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公开(公告)号：US06787649B2
公开(公告)日：2004-09-07
申请号：US10258624
申请日：2003-02-12
IPC分类号： C07D50136
CPC分类号： C07D501/00 , C07D277/46
摘要： A process which comprises (i) acylating a compound of formula II with a compound of formula IV to obtain a compound of formula I and (ii) deformylating said compound of formula I to obtain a compound of formula III
摘要翻译： 一种方法，其包括（i）用式IV化合物酰化式II化合物以获得式I化合物和（ii）使所述式I化合物变形，得到式III化合物
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公开(公告)号：US20080081906A1
公开(公告)日：2008-04-03
申请号：US11766132
申请日：2007-06-21
IPC分类号： C07D277/02 , C07D279/04
CPC分类号： C07D501/00
摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula (I), in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula (I) in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.
摘要翻译： 以式（I）表示的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸的结晶盐及其用途， 例如 在制备纯头孢地尼。 另一方面，本发明涉及任选呈结晶形式的盐形式的式（I）化合物，其中所述盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和 氨基磺酸盐。
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公开(公告)号：US07250508B2
公开(公告)日：2007-07-31
申请号：US10524397
申请日：2003-08-12
IPC分类号： C07D501/22 , C07D417/12
CPC分类号： C07D501/00
摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.
摘要翻译： 具有结晶盐形式的式I的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸及其用途， 在制备纯头孢地尼。 在另一方面，本发明涉及任选呈结晶形式的盐形式的式I化合物，其中盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和氨基磺酸盐。
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公开(公告)号：US07825241B2
公开(公告)日：2010-11-02
申请号：US11766132
申请日：2007-06-21
IPC分类号： C07D501/22
CPC分类号： C07D501/00
摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula (I), in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula (I) in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.
摘要翻译： 以式（I）表示的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸的结晶盐及其用途， 例如 在制备纯头孢地尼。 另一方面，本发明涉及任选呈结晶形式的盐形式的式（I）化合物，其中所述盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和 氨基磺酸盐。
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公开(公告)号：US20060025586A1
公开(公告)日：2006-02-02
申请号：US10524397
申请日：2003-08-12
IPC分类号： C07D501/14
CPC分类号： C07D501/00
摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula I in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula I in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.
摘要翻译： 具有结晶盐形式的式I的7- [2-（2-氨基噻唑-4-基）-2-（甲基羰氧基亚氨基）乙酰氨基] -3-乙烯基头孢烯-4-羧酸及其用途， 在制备纯头孢地尼。 在另一方面，本发明涉及任选呈结晶形式的盐形式的式I化合物，其中盐选自磷酸盐，磷酸氢盐，甲磺酸盐，甲苯磺酸盐，硫酸盐，硫酸氢盐和氨基磺酸盐。
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公开(公告)号：US09139597B2
公开(公告)日：2015-09-22
申请号：US13320430
申请日：2010-05-25
IPC分类号： C07D501/56 , C07D501/04 , C07D501/18
CPC分类号： C07D501/56 , C07D501/04 , C07D501/18
摘要： The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.
摘要翻译： 本发明涉及一种生产有机化合物的方法，特别是（6R，7R）-7 - [（Z）-2-（5-氨基 - [1,2,4]噻二唑-3-基） -2-羟基亚氨基 - 乙酰氨基] -8-氧代-3 - [（E） - （R）-1' - （5-甲基-2-氧代 - [1,3] - 二氧杂环戊烯-4-基甲氧基羰基）-2- 氧基 - [1,3']联吡咯烷基-3-亚基甲基] -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸酯（头孢噻肟中间体）和通式（ 1）和通式（2），本发明的生产中的化合物本身和中间体。
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公开(公告)号：US09096610B2
公开(公告)日：2015-08-04
申请号：US13320414
申请日：2010-05-25
IPC分类号： C07D501/56 , C07D501/04 , C07D501/18
CPC分类号： C07D501/56 , C07D501/04 , C07D501/18
摘要： The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.
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公开(公告)号：US20120116070A1
公开(公告)日：2012-05-10
申请号：US13320414
申请日：2010-05-25
IPC分类号： C07D501/46 , C07D501/18
CPC分类号： C07D501/56 , C07D501/04 , C07D501/18
摘要： The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.
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公开(公告)号：US20120108807A1
公开(公告)日：2012-05-03
申请号：US13320430
申请日：2010-05-25
IPC分类号： C07D501/56 , C07D501/18 , C07F7/18 , C07D501/04
CPC分类号： C07D501/56 , C07D501/04 , C07D501/18
摘要： The present invention relates to a method for the production of organic compounds, in particular sodium (6R,7R)-7-[(Z)-2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxyimino-acetylamino]-8-oxo-3-[(E)-(R)-1′-(5-methyl-2-oxo-[1,3]-dioxol-4-ylmethoxycarbonyl)-2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl]-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylate (ceftobiprole medocaril), and compounds of the general formula (1) and of the general formula (2), the compounds themselves and intermediates in the production according to the invention.
摘要翻译： 本发明涉及一种生产有机化合物的方法，特别是（6R，7R）-7 - [（Z）-2-（5-氨基 - [1,2,4]噻二唑-3-基） -2-羟基亚氨基 - 乙酰氨基] -8-氧代-3 - [（E） - （R）-1' - （5-甲基-2-氧代 - [1,3] - 二氧杂环戊烯-4-基甲氧基羰基）-2- 氧基 - [1,3']联吡咯烷基-3-亚基甲基] -5-硫杂-1-氮杂 - 双环[4.2.0]辛-2-烯-2-羧酸酯（头孢噻肟中间体）和通式（ 1）和通式（2），本发明的生产中的化合物本身和中间体。
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公开(公告)号：US20070225337A1
公开(公告)日：2007-09-27
申请号：US10599567
申请日：2005-03-30
申请人： Julia Greil , Siegfried Wolf , Johannes Ludescher
发明人： Julia Greil , Siegfried Wolf , Johannes Ludescher
IPC分类号： A61K31/44 , C07D417/02
CPC分类号： A61K9/1635 , A61K9/1623 , A61K9/1694 , C07D417/12
摘要： A novel coprecipitate of amorphous rosiglitazone maleate with a pharmaceutically acceptable carrier, e.g. polyvinylpyrolidone, mannitol, lactose, methylcellulose, cyclodextrin or silicon dioxide, a process for the preparation of said novel co-precipitate and the use of said novel coprecipitate of amorphous rosiglitazone with a pharmaceutically acceptable carrier in the treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, are disclosed. A novel solid solution of rosiglitazone maleate with a pharmaceutically acceptable carrier, preferably with polyethylene glycol PEG from 4000 to 40.000 of average mol. wt., a process for the preparation thereof and use are disclosed. A novel coprecipitate of amorphous rosiglitazone maleate with a pharmaceutically acceptable carrier and a novel solid solution of rosiglitazone maleate with a pharmaceutically acceptable inert carrier are stable and may be particularly suitable for bulk preparation, handling and formulation advantages.
摘要翻译： 具有药学上可接受的载体的非晶罗格列酮马来酸盐的新型共沉淀物。 聚乙烯吡咯烷酮，甘露糖醇，乳糖，甲基纤维素，环糊精或二氧化硅，制备所述新型共沉淀物的方法以及所述新型无定形罗格列酮的共沉淀物与药学上可接受的载体用于治疗和/或预防糖尿病， 公开了与糖尿病及其某些并发症相关的病症。 马来酸罗格列酮与药学上可接受的载体的新型固溶体，优选具有4000至40.000的平均摩尔的聚乙二醇PEG。 公开了其制备方法和用途。 具有药学上可接受的载体的非晶罗格列酮马来酸的新型共沉淀物和马来酸罗格列酮与药学上可接受的惰性载体的新型固溶体是稳定的，并且可以特别适合于批量制备，处理和制剂优点。
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