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11.发明公开Ｎ,Ｎ―디메틸 이미도디카르본이미딕 디아미드의 부틸산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 无效N，N-二甲基咪唑偶氮二异丁酸丁酯，其制备方法，包含其的药物组合物和包括其的组合制剂
公开(公告)号：KR1020120032502A
公开(公告)日：2012-04-05
申请号：KR1020120016834
申请日：2012-02-20
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C53/124 , A61K31/155 , A61P35/00
CPC classification number: A61K31/155 , C07C53/124 , C07C279/26
Abstract: PURPOSE: Metformin butyrate is provided to have excellent solubility, stability, non-hygroscopic, adhesion preventing property, processability as formulation, pharmacological effect, and to be manufactured under mild condition with high yield. CONSTITUTION: Metformin butyrate comprises a structure in chemical formula 1. The melting point of the crystal shape is 162 °C. A manufacturing method of the metformin in chemical formula 1 comprises a step of manufacturing metformin free base in chemical formula 3, by reacting metformin hydrochloride in chemical formula 2 with a base under organic solvent, and a step of reacting the metformin free base with butyl acid.
Abstract translation: 目的：提供二甲双胍丁酸酯具有优异的溶解性，稳定性，非吸湿性，防粘连性，作为制剂的加工性，药理作用，并以高产率在温和条件下制备。 构成：丁二酸二甲酯包括化学式1的结构。晶体形状的熔点为162℃。 化学式1中的二甲双胍的制造方法包括通过化学式2中的二甲双胍盐酸盐与有机溶剂中的碱反应制备化学式3中的二甲双胍游离碱的步骤，以及使二甲双胍游离碱与丁酸反应的步骤 。
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12.发明公开
公开(公告)号：KR1020110021693A
公开(公告)日：2011-03-04
申请号：KR1020100082555
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07D307/32 , A61K31/341 , A61P3/10
CPC classification number: C07D307/62
Abstract: PURPOSE: A metformin ascorbate and a pharmaceutical composition containing the same are provided to ensure excellent stability and proceesibility of tablet. CONSTITUTION: A metformin ascorbate is denoted by chemical formula 1. The melting point of metformin ascorbate is 145 degree celsius. A pharmaceutical composition for preventing or treating diabetes, metabolic syndrome, diabetic complication, hypertension, fatty liver, or cancer contains metformin ascorbate of chemical formula 1 as an active ingredient. The composition is combined with a second drug, such as anti-cancer drug, anti-hypertension agent, or anti-obesity agent. The pharmaceutical composition is manufactured in the form of tablet, soft capsule, hard capsule, pill, granule, powder, injection, or liquid. The composition is sustained release or rapid release.
Abstract translation: 目的：提供二甲双胍抗坏血酸盐和含有它们的药物组合物，以确保片剂的优异稳定性和可操作性。 构成：二甲双胍抗坏血酸由化学式1表示。二甲双胍抗坏血酸的熔点为145摄氏度。 用于预防或治疗糖尿病，代谢综合征，糖尿病并发症，高血压，脂肪肝或癌症的药物组合物含有化学式1的二甲双胍抗坏血酸作为活性成分。 该组合物与第二种药物如抗癌药物，抗高血压剂或抗肥胖剂组合。 药物组合物以片剂，软胶囊，硬胶囊，丸剂，颗粒剂，粉剂，注射剂或液体的形式制备。 组合物持续释放或快速释放。
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公开(公告)号：KR1020110021690A
公开(公告)日：2011-03-04
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: PURPOSE: A metformin taurine salt is provided to ensure excellent stability, low toxicity, antioxidant activity and excellent AMPKa-activating effects, to enable easy tabletting, and thereby enabling use in treating glycosuria, diabetes, metabolic syndrome, and diabetes complications. CONSTITUTION: A metformin taurine salt is represented by chemical formula 1 and has a melting point of 134.1 °C. A pharmaceutical composition contains the metformin taurine salt as an active ingredient. The metformin taurate can be effectively used in treating 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, climacterium and rhabdomyolysis, etc., and provides antioxidant activity.
Abstract translation: 目的：提供二甲双胍牛磺酸盐，以确保优异的稳定性，低毒性，抗氧化活性和优异的AMPKa活化作用，使易于制片，从而可用于治疗糖尿病，糖尿病，代谢综合征和糖尿病并发症。 构成：二甲双胍牛磺酸盐由化学式1表示，熔点为134.1℃。 药物组合物含有二甲双胍牛磺酸盐作为活性成分。 二甲双胍牛磺酸可有效用于治疗糖尿病，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，肌肉细胞毒性症状， 和横纹肌溶解等，并提供抗氧化活性。
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14.发明公开Ｎ,Ｎ―디메틸 이미도디카르본이미딕 디아미드의 프로피온산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 无效N，N-二甲基咪唑二恶烷二酸酯，其制备方法，包含其的药物组合物和包括其的组合制剂
公开(公告)号：KR1020110007984A
公开(公告)日：2011-01-25
申请号：KR1020100069243
申请日：2010-07-16
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C277/00 , A61K31/155 , A61P3/10
CPC classification number: C07C53/122 , C07C277/00 , C07C279/26
Abstract: PURPOSE: A metformin propionate is provided to ensure an excellent pharmacological effect as compared with metformin hydrochloride and to achieve a therapeutic purpose by administering an amount less than metformin hydrochloride. CONSTITUTION: A metformin propionate is represented by chemical formula 1. A method for preparing the metformin propionate represented by chemical formula 1 comprises the steps of: reacting metformin hydrochloride represented by chemical formula 2 with base in an organic solvent to prepare metformin free base represented by chemical formula 3; and reacting the metformin free base with propionic acids.
Abstract translation: 目的：提供丙酸二甲双胍以确保与二甲双胍盐酸盐相比具有优异的药理作用，并通过施用少于二甲双胍盐酸盐的量来达到治疗目的。 构成：丙酸二甲双胍由化学式1表示。由化学式1表示的制备丙酸二甲双胍的方法包括以下步骤：将由化学式2表示的二甲双胍盐酸盐与碱在有机溶剂中反应，制备由 化学式3; 并使二甲双胍游离碱与丙酸反应。
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公开(公告)号：KR101274981B1
公开(公告)日：2013-06-18
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: 본 발명은 N1-N5-치환된 하기 화학식 1로 표시되는 바이구아나이드 유도체 또는 그의 약학적으로 허용 가능한 염, 이의 제조방법 및 이를 유효성분으로 약학 조성물을 제공한다. 본 발명의 바이구아나이드 유도체는 기존 약물에 비해 적은 양으로도 우수한 AMPKα 활성화 효과 및 암세포 증식 억제 효과를 나타내어 당뇨, 비만, 고지혈증, 고콜레스테롤혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군, 대사성 증후군, 암 등의 치료를 위해 유용하게 이용될 수 있다.
[화학식 1]-
Patent Agency Ranking16.发明授权
公开(公告)号：KR101104912B1
公开(公告)日：2012-01-12
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: 본 발명은 N,N-디메틸 이미도디카르본이미딕 디아미드의 니코틴산염, 그의 제조방법 및 그를 포함하는 약제학적 조성물에 관한 것으로서, 더욱 상세하게는 용해도, 안정성, 비흡습성, 정제 제형으로서의 가공성 등의 물리화학적 성질이 개선되었을 뿐 아니라, 독성이 낮고, N,N-디메틸 이미도디카르본이미딕 디아미드가 본질적으로 발휘하는 약화학적 특성인 당뇨 및 당뇨병, 비만증, 고지혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군 등이 복합적으로 나타나는 이른바 대사성 증후군을 지닌 자들의 당뇨병 치료, 당뇨병자의 합병증의 근본 핵심 원인 물질인 중성 지질 저하 작용에 의한 합병증 예방 및 치료 그리고 p53 유전자가 결여된 암, 근육통, 근육세포 독성 및 횡문근 융해의 예방 및 치료 효과를 더욱 증가시켜줄 수 있는 치료제로서 유� ��한 N,N-디메틸 이미도디카르본이미딕 디아미드의 니코틴산염, 그의 제조방법과 그의 약제학적 조성물에 관한 것이다.
메트포르민, 메트포르민 니코틴산염, 메트포르민 이니코틴산염, N,N-디메틸 이미도디카르본이미딕 디아미드, 니코틴산염, 결정성 산부가염, 당뇨병, 대사성증후군-
17.发明公开Ｎ,Ｎ―디메틸 이미도디카르본이미딕 디아미드의 부틸산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 无效N，N-二甲基咪唑偶氮二异丁酸丁酯，其制备方法，包含其的药物组合物和包括其的组合制剂
公开(公告)号：KR1020110007985A
公开(公告)日：2011-01-25
申请号：KR1020100069244
申请日：2010-07-16
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C277/00 , A61K31/155 , A61P3/10
CPC classification number: A61K31/155 , C07C53/124 , C07C279/26
Abstract: PURPOSE: N,N-dimethyl imidodicarbonimidic diamide butyrate is provided to ensure excellent physicochemical properties such as solubility, stability, hygroscopicity and adsorption preventing property, processibility of formulations. CONSTITUTION: A metformin butyrate is represented by chemical formula 1. The metformin butyrate has a crystal form. A melting point of the crystal form is 162°C. A method for preparing the metformin butyrate represented by chemical formula 1 comprises the steps of: reacting metformin hydrochloride represented by chemical formula 2 with base in an organic solvent to prepare metformin free base represented by chemical formula 3; and reacting the metformin free base with butyric acids.
Abstract translation: 目的：提供N，N-二甲基亚氨基二酰亚胺二酰胺丁酸酯，以确保优异的物理化学性质，如溶解度，稳定性，吸湿性和吸附防止性能，配方的加工性。 构成：二甲双胍丁酸酯由化学式1表示。二甲双胍丁酸酯具有晶体形式。 晶体的熔点为162℃。 由化学式1表示的制备丁酸二甲双胍的方法包括以下步骤：将由化学式2表示的二甲双胍盐酸盐与碱在有机溶剂中反应制备由化学式3表示的游离二甲双胍碱; 并使二甲双胍游离碱与丁酸反应。
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18.发明授权
公开(公告)号：KR101211227B1
公开(公告)日：2012-12-11
申请号：KR1020100082555
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07D307/32 , A61K31/341 , A61P3/10
CPC classification number: C07D307/62
Abstract: 본발명은메트포르민아스코르브산염, 그의제조방법, 그를포함하는약학조성물및 그를포함하는복합제제를제공한다. 본발명의메트포르민아스코르브산염은우수한안정성및 정제의가공용이성을가지며, 독성이낮고, 당뇨, 당뇨병, 대사성증후군, 당뇨병합병증, 월경불순, 고혈압, 고지혈증, 지방간, 관상동맥질환, 골다공증, 다낭성난소증후군, 암, 근육통, 근육세포독성증, 횡문근융해증폐경기증후군, 및/또는항산화등에효과적이다.
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19.发明公开Ｎ,Ｎ-디메틸 이미도디카르본이미딕 디아미드의 프로피온산염, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이를 포함하는 복합제제 无效N，N-二甲基咪唑二恶烷二酸酯，其制备方法，包含其的药物组合物和包括其的组合制剂
公开(公告)号：KR1020120031288A
公开(公告)日：2012-04-02
申请号：KR1020120016856
申请日：2012-02-20
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C53/122 , A61K31/155 , A61P3/10
CPC classification number: C07C53/122 , C07C277/00 , C07C279/26
Abstract: PURPOSE: A N,N-dimethyl imidodicarbonimidic diamide propionate is provided to have excellent solubility, stability, non-hygroscopicity, adhesion preventing properties, processability, and pharmacological effects, and can be manufactured under mild conditions with high yield. CONSTITUTION: The N,N-dimethyl imidodicarbonimidic diamide propionate is in chemical formula 1, and has the melting point of the crystal structure in chemical formula 1 which is 194 - 194.5 °C. The manufacturing method of the N,N-dimethyl imidodicarbonimidic diamide propionate in chemical formula 1 comprises a step of manufacturing the metformin glass base in chemical formula 3 by reacting the metformin hydrochloride in chemical formula 2 with a base under organic solvent, and a step of reacting the metformin glass base with propionic acid.
Abstract translation: 目的：提供N，N-二甲基亚氨基二酰亚胺二酰丙酸丙酸酯具有优异的溶解性，稳定性，不吸湿性，防粘连性，加工性和药理作用，可以在温和条件下以高产率制备。 构成：化学式1中的N，N-二甲基亚氨基二酰亚胺二酰胺丙酸酯为化学式1中的结晶结构的熔点为194-194.5℃。 化学式1中的N，N-二甲基亚氨基二亚氨基二酰丙酸丙酸酯的制造方法包括通过化学式2中的二甲双胍盐酸盐与有机溶剂中的碱反应制造化学式3中的二甲双胍玻璃碱的步骤， 二甲双胍玻璃碱与丙酸反应。
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公开(公告)号：KR1020110021691A
公开(公告)日：2011-03-04
申请号：KR1020100082553
申请日：2010-08-25
Applicant: 한올바이오파마주식회사
IPC: C07C279/26 , C07C309/02 , A61K31/155 , A61P3/10
CPC classification number: C07C309/04 , C07C279/26
Abstract: PURPOSE: A metformin methanesulfonate and a pharmaceutical composition comprising the same are provided to ensure excellent activation of AMPKα, relatively low toxicity, stability, and non-hygroscopic property. CONSTITUTION: A metformin methanesulfonate represented by chemical formula 1 has a melting point of 194.0~194.5 °C. A pharmaceutical composition contains the metformin methanesulfonic acid salt as an active ingredient. The metformin methanesulfonate can be effectively used in treating 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 and/or climacterium, etc.
Abstract translation: 目的：提供二甲双胍甲磺酸盐和包含其的药物组合物以确保AMPKα的优异活化，相对低毒性，稳定性和非吸湿性。 构成：由化学式1表示的二甲双胍甲磺酸盐的熔点为194.0〜194.5℃。 药物组合物含有二甲双胍甲磺酸盐作为活性成分。 二甲双胍甲磺酸盐可有效用于治疗糖尿病，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，肌肉细胞毒性症状，横纹肌溶解 和/或气候等
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