AR078475A1 - Procedimiento para preparar una forma cristalina - Google Patents
Procedimiento para preparar una forma cristalinaInfo
- Publication number
- AR078475A1 AR078475A1 ARP100103543A ARP100103543A AR078475A1 AR 078475 A1 AR078475 A1 AR 078475A1 AR P100103543 A ARP100103543 A AR P100103543A AR P100103543 A ARP100103543 A AR P100103543A AR 078475 A1 AR078475 A1 AR 078475A1
- Authority
- AR
- Argentina
- Prior art keywords
- solvent
- solution
- compound
- crystalline form
- group
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/20—Carbocyclic rings
- C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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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
- A61K31/7042—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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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
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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
- A61P3/04—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
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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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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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
- A61P3/08—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
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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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
- C07H7/04—Carbocyclic radicals
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Una composicion farmacéutica y al uso de la misma para preparar medicamentos para tratar trastornos metabolicos. Reivindicacion 1: Un método para preparar una forma cristalina de un compuesto 1-cloro-4-(Beta-D-glucopiranos-1-il)-2-[4-((S)-tetrahidrofurano-3-iloxi)-bencil]-benceno caracterizado porque comprende las siguientes etapas: (a) disolver el compuesto en una mezcla de al menos dos disolventes para formar una disolucion en la que el primer disolvente se selecciona del grupo de disolventes que consiste en tolueno y tetrahidrofurano, y el segundo disolvente se selecciona del grupo de disolventes que consiste en metanol, etanol, 1-propanol y 2-propanol, o el primer disolvente es etanol y el segundo disolvente se selecciona del grupo de disolventes que consiste en acetato de etilo, acetato de n-propilo y etilmetilcetona; (b) almacenar la disolucion para que precipite de la disolucion la forma cristalina del compuesto; (c) aislar de la disolucion la forma cristalina del compuesto. Reivindicacion 5: Un método de acuerdo con la reivindicacion 1, caracterizado porque la forma cristalina se caracteriza por un patron de difraccion de rayos X de polvo que comprende picos a 18,84, 20,36 y 25.21 grados 2theta (2theta+- 0,1 grados), en el que dicho patron de difraccion de rayos X de polvo se hace usando radiacion de CuKalfa1.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP09171847 | 2009-09-30 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR078475A1 true AR078475A1 (es) | 2011-11-09 |
Family
ID=42942225
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100103543A AR078475A1 (es) | 2009-09-30 | 2010-09-29 | Procedimiento para preparar una forma cristalina |
Country Status (21)
Country | Link |
---|---|
US (1) | US8802842B2 (es) |
EP (1) | EP2483286B1 (es) |
JP (1) | JP5736377B2 (es) |
KR (1) | KR101811997B1 (es) |
CN (1) | CN102549005B (es) |
AR (1) | AR078475A1 (es) |
AU (1) | AU2010303123B2 (es) |
BR (1) | BR112012007092B1 (es) |
CA (1) | CA2775961C (es) |
CL (1) | CL2012000810A1 (es) |
DK (1) | DK2483286T3 (es) |
EA (1) | EA020798B1 (es) |
ES (1) | ES2596202T3 (es) |
HU (1) | HUE029381T2 (es) |
IL (1) | IL218102B (es) |
IN (1) | IN2012DN02756A (es) |
MX (1) | MX2012002942A (es) |
NZ (1) | NZ598318A (es) |
PL (1) | PL2483286T3 (es) |
TW (1) | TWI482778B (es) |
WO (1) | WO2011039107A1 (es) |
Families Citing this family (68)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA91546C2 (uk) * | 2005-05-03 | 2010-08-10 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | КРИСТАЛІЧНА ФОРМА 1-ХЛОР-4-(β-D-ГЛЮКОПІРАНОЗ-1-ИЛ)-2-[4-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)-БЕНЗИЛ]-БЕНЗОЛУ, СПОСІБ ЇЇ ОДЕРЖАННЯ ТА ЇЇ ЗАСТОСУВАННЯ ПРИ ПРИГОТУВАННІ ЛІКАРСЬКИХ ЗАСОБІВ |
US7772191B2 (en) | 2005-05-10 | 2010-08-10 | Boehringer Ingelheim International Gmbh | Processes for preparing of glucopyranosyl-substituted benzyl-benzene derivatives and intermediates therein |
DE602006018961D1 (de) * | 2005-09-08 | 2011-01-27 | Boehringer Ingelheim Pharma | KRISTALLINE FORMEN VON 1-CHLORO-4-(ß-D-GLUCOPYRANOS-1-YL)-2-(4-ETHYNYL-BENZYL)-BENZOL, ZUBEREITUNGSVERFAHREN DAFÜR UND DESSEN VERWENDUNG ZUR ARZNEIMITTELHERSTELLUNG |
PE20080697A1 (es) | 2006-05-03 | 2008-08-05 | Boehringer Ingelheim Int | Derivados de benzonitrilo sustituidos con glucopiranosilo, composiciones farmaceuticas que contienen compuestos de este tipo, su uso y procedimiento para su fabricacion |
US8283326B2 (en) * | 2006-10-27 | 2012-10-09 | Boehringer Ingelheim International Gmbh | Crystalline form of 4-(beta-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, a method for its preparation and the use thereof for preparing medicaments |
PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
JP5498392B2 (ja) | 2007-11-30 | 2014-05-21 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 1,5−ジヒドロ−ピラゾロ[3,4−d]ピリミジン−4−オン誘導体及びcns障害の治療のためのpde9aモジュレーターとしてのそれらの使用 |
UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
EP2334684B1 (en) | 2008-09-08 | 2017-08-02 | Boehringer Ingelheim International GmbH | Pyrazolopyrimidines and their use for the treatment of cns disorders |
PT2395983T (pt) | 2009-02-13 | 2020-07-03 | Boehringer Ingelheim Int | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dp-iv e opcionalmente um agente antidiabético adicional e suas utilizações |
DK2414363T3 (da) | 2009-03-31 | 2014-01-27 | Boehringer Ingelheim Int | 1-heterocyklyl-1,5-dihydro-pyrazol[3,4-d]pyrimidin-4-on-derivater og anvendelse af disse som PDE9A-modulatorer. |
BR112012007085B8 (pt) | 2009-09-30 | 2021-05-25 | Boehringer Ingelheim Int | processos para a preparação de derivados de benzil-benzeno substituídos com glicopiranosila |
AU2010303123B2 (en) | 2009-09-30 | 2014-02-27 | Boehringer Ingelheim International Gmbh | Method for the preparation of a crystalline form of 1-chloro-4- (Beta-D-glucopyranos-1-yl)-2-(4-((S)-tetrahydrofuran-3-yloxy)benzyl)benzene |
US10610489B2 (en) | 2009-10-02 | 2020-04-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, pharmaceutical dosage form, process for their preparation, methods for treating and uses thereof |
SG187081A1 (en) | 2010-08-12 | 2013-03-28 | Boehringer Ingelheim Int | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
US20130035281A1 (en) * | 2011-02-09 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
UY33937A (es) | 2011-03-07 | 2012-09-28 | Boehringer Ingelheim Int | Composiciones farmacéuticas que contienen inhibidores de dpp-4 y/o sglt-2 y metformina |
AU2012264736A1 (en) | 2011-06-03 | 2013-11-28 | Boehringer Ingelheim International Gmbh | SGLT-2 inhibitors for treating metabolic disorders in patients treated with neuroleptic agents |
US20130035298A1 (en) * | 2011-07-08 | 2013-02-07 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
US9192617B2 (en) * | 2012-03-20 | 2015-11-24 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
WO2013152476A1 (en) * | 2012-04-10 | 2013-10-17 | Theracos, Inc. | Process for the preparation of benzylbenzene sglt2 inhibitors |
US9193751B2 (en) | 2012-04-10 | 2015-11-24 | Theracos, Inc. | Process for the preparation of benzylbenzene SGLT2 inhibitors |
EP2981269B9 (en) | 2013-04-04 | 2023-12-06 | Boehringer Ingelheim Vetmedica GmbH | Treatment of metabolic disorders in equine animals |
US11813275B2 (en) | 2013-04-05 | 2023-11-14 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
US20140303097A1 (en) | 2013-04-05 | 2014-10-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
PT2981271T (pt) | 2013-04-05 | 2019-02-19 | Boehringer Ingelheim Int | Utilizações terapêuticas de empagliflozina |
WO2014170383A1 (en) | 2013-04-18 | 2014-10-23 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
EP4285995A3 (en) | 2013-12-17 | 2024-02-28 | Boehringer Ingelheim Vetmedica GmbH | An sglt-2 inhibitor for use in the treatment of a metabolic disorder in feline animals |
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WO2015110402A1 (en) | 2014-01-23 | 2015-07-30 | Boehringer Ingelheim Vetmedica Gmbh | Treatment of metabolic disorders in canine animals |
KR20220079690A (ko) | 2014-04-01 | 2022-06-13 | 베링거잉겔하임베트메디카게엠베하 | 말과 동물에서 대사 장애의 치료 |
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CN105481843A (zh) * | 2014-09-19 | 2016-04-13 | 重庆医药工业研究院有限责任公司 | 一种恩格列净无定型物及其制备方法 |
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KR20180122004A (ko) * | 2016-03-16 | 2018-11-09 | 베링거 인겔하임 인터내셔날 게엠베하 | 엠파글리플로진을 포함하는 약제학적 조성물 및 이의 용도 |
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JP2019533709A (ja) | 2016-11-10 | 2019-11-21 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 医薬組成物、治療方法及びその使用 |
CN108794548B (zh) * | 2017-04-28 | 2023-06-16 | 正大天晴药业集团股份有限公司 | 制备恩格列净及其中间体的方法 |
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KR102150825B1 (ko) | 2020-04-06 | 2020-09-03 | 유니셀랩 주식회사 | 새로운 sglt-2 억제제의 신규한 공결정 |
JP2023520899A (ja) | 2020-04-07 | 2023-05-22 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 頭痛障害の処置のための方法 |
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KR102218323B1 (ko) | 2020-09-09 | 2021-02-22 | 유니셀랩 주식회사 | 효율적이고 상전이가 되지 않는 엠파글리플로진 무정형의 제조방법 |
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EP4376830A1 (en) | 2021-07-28 | 2024-06-05 | Boehringer Ingelheim Vetmedica GmbH | Use of sglt-2 inhibitors for the prevention and/or treatment of renal diseases in non-human mammals |
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- 2010-09-24 CA CA2775961A patent/CA2775961C/en active Active
- 2010-09-24 IN IN2756DEN2012 patent/IN2012DN02756A/en unknown
- 2010-09-24 CN CN201080043252.2A patent/CN102549005B/zh active Active
- 2010-09-24 KR KR1020127008069A patent/KR101811997B1/ko active IP Right Grant
- 2010-09-24 MX MX2012002942A patent/MX2012002942A/es active IP Right Grant
- 2010-09-24 DK DK10755201.0T patent/DK2483286T3/en active
- 2010-09-24 HU HUE10755201A patent/HUE029381T2/en unknown
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BR112012007092B1 (pt) | 2020-03-31 |
IL218102A0 (en) | 2012-04-30 |
HUE029381T2 (en) | 2017-02-28 |
CA2775961C (en) | 2017-11-07 |
CN102549005A (zh) | 2012-07-04 |
WO2011039107A1 (en) | 2011-04-07 |
JP2013505974A (ja) | 2013-02-21 |
PL2483286T3 (pl) | 2017-04-28 |
AU2010303123B2 (en) | 2014-02-27 |
IN2012DN02756A (es) | 2015-09-18 |
KR101811997B1 (ko) | 2017-12-26 |
IL218102B (en) | 2020-06-30 |
AU2010303123A1 (en) | 2012-03-15 |
KR20120091024A (ko) | 2012-08-17 |
EA201200506A1 (ru) | 2012-11-30 |
EA020798B1 (ru) | 2015-01-30 |
MX2012002942A (es) | 2012-04-11 |
CA2775961A1 (en) | 2011-04-07 |
US20110237526A1 (en) | 2011-09-29 |
NZ598318A (en) | 2014-02-28 |
DK2483286T3 (en) | 2016-09-19 |
TWI482778B (zh) | 2015-05-01 |
US8802842B2 (en) | 2014-08-12 |
EP2483286B1 (en) | 2016-07-13 |
ES2596202T3 (es) | 2017-01-05 |
CN102549005B (zh) | 2015-08-26 |
CL2012000810A1 (es) | 2012-08-31 |
TW201127849A (en) | 2011-08-16 |
JP5736377B2 (ja) | 2015-06-17 |
BR112012007092A2 (pt) | 2016-08-23 |
EP2483286A1 (en) | 2012-08-08 |
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