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1. 发明申请

US20100234566A1 Processes for Preparing a Polypeptide 审中-公开
标题翻译：制备多肽的方法
公开(公告)号：US20100234566A1
公开(公告)日：2010-09-16
申请号：US12727653
申请日：2010-03-19
申请人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
发明人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
IPC分类号： C07K1/08
CPC分类号： C08G69/10 , A61K38/00 , C07K14/001
摘要： The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceuticaly acceptable salt thereof.
摘要翻译：本发明涉及制备包含L-酪氨酸，L-丙氨酸，L-谷氨酸和L-赖氨酸的多肽或其药学上可接受的盐的改进方法。多肽或其药学上可接受的盐优选为醋酸格拉司他。该方法包括：（a）将L-酪氨酸的N-羧酸酐，L-丙氨酸的N-羧酸酐，受保护的L-谷氨酸的N-羧酸酐和受保护的L-赖氨酸的N-羧酸酐的极性在引发剂存在下的非质子溶剂，以形成受保护的多肽; （b）将酸与步骤（a）中形成的被保护的多肽和溶剂混合以形成产物; 和（c）将选自碱金属或碱土金属氢氧化物，碳酸盐，碳酸氢盐及其混合物的物质与步骤（b）中形成的产物和溶剂或溶剂的混合物和水，以形成去保护的多肽或其药学上可接受的盐。

2. 发明授权

US08729229B2 Processes for preparing a polypeptide 有权
标题翻译：制备多肽的方法
公开(公告)号：US08729229B2
公开(公告)日：2014-05-20
申请号：US12726571
申请日：2010-03-18
申请人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
发明人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
IPC分类号： A61K38/00 , C07K1/00 , C07K2/00
CPC分类号： C08G69/10 , A61K38/00 , C07K14/001
摘要： The present invention relates to processes for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate.
摘要翻译：本发明涉及制备包含L-酪氨酸，L-丙氨酸，L-谷氨酸和L-赖氨酸的多肽或其药学上可接受的盐的方法。多肽或其药学上可接受的盐优选为醋酸格拉司他。

3. 发明授权

US07834176B2 Polymorph E of Olanzapine and preparation of anhydrous non-solvated crystalline polymorphic Form I of 2-methyl-4(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5] benzodiazepine (Olanzapine Form I) from the polymorphic Olanzapine Form E 有权
标题翻译：奥氮平的多晶型物E和2-甲基-4（4-甲基-1-哌嗪基）-10H-噻吩并[2,3-b] [1,5]苯并二氮杂（奥氮平）的无水非溶剂化结晶多晶型物I的制备 I）从多态奥氮平形式E
公开(公告)号：US07834176B2
公开(公告)日：2010-11-16
申请号：US11340284
申请日：2006-01-26
申请人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mahendra R. Patel
发明人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mahendra R. Patel
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention provides an Olanzapine pseudopolymoph Form E. The invention provides methods of preparing polymorphic Olanzapine Form E employing rapid crystallization and seeding. The invention provides methods of preparing anhydrous Olanzapine Form I from the Olanzapine Form E by step-wise drying.
摘要翻译：本发明提供了一种奥氮平假多产的形式E.本发明提供了使用快速结晶和接种制备多晶型奥氮平片E的方法。本发明提供了通过逐步干燥从奥氮平形式E制备无水奥氮平I型的方法。

4. 发明申请

US20100234272A1 Processes for Preparing a Polypeptide 有权
公开(公告)号：US20100234272A1
公开(公告)日：2010-09-16
申请号：US12726571
申请日：2010-03-18
申请人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
发明人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
IPC分类号： A61K38/16 , C07K1/06 , C07K14/00 , A61P37/06
CPC分类号： C08G69/10 , A61K38/00 , C07K14/001
摘要： The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceutically acceptable salt thereof.

5. 发明申请

US20100174048A1 Processes for Preparing a Polypeptide 审中-公开
标题翻译：制备多肽的方法
公开(公告)号：US20100174048A1
公开(公告)日：2010-07-08
申请号：US12727758
申请日：2010-03-19
申请人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
发明人： Anup Kumar Ray , Hiren Kumar V. Patel , Johannes Ludescher , Mariappan Anbazhagan , Mahendra R. Patel , Ingolf Macher
IPC分类号： C07K1/06 , C07K2/00
CPC分类号： C08G69/10 , A61K38/00 , C07K14/001
摘要： The present invention relates to an improved process for preparing a polypeptide or pharmaceutically acceptable salt thereof comprising L-tyrosine, L-alanine, L-glutamate, and L-lysine. The polypeptide or pharmaceutically acceptable salt thereof is preferably glatiramer acetate. The process comprises: (a) polymerizing a mixture of N-carboxyanhydride of L-tyrosine, N-carboxyanhydride of L-alanine, N-carboxyanhydride of a protected L-glutamate and N-carboxyanhydride of a protected L-lysine, in a polar aprotic solvent in the presence of an initiator, to form a protected polypeptide; (b) admixing an acid with the protected polypeptide formed in Step (a) and a solvent, to form a product; and (c) admixing a substance selected from the group consisting of an alkali or alkaline earth metal hydroxide, a carbonate, a hydrogencarbonate, and mixtures thereof, with the product formed in Step (b), and a solvent or a mixture of a solvent and water, to form a deprotected polypeptide or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及制备包含L-酪氨酸，L-丙氨酸，L-谷氨酸和L-赖氨酸的多肽或其药学上可接受的盐的改进方法。多肽或其药学上可接受的盐优选为醋酸格拉司他。该方法包括：（a）将L-酪氨酸的N-羧酸酐，L-丙氨酸的N-羧酸酐，受保护的L-谷氨酸的N-羧酸酐和受保护的L-赖氨酸的N-羧酸酐的极性在引发剂存在下的非质子溶剂，以形成受保护的多肽; （b）将酸与步骤（a）中形成的被保护的多肽和溶剂混合以形成产物; 和（c）将选自碱金属或碱土金属氢氧化物，碳酸盐，碳酸氢盐及其混合物的物质与步骤（b）中形成的产物和溶剂或溶剂的混合物和水，以形成去保护的多肽或其药学上可接受的盐。

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