-mer peptide pramlintide 有权
标题翻译：合成37-mer肽普兰林肽的方法
公开(公告)号：US08846614B2
公开(公告)日：2014-09-30
申请号：US13591647
申请日：2012-08-22
申请人： Nikhil Umesh Mohe , Praful Shamrao Chavre , Bharti Prabhakarrao Deshmukh , Chandrakesan Muralidharan , Lester John Lobo , Digamber Shripati Pawar , Divya Lal Saksena
发明人： Nikhil Umesh Mohe , Praful Shamrao Chavre , Bharti Prabhakarrao Deshmukh , Chandrakesan Muralidharan , Lester John Lobo , Digamber Shripati Pawar , Divya Lal Saksena
IPC分类号： A61K38/00 , C07K14/00 , C07K14/575 , C07K1/04 , C07K14/01
CPC分类号： C07K1/04 , A61K38/00 , C07K14/01 , C07K14/575
摘要： A process for the production of pramlintide, a 37-mer peptide, is provided. The synthesis provides a high yield synthesis of the peptide in relatively pure form. Further purification can be achieved by preparative HPLC.
摘要翻译：提供了一种生产普兰米特，一种37聚体肽的方法。该合成以相对纯的形式提供肽的高产率合成。可通过制备型HPLC进一步纯化。

7. 发明申请

US20130109622A1 NOVEL PROCESS FOR THE SYNTHESIS OF 37-MER PEPTIDE PRAMLINTIDE 有权
标题翻译：用于合成37肽多肽的新方法
公开(公告)号：US20130109622A1
公开(公告)日：2013-05-02
申请号：US13591647
申请日：2012-08-22
申请人： Nikhil Umesh Mohe , Praful Shamrao Chavre , Bhartri Prabhakarrao Deshmukh , Chandrakesan Muralidharan , Lester John Lobo , Digamber Shripati Pawar , Divya Lal Saksena
发明人： Nikhil Umesh Mohe , Praful Shamrao Chavre , Bhartri Prabhakarrao Deshmukh , Chandrakesan Muralidharan , Lester John Lobo , Digamber Shripati Pawar , Divya Lal Saksena
IPC分类号： C07K1/04
CPC分类号： C07K1/04 , A61K38/00 , C07K14/01 , C07K14/575
摘要： A process for the production of pramlintide, a 37-mer peptide, is provided. The synthesis provides a high yield synthesis of the peptide in relatively pure form. Further purification can be achieved by preparative HPLC.
摘要翻译：提供了一种生产普兰米特，一种37聚体肽的方法。该合成以相对纯的形式提供肽的高产率合成。可通过制备型HPLC进一步纯化。

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