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1. 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。

2. 发明专利

CA2560007A1 PROCESS FOR THE PREPARATION OF PEPTIDES 未知
公开(公告)号：CA2560007A1
公开(公告)日：2005-12-22
申请号：CA2560007
申请日：2004-10-10
申请人： USV LTD
发明人： PATIL NILESH , MISHRA SHRIKANT , SAKSENA DIVYA LAL , KHARE ARUNA , THAKARE MILIND , MURALIDHARAN CHANDRAKESAN
IPC分类号： C07K1/00 , C07K1/06 , C07K7/06
摘要： The present invention relates to an improved process for the preparation of N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-alpha-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.

3. 发明专利

DE602004024593D1 未知
公开(公告)号：DE602004024593D1
公开(公告)日：2010-01-21
申请号：DE602004024593
申请日：2004-10-10
申请人： USV LTD
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
摘要： The present invention relates to an improved process for the preparation of N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-alpha-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.

4. 发明专利

AT451384T 未知
公开(公告)号：AT451384T
公开(公告)日：2009-12-15
申请号：AT04817655
申请日：2004-10-10
申请人： USV LTD
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
摘要： The present invention relates to an improved process for the preparation of N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-alpha-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.

5. 发明专利

AU2004320599A1 Process for the preparation of peptides 未知
公开(公告)号：AU2004320599A1
公开(公告)日：2005-12-22
申请号：AU2004320599
申请日：2004-10-10
申请人： USV LTD
发明人： SAKSENA DIVYA LAL , MISHRA SHRIKANT , THAKARE MILIND , MURALIDHARAN CHANDRAKESAN , PATIL NILESH , KHARE ARUNA
IPC分类号： C07K1/00 , C07K1/06 , C07K7/06
摘要： The present invention relates to an improved process for the preparation of N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl-L-lysylglycyl-L-alpha-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.

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