CN102985075A - 含卡纳格列净的片剂 - Google Patents

含卡纳格列净的片剂 Download PDF

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Publication number
CN102985075A
CN102985075A CN2011800233805A CN201180023380A CN102985075A CN 102985075 A CN102985075 A CN 102985075A CN 2011800233805 A CN2011800233805 A CN 2011800233805A CN 201180023380 A CN201180023380 A CN 201180023380A CN 102985075 A CN102985075 A CN 102985075A
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tablet
amount
exists
weight
chemical compound
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Chinese (zh)
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杉本昌阳
木下肇
德田卓之
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Mitsubishi Tanabe Pharma Corp
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Mitsubishi Tanabe Pharma Corp
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Priority to CN201610946887.2A priority Critical patent/CN106890147A/zh
Publication of CN102985075A publication Critical patent/CN102985075A/zh
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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2011800233805A 2010-05-11 2011-05-11 含卡纳格列净的片剂 Pending CN102985075A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610946887.2A CN106890147A (zh) 2010-05-11 2011-05-11 含1‑(β‑D‑吡喃葡糖基)‑3‑(苯基噻吩基甲基)苯化合物的片剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33331210P 2010-05-11 2010-05-11
US61/333,312 2010-05-11
PCT/JP2011/061354 WO2011142478A1 (en) 2010-05-11 2011-05-11 Canagliflozin containing tablets

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN201610946887.2A Division CN106890147A (zh) 2010-05-11 2011-05-11 含1‑(β‑D‑吡喃葡糖基)‑3‑(苯基噻吩基甲基)苯化合物的片剂
CN201610158907.XA Division CN105769792A (zh) 2010-05-11 2011-05-11 含1-(β-D-吡喃葡糖基)-3-(苯基噻吩基甲基)苯化合物的片剂

Publications (1)

Publication Number Publication Date
CN102985075A true CN102985075A (zh) 2013-03-20

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Family Applications (3)

Application Number Title Priority Date Filing Date
CN2011800233805A Pending CN102985075A (zh) 2010-05-11 2011-05-11 含卡纳格列净的片剂
CN201610158907.XA Pending CN105769792A (zh) 2010-05-11 2011-05-11 含1-(β-D-吡喃葡糖基)-3-(苯基噻吩基甲基)苯化合物的片剂
CN201610946887.2A Pending CN106890147A (zh) 2010-05-11 2011-05-11 含1‑(β‑D‑吡喃葡糖基)‑3‑(苯基噻吩基甲基)苯化合物的片剂

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CN201610158907.XA Pending CN105769792A (zh) 2010-05-11 2011-05-11 含1-(β-D-吡喃葡糖基)-3-(苯基噻吩基甲基)苯化合物的片剂
CN201610946887.2A Pending CN106890147A (zh) 2010-05-11 2011-05-11 含1‑(β‑D‑吡喃葡糖基)‑3‑(苯基噻吩基甲基)苯化合物的片剂

Country Status (8)

Country Link
US (2) US20130052266A1 (enExample)
EP (1) EP2568971B1 (enExample)
JP (1) JP5596799B2 (enExample)
KR (1) KR101869110B1 (enExample)
CN (3) CN102985075A (enExample)
ES (1) ES2836952T3 (enExample)
TW (1) TWI564034B (enExample)
WO (1) WO2011142478A1 (enExample)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103641822A (zh) * 2013-10-21 2014-03-19 江苏奥赛康药业股份有限公司 一种卡格列净化合物及其药物组合物
CN103655539A (zh) * 2013-12-13 2014-03-26 重庆医药工业研究院有限责任公司 一种卡格列净的口服固体制剂及其制备方法
CN103980262A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的b晶型及其结晶制备方法
CN103980261A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的a晶型及其结晶制备方法
CN104402946A (zh) * 2014-11-17 2015-03-11 连云港恒运医药科技有限公司 卡格列净中间体及其无定形的制备方法
CN104523573A (zh) * 2014-12-29 2015-04-22 成都恒瑞制药有限公司 一种卡格列净快速释放片剂及其制备方法
WO2015071761A3 (en) * 2013-11-11 2015-09-24 Crystal Pharmatech Co., Ltd. Crystalline forms b, c, and d of canagliflozin
CN105330706A (zh) * 2014-06-05 2016-02-17 江苏豪森药业股份有限公司 卡格列净中间体的制备方法
CN105503845A (zh) * 2015-12-01 2016-04-20 北京普德康利医药科技发展有限公司 去氟卡格列净化合物及其制备方法和应用
CN105769803A (zh) * 2014-12-16 2016-07-20 康普药业股份有限公司 一种用于治疗2型糖尿病的药物组合物及其制备方法
CN106279134A (zh) * 2015-06-23 2017-01-04 中美华世通生物医药科技（武汉）有限公司 卡格列净单晶及其制备方法和用途
CN106749212A (zh) * 2015-11-24 2017-05-31 重庆圣华曦药业股份有限公司 一种卡格列净中间体的精制方法
CN110946840A (zh) * 2019-12-31 2020-04-03 常州恒邦药业有限公司 一种卡格列净药物组合物及其制备方法
CN115531376A (zh) * 2022-10-26 2022-12-30 河南省人民医院 卡格列净在菌群调节方面的新应用

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US20110009347A1 (en) 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
US9408835B2 (en) 2013-03-29 2016-08-09 Astellas Pharma Inc. Pharmaceutical composition for oral administration
US20160083374A1 (en) * 2013-05-30 2016-03-24 Cadila Healthcare Limited Amorphous form of canagliflozin and process for preparing thereof
WO2015139386A1 (zh) 2014-03-19 2015-09-24 杭州普晒医药科技有限公司 坎格列净一水合物及其晶型、它们的制备方法和用途
EP2947077A1 (en) 2014-05-19 2015-11-25 LEK Pharmaceuticals d.d. Stereoselective synthesis of intermediates in the preparation of ß-C-arylglucosides
TN2016000484A1 (en) * 2014-05-29 2018-04-04 Novartis Ag Ceritinib formulation.
US20160002275A1 (en) * 2014-07-03 2016-01-07 Cadila Healthcare Limited Process for preparation and purification of canagliflozin
EP2990029A1 (en) 2014-08-29 2016-03-02 Sandoz Ag Pharmaceutical compositions comprising Canagliflozin
WO2016104643A1 (ja) * 2014-12-25 2016-06-30 田辺三菱製薬株式会社 糖尿病治療用固形製剤
WO2016142950A1 (en) * 2015-03-11 2016-09-15 Harman Finochem Limited A novel process for preparing (2s,3r,4r,5s,6r)-2-{3-[5-[4-fluoro-phenyl)- thiophen-2-ylmethyl]-4-methyl-phenyl}-6-hydroxymethyl-tetrahydro-pyran-3,4,5- triol and its stable amorphous hemihydrate form
US20170071970A1 (en) * 2015-09-15 2017-03-16 Janssen Pharmaceutica Nv Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders
TWI835735B (zh) * 2017-06-12 2024-03-21 比利時商健生藥品公司 減少或預防第ii型糖尿病患者中心血管事件之方法
CN109553609B (zh) * 2017-09-26 2020-09-04 北大方正集团有限公司 一种卡格列净的制备方法
CN109553649B (zh) * 2017-09-26 2020-12-04 北大方正集团有限公司 一种卡格列净中间体的制备方法
US11857559B2 (en) 2018-09-10 2024-01-02 Aurobindo Pharma Ltd. Pharmaceutical composition comprising Canagliflozin, process of preparation and use thereof
WO2024053680A1 (ja) * 2022-09-07 2024-03-14 田辺三菱製薬株式会社 口腔内崩壊錠

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WO2009022010A1 (en) * 2007-08-16 2009-02-19 Boehringer Ingelheim International Gmbh Pharmaceutical composition comprising a sglt2 inhibitor in combination with a dpp-iv inhibitor

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UY30730A1 (es) 2006-12-04 2008-07-03 Mitsubishi Tanabe Pharma Corp Forma cristalina del hemihidrato de 1-(b (beta)-d-glucopiranosil) -4-metil-3-[5-(4-fluorofenil) -2-tienilmetil]benceno
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PE20120017A1 (es) * 2009-02-13 2012-02-12 Boehringer Ingelheim Int Composicion farmaceutica que comprende un inhibidor de sglt2, un inhibidor de dpp-iv, opcionalmente, un agente antidiabetico adicional, y sus usos

Patent Citations (2)

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WO2005012326A1 (en) * 2003-08-01 2005-02-10 Tanabe Seiyaku Co., Ltd. Novel compounds having inhibitory activity against sodium-dependant transporter
WO2009022010A1 (en) * 2007-08-16 2009-02-19 Boehringer Ingelheim International Gmbh Pharmaceutical composition comprising a sglt2 inhibitor in combination with a dpp-iv inhibitor

Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103641822B (zh) * 2013-10-21 2016-06-08 江苏奥赛康药业股份有限公司 一种卡格列净化合物及其药物组合物
CN103641822A (zh) * 2013-10-21 2014-03-19 江苏奥赛康药业股份有限公司 一种卡格列净化合物及其药物组合物
WO2015071761A3 (en) * 2013-11-11 2015-09-24 Crystal Pharmatech Co., Ltd. Crystalline forms b, c, and d of canagliflozin
CN103655539A (zh) * 2013-12-13 2014-03-26 重庆医药工业研究院有限责任公司 一种卡格列净的口服固体制剂及其制备方法
CN103655539B (zh) * 2013-12-13 2019-09-13 重庆医药工业研究院有限责任公司 一种卡格列净的口服固体制剂及其制备方法
CN103980262A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的b晶型及其结晶制备方法
CN103980261A (zh) * 2014-04-01 2014-08-13 天津大学 卡格列净的a晶型及其结晶制备方法
CN103980262B (zh) * 2014-04-01 2016-06-22 天津大学 卡格列净的b晶型及其结晶制备方法
CN105330706B (zh) * 2014-06-05 2019-04-16 江苏豪森药业集团有限公司 卡格列净中间体的制备方法
CN105330706A (zh) * 2014-06-05 2016-02-17 江苏豪森药业股份有限公司 卡格列净中间体的制备方法
CN104402946B (zh) * 2014-11-17 2018-01-02 连云港恒运药业有限公司 卡格列净中间体及其无定形的制备方法
CN104402946A (zh) * 2014-11-17 2015-03-11 连云港恒运医药科技有限公司 卡格列净中间体及其无定形的制备方法
CN105769803A (zh) * 2014-12-16 2016-07-20 康普药业股份有限公司 一种用于治疗2型糖尿病的药物组合物及其制备方法
CN104523573A (zh) * 2014-12-29 2015-04-22 成都恒瑞制药有限公司 一种卡格列净快速释放片剂及其制备方法
CN106279134A (zh) * 2015-06-23 2017-01-04 中美华世通生物医药科技（武汉）有限公司 卡格列净单晶及其制备方法和用途
CN106749212A (zh) * 2015-11-24 2017-05-31 重庆圣华曦药业股份有限公司 一种卡格列净中间体的精制方法
CN105503845A (zh) * 2015-12-01 2016-04-20 北京普德康利医药科技发展有限公司 去氟卡格列净化合物及其制备方法和应用
CN110946840A (zh) * 2019-12-31 2020-04-03 常州恒邦药业有限公司 一种卡格列净药物组合物及其制备方法
CN110946840B (zh) * 2019-12-31 2021-11-26 常州恒邦药业有限公司 一种卡格列净药物组合物及其制备方法
CN115531376A (zh) * 2022-10-26 2022-12-30 河南省人民医院 卡格列净在菌群调节方面的新应用

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Publication number Publication date
JP5596799B2 (ja) 2014-09-24
CN105769792A (zh) 2016-07-20
TWI564034B (zh) 2017-01-01
US20130052266A1 (en) 2013-02-28
EP2568971B1 (en) 2020-10-14
KR101869110B1 (ko) 2018-06-19
ES2836952T3 (es) 2021-06-28
CN106890147A (zh) 2017-06-27
US20160228375A1 (en) 2016-08-11
WO2011142478A1 (en) 2011-11-17
US9655852B2 (en) 2017-05-23
KR20130106279A (ko) 2013-09-27
TW201200164A (en) 2012-01-01
JP2013526482A (ja) 2013-06-24
EP2568971A1 (en) 2013-03-20

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