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31. 发明授权

US3843642A Cephalosporin c derivatives 失效
标题翻译： CEPHALOSPORIN C衍生物
公开(公告)号：US3843642A
公开(公告)日：1974-10-22
申请号：US30613072
申请日：1972-11-13
申请人： LILLY CO ELI
发明人： BOTTORFF E , JACKSON B , STAMPER M
IPC分类号： C07D20060101 , C07D501/14 , C07D501/20 , C07D99/24
CPC分类号： C07D501/12
摘要： N-(4-chlorobenzoyl)- and N-(2,4-dichlorobenzoyl)-cephalosporin C values are useful in processes for separating the cephalosporin C values from fermentation liquors containing polysaccharide and proteinaceous impurities. These new intermediates can be used as starting materials in cleavage processes for forming 7-aminocephalosporin values, and the 7-amino cephalosporin values can be used to form cephalosporin antibiotics such as cephalothin, cephaloridine, and cephalexin.

32. 发明授权

US3819619A N-isobornyloxycarbonylcephalosporin c 失效
标题翻译： N-异丁酰胆碱酯
公开(公告)号：US3819619A
公开(公告)日：1974-06-25
申请号：US22916972
申请日：1972-02-24
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： HORII S , MIZOKAMI N , FUJINO M , OKUTANI T , SHINAGAWA S , OCHIAI M
IPC分类号： C07D213/74 , C07D501/12 , C07D501/28 , C07D99/24
CPC分类号： C07D213/74 , C07D501/12
摘要： THIS INVENTION RELATES TO N-ISOBORNYLOXYCARBONYLCEPHALOSPORON C WHICH IS USEFUL AS AN INTERMEDIATE FOR THE PRODUCTON OF CEPHALOSPORIN C AND OTHER CEPHALOSPORANIC ACID DERIVATIVES AND IS ALSO USEFUL AS AN ANTIMICROBIAL AGENT.

33. 发明授权

US3714157A PROCESS FOR THE DECOLORIZATION OF 7-[ alpha -(4-PYRIDYLTHIO)ACETAMIDO]CEPHALOSPORANIC ACID 失效
标题翻译： 7- [α-（4-吡啶基）乙酰氨基]癸酸的分解方法CEPHALOSPORANIC酸
公开(公告)号：US3714157A
公开(公告)日：1973-01-30
申请号：US3714157D
申请日：1970-10-23
申请人： BRISTOL MYERS CO
发明人： RICHARDSON E
IPC分类号： A23K20060101 , A61K20060101 , C07C20060101 , C07D501/12 , C07D501/34 , C07D99/24
CPC分类号： C07D501/12
摘要： The purification and decolorization of 7-( Alpha -(4pyridylthio)-acetamido)cephalosporanic acid has been accomplished by the recrystallization of the acid from dimethylformamide (DMF) containing a quantity of ascorbic acid. The essentially pure, colorless product crystallizes from solution as a DMF solvate.
摘要翻译：通过从含有一定量抗坏血酸的二甲基甲酰胺（DMF）中重结晶酸已经完成了7- [α-（4-吡啶硫基） - 乙酰胺基]头孢烷酸的纯化和脱色。基本上纯的无色产物作为DMF溶剂化物从溶液中结晶。

34. 发明授权

US3709880A Antibiotic purification process 失效
标题翻译：抗生素净化工艺
公开(公告)号：US3709880A
公开(公告)日：1973-01-09
申请号：US3709880D
申请日：1970-12-09
申请人： MERCK & CO INC
发明人： GOEGELMAN R , MILLER T
IPC分类号： C07D501/57 , C07D99/24
CPC分类号： C07D501/57 , C07D501/12
摘要： FERMENTATION BROTHS OR IMPURE SOLUTIONS CONTAINING 7(D-5-AMINO-5-CARBOXYVALERAMIDO)-3-(CARBAMOYLOXYMETHYL)-7-METHOXY-3-CEPHEM-4-CARBOXYLIC ACID, A SUBSTANCE HAVING ANTIBIOTIC ACTIVITY AGAINST GRAM-NEGATIVE AND GRAM-POSITIVE MICROORGANISMS, ARE PURIFIED USING ION EX CHANGE RESINS OR ADSORBENTS SUCH AS ACTIVATED CARBON AND POLY-ACRYLAMIDE OR DEXTRAN GELS.

35. 发明授权

US3634416A Purification of 7alpha-aminoarylacetamido delta**3-4-carboxy-cephalosporins 失效
公开(公告)号：US3634416A
公开(公告)日：1972-01-11
申请号：US3634416D
申请日：1969-04-03
申请人： GLAXO LAB LTD
发明人： SCHOFIELD HARRY
IPC分类号： A61K31/545 , C07D501/22 , C07D99/24
CPC分类号： C07D501/22 , A61K31/545 , C07D501/12 , C07D501/32
摘要： PURIFICATION OF A CEPHALOSPORIN DERIVATIVE HAVING A 7-AAMINOARYLACETAMIDO SIDE CHAIN BY PRECIPITATING AS A CRYSTALLINE SALT BY REACTION WITH COLLIDINE, A CORRESPONDING COMPOUND HAVING THE AMINO GROUP PROTECTED, SEPARATING THE SALT CONVERTING THE SALT TO THE CORRESPONDING ACID, THE PROTECTIVE GROUP BEING REMOVED.

36. 发明申请

US20180111949A1 NOVEL INDUSTRIAL CRYSTALLIZATION METHOD OF CEFUROXIME SODIUM AND PREPARATION THEREOF 审中-公开
公开(公告)号：US20180111949A1
公开(公告)日：2018-04-26
申请号：US15687377
申请日：2017-08-25
申请人： HAINAN LINGKANG PHARMACEUTICAL CO., LTD , TIANJIN UNIVERSITY
发明人： Linggang TAO , Hongxun HAO , Jingkang WANG
IPC分类号： C07D501/12 , A61K9/00 , A61K9/14 , A61K31/546 , B01D11/04 , B01D9/00
CPC分类号： C07D501/12 , A61K9/0019 , A61K9/14 , A61K31/546 , B01D9/0054 , B01D11/0411 , B01D2009/0095 , C07B2200/13 , Y02P20/544
摘要： It discloses a new industrial crystallization method of Cefuroxime Sodium, wherein supercritical fluid extraction technology and traditional crystalline technology are combined to realize the recrystallization of Cefuroxime Sodium. Processes such as extraction, adsorption, crystallization and drying are carried out with a supercritical fluid, a solvent, an extraction cell and a crystallization tank to realize the recrystallization of Cefuroxime Sodium under a specific pressure at a specific temperature.

37. 发明授权

US09834567B1 Crystalline form of cefamandole nafate compound, preparation and preparing method thereof 有权
公开(公告)号：US09834567B1
公开(公告)日：2017-12-05
申请号：US15687359
申请日：2017-08-25
申请人： TIANJIN UNIVERSITY , HAINAN LINGKANG PHARMACEUTICAL CO., LTD
发明人： Hongxun Hao , Linggang Tao , Fang He , Baohong Hou , Jingkang Wang , Jun Lv , Qiuxiang Yin , Yongli Wang , Junbo Gong , Chuang Xie , Ying Bao
IPC分类号： C07D501/36 , C07D501/12
CPC分类号： C07D501/36 , C07B2200/13 , C07D501/12
摘要： A novel crystalline form is defined by diffraction angle 2θ° of X-ray powder diffraction pattern and characteristic peak of differential scanning calorimetry (DSC). The novel crystalline form of Cefamandole Nafate is prepared as follows: adding Cefamandole Nafate in solid state to an organic solvent to form a suspension with a concentration of 0.04˜0.3 g/ml, stirring the suspension at 40˜50° C. for a period of time, and then cooling to 5˜15° C. at certain cooling rate, continuing to stir for a period of time, then suction filtrating the obtained suspension, the resulting filer cake is Cefamandole Nafate as wet product, which is dried to constant weight to provide the novel crystalline form of Cefamandole Nafate as final product.

38. 发明申请

US20170044184A1 NEW CRYSTAL FORM OF CEFATHIAMIDINE COMPOUND AND PREPARATION METHOD THEREFOR 有权
标题翻译：新戊酰胺化合物的新晶体形式及其制备方法
公开(公告)号：US20170044184A1
公开(公告)日：2017-02-16
申请号：US15304824
申请日：2015-11-20
申请人： TIANJIN UNIVERSITY , HAINAN LINGKANG PHARMACEUTICAL CO., LTD
发明人： Hongxun HAO , Linggang TAO , Zhihong SUN , Baohong HOU , Jun LV , Qiuxiang YIN , Yongli WANG , Junbo GONG , Chuang XIE , Ying BAO
IPC分类号： C07D501/60
CPC分类号： C07D501/60 , C07B2200/13 , C07D501/12 , C07D501/28
摘要： A novel crystalline form of Cefathiamidine compound and its preparation method, characterizing in its X-ray powder diffraction pattern and differential scanning calorimetry thermogram. Dissolving Cefathiamidine compound with a purity of 98% or higher in a solvent at a temperature of 30˜45° C. to form a solution, whose concentration is controlled within 0.05˜0.2 g/mL, and then adding a solventing-out agent to the solution, wherein the amount of the solventing-out agent is 3˜5 times (in volume) of that of the solvent; followed by cooling the solution down to 0˜10° C. at a rate of 0.2˜1° C./min; continuing to stir for 1˜3 hours, and separating the obtained solid-liquid suspension to provide a novel crystalline form of Cefathiamidine compound after drying.
摘要翻译：尖晶石化合物的新型结晶形式及其制备方法，其X射线粉末衍射图和差示扫描量热法热分析图表征。在溶剂中在30〜45℃的温度下溶解纯度为98％以上的头孢硫脒化合物，形成浓度为0.05〜0.2g / mL的溶液，然后加入溶剂溶剂，其中溶剂量为溶剂量的3〜5倍（体积）; 然后以0.2〜1℃/分钟的速度将溶液冷却至0〜10℃; 继续搅拌1〜3小时，分离得到的固液悬浮液，干燥后提供新型的头孢噻肟化合物结晶形式。

39. 发明授权

US09090631B2 Process for purifying cefotiam hydrochloride 有权
标题翻译：盐酸头孢菌素的方法
公开(公告)号：US09090631B2
公开(公告)日：2015-07-28
申请号：US13997618
申请日：2011-04-14
申请人： Linggang Tao
发明人： Linggang Tao
IPC分类号： C07D501/12 , C07D501/36
CPC分类号： C07D501/12 , C07D501/36
摘要： A method for treating cefotiam hydrochloride, comprises the following steps: step 1), dissolving the raw material cefotiam hydrochloride in water, treating it with an acidic salt, then cooling it, and filtering the precipitate to obtain an aqueous filtrate; step 2), adding a water-immiscible solvent to the above aqueous solution for extraction, and then separating the organic phase containing impurities to obtain an aqueous solution containing cefotiam hydrochloride; step 3) adding to the aqueous solution a poor solvent of cefotiam hydrochloride and controlling the temperature for recrystallization, washing the educed crystals by centrifugation, and drying them to obtain purified cefotiam hydrochloride. The cefotiam content of the refined cefotiam hydrochloride obtained by the method of the present invention is not less than 86%, the content of polymeric impurities is less than 0.3%, and the content of insoluble microparticles in the injection prepared therefrom is quite low.
摘要翻译：一种治疗头孢曲松盐酸盐的方法，包括以下步骤：步骤1）将原料盐酸头孢氨酸溶于水中，用酸性盐处理，然后冷却，过滤沉淀得到水性滤液; 步骤2），向上述水溶液中加入与水不混溶的溶剂萃取，然后分离含有杂质的有机相，得到含有头孢氨苄盐酸盐的水溶液; 步骤3）向水溶液中加入头孢氨苄盐酸盐的不良溶剂并控制重结晶温度，通过离心洗涤所得结晶，并干燥，得到纯化的盐酸头孢氨酸。通过本发明方法得到的精制头孢他坦盐酸头孢氨肟含量不低于86％，聚合物杂质含量小于0.3％，并且由其制备的注射液中的不溶性微粒含量相当低。

40. 发明授权

US08853389B2 Process for refining cefmetazole sodium 有权
标题翻译：头孢唑唑钠精制方法
公开(公告)号：US08853389B2
公开(公告)日：2014-10-07
申请号：US13997613
申请日：2011-04-14
申请人： Linggang Tao
发明人： Linggang Tao
IPC分类号： C07D501/12 , C07B63/00
CPC分类号： C07D501/12 , C07B63/00
摘要： The present invention relates to a novel process for refining Cefmetazole sodium, comprising the steps of: 1) dissolving Cefmetazole sodium material in water, and extracting after adding a water-immiscible organic solvent(s), followed by separating the organic phase containing impurities, to provide an aqueous phase containing Cefmetazole sodium; 2) treating by adding an alkoxide of alkali metal or alkaline earth metal into the above aqueous phase, followed by filtrating the precipitate, to provide an aqueous filtrate; and 3) adding ethanol or acetone in the aqueous solution and recrystallizing, followed by centrifuging and washing the resultant crystals, to provide the refined and purified Cefmetazole sodium after drying. The purity of Cefmetazole sodium material can be greatly improved by the process of the present invention.
摘要翻译：本发明涉及一种精细头孢咪唑钠的新方法，包括以下步骤：1）将头孢美唑钠物质溶解在水中，加入不溶于水的有机溶剂萃取，然后分离含有杂质的有机相，提供含有头孢美唑钠的水相; 2）通过向上述水相中加入碱金属或碱土金属的醇盐进行处理，然后过滤沉淀物，得到水性滤液; 和3）在水溶液中加入乙醇或丙酮并重结晶，然后离心和洗涤所得晶体，干燥后提供精制和纯化的头孢唑唑钠。通过本发明的方法可以大大改善头孢美唑钠材料的纯度。

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