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21.发明公开
公开(公告)号：KR1020090076827A
公开(公告)日：2009-07-13
申请号：KR1020090001170
申请日：2009-01-07
Applicant: 한올바이오파마주식회사
IPC: C07D213/80 , A61K31/4406 , A61P3/10 , A61P3/06
CPC classification number: C07D213/80
Abstract: A N,N-dimethyl imidodicarbonimidic diamide nicotinate is provided to improve manufacturing with low toxicity and prevent and treat diabetes and complication of diabetes. A metformin nicotinic acid salt is denoted by the chemical formula 1. In the chemical formula 1, n is 1 or 2. The metformin nicotinic acid salt is anhydrous or hydrous state. A method for manufacturing the metformin nicotinic acid salt comprises: a step of reacting 1-4 mole equivalent of inorganic base in sodium hydroxide or potassium hydroxide in water or organic solvent to produce metformin free base of the chemical formula 3; and a step of removing inorganic salt in the compound of the chemical formula 3 and reacting with 1-4 mole equivalent of nicotinic acid of the chemical formula 4. The organic solvent is methanole, ethanol, isopropanol, acetone, or acetonitrile. A pharmaceutical composition comprises the metformin nicotinic acid salt of the chemical formula 1 as an active ingredient.
Abstract translation: 提供N，N-二甲基亚氨基二亚胺二酰胺烟酸酯以改善低毒制剂，预防和治疗糖尿病和糖尿病并发症。 二甲双胍烟酸盐由化学式1表示。在化学式1中，n为1或2.二甲双胍烟酸盐为无水或含水状态。 制备二甲双胍烟酸盐的方法包括：使1-4摩尔当量无机碱在氢氧化钠或氢氧化钾在水或有机溶剂中反应以制备化学式3的二甲双胍游离碱的步骤; 以及除去化学式3的化合物中的无机盐并与1-4摩尔当量的化学式4的烟酸反应的步骤。有机溶剂是甲醇，乙醇，异丙醇，丙酮或乙腈。 药物组合物包含化学式1的二甲双胍烟酸盐作为活性成分。
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公开(公告)号：KR101324283B1
公开(公告)日：2013-11-01
申请号：KR1020110036955
申请日：2011-04-20
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C277/08 , A61K31/155 , A61P35/00
Abstract: 바이구아나이드 화합물의 신규한 글라이포세이트염, 그의 제조방법, 그를 포함하는 의약, 약제학적 조성물이 제공된다. 본 발명에 따른 바이구아나이드 화합물의 글라이포세이트염은 메트포르민 염산염에 비해 항암 효과가 훨씬 우수하면서동등한 수준의 AMPK 활성을 나타내어 메트포르민 염산염이 나타내는 우수한 혈당 강하 효과, 항산화 효과, 지질 저하 작용 및 대사 증후군(metabolic syndrome) 개선 효과를 발휘한다. 또한, 본 발명에 따른 바이구아나이드 화합물의 글라이포세이트염은 메트포르민 염산염에 비해 용해도, 안정성, 비흡습성, 정제 제형으로서의 가공성 등의 물리화학적 성질이 우수하여 바이구아나이드 화합물의 약제학적으로 허용되는 염으로써 유용하게 이용될 수 있다.
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Patent Agency Ranking
公开(公告)号：KR101190957B1
公开(公告)日：2012-10-15
申请号：KR1020100082554
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C59/52 , A61K31/155 , A61P35/00
CPC classification number: C07C59/11 , A61K31/155 , A61K31/192 , C07C279/26
Abstract: 본 발명은 메트포르민 카페익산염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제를 제공한다. 본 발명의 메트포르민 카페익산염은 우수한 안정성 및 정제의 가공 용이성을 가지며, 독성이 낮고, 당뇨, 당뇨병, 대사성 증후군, 당뇨병 합병증, 월경불순, 고혈압, 고지혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군, 암, 근육통, 근육세포 독성증, 횡문근융해증, 폐경기증후군, 및/또는 항산화 등에 효과적이다.
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公开(公告)号：KR101190953B1
公开(公告)日：2012-10-12
申请号：KR1020100082552
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C309/14 , A61K31/155 , A61P3/10
CPC classification number: A61K31/145 , A61K31/155 , C07C279/26 , C07C309/14
Abstract: 본 발명은 메트포르민 타우린염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제를 제공한다. 본 발명의 메트포르민 타우린염은 우수한 안정성 및 정제의 가공 용이성을 가지며, 독성이 낮고, 우수한 AMPKα의 활성화 작용을 나타내어, 당뇨, 당뇨병, 대사성 증후군, 당뇨병 합병증, 월경불순, 고혈압, 고지혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군, 암, 근육통, 근육세포 독성증, 폐경기증후군 및 횡문근융해증에 효과적이며, 항산화 작용을 나타낸다.
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公开(公告)号：KR1020110119542A
公开(公告)日：2011-11-02
申请号：KR1020110036955
申请日：2011-04-20
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C277/08 , A61K31/155 , A61P35/00
Abstract: PURPOSE: A novel salt of a biguanide compound is provided to ensure excellent anticancer effects and the same AMPK activity as metformin hydrochlorides, and excellent blood glucose decrease effects, and antioxidant effects. CONSTITUTION: A novel salt of a biguanide compound has the structure of chemical formula 1. A method for preparing the acid addition salts of the biguanide compound comprises a step of reacting the free base of the biguanide compound represented by chemical formula 5 with glyphosate. In chemical formula 1, R1 or R2 are independently hydrogen, C1-4 alkyl, and phenyl-substituted C1-4 alkyl; and A is glyphosate. The free base of the biguanide compound reacts with 0.5-4 mole equivalent of glyphosate per 1 molar equivalent.
Abstract translation: 目的：提供双胍化合物的新型盐，以确保优异的抗癌作用和与二甲双胍盐酸盐相同的AMPK活性，以及优异的血糖降低作用和抗氧化作用。 组分：双胍化合物的新型盐具有化学式1的结构。双胍化合物的酸加成盐的制备方法包括使由化学式5表示的双胍化合物的游离碱与草甘膦反应的步骤。 在化学式1中，R 1或R 2独立地为氢，C 1-4烷基和苯基取代的C 1-4烷基; 而A是草甘膦。 双胍化合物的游离碱与每摩尔当量0.5-4摩尔当量的草甘膦反应。
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公开(公告)号：KR1020110081093A
公开(公告)日：2011-07-13
申请号：KR1020110001438
申请日：2011-01-06
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C277/00 , A61K31/155 , A61P3/10
CPC classification number: A61K31/155 , A61K31/341 , A61K31/4406 , A61K31/472 , C07C277/04 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/16 , C07C279/18 , C07C279/26 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D213/38 , C07D307/52 , C07D317/58 , C07D333/20
Abstract: PURPOSE: Biguanide derivatives are provided to ensure excellent AMPKa activation effect and an inhibitory effect of cancer cell proliferation in a small amount. CONSTITUTION: Biguanide derivatives are a compound of chemical formula 1 or pharmaceutically acceptable salts thereof. In chemical formula 1, R1, R2, R3 and R4 respectively represent non-hydrogen substituents or hydrogen. The non-hydrogen substituent is selected from the group consisting of: C1-12 alkyl substituted or unsubstituted with one or more selected from the group consisting of C3-10 cycloalkyl, C5-12 aryl, C5-12 heteroaryl, hydroxyl, halogen, and C1-4 alkoxycarbonyl; C3-10 cycloalkyl; C1-12 alkoxy; C5-12 aryl; C5-12 heteroaryl; hydroxyl; and halogen.
Abstract translation: 目的：提供双胍衍生物，以确保极好的AMPKa活化作用和少量癌细胞增殖的抑制作用。 组分：双胍衍生物是化学式1的化合物或其药学上可接受的盐。 在化学式1中，R 1，R 2，R 3和R 4分别表示非氢取代基或氢。 非氢取代基选自：取代或未取代的C1-12烷基，其中一个或多个选自C3-10环烷基，C5-12芳基，C5-12杂芳基，羟基，卤素和 C 1-4烷氧基羰基; C3-10环烷基; C 1-12烷氧基; C5-12芳基; C5-12杂芳基; 羟; 和卤素。
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27.发明公开메트포르민 카페익산염, 그의 제조방법, 그를 포함하는 약학 조성물 및 그를 포함하는 복합제제 有权METFORMIN CAFFEIC ACID盐，其制备方法，包含其的药物组合物和包含其的组合制剂
公开(公告)号：KR1020110021692A
公开(公告)日：2011-03-04
申请号：KR1020100082554
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C59/52 , A61K31/155 , A61P35/00
CPC classification number: C07C59/11 , A61K31/155 , A61K31/192 , C07C279/26
Abstract: PURPOSE: A metformin caffeic acid salt is provided to ensure excellent stability, low toxicity, and excellent stability, and to enable easy tabletting. CONSTITUTION: A metformin caffeic acid salt is represented by chemical formula 1 and has a melting point of 147.1 °C. The pharmaceutical composition includes the metformin caffeic acid salt as an active ingredient. The metformin caffeic acid salt can be valuably used in the treatment of glycosuria, diabetes, metabolic syndrome, diabetes complications, menstrual irregularities, hypertension, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome, cancer, myalgia, symptoms of muscle cell cytotoxicity, rhabdomyolysis, climacterium, etc., and/or provides antioxidant activity. The cancer is such that p53-gene is deficient.
Abstract translation: 目的：提供二甲双胍咖啡酸盐，以确保优异的稳定性，低毒性和优异的稳定性，并使易于压片。 构成：二甲双胍咖啡酸盐由化学式1表示，熔点为147.1℃。 药物组合物包括二甲双胍咖啡酸盐作为活性成分。 二甲双胍咖啡酸盐可用于治疗糖尿病，糖尿病，代谢综合征，糖尿病并发症，月经不调，高血压，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，癌症，肌痛，肌肉症状 细胞毒性，横纹肌溶解，长杆菌等，和/或提供抗氧化活性。 癌症是p53基因缺陷。
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