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    COMPOSITE PREPARATION
    1.
    发明申请
    COMPOSITE PREPARATION 审中-公开
    复合制剂

    公开(公告)号：US20110038931A1

    公开(公告)日：2011-02-17

    申请号：US12919000

    申请日：2009-02-21

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Sang Ouk Sun ,  Jung-won Bae

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Sang Ouk Sun ,  Jung-won Bae

    IPC分类号： A61K9/22 ,  A61K31/616 ,  A61K9/14 ,  A61P9/00

    CPC分类号： A61K9/2077 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2081 ,  A61K9/209 ,  A61K9/2866 ,  A61K9/4808 ,  A61K9/5078 ,  A61K9/5084 ,  A61K31/4365 ,  A61K31/60 ,  A61K31/616 ,  A61K2300/00

    摘要： The present invention provides a combination preparation which comprises: a prior-release section comprising aspirin or a pharmaceutically acceptable salt thereof as a pharmacologically active component; and a delayed-release section comprising clopidogrel, an isomer thereof or a pharmaceutically acceptable salt thereof as a pharmacologically active component. The combination preparation of the present invention exhibits a far better effect in preventing platelet aggregation than does simultaneous oral therapy or treatment with the respective single preparations, and not only can it improve the patient's drug-taking compliance by administration once a day but it can also reduce the adverse reactions which follow long-term administration of aspirin. The combination preparation of the present invention is also advantageous in that it exhibits an outstanding effect in inhibiting blood platelet aggregation despite a reduction in the amount of aspirin ingested, and in that it converts clopidogrel resistance into susceptibility and prevents serious adverse reactions caused by clopidogrel resistance and in that it can be stored over the longer term since it is stable under common storage conditions.

    摘要翻译： 本发明提供了一种组合制剂，其包含：包含阿司匹林或其药学上可接受的盐作为药理活性成分的先前释放部分; 以及包含氯吡格雷，其异构体或其药学上可接受的盐作为药理活性成分的延迟释放部分。 本发明的组合制剂表现出比同时口服治疗或用单一制剂治疗的预防血小板聚集效果好得多，并且不仅可以通过一天一次的给药来改善患者的药物依从性，而且还可以 减少长期服用阿司匹林后的不良反应。 本发明的组合制剂的优点还在于尽管阿司匹林的摄取量减少，但是其表现出抑制血小板聚集的突出效果，并且将氯吡格雷耐药性转化为易感性并防止由氯吡格雷抗性引起的严重不良反应 并且由于它在常见的储存条件下是稳定的，因此可以长期储存。

    COMBINATION PREPARATION COMPRISING INHIBITOR OF HMG-COA REDUCTASE AND ASPIRIN AND METHOD FOR MANUFACTURING THE SAME
    2.
    发明申请
    COMBINATION PREPARATION COMPRISING INHIBITOR OF HMG-COA REDUCTASE AND ASPIRIN AND METHOD FOR MANUFACTURING THE SAME 审中-公开
    包含HMG-COA还原酶和阿司匹林的抑制剂的组合制剂及其制备方法

    公开(公告)号：US20120015032A1

    公开(公告)日：2012-01-19

    申请号：US12672630

    申请日：2008-08-08

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Sang Ouk Sun

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Sang Ouk Sun

    IPC分类号： A61K9/28 ,  A61P9/00 ,  A61P9/10 ,  A61K31/60

    CPC分类号： A61K31/35 ,  A61K31/616 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to a chronotherapeutically combined pharmaceutical formulation for preventing and treating cardiovascular diseases, which is based on the principle of administering a plurality of drugs at certain time intervals (chronotherapy). Specifically, the combined pharmaceutical formulation comprises a HMG-CoA reductase inhibitor, such as simvastatin, and aspirin. Because the combined pharmaceutical formulation was developed based on the principle of administering drugs at certain time intervals, so-called chronotherapy, it shows an excellent effect of preventing or treating cardiovascular disease compared to those of the individual administration and simultaneous administration of the single preparations. Also, it is a once-daily dosage form which increases the medication compliance of patients. Particularly, even though the content of aspirin in the combined pharmaceutical formulation is reduced, the platelet aggregation inhibitory effect of aspirin in the combined pharmaceutical formulation is equal to that of the amount of aspirin used in the prior art, while the aspirin in the combined pharmaceutical formulation shows a antihypertensive effect. In addition, the chronotherapeutically combined pharmaceutical formulation allows the two drugs, which interact with each other, to be stored for a long period of time, and the combined pharmaceutical formulation ensures the human body-safety and efficacy of the two drugs.

    摘要翻译： 本发明涉及一种用于预防和治疗心血管疾病的时间疗法组合药物制剂，其基于以特定时间间隔施用多种药物的原则（即时间疗法）。 具体地，组合的药物制剂包含HMG-CoA还原酶抑制剂，例如辛伐他汀和阿司匹林。 因为组合的药物制剂是基于以特定时间间隔给药药物的原理而开发的，即所谓的时间疗法，与单独给药和单次制剂同时给药相比，它显示了预防或治疗心血管疾病的优异效果。 此外，它是一种每日一次的剂型，其增加患者的药物依从性。 特别是，尽管组合药物制剂中阿司匹林的含量降低，但组合药物制剂中阿司匹林的血小板聚集抑制作用等于现有技术中所用阿司匹林的量，而组合药物中阿司匹林 制剂显示抗高血压作用。 另外，按时间顺序组合的药物制剂允许两种彼此相互作用的药物长时间储存​​，并且组合的药物制剂确保了两种药物的人体安全性和功效。

    COMBINED PREPARATION FOR THE TREATMENT OF CARDIOVASCULAR DISEASES BASED ON CHRONOTHERAPY THEORY
    4.
    发明申请
    COMBINED PREPARATION FOR THE TREATMENT OF CARDIOVASCULAR DISEASES BASED ON CHRONOTHERAPY THEORY 审中-公开
    基于循环理论治疗心血管疾病的联合制剂

    公开(公告)号：US20100047341A1

    公开(公告)日：2010-02-25

    申请号：US12445204

    申请日：2007-10-10

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja-Seong Koo ,  Sang Ouk Sun

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja-Seong Koo ,  Sang Ouk Sun

    IPC分类号： A61K9/54 ,  A61K9/24 ,  A61K31/4178

    CPC分类号： A61K31/4184 ,  A61K9/2077 ,  A61K9/2081 ,  A61K9/2086 ,  A61K9/209 ,  A61K9/2853 ,  A61K9/2866 ,  A61K9/5084 ,  A61K31/4178 ,  A61K31/4422 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to a functional combination preparation comprising a dihydropyridine-based calcium channel blocker such as amlodipine and an ARB (Angiotensin-2 receptor blocker) such as losartan. In particular, the present invention relates to a chronotherapeutical combination pharmaceutical formulations with controlled-release for the prevention or treatment of cardiovascular disease, which is formulated in accordance with xenobiotics and chronotherapy for enabling the two drugs to be chronotherapeutically released, thereby improving the therapeutic activity as compared to the co-administration of each drug in the form of a single pill, while reducing side effects and maintaining the therapeutic activity as high as possible at the time of day when the risk of a complication of cardiovascular disease is highest.

    摘要翻译： 本发明涉及包含二氢吡啶类钙通道阻断剂如氨氯地平和ARB（血管紧张素-2受体阻断剂）如洛沙坦的功能性组合制剂。 特别地，本发明涉及具有控制释放以用于预防或治疗心血管疾病的时间疗法组合药物制剂，所述药物制剂根据异生素和时间疗法配制，以使两种药物能够进行治疗性释放，从而改善治疗活性 与单一药丸形式的每种药物的共同给药相比，同时在心血管疾病并发症的风险最高的一天中减少副作用并保持尽可能高的治疗活性。

    N,N-dimethyl imidodicarbonimidic diamide dicarboxylate, method for producing the same and pharmaceutical compositions comprising the same
    7.
    发明授权
    N,N-dimethyl imidodicarbonimidic diamide dicarboxylate, method for producing the same and pharmaceutical compositions comprising the same 有权
    N，N-二甲基亚氨基二酰亚胺二酰胺二羧酸酯，其制备方法和包含其的药物组合物

    公开(公告)号：US08076377B2

    公开(公告)日：2011-12-13

    申请号：US12733711

    申请日：2008-09-19

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim ,  Byoung Ha Kim ,  Duck Kim

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim ,  Byoung Ha Kim ,  Duck Kim

    IPC分类号： A01N37/52 ,  A01N37/10 ,  A61K31/155 ,  A61K31/235

    CPC分类号： C07C279/26 ,  C07C55/08 ,  C07C55/12 ,  C07C55/14 ,  C07C59/245

    摘要： Disclosed herein are a novel dicarboxylic acid salt of N,N-dimethylimidodicarbonimidic diamide, a preparation method thereof and a pharmaceutical composition comprising the same. More specifically, disclosed herein are a novel dicarboxylic acid salt of N,N-dimethylimidodicarbonimidic diamide, a crystalline acid addition salt prepared by allowing N,N-dimethylimidodicarbonimidic diamide to react with a specific dicarboxylic acid, which has improved physical and chemical properties including solubility, stability, non-hygroscopicity and anti-adhesive properties, and low toxicity, and thus is very effective in the prevention and treatment of not only diabetes and its complications in patients with so-called metabolic syndromes, in which diabetes, obesity, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndromes, etc. appear in combination, but also p53 gene-deficient cancers, muscular pain, muscle cytotoxicity and rhabdomyolysis, as well as a preparation method thereof and a pharmaceutical composition comprising the same.

    摘要翻译： 本文公开了N，N-二甲基亚氨基二亚甲基二酰胺的新型二羧酸盐及其制备方法和包含其的药物组合物。 更具体地，本文公开了N，N-二甲基亚氨基二甲酰亚胺二酰胺的新型二羧酸盐，通过使N，N-二甲基亚氨基二碳二亚胺二酰胺与特定二羧酸反应制备的结晶酸加成盐，其具有改善的物理和化学性质，包括溶解度 稳定性，非吸湿性和抗粘连性，低毒性，因此在预防和治疗不仅糖尿病及其所谓的代谢综合征患者的并发症方面非常有效，其中糖尿病，肥胖，高脂血症， 脂肪肝，冠状动脉疾病，骨质疏松症，多囊卵巢综合征等组合，还包括p53基因缺陷型癌症，肌肉酸痛，肌肉细胞毒性和横纹肌溶解症，以及其制备方法和包含其的药物组合物。

    N, N-dimethyl imidodicarbonimidic diamide acetate, method for producing the same and pharmaceutical compositions comprising the same
    8.
    发明授权
    N, N-dimethyl imidodicarbonimidic diamide acetate, method for producing the same and pharmaceutical compositions comprising the same 有权
    N，N-二甲基亚氨基二甲酰亚胺二酰胺乙酸盐，其制备方法和包含其的药物组合物

    公开(公告)号：US08058312B2

    公开(公告)日：2011-11-15

    申请号：US12524695

    申请日：2008-01-29

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim

    IPC分类号： A01N37/52 ,  A61K31/155 ,  C07C277/00 ,  C07C279/00

    CPC分类号： A61K31/155 ,  C07C279/26

    摘要： The present invention relates to N,N-dimethyl imidodicarbonimidic diamide acetate, a method of preparing the same and a pharmaceutical composition comprising the same, and more particularly, to N,N-dimethyl imidodicarbonimidic diamide acetate which is a crystalline acid addition salt prepared by reacting N,N-dimethyl imidodicarbonimidic diamide with acetic acid, and which is very effective as a therapeutic agent for treating metabolic syndromes that glycosuria and diabetes mellitus, obesity, hyperlipidemia, fatty liver, coronary heart disease, osteoporosis, polycystic ovarian syndrome, a cancer depleted of gene P53, etc. are complexly occurred; treating diabetes mellitus and preventing its complication; and treating a cancer and preventing myalgia, muscle cell cytotoxicity and rhabdomyolysis, etc. since the acid addition salt is excellent in physicochemical properties such as solubility, stability, non-hygroscopicity, anti-adhering property, etc., and low toxicity, a method of preparing the same and a pharmaceutical composition comprising the same.

    摘要翻译： 本发明涉及N，N-二甲基亚氨基二甲酰亚胺二酰胺乙酸盐，其制备方法和包含其的药物组合物，更具体地涉及作为结晶酸加成盐的N，N-二甲基亚氨基二甲酰亚胺二酰胺乙酸盐，其是由 使N，N-二甲基亚氨基二亚甲基二酰胺与乙酸反应，作为治疗代谢综合征的糖尿病，糖尿病，肥胖症，高脂血症，脂肪肝，冠心病，骨质疏松症，多囊卵巢综合症，癌症， 贫血基因P53等复杂发生; 治疗糖尿病并预防其并发症; 并且由于酸加成盐在溶解性，稳定性，非吸湿性，抗附着性等等的物理化学性质和低毒性方面都是优异的，因此治疗癌症并防止肌肉痛，肌肉细胞毒性和横纹肌溶解等。 的制备方法和包含其的药物组合物。

    N, N -DIMETHYL IMIDODICARBONIMIDIC DIAMIDE ACETATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
    10.
    发明申请
    N, N -DIMETHYL IMIDODICARBONIMIDIC DIAMIDE ACETATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 有权
    N，N-二甲基咪唑二羧酸二乙酸酯，其制备方法和包含其的药物组合物

    公开(公告)号：US20100087544A1

    公开(公告)日：2010-04-08

    申请号：US12524695

    申请日：2008-01-29

    申请人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim

    发明人： Sung Wuk Kim ,  Sung Soo Jun ,  Young Gwan Jo ,  Ja Seong Koo ,  Young Woong Kim

    IPC分类号： A61K31/155 ,  C07C279/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P35/00 ,  A61P19/10

    CPC分类号： A61K31/155 ,  C07C279/26

    摘要： The present invention relates to N,N-dimethyl imidodicarbonimidic diamide acetate, a method of preparing the same and a pharmaceutical composition comprising the same, and more particularly, to N,N-dimethyl imidodicarbonimidic diamide acetate which is a crystalline acid addition salt prepared by reacting N,N-dimethyl imidodicarbonimidic diamide with acetic acid, and which is very effective as a therapeutic agent for treating metabolic syndromes that glycosuria and diabetes mellitus, obesity, hyperlipidemia, fatty liver, coronary heart disease, osteoporosis, polycystic ovarian syndrome, a cancer depleted of gene P53, etc. are complexly occurred; treating diabetes mellitus and preventing its complication; and treating a cancer and preventing myalgia, muscle cell cytotoxicity and rhabdomyolysis, etc. since the acid addition salt is excellent in physicochemical properties such as solubility, stability, non-hygroscopicity, anti-adhering property, etc., and low toxicity, a method of preparing the same and a pharmaceutical composition comprising the same.

    摘要翻译： 本发明涉及N，N-二甲基亚氨基二甲酰亚胺二酰胺乙酸盐，其制备方法和包含其的药物组合物，更具体地涉及作为结晶酸加成盐的N，N-二甲基亚氨基二甲酰亚胺二酰胺乙酸盐，其是由 使N，N-二甲基亚氨基二亚甲基二酰胺与乙酸反应，作为治疗代谢综合征的糖尿病，糖尿病，肥胖症，高脂血症，脂肪肝，冠心病，骨质疏松症，多囊卵巢综合征，癌症， 贫血基因P53等复杂发生; 治疗糖尿病并预防其并发症; 并且由于酸加成盐在溶解性，稳定性，非吸湿性，抗附着性等等的物理化学性质和低毒性方面都是优异的，因此治疗癌症并防止肌肉痛，肌肉细胞毒性和横纹肌溶解等。 的制备方法和包含其的药物组合物。