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1. 发明授权

US06441162B2 Crystalline substance of cefditoren pivoxyl and the production of the same 有权
标题翻译：头孢托仑的新型结晶物质及其生产
公开(公告)号：US06441162B2
公开(公告)日：2002-08-27
申请号：US09854462
申请日：2001-05-15
申请人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
发明人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： A crystalline substance of Cefditoren pivoxyl is provided which has a high purity and enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving an amorphous form of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous form well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.
摘要翻译：提供了新戊酸头孢托仑的结晶物质，其具有高纯度和增强的储存热稳定性。这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，该方法包括将无定形形式的新戊酰氧基头孢托仑溶解在能够将所述无定形形式溶解在其中的无水第一有机溶剂中，以及将所得溶液的第一有机溶剂组分通过具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后浓缩至15℃以下。减压下等。由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

2. 发明授权

US06713625B2 Process for the preparation of cefditoren using the thioester of thiazolylacetic acid 失效
标题翻译：使用噻唑乙酸硫酯制备头孢托仑的方法
公开(公告)号：US06713625B2
公开(公告)日：2004-03-30
申请号：US10152791
申请日：2002-05-23
申请人： Pandurang Balwant Deshpande , Parven Kumar Luthra
发明人： Pandurang Balwant Deshpande , Parven Kumar Luthra
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： The present invention provides a process for the preparation of Cefditoren of the formula (I) which comprises acylating 7-amino-cephem carboxylic acids of the general formula (IV) where R3 is hydrogen or trimethylsilyl with thioester derivatives of the formula (II) wherein R1 represents C1-C4 alkyl or phenyl in an organic solvent in the presence of an organic base at a temperature in the range of −10° C. to 30° C.
摘要翻译：本发明提供制备式（I）的头孢托仑的方法，该方法包括酰化通式（Ⅳ）的7-氨基头孢烯羧酸，其中R 3是氢或三甲基甲硅烷基与式（II）的硫酯衍生物，其中 R1在有机碱的存在下，在-10℃至30℃的温度范围内，在有机溶剂中代表C1-C4烷基或苯基。

3. 发明授权

US06531465B1 Antibacterial cephalosporins 失效
标题翻译：抗菌头孢菌素
公开(公告)号：US06531465B1
公开(公告)日：2003-03-11
申请号：US09861838
申请日：2001-05-21
申请人： Gerd Ascher , Johannes Ludescher
发明人： Gerd Ascher , Johannes Ludescher
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： A compound of formula wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.
摘要翻译：阿魏酸的化合物Ac，R 1和R 2具有各种含义，其制备方法及其作为药物的用途即抗菌剂。

4. 发明授权

US06825344B2 Process for the preparation of cephalosporin compounds and synthetic intermediates 有权
标题翻译：制备头孢菌素化合物和合成中间体的方法
公开(公告)号：US06825344B2
公开(公告)日：2004-11-30
申请号：US09918152
申请日：2001-07-30
申请人： Desmond John Best , George Burton , Brian Charles Gasson , Neal Frederick Osborne , Graham Walker
发明人： Desmond John Best , George Burton , Brian Charles Gasson , Neal Frederick Osborne , Graham Walker
IPC分类号： C07D50124
CPC分类号： C07D501/00 , Y02P20/55
摘要： There is provided a process for the preparation of a compound according to Formula (II): which includes the step of cyclising a compound of Formula (III): wherein R1, R2, R3, R4, X and m have meanings which are given in the description.
摘要翻译：提供了制备根据式（II）的化合物的方法：其包括使式（III）化合物环化的步骤：其中R 1，R 2，R 3，R 3， 4>，X和m具有在说明书中给出的含义。

5. 发明授权

US06583133B1 Propenyl cephalosporin derivatives and process for the manufacture thereof 失效
标题翻译：丙烯基头孢菌素衍生物及其制备方法
公开(公告)号：US06583133B1
公开(公告)日：2003-06-24
申请号：US09337908
申请日：1999-06-22
申请人： Peter Angehrn , Erwin Götschi , Ingrid Heinze-Krauss , Hans G. F. Richter
发明人： Peter Angehrn , Erwin Götschi , Ingrid Heinze-Krauss , Hans G. F. Richter
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms, as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.
摘要翻译：公开了通式化合物的头孢菌素衍生物R是分子量不超过400的有机残基，其通过碳与相邻的硫原子键合，并由碳，氢和任选的氧，硫，氮和/或卤素原子组成; R1是氢，低级烷基或苯基; A是与丙烯基直接键合并被分子量不超过400的有机残基取代的仲，叔或季氮原子，由碳，氢和任选的氧，硫，氮和/或卤素原子组成，以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其酯和盐。

6. 发明授权

US06693095B2 Antibacterial substituted 7-acylamino-3-(methylhydrazono) methyl-cephalosporins and intermediates 失效
标题翻译：抗菌取代的7-酰氨基-3-（甲基亚肼基）甲基头孢菌素和中间体
公开(公告)号：US06693095B2
公开(公告)日：2004-02-17
申请号：US10014651
申请日：2001-11-13
申请人： Gerd Ascher , Josef Wieser , Michael Schranz , Johannes Ludescher , Johannes Hildebrandt
发明人： Gerd Ascher , Josef Wieser , Michael Schranz , Johannes Ludescher , Johannes Hildebrandt
IPC分类号： C07D50124
CPC分类号： C07D295/215 , C07D501/00 , C07D501/46
摘要： A compound of formula wherein W, V, R1, R5, R2, R3 and R4 have various meanings, a process for their production and their use as a pharmaceutical.
摘要翻译：制剂的化合物W，V，R 1，R 5，R 2，R 3和R 4具有各种含义，其制备方法及其作为药物的用途。

7. 发明授权

US06504025B2 Process for the preparation of vinyl-pyrrolidinone cephalosporin derivatives 有权
标题翻译：乙烯基吡咯烷酮头孢菌素衍生物的制备方法
公开(公告)号：US06504025B2
公开(公告)日：2003-01-07
申请号：US09860157
申请日：2001-05-17
申请人： Paul Hebeisen , Hans Hilpert , Roland Humm
发明人： Paul Hebeisen , Hans Hilpert , Roland Humm
IPC分类号： C07D50124
CPC分类号： C07F9/65613 , C07D501/00 , C07F9/572 , C07F9/65583 , C07F9/65586 , Y02P20/582
摘要： Disclosed is a process for the preparation of vinyl-pyrrolidinone cephalosporine derivatives of formula Also disclosed are intermediate compounds of formulas wherein R1 and R2 are as defined herein.
摘要翻译：公开了一种制备式的乙烯基 - 吡咯烷酮头孢菌素衍生物的方法，还公开了中间体化合物，其中R1和R2如本文所定义。

8. 发明授权

US06384212B1 Process for preparing cephalosporin antibiotics using new thiazole compound 失效
标题翻译：使用新的噻唑化合物制备头孢菌素抗生素的方法
公开(公告)号：US06384212B1
公开(公告)日：2002-05-07
申请号：US09564980
申请日：2000-05-04
申请人： Dae-chul Yoon , Seung Won Yoo , Dong Gyun Shin , Myoung Ki Lee , Mi Soon Park , Yoon Seok Lee , Yoon Seok Song , Ju Cheol Lee , Sang Mi Oh
发明人： Dae-chul Yoon , Seung Won Yoo , Dong Gyun Shin , Myoung Ki Lee , Mi Soon Park , Yoon Seok Lee , Yoon Seok Song , Ju Cheol Lee , Sang Mi Oh
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： The present invention relates to a new, simple, and easy process for preparing cephalosporin antibiotics of the following formula (I), such as ceftazidime and cefixime. The process comprises acylating a 7-amino cephalosporanic acid derivative of the following formula (III) with a crystalline aminothiazole compound of the following formula (II): wherein R1 and R2 are the same or different and independently represent H, a C1-4 alkyl or C3-5 cycloalkyl group, R4 represents acetoxymethyl, methylpyridine, or vinyl, X represents chlorine or bromine, and the acid in the acid addition salt represents an inorganic acid, such as hydrochloric acid, or an organic acid, such as formic acid or acetic acid.
摘要翻译：本发明涉及用于制备下列通式（I）的头孢菌素抗生素的新的，简单的和容易的方法，例如头孢他啶和头孢克肟。该方法包括用下式（II）的结晶氨基噻唑化合物酰化下式（III）的7-氨基头孢菌酸衍生物：其中R 1和R 2相同或不同并且独立地代表H，C 1-4烷基或C3-5环烷基，R4表示乙酰氧基甲基，甲基吡啶或乙烯基，X表示氯或溴，酸加成盐中的酸表示无机酸，如盐酸或有机酸，如甲酸或醋酸。

9. 发明授权

US06294669B1 Crystalline substance of cefditoren pivoxyl and the production of the same 有权
标题翻译：头孢托仑的新型结晶物质及其生产
公开(公告)号：US06294669B1
公开(公告)日：2001-09-25
申请号：US09269109
申请日：1999-03-19
申请人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
发明人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： As a novel substance is provided such a new, crystalline substance of Cefditoren povoxyl which has a high purity and an enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving amorphous substance of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous substance well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.
摘要翻译：作为一种新物质，提供了这样一种具有高纯度和增加的储存热稳定性的新型头孢托仑聚氧乙烯醚的结晶物质。这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，所述方法包括将能够将所述无定形物质溶解在其中的无水的第一有机溶剂中溶解新戊酰氧基甲基头孢托仑的无定形物质，以及将所得溶液的第一有机溶剂组分置换为将具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后在15℃以下浓缩减压等。由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

10. 发明授权

US06384214B1 Process for producing cephalosporin derivatives 有权
标题翻译：生产头孢菌素衍生物的方法
公开(公告)号：US06384214B1
公开(公告)日：2002-05-07
申请号：US09610647
申请日：2000-06-29
申请人： Paul Spurr , Georg Trickes
发明人： Paul Spurr , Georg Trickes
IPC分类号： C07D50124
CPC分类号： C07D501/00 , Y02P20/55
摘要： The present invention is concerned with a novel process for the manufacture of cephalosporin derivatives of the formula by converting a phosphonium salt into the corresponding ylide and reacting same with an aldehyde wherein R1 and R2 are as above.
摘要翻译：本发明涉及用于制造将鏻盐转化为相应的叶立德并将其与其中R1和R2如上所述的醛反应的制剂的头孢菌素衍生物的新方法。

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