ES2530345T3 - Derivados de pirazolopiridinona como antagonistas del receptor del LPA - Google Patents
Derivados de pirazolopiridinona como antagonistas del receptor del LPA Download PDFInfo
- Publication number
- ES2530345T3 ES2530345T3 ES11741410T ES11741410T ES2530345T3 ES 2530345 T3 ES2530345 T3 ES 2530345T3 ES 11741410 T ES11741410 T ES 11741410T ES 11741410 T ES11741410 T ES 11741410T ES 2530345 T3 ES2530345 T3 ES 2530345T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- aryl
- heterocyclyl
- cycloalkyl
- heteroaryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 102000004137 Lysophosphatidic Acid Receptors Human genes 0.000 title 1
- 108090000642 Lysophosphatidic Acid Receptors Proteins 0.000 title 1
- TUPZMLLDXCWVKH-UHFFFAOYSA-N pyrazolo[4,3-b]pyridin-3-one Chemical class C1=CN=C2C(=O)N=NC2=C1 TUPZMLLDXCWVKH-UHFFFAOYSA-N 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 3
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 3
- -1 -OH Chemical group 0.000 abstract 2
- 229910006069 SO3H Inorganic materials 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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- 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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- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Communicable Diseases (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10009117 | 2010-09-02 | ||
| PCT/EP2011/003949 WO2012028243A1 (en) | 2010-09-02 | 2011-08-05 | Pyrazolopyridinone derivatives as lpa receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2530345T3 true ES2530345T3 (es) | 2015-03-02 |
Family
ID=44532738
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES11741410T Active ES2530345T3 (es) | 2010-09-02 | 2011-08-05 | Derivados de pirazolopiridinona como antagonistas del receptor del LPA |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8859775B2 (enExample) |
| EP (1) | EP2611808B1 (enExample) |
| JP (1) | JP6039559B2 (enExample) |
| CN (1) | CN103189378B (enExample) |
| AR (1) | AR082880A1 (enExample) |
| AU (1) | AU2011297961B2 (enExample) |
| CA (1) | CA2809892C (enExample) |
| ES (1) | ES2530345T3 (enExample) |
| IL (1) | IL225015A (enExample) |
| WO (1) | WO2012028243A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2744807A4 (en) | 2011-08-15 | 2015-03-04 | Intermune Inc | COMPOUNDS AS LYSOPHOSPHIC ACID RECEPTOR ANTAGONISTS |
| DK2882715T3 (en) | 2012-05-18 | 2017-02-13 | Sanofi Sa | PYRAZOL DERIVATIVES AND USE THEREOF AS LPAR5 ANTAGONISTS |
| JP2015521183A (ja) | 2012-05-18 | 2015-07-27 | サノフイ | ピリジン誘導体および病理学的血栓形成に関連する状態の治療へのその使用 |
| SI2861566T1 (sl) | 2012-06-13 | 2017-03-31 | F. Hoffmann-La Roche Ag | Novi diazaspirocikloalkan in azaspirocikloalkan |
| ES2563861T3 (es) | 2012-06-14 | 2016-03-16 | Daiichi Sankyo Company, Limited | Derivado de piperidinilpirazolopiridina |
| PL2900669T3 (pl) * | 2012-09-25 | 2020-01-31 | F. Hoffmann-La Roche Ag | Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| WO2015050148A1 (ja) * | 2013-10-04 | 2015-04-09 | 第一三共株式会社 | ３－アリールピラゾロピリジン誘導体 |
| WO2015076353A1 (ja) * | 2013-11-25 | 2015-05-28 | 第一三共株式会社 | ３－アルキルピラゾロピリジン誘導体 |
| AU2014356583B2 (en) | 2013-11-26 | 2019-02-28 | F. Hoffmann-La Roche Ag | New octahydro-cyclobuta (1,2-c;3,4-c')dipyrrol-2-yl |
| WO2015087996A1 (ja) * | 2013-12-13 | 2015-06-18 | 第一三共株式会社 | イミダゾピリジン誘導体 |
| WO2015087995A1 (ja) * | 2013-12-13 | 2015-06-18 | 第一三共株式会社 | シクロアルキル又はヘテロシクリルピラゾロピリジン誘導体 |
| KR20160096612A (ko) * | 2013-12-13 | 2016-08-16 | 다이이찌 산쿄 가부시키가이샤 | 5-하이드록시-4-(트리플루오로메틸)피라졸로피리딘 유도체 |
| WO2015102856A1 (en) * | 2013-12-30 | 2015-07-09 | Rxbio Inc. | Crystalline salts of (z)-o-octadec-9-en-1-yl o,o-dihydrogen phosphorothioate |
| WO2015111545A1 (ja) * | 2014-01-21 | 2015-07-30 | 第一三共株式会社 | 縮合ピラゾール誘導体 |
| CR20160418A (es) | 2014-03-26 | 2016-11-07 | Hoffmann La Roche | Nuevos compuestos biciclicos de 7 eslabones |
| MA50635A (fr) | 2014-03-26 | 2020-08-12 | Hoffmann La Roche | Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| US10118904B2 (en) | 2015-06-05 | 2018-11-06 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of Demyelinating Diseases |
| TWI713534B (zh) * | 2015-06-11 | 2020-12-21 | 日商第一三共股份有限公司 | 5-羥基-4-(三氟甲基)吡唑并吡啶衍生物之結晶及其用途 |
| EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
| AU2016324483B2 (en) | 2015-09-18 | 2021-07-29 | Memorial Sloan Kettering Cancer Center | Methods and compositions of inhibiting DCN1-UBC12 interaction |
| WO2017050747A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| AU2016328437A1 (en) | 2015-09-24 | 2018-01-25 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| MA42918A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| BR112018006080A2 (pt) | 2015-09-24 | 2018-10-09 | F. Hoffmann-La Roche Ag | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| RU2742608C2 (ru) * | 2016-04-14 | 2021-02-09 | Марс, Инкорпорейтед | Способы идентификации модуляторов gpr92 |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
| WO2018106641A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
| WO2018106646A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Aminotriazoles for the treatment of demyelinating diseases |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| JP7050165B2 (ja) | 2018-02-26 | 2022-04-07 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｂｖ複製阻害剤としての置換ピロリジン化合物 |
| KR20200138202A (ko) | 2018-03-30 | 2020-12-09 | 다이이찌 산쿄 가부시키가이샤 | Lcat 결손증 치료약 |
| CN108558876B (zh) * | 2018-05-28 | 2020-08-04 | 中南大学 | 吡唑[3,4-b]并吡啶类衍生物及其制备方法和应用 |
| CN108379275B (zh) * | 2018-05-29 | 2020-05-22 | 中国医学科学院阜外医院 | 溶血磷脂酸、溶血磷脂酸受体3以及溶血磷脂酸受体3激动剂的应用 |
| EP3846640A1 (en) | 2018-09-07 | 2021-07-14 | Mars Incorporated | Compounds that modulate gpr92 receptor activity and pet food products containing the same |
| US12479816B2 (en) | 2019-02-08 | 2025-11-25 | University of Pittsburgh—of the Commonwealth System of Higher Education | 20-HETE formation inhibitors |
| US12409171B2 (en) | 2019-06-20 | 2025-09-09 | University Of Kentucky Research Foundation | Pharmaceutically active pyrazolo-pyridone modulators of DCN1/2-mediated cullin neddylation |
| US20230061417A1 (en) * | 2019-12-12 | 2023-03-02 | Chiesi Farmaceutici S.P.A. | Thienopyrimidine derivatives as lpa receptor 2 inhibitors |
| US12404270B2 (en) | 2019-12-12 | 2025-09-02 | Chiesi Farmaceutici S.P.A. | Quinazoline derivatives as LPA receptor 2 inhibitors |
| JP2023505703A (ja) | 2019-12-12 | 2023-02-10 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | Ｌｐａ受容体２阻害剤としての芳香族アミド誘導体 |
| ES2991765T3 (es) | 2020-07-16 | 2024-12-04 | Chiesi Farm Spa | Derivados del ácido amido ciclohexano como inhibidores del receptor de LPA |
| WO2022174882A1 (en) | 2021-02-16 | 2022-08-25 | Chiesi Farmaceutici S.P.A. | 5-membered heterocyclyl carbamate derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors |
| WO2022174883A1 (en) | 2021-02-16 | 2022-08-25 | Chiesi Farmaceutici S.P.A. | 5-membered heterocyclyl derivatives as dual lpa receptor 1 and lpa receptor 2 inhibitors |
| US20240190860A1 (en) | 2021-03-24 | 2024-06-13 | Chiesi Farmaceutici S.P.A. | 8-cyclo-substituted quinazoline derivatives as lpa receptor 2 inhibitors |
| US20250066341A1 (en) | 2021-12-23 | 2025-02-27 | Chiesi Farmaceutici S.P.A. | Cyclohexane acid derivatives as lpa receptor inhibitors |
| WO2023170025A1 (en) | 2022-03-08 | 2023-09-14 | Chiesi Farmaceutici S.P.A. | Amido cyclopropyl derivatives as lpa receptor inhibitors |
| WO2025247961A1 (en) | 2024-05-31 | 2025-12-04 | Centre Hospitalier Universitaire Vaudois (C.H.U.V.) | Lpa-lpar signaling as a therapeutic target or diagnostic tool for brain diseases |
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| GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
| EP1187633A4 (en) | 1999-04-08 | 2005-05-11 | Arch Dev Corp | USE OF ANTI-VEGF ANTIBODIES TO ENHANCE RADIATION IN ANTICANCER THERAPY |
| BRPI0113757B8 (pt) | 2000-09-11 | 2017-11-07 | Chiron Corp | derivados de quinolinona como inibidores de tirosina quinase |
| EP1364659B1 (en) | 2001-02-08 | 2009-11-11 | Ono Pharmaceutical Co., Ltd. | Remedies for urinary diseases comprising lpa receptor controlling agents |
| CA2473740A1 (en) | 2002-01-18 | 2003-07-31 | David Solow-Cordero | Methods of treating conditions associated with an edg receptor |
| AU2003229305A1 (en) | 2002-05-17 | 2003-12-02 | Scios, Inc. | TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS |
| PA8580301A1 (es) | 2002-08-28 | 2005-05-24 | Pfizer Prod Inc | Nuevos derivados de benzoimidazol utiles como agentes antiproliferativos |
| US20040167192A1 (en) * | 2003-01-16 | 2004-08-26 | David Solow-Cordero | Methods of treating conditions associated with an Edg-7 receptor |
| CA2525245C (en) * | 2003-06-27 | 2010-10-19 | Pfizer Products Inc. | Pyrazolo[3,4-b]pyridin-6-ones as gsk-3 inhibitors |
| JP5048333B2 (ja) | 2003-10-09 | 2012-10-17 | ユニバーシティ オブ テネシー リサーチ ファウンデーション | Ｌｐａ受容体アゴニストおよびアンタゴニストならびに使用法 |
| EP1750722A4 (en) | 2004-05-06 | 2010-03-10 | Univ Virginia | NEW LYSOPHOSPHIC ACID RECEPTORSELECTIVE ANTAGONISTS |
| WO2007139946A2 (en) * | 2006-05-25 | 2007-12-06 | University Of Tennessee Research Foundation | Gpcr ligands identified by computational modeling |
| AU2009243756B2 (en) | 2008-05-05 | 2013-06-27 | Sanofi-Aventis | Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals |
| GB2466121B (en) | 2008-12-15 | 2010-12-08 | Amira Pharmaceuticals Inc | Antagonists of lysophosphatidic acid receptors |
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- 2011-08-05 WO PCT/EP2011/003949 patent/WO2012028243A1/en not_active Ceased
- 2011-08-05 CN CN201180042323.1A patent/CN103189378B/zh not_active Expired - Fee Related
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| JP6039559B2 (ja) | 2016-12-07 |
| EP2611808B1 (en) | 2014-11-12 |
| US20140350046A1 (en) | 2014-11-27 |
| CN103189378A (zh) | 2013-07-03 |
| AR082880A1 (es) | 2013-01-16 |
| CN103189378B (zh) | 2016-03-02 |
| EP2611808A1 (en) | 2013-07-10 |
| CA2809892C (en) | 2019-05-28 |
| US9067938B2 (en) | 2015-06-30 |
| CA2809892A1 (en) | 2012-03-08 |
| IL225015A (en) | 2016-06-30 |
| US20130165478A1 (en) | 2013-06-27 |
| AU2011297961B2 (en) | 2015-07-02 |
| AU2011297961A1 (en) | 2013-04-18 |
| WO2012028243A1 (en) | 2012-03-08 |
| JP2013536807A (ja) | 2013-09-26 |
| US8859775B2 (en) | 2014-10-14 |
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