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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。

6. 发明授权

US06962924B2 Salt and polymorphs of desloratadine hemifumarate 失效
标题翻译：地氯雷他定半富马酸盐和多晶型物
公开(公告)号：US06962924B2
公开(公告)日：2005-11-08
申请号：US10621670
申请日：2003-07-17
申请人： Anup Kumar Ray , Hiren Patel , Mahendra R Patel
发明人： Anup Kumar Ray , Hiren Patel , Mahendra R Patel
IPC分类号： A61K31/4545 , A61P37/08 , A61P43/00 , C07D401/04 , A61K31/445 , C07D401/08
CPC分类号： C07D401/04
摘要： This invention provides a process of preparation of novel polymorphic hemifumarate salts of 8-chloro-6,11-dihyfro-11-(4-piperidylidene)-5H-benzo[5,6]-cyclohepta[1,2-b]pyridine, hereinafter called “desloratadine”. These polymorphic salt forms show much higher solubility in water and also in protic organic solvents compare to the parent desloratadine. The process of preparing the polymorphic forms comprising: a) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of from about 55° C. to 70° C., and stirring for 30 to 45 minutes after mixing, and thereafter filtering the solid thereby prepared in hot condition; to yield the polymorphic form 2 having a DSC of 232° C.±2° C.; or b) mixing the ethanolic solution of desloratadine and fumaric acid at a temperature of form about 15° C. room temperature (25° C.) and stirring at this temperature for 30 to 45 minutes, then filtering at room temperature; to yield the polymorphic form 1 having a DSC of 224° C.±2° C.
摘要翻译：本发明提供了8-氯-6,11-二氢-10-（4-哌啶基）-5H-苯并[5,6]环庚并[1,2-b]吡啶的新型多晶型富马酸盐的制备方法，以下称为“地氯雷他定”。与母体地氯雷他定相比，这些多晶型盐形式在水中以及在质子有机溶剂中显示出高得多的溶解度。制备多晶型体的方法包括：a）在约55℃至70℃的温度下混合去氯雷他定和富马酸的乙醇溶液，并在混合后搅拌30至45分钟，然后过滤固体，因此在热状态下制备; 得到DSC为232℃±2℃的多晶型2。或b）在约15℃室温（25℃）的温度下将脱氯雷他定和富马酸的乙醇溶液混合并在该温度下搅拌30至45分钟，然后在室温下过滤; 得到DSC为224℃±2℃的多晶型1

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