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11. 发明授权

US5003064A Method for the preparation of monohydrate 失效
标题翻译：一水合物的制备方法
公开(公告)号：US5003064A
公开(公告)日：1991-03-26
申请号：US314026
申请日：1989-02-23
申请人： Luigi Ratti , Leone Dall'Asta
发明人： Luigi Ratti , Leone Dall'Asta
IPC分类号： C07D501/00 , C07D501/04 , C07D501/22
CPC分类号： C07D501/00
摘要： Cefadroxil monohydrate is prepared by solubilizing 7-[D-(-)-.alpha.-benzyloxycarbonylamino-.alpha.-(p-hydroxyphenyl)acetamido]-3-methyl-3-cephem-4-carboxylic acid by silylation or by salification in an organic solvent, subjecting the solubilized acid in the solvent to catalytic hydrogenation, separating the catalyst from the solution, and adding water to the solution at a pH of about 4 to precipitate cefadroxil monohydrate.
摘要翻译：通过甲硅烷基化或通过在有机溶剂中成盐溶解7- [D - （ - ） - α-苄氧基羰基氨基-α-（对羟基苯基）乙酰氨基] -3-甲基-3-头孢烯-4-羧酸来制备头孢羟氨酸一水合物使溶解的酸在溶剂中进行催化氢化，从溶液中分离催化剂，并在约4的pH下向溶液中加入水以沉淀头孢羟氨酸一水合物。

12. 发明授权

US4965355A Process for the prepartion of cefatrizine 1,2-propylene glycolate 失效
标题翻译：头孢菌素1,2-丙二醇酸酯的制备方法
公开(公告)号：US4965355A
公开(公告)日：1990-10-23
申请号：US314025
申请日：1989-02-23
申请人： Luigi Ratti , Leone Dall'Asta
发明人： Luigi Ratti , Leone Dall'Asta
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/04 , C07D501/24 , C07D501/36
CPC分类号： C07D501/00
摘要： Cefatrizine 1,2-propylene glycolate is prepared by reacting p-hydroxyphenylglycine chloride hydrochloride with 7-amino-3-iodomethyl-3-cephem-4-carboxylic acid, and then reacting the thus obtained novel intermediate, 7-[D(-)-.alpha.-amino-.alpha.-(p-hydroxyphenyl)-acetamido]-3-iodomethyl-3-cephem-4-carboxylic acid, with the sodium salt of 1,2,3-triazol-4(5)-thiol in 1,2-propylene glycol. The addition of water to the reaction mixture causes the cefatrizine, 1,2-propylene glycolate to precipate.
摘要翻译：通过使对羟基苯基甘氨酸氯化物盐酸盐与7-氨基-3-碘甲基-3-头孢烯-4-羧酸反应，然后使得到的新型中间体7- [D（ - ） - - α-氨基-α-（对羟基苯基） - 乙酰氨基] -3-碘甲基-3-头孢烯-4-羧酸与1,2,3-三唑-4（5） - 硫醇的钠盐在1 ，2-丙二醇。向反应混合物中加入水使得头孢菌素，1,2-丙二醇乙酸酯沉淀。

13. 发明授权

US4950687A Diacetylrhein salts and their therapeutical use in the treatment of arthrosis 失效
标题翻译：二乙酰赖氨酸盐及其在治疗关节病中的治疗用途
公开(公告)号：US4950687A
公开(公告)日：1990-08-21
申请号：US379787
申请日：1989-07-17
申请人： Leone Dall'Asta , Germano Coppi , Mario Ercole Scevola
发明人： Leone Dall'Asta , Germano Coppi , Mario Ercole Scevola
IPC分类号： A61K31/215 , A61K31/22 , A61P29/00 , C07C69/16
CPC分类号： A61K31/215 , C07C69/16 , Y10S514/903
摘要： A therapeutic treatment for the athrosis diseases comprising administering by intraarticular route from 1 to 5 ml of an aqueous solution containing from 10 to 50 mg of a diacetyl rhein salt having formula (I): ##STR1## wherein M represents an alkali or an earth alkali metal or the residue of an organic base.The diacetyl rhein salts administered by intraarticular route exhibit higher pharmacological activity than the corresponding diacetylrhein administered orally.
摘要翻译：一种治疗疾病的治疗方法，包括通过关节内途径施用1至5ml含有10至50mg具有式（I）的二乙酰大黄酸盐的水溶液：其中M表示碱或碱土金属或有机碱的残基。通过关节内途径施用的二乙酰大黄酸盐相对于口服施用的相应的二乙酰胆碱具有较高的药理活性。

14. 发明授权

US4485248A Process for producing 2,4-diamino-(3,5-dimethoxy-4-methoxyethoxy-benzyl)-pyrimidine 失效
标题翻译：制备2,4-二氨基 - （3,5-二甲氧基-4-甲氧基乙氧基 - 苄基） - 嘧啶的方法
公开(公告)号：US4485248A
公开(公告)日：1984-11-27
申请号：US399343
申请日：1982-07-19
申请人： Leone Dall'Asta
发明人： Leone Dall'Asta
IPC分类号： C07D239/48 , C07D239/49
CPC分类号： C07D239/49
摘要： A process for preparing Tetroxoprim starting from 3,5-dimethoxy-4-methoxyethoxy-benzaldehyde and 2,4-diamino-6-hydroxy-pyrimidine, by successive hydrogenation, halogenation and hydrogenolysis of the 2,4-diamino-6-oxo-5-(3,5-dimethoxy-4-methoxyethoxy-benzylidene)-pyrimidine obtained in the initial reaction.
摘要翻译：通过连续氢化，卤化和氢解2,4-二氨基-6-氧代 - 嘧啶，由3,5-二甲氧基-4-甲氧基乙氧基 - 苯甲醛和2,4-二氨基-6-羟基 - 嘧啶开始制备四氮丙啶的方法，在初始反应中获得的5-（3,5-二甲氧基-4-甲氧基乙氧基 - 亚苄基） - 嘧啶胺。

15. 发明授权

US5721360A Process for the preparation of a thiazoline-azetidinone 失效
标题翻译：制备噻唑啉 - 氮杂环丁酮的方法
公开(公告)号：US5721360A
公开(公告)日：1998-02-24
申请号：US656979
申请日：1996-06-06
申请人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
发明人： Gianfranco Cainelli , Achille Umani Ronchi , Michele Contento , Mauro Panunzio , Sergio Sandri , Marco Da Col , Leone Dall'Asta
IPC分类号： C07D205/085 , C07D513/04 , C07D205/12
CPC分类号： C07D513/04
摘要： The present invention refers to process for the preparation of a tiazoline-azetidinone of formula I ##STR1## which comprises N-protecting in position 1 of (3S,4S)-3-phenylace tamido-4-acetoxy-azetidin-2-one, converting the product thus obtained into the corresponding thioamide and subsequently ciclyzing and deprotecting.
摘要翻译：本发明涉及制备（3S，4S）-3-苯基三氨基-4-乙酰氧基 - 氮杂环丁烷-2-酮的式Ⅰ的噻唑烷 - 氮杂环丁酮的方法，将所得产物转化为相应的硫代酰胺随后凝结和脱保护。

16. 发明授权

US5656735A Process for the preparation of amikacin precursors 失效
标题翻译：制备阿米卡星前体的方法
公开(公告)号：US5656735A
公开(公告)日：1997-08-12
申请号：US402328
申请日：1995-03-10
申请人： Leone Dall'Asta , Eugenio Garegnani
发明人： Leone Dall'Asta , Eugenio Garegnani
IPC分类号： C07H15/234 , C07H15/236 , C07H15/26 , C07H1/00
CPC分类号： C07H15/26 , C07H15/234 , Y02P20/55
摘要： Process for the preparation of a 3,6'-di-N-Acyl-1-[L-(-)-4-Acylamino-2-hydroxybutyryl] kanamycin A, wherein Acyl is a N-protecting acylating group, which comprises reacting kanamycin A with an aluminum salt in an inert organic solvent, treating the aluminum complex thus obtained with a N-acylating agent end acidifiying the reaction mixture, as such or after having removed the complexing aluminum in basic medium and isolated the 3,6'-di-N-Acyl-kanamycin A, to pH 6, treating the protonated 3,6'-di-N-Acyl-kanamycin A, in form of a salt thereof, with an active derivative of L-(-)-4-Acyl-amino-2-hydroxybutyric acid, wherein Acyl is a N-protecting group preferably identical with that which protects the amino groups in the positions 3 and 6' of kanamycin A, and isolating the product thus obtained by simple correction of the pH.
摘要翻译：制备3,6'-二-N-酰基-1- [L - （ - ） - 4-酰基氨基-2-羟基丁酰基]卡那霉素A的方法，其中酰基是N-保护性酰化基团，其包括使卡那霉素A与铝盐在惰性有机溶剂中反应，用N-酰化剂处理由此得到的铝络合物，其酸化反应混合物，或在除去碱性介质中的络合铝并分离出3,6'- 将二-N-酰基卡那霉素A转化至pH6，用其盐形式的质子化的3,6'-二-N-酰基卡那霉素A与活性衍生物L - （ - ） - 酰基 - 氨基-2-羟基丁酸，其中酰基是N-保护基，优选与保护卡那霉素A的3'和6'位氨基的那些相同，并通过简单的pH校正分离由此获得的产物。

17. 发明授权

US5589593A Crystalline form of a cephalosporin antibiotic 失效
标题翻译：结晶形式的头孢菌素抗生素
公开(公告)号：US5589593A
公开(公告)日：1996-12-31
申请号：US483888
申请日：1995-06-07
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta
IPC分类号： A61K31/545 , C07D501/00 , C07D501/59 , C07D501/32
CPC分类号： C07D501/00 , A61K31/545
摘要： The preparation of a novel crystalline cefaclor and the conversion of such a product to cefaclor monohydrate are described. The new intermediate cefaclor is a particular crystalline form and possesses the same antibiotic properties as cefaclor monohydrate.
摘要翻译：描述了新型结晶头孢克洛的制备和这种产物转化为头孢克洛一水合物。新的中间体头孢克洛是一种特殊的结晶形式，具有与头孢克洛一水合物相同的抗生素特性。

18. 发明授权

US5532353A Process for the preparation of halogenated .beta.-lactam compounds 失效
标题翻译：卤代β-内酰胺化合物的制备方法
公开(公告)号：US5532353A
公开(公告)日：1996-07-02
申请号：US58714
申请日：1993-05-10
申请人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
发明人： Marco Da Col , Leone Dall'Asta , Irene Resta , Gianfranco Cainelli , Michele Contento , Mauro Panunzio , Achille Umani Ronchi
IPC分类号： C07D501/00 , C07D501/59 , C07D501/02
CPC分类号： C07D501/00
摘要： There is described the preparation of halogenated .beta.-lactam derivatives by introduction of a chlorine atom in the 3-position of the cephem nucleus starting from a 3-sulfonyloxycephem. Such starting materials are reacted with a chlorine ions donor in a basic medium.
摘要翻译：描述了由3-磺酰氧基头孢烯引入头孢烯核的3-位上的氯原子制备卤代β-内酰胺衍生物。这样的原料与碱性介质中的氯离子供体反应。

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