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1. 发明申请

US20080182781A1 Process for the Preparation of Peptides 审中-公开
标题翻译：肽的制备方法
公开(公告)号：US20080182781A1
公开(公告)日：2008-07-31
申请号：US10592118
申请日：2004-10-10
申请人： Divya Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Milind Thakare , Nilesh Patil , Aruna Khare
发明人： Divya Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Milind Thakare , Nilesh Patil , Aruna Khare
IPC分类号： A61K38/12 , C07K7/64 , 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-α-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 of formula (4), preparing silver peptide of formula (5), followed by simultaneous deprotection, obtaining silver peptide of formula (5) and oxidation of 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N 6 - （氨基亚氨基甲基）-N 2 - （3-巯基-1-氧代丙基-L-赖氨酰甘氨酰-L- -α-天冬氨酰基-L-色氨酰-L-脯氨酰基-L-半胱氨酰胺，式（1）的环状（1-> 6） - 二硫化物，其包括将氨基酸残基和硫代烷基羧酸与固体上适当的保护基团组装通过除去除巯基部分的Acm保护基之外的侧链保护基除去由树脂得到的肽，从而得到式（3）的肽酰胺，转化具有被保护的硫醇的式（3）的肽酰胺的赖氨酸残基通过胍基化得到高精氨酸残基，得到式（4）的肽，制备式（5）的银肽，然后同时去保护，得到式（5）的银肽和银肽的氧化，得到粗肽酰胺，式（1），最后进行色谱 c净化。描述的过程简单，容易，环保，成本效益高。

2. 发明申请

US20090035815A1 Synthetic Gene for Enhanced Expression in E. Coli 审中-公开
标题翻译：在大肠杆菌中增强表达的合成基因
公开(公告)号：US20090035815A1
公开(公告)日：2009-02-05
申请号：US12126319
申请日：2008-05-23
申请人： Laxmi Srinivas Rao , Monsur Borbhuiya Ahmed , Milind Niphadkar , Dinesh Paliwal , Rakesh Shekhawat , Aruna Khare , Radhika Samant , Priti Thakur , Anjali Chutke , Neelesh Surlikar , Sagar Zawar , Shrikant Mishra
发明人： Laxmi Srinivas Rao , Monsur Borbhuiya Ahmed , Milind Niphadkar , Dinesh Paliwal , Rakesh Shekhawat , Aruna Khare , Radhika Samant , Priti Thakur , Anjali Chutke , Neelesh Surlikar , Sagar Zawar , Shrikant Mishra
IPC分类号： C12P21/06 , C12N15/62 , C12P41/00 , C07H21/04 , C12N15/12
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，其同时对大肠杆菌进行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。

3. 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。

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