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1. 发明申请

WO2021206309A1 PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF DISEASES CAUSED BY SARS-COV-2 审中-公开
公开(公告)号：WO2021206309A1
公开(公告)日：2021-10-14
申请号：PCT/KR2021/003462
申请日：2021-03-19
申请人： DONG WHA PHARM. CO., LTD.
发明人： YOON, Joo Byoung , HWANG, Yun Ha , LEE, Ma Se , LEE, Hyun Yong
IPC分类号： A61K36/19 , A61K31/36 , A61P31/14 , A61P11/00 , A23L33/105
摘要： The present invention relates to a pharmaceutical composition for preventing or treating COVID-19 diseases, comprising an organic solvent extract of Justicia procumbens as an effective ingredient, a pharmaceutical composition for preventing or treating COVID-19 diseases, comprising justicidin-A as an effective ingredient, a pharmaceutical composition for preventing or treating COVID-19 diseases, comprising justicidin-B as an effective ingredient, or a pharmaceutical composition for preventing or treating COVID-19 diseases, comprising 6' hydroxyl justicidin-B as an effective ingredient, and a food composition thereof for preventing or ameliorating COVID-19 diseases. According to the present invention, an anhydrous ethanol extract of Justicia procumbens, justicidin-A, justicidin-B, and 6' hydroxyl justicidin-B effectively inhibit SARS-CoV-2 virus, and thus may effectively prevent, treat, or ameliorate diseases caused by SARS-CoV-2 virus.

2. 发明申请

WO2011013992A2 R-7-(3-AMINOMETHYL-4-METHOXYIMINO-3-METHYL-PYRROLIDIN-1-YL)-1-CYCLOPROPYL-6-FLUORO-4-OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID AND L-ASPARTIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR ANTIMICROBIAL 审中-公开
标题翻译： R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]萘啶-3- - 羧酸和L-阿糖酸盐，其制备方法和包含其的药物组合物
公开(公告)号：WO2011013992A2
公开(公告)日：2011-02-03
申请号：PCT/KR2010/004938
申请日：2010-07-27
申请人： DONG WHA PHARM. CO., LTD. , CHOI, Dong Rack , YANG, Jin , YOON, Sue Hye , PYUN, Sung Jae , KIM, Seung Hwan , SEONG, Seung-Kyoo , RYU, Jei Man
发明人： CHOI, Dong Rack , YANG, Jin , YOON, Sue Hye , PYUN, Sung Jae , KIM, Seung Hwan , SEONG, Seung-Kyoo , RYU, Jei Man
IPC分类号： C07D403/04 , C07D487/04 , A61K31/445 , A61P31/00
CPC分类号： C07D215/56 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K9/4858 , A61K31/4375 , C07C229/24 , C07D471/04 , C07D487/04 , C07D498/06
摘要： Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.
摘要翻译：本文公开了R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8] 萘啶-3-羧酸和L-天冬氨酸盐，其制备方法和包含其的抗微生物剂的药物组合物。因为R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]萘啶 -3-羧酸和L-天冬氨酸盐比常规使用的盐酸盐和其他盐（D-天冬氨酸盐和磷酸盐）更易溶解，毒性更小，作为抗微生物剂具有较少的副作用，该盐可用于口服和注射给药。

3. 发明申请

WO2012134126A2 USE OF COMPOUNDS ISOLATED FROM MORUS BARK 审中-公开
标题翻译：使用从MORUS BARK分离的化合物
公开(公告)号：WO2012134126A2
公开(公告)日：2012-10-04
申请号：PCT/KR2012/002162
申请日：2012-03-26
申请人： DONG WHA PHARM. CO., LTD. , CHANG, Hwan-Bong , YOON, Joo-Byoung , LEE, Hyun-Yong , CHOI, Hyun-Sik , LEE, Hyung-Bok
发明人： CHANG, Hwan-Bong , YOON, Joo-Byoung , LEE, Hyun-Yong , CHOI, Hyun-Sik , LEE, Hyung-Bok
IPC分类号： A61K31/353
CPC分类号： A61K31/352 , A23L33/10 , A61K31/05 , A61K31/353
摘要： The present invention provides an AGE inhibitor and a health functional food for inhibiting an occurrence of diabetic complications. Particularly, the present invention comprises a compound selected from the group consisting of mulberrofuran G, mulberrofuran K, kuwanon G, kuwanon Z, oxyresveratrol, 2`,4`,5,7-tetrahydroxyflavanone, morusignin L and dihydromorin isolated from Morus Bark as an active ingredient. The compounds disclosed above inhibit the production of AGE which is a causative substance of diabetic complications. Thus, the compounds could be used as an AGE inhibitor and a health functional food for inhibiting diabetic nephropathy, diabetic retinopathy and diabetic neuropathy.
摘要翻译：本发明提供了AGE抑制剂和用于抑制糖尿病并发症发生的健康功能性食品。特别地，本发明包括选自以下的化合物：由桑树呋喃G，呋喃孢子K，库布宁G，奎宁酮Z，氧基维生素，2'，4'，5,7-四羟基黄烷酮，morusignin L和从Morus Bark分离的二氢肌醇有效成分。上述公开的化合物抑制作为糖尿病并发症的病因的AGE的产生。因此，该化合物可用作AGE抑制剂和用于抑制糖尿病性肾病，糖尿病性视网膜病变和糖尿病性神经病变的健康功能食品。

4. 发明申请

WO2011083955A2 METHOD FOR MANUFACTURING CRYSTALLINE FORM (I) OF CLOPIDOGREL HYDROGEN SULPHATE 审中-公开
标题翻译：制备氢化萘磺酸盐的结晶形式（I）的方法
公开(公告)号：WO2011083955A2
公开(公告)日：2011-07-14
申请号：PCT/KR2011/000038
申请日：2011-01-05
申请人： DONG WHA PHARM. CO., LTD. , OH, Yoon Seok , SHIN, Dong Hyuk , JUNG, Jin Yong
发明人： OH, Yoon Seok , SHIN, Dong Hyuk , JUNG, Jin Yong
IPC分类号： C07D495/04 , C07D495/02
CPC分类号： C07D495/04
摘要： The present invention provides a method for manufacturing a crystalline form (I) of clopidogrel hydrogen sulphate(clopidogrel hydrogen sulfate), including reacting a clopidogrel free base with concentrated sulfuric acid in the presence of a mixed solvent containing water in an amount of 4 to 14% by weight based on the weight of the clopidogrel free base and 2-butanol.
摘要翻译：本发明提供硫酸氢氯吡格雷（硫酸氢氯吡格雷）的结晶形式（I）的制造方法，其包括使氯吡格雷游离碱与浓硫酸在含有4〜14的水的混合溶剂的存在下反应基于氯吡格雷游离碱和2-丁醇的重量的重量％。

5. 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。

6. 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。

7. 发明申请

WO2014168458A1 USE OF COMPOUNDS ISOLATED FROM MORUS BARK 审中-公开
标题翻译：使用从MORUS BARK分离的化合物
公开(公告)号：WO2014168458A1
公开(公告)日：2014-10-16
申请号：PCT/KR2014/003163
申请日：2014-04-11
申请人： DONG WHA PHARM. CO., LTD.
发明人： CHANG, Hwan Bong , YOON, Joobyoung , LEE, Hyunyong , RHO, Yang Kook
IPC分类号： A61K31/05 , A61K31/045 , A61K36/605 , A61P3/10
CPC分类号： A61K36/605 , A23L33/105 , A61K31/352
摘要： The present invention relates to pharmaceutical composition for the prevention and treatment of diabetic complications, or health food, comprising Cathayanin B or Kuwanol A isolated from Morus Bark. The compound Cathayanin B according to the present invention is isolated from Morus Bark and inhibits the formation of advanced glycation end-products (AGEs), which cause diabetic complications, and inhibits aldose reductase activity. Kuwanol A, another compound isolated from Morus Bark, inhibits TGF-β1 signaling. Therefore, the pharmaceutical composition or health food comprising Cathayanin B or Kuwanol A according to the present invention can be used to inhibit diabetic nephritis, diabetic retinopathy, and diabetic neuropathy, which are diabetic complications. In particular, Kuwanol A can also be used for pharmaceutical composition for the prevention and treatment of various fibrosis and metastasis conditions as well as health food to improve said conditions.
摘要翻译：本发明涉及用于预防和治疗糖尿病并发症的药物组合物或保健食品，其包含从桑树分离的Cathayanin B或Kuwanol A。根据本发明的化合物Cathayanin B从桑树皮分离并抑制引起糖尿病并发症并抑制醛糖还原酶活性的晚期糖基化终产物（AGEs）的形成。 Kuwanol A，从Morus Bark分离的另一种化合物抑制TGF-β1信号传导。因此，根据本发明的包含Cathayanin B或Kuwanol A的药物组合物或保健食品可用于抑制作为糖尿病并发症的糖尿病性肾炎，糖尿病性视网膜病变和糖尿病性神经病变。特别地，Kuwanol A也可用于预防和治疗各种纤维化和转移病症的药物组合物以及保健食品以改善所述条件。

8. 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。

9. 发明申请

WO2010064845A2 THE PHARMACEUTICAL COMPOSITION OR THE FUNCTIONAL FOODS FOR THE TREATMENT OR PREVENTION OF OBESITY COMPRISING THE EXTRACT FROM MYRISTICA FRAGRANS HOUTTUYN 审中-公开
标题翻译：用于治疗或预防肥胖症的药物组合物或功能性食品，包含来自香菇提取物
公开(公告)号：WO2010064845A2
公开(公告)日：2010-06-10
申请号：PCT/KR2009/007158
申请日：2009-12-02
申请人： DONG WHA PHARM. CO., LTD. , RYU, Jei-Man , LEE, Seung-Ryul , BAEK, Nam-Hyun , LEEM, Moon-Jung , SEONG, Seung-Kyoo , LEE, Sang-Ho
发明人： RYU, Jei-Man , LEE, Seung-Ryul , BAEK, Nam-Hyun , LEEM, Moon-Jung , SEONG, Seung-Kyoo , LEE, Sang-Ho
IPC分类号： A61K36/185 , A61P3/04 , A23L1/30
CPC分类号： A23L33/105
摘要： There is provided a pharmaceutical composition and functional foods for the prevention and treatment of obesity, comprising an extract from Myristica fragrans Houttuyn as an effective component. The Myristica fragrans Houttuyn extract may be used for the pharmaceutical composition for the prevention and treatment of obesity caused by the intake of high-fat diets by suppressing an increase in body weights caused by the intake of high-fat diets, an increase in weights of periovarian fats and an accumulation of abdominal fats caused by the hypertrophy of adipocytes (fat cells). Furthermore, the extract from Myristica fragrans Houttuyn may be effectively used for the functional foods for the amelioration and prevention of obesity in humans including juveniles, adults and the old since it is used to ameliorate and prevent the obesity caused by the intake of high-fat diets.
摘要翻译：本发明提供了用于预防和治疗肥胖的药物组合物和功能性食品，其包含来自肉豆蔻提取物鱼腥草提取物作为有效成分。肉豆蔻鱼腥草提取物可以用于通过抑制由高脂肪饮食摄入所引起的体重增加，由高脂肪饮食引起的体重增加来预防和治疗由摄入高脂肪饮食引起的肥胖症的药物组合物卵巢脂肪和由脂肪细胞（脂肪细胞）肥大引起的腹部脂肪的积累。此外，由于用于改善和预防由高脂肪摄入引起的肥胖症，因此可将来自肉豆蔻提取物的肉豆蔻提取物有效地用于改善和预防包括青少年，成人和老年人在内的肥胖症的功能性食品饮食。

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