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1. 发明申请

WO2009005973A2 SYNTHETIC GENE FOR ENHANCED EXPRESSION IN E.COLI 审中-公开
标题翻译：合成基因在E.COLI中的增强表达
公开(公告)号：WO2009005973A2
公开(公告)日：2009-01-08
申请号：PCT/US2008/066496
申请日：2008-06-11
申请人： PHARMACEUTICAL PATENT ATTORNEYS, LLC , USV LTD. , RAO, Laxmi, Srinivas , AHMED, Monsur, Borbhuiya , NIPHADKAR, Milind , PALIWAL, Dinesh , SHEKHAWAT, Rakesh , KHARE, Aruna , SAMANT, Radhika , THAKUR, Priti , CHUTKE, Anjali , SURLIKAR, Nilesh , ZAWAR, Sagar , MISHRA, Shrikant
发明人： RAO, Laxmi, Srinivas , AHMED, Monsur, Borbhuiya , NIPHADKAR, Milind , PALIWAL, Dinesh , SHEKHAWAT, Rakesh , KHARE, Aruna , SAMANT, Radhika , THAKUR, Priti , CHUTKE, Anjali , SURLIKAR, Nilesh , ZAWAR, Sagar , MISHRA, Shrikant
IPC分类号： C12P21/06
CPC分类号： C12P21/02 , C07K14/58
摘要： A novel nesiritide synthetic cDNA chimera encoding human b-type natriuretic peptide (hBNP) or nesiritide and a process for the preparation of the said novel chimera. Further, the inventors disclose the use of nesiritide synthetic cDNA chimera to obtain an expressible construct to produce mature nesiritide. Particularly, the inventors disclose an application of recombinant cloning method to prepare an ORF of a nesiritide chimeric construct, which is simultaneously codon optimized for E.coli and has optimal RNA stability. The inventors also provide a process for large scale purification of nesiritide by pH precipitation and chromatography.
摘要翻译：编码人b型利尿钠肽（hBNP）或奈西立肽的新型奈西立肽合成cDNA嵌合体及其制备方法。此外，发明人公开了使用奈西立肽合成cDNA嵌合体以获得可表达的构建体以产生成熟的奈西立肽。特别地，本发明人公开了重组克隆方法的应用，以制备奈西立肽嵌合构建体的ORF，该嵌合构建体对于大肠杆菌同时密码子优化并具有最佳的RNA稳定性。本发明人还提供了通过pH沉淀和色谱法大规模纯化奈西立胺的方法。

2. 发明申请

WO2010089756A3 AN IMPROVED PROCESS FOR PEGYLATION OF PROTEINS 审中-公开
标题翻译：一种改进的蛋白质PEG化过程
公开(公告)号：WO2010089756A3
公开(公告)日：2010-12-16
申请号：PCT/IN2009000262
申请日：2009-05-04
申请人： USV LTD , MOHE NIKHIL UMESH , TARUR RADHARKRISHNAN VENKATSUBRAMANIAN , PALIWAL DINESH KUMAR , SAKSENA DIVYA LAL , PATIL NILESH DAGDU , CHANDRAKESAN MURALIDHARAN , PAWAR DIGAMBER SHRIPATI , SHEKHAWAT RAKESH , KHARE ARUNA , ZAWAR SAGAR SATYANARAYAN , MALPURE PANKAJ PRABHAKAR , RANA DILIP KUMAR
发明人： MOHE NIKHIL UMESH , TARUR RADHARKRISHNAN VENKATSUBRAMANIAN , PALIWAL DINESH KUMAR , SAKSENA DIVYA LAL , PATIL NILESH DAGDU , CHANDRAKESAN MURALIDHARAN , PAWAR DIGAMBER SHRIPATI , SHEKHAWAT RAKESH , KHARE ARUNA , ZAWAR SAGAR SATYANARAYAN , MALPURE PANKAJ PRABHAKAR , RANA DILIP KUMAR
IPC分类号： C07K14/535 , A61K47/48
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：本发明涉及用于改善r-metHuG-CSF的聚乙二醇化反应产率的方法，其包括在还原剂存在下在G-CSF的N末端的游离胺部分将r-metHuG-CSF缀合至PEG醛在包含具有式C n H 2n + 2 O n（其中n为3至6）的多元醇或碳水化合物或其衍生物的聚乙二醇化缓冲溶液中，所述多元醇或碳水化合物或其衍生物的浓度在0.1％至10 ％w / w。

3. 发明申请

WO2009005973A3 SYNTHETIC GENE FOR ENHANCED EXPRESSION IN E.COLI 审中-公开
标题翻译：在E.COLI中增强表达的合成基因
公开(公告)号：WO2009005973A3
公开(公告)日：2009-12-30
申请号：PCT/US2008066496
申请日：2008-06-11
申请人： PHARMACEUTICAL PATENT ATTORNEY , RAO LAXMI SRINIVAS , AHMED MONSUR BORBHUIYA , NIPHADKAR MILIND , PALIWAL DINESH , SHEKHAWAT RAKESH , KHARE ARUNA , SAMANT RADHIKA , THAKUR PRITI , CHUTKE ANJALI , SURLIKAR NILESH , ZAWAR SAGAR , MISHRA SHRIKANT , USV LTD
发明人： RAO LAXMI SRINIVAS , AHMED MONSUR BORBHUIYA , NIPHADKAR MILIND , PALIWAL DINESH , SHEKHAWAT RAKESH , KHARE ARUNA , SAMANT RADHIKA , THAKUR PRITI , CHUTKE ANJALI , SURLIKAR NILESH , ZAWAR SAGAR , MISHRA SHRIKANT
IPC分类号： C12P21/04
CPC分类号： C12P21/02 , C07K14/58
摘要： A novel nesiritide synthetic cDNA chimera encoding human b-type natriuretic peptide (hBNP) or nesiritide and a process for the preparation of the said novel chimera. Further, the inventors disclose the use of nesiritide synthetic cDNA chimera to obtain an expressible construct to produce mature nesiritide. Particularly, the inventors disclose an application of recombinant cloning method to prepare an ORF of a nesiritide chimeric construct, which is simultaneously codon optimized for E.coli and has optimal RNA stability. The inventors also provide a process for large scale purification of nesiritide by pH precipitation and chromatography.
摘要翻译：编码人b型利尿钠肽（hBNP）或奈西立肽的新型奈西立肽合成cDNA嵌合体以及制备所述新嵌合体的方法。此外，本发明人公开了使用奈西立肽合成cDNA嵌合体获得可表达的构建体以产生成熟的奈西立肽。具体而言，本发明人公开了应用重组克隆方法来制备奈西立肽嵌合构建体的ORF，其对大肠杆菌同时密码子优化并且具有最佳的RNA稳定性。本发明人还提供了通过pH沉淀和色谱法大规模纯化奈西立肽的方法。

4. 发明申请

WO2010089756A2 AN IMPROVED PROCESS FOR PEGYLATION OF PROTEINS 审中-公开
标题翻译：改进蛋白质聚集过程
公开(公告)号：WO2010089756A2
公开(公告)日：2010-08-12
申请号：PCT/IN2009/000262
申请日：2009-05-04
申请人： USV LIMITED , MOHE, Nikhil, Umesh , TARUR, Radharkrishnan, Venkatsubramanian , PALIWAL, Dinesh, Kumar , SAKSENA, Divya, Lal , PATIL, Nilesh, Dagdu , CHANDRAKESAN, Muralidharan , PAWAR, Digamber, Shripati , SHEKHAWAT, Rakesh , KHARE, Aruna , ZAWAR, Sagar, Satyanarayan , MALPURE, Pankaj, Prabhakar , RANA, Dilip, Kumar
发明人： MOHE, Nikhil, Umesh , TARUR, Radharkrishnan, Venkatsubramanian , PALIWAL, Dinesh, Kumar , SAKSENA, Divya, Lal , PATIL, Nilesh, Dagdu , CHANDRAKESAN, Muralidharan , PAWAR, Digamber, Shripati , SHEKHAWAT, Rakesh , KHARE, Aruna , ZAWAR, Sagar, Satyanarayan , MALPURE, Pankaj, Prabhakar , RANA, Dilip, Kumar
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 C n H 2n+2 O n 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。

5. 发明申请

WO2005121164A9 PROCESS FOR THE PREPARATION OF PEPTIDES 审中-公开
标题翻译：制备肽的方法
公开(公告)号：WO2005121164A9
公开(公告)日：2006-03-02
申请号：PCT/IN2004000315
申请日：2004-10-10
申请人： USV LTD , SAKSENA DIVYA LAL , MISHRA SHRIKANT , MURALIDHARAN CHANDRAKESAN , THAKARE MILIND , PATIL NILESH , KHARE ARUNA
发明人： SAKSENA DIVYA LAL , MISHRA SHRIKANT , MURALIDHARAN CHANDRAKESAN , THAKARE MILIND , PATIL NILESH , KHARE ARUNA
IPC分类号： C07K1/00 , C07K1/06 , C07K7/06
CPC分类号： C07K7/06 , Y02P20/55
摘要： The present invention relates to an improved process for the preparation of N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl-L-lysylglycyl-L- -aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(1 6)-disulfide of formula (1), which involves assembling amino acid residues and a thioalkyl carboxylic acid with appropriate protecting groups on a solid phase resin, cleaving the peptide thus obtained from the resin with concomitant removal of side chain protecting groups except Acm protecting group of thiol moiety to obtain peptide amide of formula(3), converting lysine residue of peptide amide of formula(3) having protected thiol group to homoarginine residue by guanylation to obtain peptide amide of formula(4), preparation of silver peptide of formula(5), followed by simultaneous deprotection and oxidation of the said silver peptide to obtain crude peptide amide comprising compound of formula(1) and finally subjecting to chromatographic purification. The described process is simple, easy, environment friendly and cost effective.
摘要翻译：本发明涉及一种制备N6-（氨基亚氨基甲基）-N2-（3-巯基-1-氧代丙基-L-赖氨酰甘氨酰基-L-天冬酰基-L-色氨酰-L-脯氨酰基-L-半胱氨酰胺，式（1）的环状（16）二硫化物，其包括将固定相树脂上的氨基酸残基和硫代烷基羧酸与合适的保护基团组装，从树脂上切下由此获得的肽，同时除去侧链保护基除了巯基部分的Acm保护基以获得式（3）的肽酰胺，通过胍基将具有保护的硫醇基的式（3）的肽酰胺的赖氨酸残基转化成高精氨酸残基，得到式（4）的肽酰胺，制备银然后将所述银肽同时去保护和氧化，得到包含式（1）化合物的粗肽酰胺，最后进行色谱纯化，所述方法简单，容易环保，性价比高。

6. 发明申请

WO2005121164A1 PROCESS FOR THE PREPARATION OF PEPTIDES 审中-公开
标题翻译：制备肽的方法
公开(公告)号：WO2005121164A1
公开(公告)日：2005-12-22
申请号：PCT/IN2004/000315
申请日：2004-10-10
申请人： USV LIMITED , SAKSENA, Divya, Lal , MISHRA, Shrikant , MURALIDHARAN, Chandrakesan , THAKARE, Milind , PATIL, Nilesh , KHARE, Aruna
发明人： SAKSENA, Divya, Lal , MISHRA, Shrikant , MURALIDHARAN, Chandrakesan , THAKARE, Milind , PATIL, Nilesh , KHARE, Aruna
IPC分类号： C07K1/00
CPC分类号： C07K7/06 , Y02P20/55
摘要： The present invention relates to an improved process for the preparation of N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl-L-lysylglycyl-L- -aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(1 6)-disulfide of formula (1), which involves assembling amino acid residues and a thioalkyl carboxylic acid with appropriate protecting groups on a solid phase resin, cleaving the peptide thus obtained from the resin with concomitant removal of side chain protecting groups except Acm protecting group of thiol moiety to obtain peptide amide of formula(3), converting lysine residue of peptide amide of formula(3) having protected thiol group to homoarginine residue by guanylation to obtain peptide amide of formula(4), preparation of silver peptide of formula(5), followed by simultaneous deprotection and oxidation of the said silver peptide to obtain crude peptide amide comprising compound of formula(1) and finally subjecting to chromatographic purification. The described process is simple, easy, environment friendly and cost effective.
摘要翻译：本发明涉及一种制备N6-（氨基亚氨基甲基）-N2-（3-巯基-1-氧代丙基-L-赖氨酰甘氨酰基-L-天冬酰基-L-色氨酰-L-脯氨酰基-L-半胱氨酰胺，式（1）的环状（16）二硫化物，其包括将固定相树脂上的氨基酸残基和硫代烷基羧酸与合适的保护基团组装，从树脂上切下由此获得的肽，同时除去侧链保护基除了巯基部分的Acm保护基以获得式（3）的肽酰胺，通过胍基将具有保护的硫醇基的式（3）的肽酰胺的赖氨酸残基转化成高精氨酸残基，得到式（4）的肽酰胺，制备银然后将所述银肽同时去保护和氧化，得到包含式（1）化合物的粗肽酰胺，最后进行色谱纯化，所述方法简单，容易环保，性价比高。

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