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1. 发明申请

WO2015178663A1 AN IMPROVED MANUFACTURING METHOD OF ZABOFLOXACIN 审中-公开
标题翻译： ZABOFLOXACIN的改进制造方法
公开(公告)号：WO2015178663A1
公开(公告)日：2015-11-26
申请号：PCT/KR2015/005009
申请日：2015-05-19
申请人： DONG WHA PHARM. CO., LTD.
发明人： CHOI, Dong-Rack , LIM, Jae-Kyung , CHOI, Jung-Uk , SHIN, Dong-Hyuk , KIM, Seung-Hwan , WON, Dae-Yeon , KIM, Jung-Hwan
IPC分类号： C07D471/04 , C07D401/04 , C07D403/04
CPC分类号： C07D471/04 , C07D487/10
摘要： The present invention provides an improved method of manufacturing Zabofloxacin D-aspartate. The present invention provides a novel method of manufacturing 8-methoxyimino-2,6-diaza-spiro[3,4]octane-2-carboxylic acid t-butyl ester succinate (TBDCS) or 2-(2,2,2-trifluoro-acetyl)-2,6-diaza-spiro[3,4]octan-8-one O-methyloxime methanesulfonate (TDMOS), which are separately the starting materials for manufacturing Zabofloxacin D-aspartate. The manufacturing method according to the present invention is suitable for mass production of Zabofloxacin D-aspartate for it enables manufacturing in high yield and high quality (HPLC purity ≥ 99.5%) as well as reducing the unit cost of production by using only 1.0~1.1 equivalents of TBDCS or TDMOS in a substitution reaction.
摘要翻译：本发明提供了一种制备扎波沙星D-天冬氨酸的改进方法。本发明提供了8-甲氧基亚氨基-2,6-二氮杂 - 螺[3,4]辛烷-2-甲酸叔丁酯琥珀酸酯（TBDCS）或2-（2,2,2-三氟乙酰基）-2,6-二氮杂 - 螺[3,4]辛-8-酮O-甲基肟甲磺酸酯（TDMOS），其分别是制备扎波沙星D-天冬氨酸的起始原料。根据本发明的制造方法适用于批量生产Zabofloxacin D-天冬氨酸酯，因为它能够以高产率和高质量（HPLC纯度≥99.5％）制造，并且通过仅使用1.0〜1.1降低单位生产成本在替代反应中TBDCS或TDMOS的等同物。

2. 发明申请

WO2015133803A1 1-CYCLOPROPYL-6-FLUORO-7-(8-METHOXYIMINO-2,6-DIAZA-SPIRO[3,4]OCT-6-YL)-4-OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID D-ASPARTATE HYDRATES AND AN ANTIBACTERIAL PHARMACEUTICAL COMPOSITIONS COMPRISING THEIR HYDRATES 审中-公开
标题翻译： 1-环丙基-6-氟-7-（8-甲氧基-2,6-二氮杂 - 螺[3,4]辛-6-基）-4-氧代-1,4-二氢 - [1,8]二氮杂萘 -3-羧酸D-ASPARTATE水解物和包含其水合物的抗菌药物组合物
公开(公告)号：WO2015133803A1
公开(公告)日：2015-09-11
申请号：PCT/KR2015/002065
申请日：2015-03-04
申请人： DONG WHA PHARM. CO., LTD.
发明人： CHOI, Dong-Rack , LIM, Jae-Kyung , CHANG, Hwan-Bong , BAEK, Nam-Hyun , KIM, Seung-Hwan , KIM, Gun-Gook
IPC分类号： C07D487/10 , C07D471/04 , A61K31/4375 , A61P31/04
CPC分类号： A61K31/4375 , C07D519/00
摘要： The present invention relates to 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3,4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid D-aspartate hydrates and an antibacterial composition comprising their hydrates. The present invention provides stable zabofloxacin D-aspartate hydrates wherein adsorption and desorption of water hardly occur, and provides specifically zabofloxacin D-aspartate sesquihydrate. Because the zabofloxacin D-aspartate hydrates according to the present invention hardly absorb moisture, they have an outstanding physicochemical property. Therefore, the drugs comprising zabofloxacin D-aspartate hydrate of the present invention do not easily break, especially in its tablet form, and changes little in the content of the main ingredient, thus exhibiting an excellent pharmaceutical stability.
摘要翻译：本发明涉及1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3,4]辛-6-基）-4-氧代-1,4-二氢 - [ 1,8]二氮杂萘-3-羧酸D-天冬氨酸水合物和包含其水合物的抗菌组合物。本发明提供稳定的扎波沙星D-天冬氨酸盐水合物，其中几乎不发生水的吸附和解吸，并且提供特异性的扎布沙星D-天冬氨酸倍半水合物。由于根据本发明的扎波沙星D-天冬氨酸盐水合物几乎不吸收水分，所以它们具有突出的物理化学性质。因此，本发明的包含扎布沙星D-天冬氨酸水合物的药物不容易破裂，特别是片剂形式，并且主要成分的含量变化很小，因此表现出优异的药物稳定性。

3. 发明申请

WO2011102645A2 AN IMPROVED PROCESS FOR PREPARING TELMISARTAN 审中-公开
标题翻译：改进TELMISARTAN的改进方法
公开(公告)号：WO2011102645A2
公开(公告)日：2011-08-25
申请号：PCT/KR2011/001041
申请日：2011-02-17
申请人： DONG WHA PHARM. CO., LTD. , OH, Yoon-Seok , LIM, Jae-Kyung , CHOI, Jung-Uk , KWON, O-Jin , LEE, Jun-Sang
发明人： OH, Yoon-Seok , LIM, Jae-Kyung , CHOI, Jung-Uk , KWON, O-Jin , LEE, Jun-Sang
IPC分类号： C07D403/10 , C07D403/04 , C07D403/06
CPC分类号： C07D403/04
摘要： The present invention relates to an improved process for preparing telmisartan from 4-methyl-6-(1-methyl-1 H -benzimidazole-2-yl)-2-propyl-1 H -benzimidazole and 2-[4-(bromomethyl)phenyl] benzoate by using condensation reaction and hydrolysis reaction wherein the condensation reaction is performed to prepare an intermediate by using mixed solvent of dimethyl sulfoxide and isopropanol as reaction solvent using dimethyl sulfoxide of 0.5~1.5 times and isopropanol of 1.5~4.5 times on the basis of the usage of 4-methyl-6-(1-methyl-1 H -benzimidazole-2-yl)-2-prophyl-1 H -benzimidazole and the hydrolysis reaction is performed to cause the reaction in mixed solvent of methanol of 7~9 times and purified water of 5~7 times on the basis of the intermediate. The process for preparing telmisartan according to the present invention provides a simple preparing process for mass production and improves a manufacturing yield with high purity by eliminating an additional process for removing an inorganic salt as a byproduct due to a base used in the condensation reaction and the hydrolysis reaction.
摘要翻译：本发明涉及从4-甲基-6-（1-甲基-1H-苯并咪唑-2-基）-2-丙基-1H-苯并咪唑和2- [4-（溴甲基）苯基]苯并咪唑制备替米沙坦的改进方法，苯甲酸酯通过使用缩合反应和水解反应，其中通过使用二甲基亚砜和异丙醇的混合溶剂作为反应溶剂进行缩合反应，使用0.5〜1.5倍的二甲基亚砜和1.5〜4.5倍的异丙醇，基于使用4-甲基-6-（1-甲基-1H-苯并咪唑-2-基）-2-预防-1H-苯并咪唑并进行水解反应，使甲醇混合溶剂中的反应为7〜9次，纯化水为中间体5〜7次。根据本发明的替米沙坦制备方法提供了一种简单的批量制备方法，通过除去由于缩合反应中使用的碱作为副产物而除去无机盐的附加方法，提高了高纯度的制造产率，水解反应。

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