JP6108631B2 - 高脂血症を予防または治療するための医薬組成物 - Google Patents
高脂血症を予防または治療するための医薬組成物 Download PDFInfo
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- JP6108631B2 JP6108631B2 JP2014544660A JP2014544660A JP6108631B2 JP 6108631 B2 JP6108631 B2 JP 6108631B2 JP 2014544660 A JP2014544660 A JP 2014544660A JP 2014544660 A JP2014544660 A JP 2014544660A JP 6108631 B2 JP6108631 B2 JP 6108631B2
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/04—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D263/06—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by oxygen atoms, attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/18—Oxygen atoms
- C07D263/20—Oxygen atoms attached in position 2
- C07D263/22—Oxygen atoms attached in position 2 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to other ring carbon atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
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- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
(1)試験方法
雄性ニュージーランド白色家兎を試験動物として使用した。G1群の動物(陰性コントロール群、n=4)を除くすべての動物に対し、放射線照射により滅菌した高コレステロール血症飼料、すなわちDYET#620007(1%コレステロール含有固形飼料Purina #5321、 Dyets,Inc., Bethlehem, PA 18017)をCentral Lab. Animal Inc.から購入して給餌した。高コレステロール血症を誘発するために、該飼料を試験動物に8週間以上給餌した。試験動物から血液サンプルを採取した後、血清生化学的分析を実施した。総コレステロールレベルが約870mg/dLである動物をコレステロール血症が誘発された動物として選択した。試験物質は、0.5%のカルボキシメチルセルロースナトリウムおよび1%のトウィーン80を含む生理食塩水に溶解し、4週間にわたって毎日1回、ラテックスカテーテルを備えた経口注射器を用いて胃内に直接投与した。試験群は、下記表1に示す通りである。
前記のようにして高コレステロール血症が誘発された動物におけるトリグリセリド濃度を以下の表2に示す。表2の値は、各群のトリグリセリド濃度の平均値(mg/dL)を示す。
(1)試験方法
雄性ニュージーランド白色家兎を試験動物として使用した。G1群の動物(陰性コントロール群)を除くすべての動物に対し、放射線照射により滅菌した高トリグリセリド血症および高コレステロール血症の飼料、すなわちDYET#621082(0.5%コレステロール、14%ココナツオイル、2%マルトースデキストリン含有固形飼料Purina #5321、Dyets、Inc.、Bethlehem、PA 18017)をSaeronbio Inc.から購入して給餌した。高トリグリセリド血症および高コレステロール血症を誘発するために、該飼料を試験動物に4週間以上給餌した。試験動物から血液サンプルを採取した後、血清生化学的分析を実施した。無処理群と比較して総コレステロールレベルおよびトリグリセリドレベルが有意に変化した動物を選択した。選択された動物を、総コレステロールレベルおよびトリグリセリドレベルに基づいて4群に分けた。このとき、いずれの群においても総コレステロールレベルおよびトリグリセリドレベルの平均値が実質的に同等となるようにした。試験物質は、0.5%カルボキシメチルセルロースナトリウムおよび1%トウィーン80を含む生理食塩水に溶解し、4週間にわたって毎日1回、ラテックスカテーテルを備えた経口注射器を用いて胃内に直接投与した。試験群は、下記表3に示す通りである。
前記のようにして高トリグリセリド血症および高コレステロール血症が誘発された動物におけるトリグリセリド濃度を以下の表4に示す。表4の値は、各群のトリグリセリド濃度の平均値(mg/dL)を示す。
Claims (7)
- 有効成分として下記式(1)の化合物またはその薬学的に許容される塩とオルメサルタンメドキソミルまたはその塩との組み合わせを含む、高脂血症を予防または治療するための医薬組成物であって、前記組み合わせが高脂血症の予防または治療に相乗効果をもたらすことを特徴とする医薬組成物。
- 前記高脂血症が高トリグリセリド血症または高トリグリセリド血症に関連する疾患である請求項1に記載の医薬組成物。
- 前記高トリグリセリド血症に関連する疾患が高トリグリセリド血症に関連するアテローム性動脈硬化症または高トリグリセリド血症に関連する膵炎である請求項2に記載の医薬組成物。
- 前記組成物が経口投与のための剤形に製剤化される請求項1〜3のいずれかに記載の医薬組成物。
- 前記経口投与のための剤形が、10〜300mg/日の投与に適した量の前記式(1)の化合物またはその薬学的に許容される塩を含む、請求項4に記載の医薬組成物。
- 前記経口投与のための剤形が、5〜320mg/日の投与に適した量のオルメサルタンメドキソミルまたはその塩を含む、請求項4に記載の医薬組成物。
- 高脂血症を予防または治療するための薬剤を製造するための、下記式(1)の化合物またはその薬学的に許容される塩とオルメサルタンメドキソミルまたはその塩との組み合わせを含む有効成分の使用であって、前記組み合わせが高脂血症の予防または治療に相乗効果をもたらすことを特徴とする使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR10-2011-0126431 | 2011-11-30 | ||
KR20110126431 | 2011-11-30 | ||
PCT/KR2012/010170 WO2013081372A1 (en) | 2011-11-30 | 2012-11-28 | Pharmaceutical composition for preventing or treating hyperlipidemia |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2015500231A JP2015500231A (ja) | 2015-01-05 |
JP6108631B2 true JP6108631B2 (ja) | 2017-04-05 |
Family
ID=48535760
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014544660A Expired - Fee Related JP6108631B2 (ja) | 2011-11-30 | 2012-11-28 | 高脂血症を予防または治療するための医薬組成物 |
JP2014544661A Expired - Fee Related JP6030147B2 (ja) | 2011-11-30 | 2012-11-28 | 高トリグリセリド血症または高トリグリセリド血症に関連する疾患を予防または治療するための医薬組成物 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2014544661A Expired - Fee Related JP6030147B2 (ja) | 2011-11-30 | 2012-11-28 | 高トリグリセリド血症または高トリグリセリド血症に関連する疾患を予防または治療するための医薬組成物 |
Country Status (13)
Country | Link |
---|---|
US (2) | US9486443B2 (ja) |
EP (2) | EP2785343A4 (ja) |
JP (2) | JP6108631B2 (ja) |
KR (2) | KR101436547B1 (ja) |
CN (2) | CN104053441B (ja) |
AU (2) | AU2012346755B2 (ja) |
BR (2) | BR112014012082A2 (ja) |
CA (2) | CA2857164A1 (ja) |
MX (2) | MX353660B (ja) |
PH (2) | PH12014501087A1 (ja) |
RU (2) | RU2616522C2 (ja) |
UA (2) | UA114492C2 (ja) |
WO (2) | WO2013081372A1 (ja) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN113121331B (zh) * | 2019-12-31 | 2024-01-05 | 华创合成制药股份有限公司 | 具有环丙基的苯氧芳酸类化合物及其药学上可接受的盐,以及它们的制备方法和应用 |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6004925A (en) * | 1997-09-29 | 1999-12-21 | J. L. Dasseux | Apolipoprotein A-I agonists and their use to treat dyslipidemic disorders |
PL348503A1 (en) * | 1998-12-23 | 2002-05-20 | Searle Llc | Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications |
US7129265B2 (en) * | 1999-04-23 | 2006-10-31 | Mason R Preston | Synergistic effects of amlodipine and atorvastatin metabolite as a basis for combination therapy |
CA2406067A1 (en) | 2000-04-19 | 2001-11-01 | Thomas Julius Borody | Compositions comprising the combination of a bile acid and a fibrate for use in therapies for hyperlipidaemia-associated disorders |
US7071210B2 (en) * | 2002-07-02 | 2006-07-04 | Pfizer Inc. | CETP inhibitors in combination with antihypertensive agents and uses thereof |
HN2005000340A (es) * | 2004-07-02 | 2009-11-06 | Merck Sharp & Dohme | Inhibidores de cetp |
DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
CA2593793A1 (en) * | 2005-01-05 | 2006-07-13 | Medicure International Inc. | Compounds and methods for regulating triglyceride levels |
BRPI0620752A2 (pt) | 2005-12-30 | 2011-11-22 | Merck & Co Inc | composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso do composto ou um sal farmaceuticamente aceitável do mesmo |
ES2559838T3 (es) * | 2007-03-16 | 2016-02-16 | Concert Pharmaceuticals, Inc. | Inhibidores de proteína de transferencia de ésteres de colesterol |
WO2010036600A1 (en) * | 2008-09-24 | 2010-04-01 | Merck Sharp & Dohme Corp. | Pharmaceutical compositions of atorvastatin |
US8354454B2 (en) * | 2008-10-01 | 2013-01-15 | Merck Sharp & Dohme Corp. | Prodrugs of oxazolidinone CETP inhibitors |
CN101822836A (zh) * | 2010-02-02 | 2010-09-08 | 王丽燕 | 包含艾力沙坦酯的药物组合物 |
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2012
- 2012-11-28 AU AU2012346755A patent/AU2012346755B2/en not_active Ceased
- 2012-11-28 WO PCT/KR2012/010170 patent/WO2013081372A1/en active Application Filing
- 2012-11-28 KR KR1020120136186A patent/KR101436547B1/ko not_active IP Right Cessation
- 2012-11-28 MX MX2014006448A patent/MX353660B/es active IP Right Grant
- 2012-11-28 AU AU2012346754A patent/AU2012346754B2/en not_active Ceased
- 2012-11-28 CN CN201280058939.2A patent/CN104053441B/zh not_active Expired - Fee Related
- 2012-11-28 CN CN201280058933.5A patent/CN104053440B/zh not_active Expired - Fee Related
- 2012-11-28 JP JP2014544660A patent/JP6108631B2/ja not_active Expired - Fee Related
- 2012-11-28 CA CA2857164A patent/CA2857164A1/en not_active Abandoned
- 2012-11-28 JP JP2014544661A patent/JP6030147B2/ja not_active Expired - Fee Related
- 2012-11-28 RU RU2014125702A patent/RU2616522C2/ru not_active IP Right Cessation
- 2012-11-28 US US14/361,365 patent/US9486443B2/en not_active Expired - Fee Related
- 2012-11-28 UA UAA201405161A patent/UA114492C2/uk unknown
- 2012-11-28 BR BR112014012082A patent/BR112014012082A2/pt not_active Application Discontinuation
- 2012-11-28 US US14/361,371 patent/US9724336B2/en not_active Expired - Fee Related
- 2012-11-28 EP EP12852736.3A patent/EP2785343A4/en not_active Withdrawn
- 2012-11-28 MX MX2014006447A patent/MX352611B/es active IP Right Grant
- 2012-11-28 RU RU2014125701/15A patent/RU2604132C2/ru not_active IP Right Cessation
- 2012-11-28 UA UAA201405160A patent/UA114491C2/uk unknown
- 2012-11-28 EP EP12852569.8A patent/EP2785342A4/en not_active Withdrawn
- 2012-11-28 WO PCT/KR2012/010175 patent/WO2013081373A1/en active Application Filing
- 2012-11-28 KR KR1020120136199A patent/KR101436551B1/ko not_active IP Right Cessation
- 2012-11-28 BR BR112014012081A patent/BR112014012081A2/pt not_active Application Discontinuation
- 2012-11-28 CA CA2857163A patent/CA2857163A1/en not_active Abandoned
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