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1. 发明授权

US08178521B2 Cefazolin sodium pentahydrate crystal and its molecular assembly preparation method 有权
标题翻译：头孢唑啉五水合物晶体及其分子装配制备方法
公开(公告)号：US08178521B2
公开(公告)日：2012-05-15
申请号：US12085110
申请日：2006-09-15
申请人： Jingkang Wang , Yuxin Qian , Meijing Zhang , Jiehua Wu , Zhan'ao Yang
发明人： Jingkang Wang , Yuxin Qian , Meijing Zhang , Jiehua Wu , Zhan'ao Yang
IPC分类号： C07D501/36 , C07D501/02 , C07D501/12 , C07D501/59 , A61K31/545
CPC分类号： C07D501/36 , C07D501/02 , C07D501/12
摘要： The present invention relates to cefazolin sodium pentahydrate crystal and a method for assembly and preparation of the crystal molecule. The cefazolin sodium pentahydrate crystal molecule contains five water molecules, orthorhombic system, space group of C222(1), in which sodium ion is bonded to the cefazolin molecule with a coordinate bond. The method for assembly and preparation of cefazolin sodium pentahydrate crystal molecule are: adding a solvent to a reactor equipped with a jacket, adding cefazolin acid and a sodium salt, heating until the reaction solution is clear, stirring continuously, adjusting pH, upon the completion of the reaction, transferring the liquid into a jacketed crystallizer, adding crystal seeds or nucleating spontaneously, controlling cooling, slowly adding a antisolvent. The particle size of cefazolin sodium pentahydrate crystal according to the present invention is adjustable, and the distribution of particle size is concentrated, the product has good flowability, smooth surface, high crystallinity, good stability, and rapid dissolving rate.
摘要翻译：本发明涉及头孢唑啉五水合物晶体及其制备方法。头孢唑啉五水合物晶体分子含有五个水分子，斜方晶系，C222（1）的空间基团，其中钠离子与头孢唑啉分子键合。头孢唑啉五水合物晶体分子的组装和制备方法是：向装有夹套的反应器中加入溶剂，加入头孢唑啉酸和钠盐，加热至反应液澄清，连续搅拌，调整pH值，完成后将液体转移到夹套结晶器中，加入晶种或自发成核，控制冷却，缓慢加入抗溶剂。本发明头孢唑啉五水合物晶体的粒度可调，粒径分布浓缩，产品流动性好，表面光滑，结晶度高，稳定性好，溶解速度快。

2. 发明申请

US20090299056A1 Cefazolin Sodium Pentahydrate Crystal and Its Molecular Assembly Preparation Method 有权
标题翻译：头孢唑啉五水合物晶体及其分子装配制备方法
公开(公告)号：US20090299056A1
公开(公告)日：2009-12-03
申请号：US12085110
申请日：2006-09-15
申请人： Jingkang Wang , Yuxin Qian , Meijing Zhang , Jiehua Wu , Zhan'ao Yang
发明人： Jingkang Wang , Yuxin Qian , Meijing Zhang , Jiehua Wu , Zhan'ao Yang
IPC分类号： C07D501/59
CPC分类号： C07D501/36 , C07D501/02 , C07D501/12
摘要： The present invention relates to cefazolin sodium pentahydrate crystal and a method for assembly and preparation of the crystal molecule. The cefazolin sodium pentahydrate crystal molecule contains five water molecules, orthorhombic system, space group of C222(1), in which sodium ion is bonded to the cefazolin molecule with a coordinate bond. The method for assembly and preparation of cefazolin sodium pentahydrate crystal molecule are: adding a solvent to a reactor equipped with a jacket, adding cefazolin acid and a sodium salt, heating until the reaction solution is clear, stirring continuously, adjusting pH, upon the completion of the reaction, transferring the liquid into a jacketed crystallizer, adding crystal seeds or nucleating spontaneously, controlling cooling, slowly adding a antisolvent. The particle size of cefazolin sodium pentahydrate crystal according to the present invention is adjustable, and the distribution of particle size is concentrated, the product has good flowability, smooth surface, high crystallinity, good stability, and rapid dissolving rate.
摘要翻译：本发明涉及头孢唑啉五水合物晶体及其制备方法。头孢唑啉五水合物晶体分子含有五个水分子，斜方晶系，C222（1）的空间基团，其中钠离子与头孢唑啉分子键合。头孢唑啉五水合物晶体分子的组装和制备方法是：向装有夹套的反应器中加入溶剂，加入头孢唑啉酸和钠盐，加热至反应液澄清，连续搅拌，调整pH值，完成后将液体转移到夹套结晶器中，加入晶种或自发成核，控制冷却，缓慢加入抗溶剂。本发明头孢唑啉五水合物晶体的粒径可调，粒径分布浓缩，产品流动性好，表面光滑，结晶度高，稳定性好，溶解速度快。

3. 发明申请

US20090092662A1 LIPOSOME FORMULATIONS OF BORONIC ACID COMPOUNDS 审中-公开
标题翻译：硼酸化合物的制备方法
公开(公告)号：US20090092662A1
公开(公告)日：2009-04-09
申请号：US12195795
申请日：2008-08-21
申请人： Anthony Huang , Bing Luo , Jingkang Wang , Yuanpeng Zhang
发明人： Anthony Huang , Bing Luo , Jingkang Wang , Yuanpeng Zhang
IPC分类号： A61K9/127 , A61K31/69 , A61P35/00
CPC分类号： A61K31/69 , A61K9/1271 , A61K41/0095 , A61K47/6911
摘要： A liposome composition comprised of liposomes having a peptide boronic acid proteasome inhibitor compound entrapped in the liposomes is described. More specifically, liposomes having a compound of Formula I or II entrapped in the interior aqueous compartment are loaded with a peptide boronic acid compound, to form a boronate ester compound inside the liposomal aqueous compartment. In one embodiment, the liposomes have an outer coating of hydrophilic polymer chains and are used to treat a solid tumor in a subject.
摘要翻译：描述了包含脂质体中包含肽硼酸蛋白酶体抑制剂化合物的脂质体的脂质体组合物。更具体地说，将含有式I或II化合物的脂质体包埋在内部水性室中，装载有肽硼酸化合物，以在脂质体水性隔室内形成硼酸酯化合物。在一个实施方案中，脂质体具有亲水性聚合物链的外涂层，并且用于治疗受试者中的实体瘤。

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