PE20091825A1 - Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 - Google Patents
Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3Info
- Publication number
- PE20091825A1 PE20091825A1 PE2009000460A PE2009000460A PE20091825A1 PE 20091825 A1 PE20091825 A1 PE 20091825A1 PE 2009000460 A PE2009000460 A PE 2009000460A PE 2009000460 A PE2009000460 A PE 2009000460A PE 20091825 A1 PE20091825 A1 PE 20091825A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- methyl
- hydroxy
- hydroximethyl
- pyrrolidines
- Prior art date
Links
Classifications
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- 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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- 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
- A61K31/425—Thiazoles
- A61K31/428—Thiazoles condensed with carbocyclic rings
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- 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
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P13/06—Anti-spasmodics
-
- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
-
- 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
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE HIDROXIMETIL PIRROLIDINAS DE FORMULA (Ia), DONDE Y ES ALCANODIILO(C1-C5), ALQUENODIILO(C2-C5), UN ENLACE, FENILO SUSTITUIDO O NO, ENTRE OTROS; Z ES FENILO, ANILLO DE BENCENO CONDENSADO CON ANILLO CARBOCICLICO C5-C10, ANILLO HETEROCICLICO DE 5-6 MIEMBROS CON 1-4 HETROATOMOS DE O, S, N, ENTRE OTROS; R3 ES -CN, OXO, ALQUILO C1-C6 SUSTITUIDO O NO, ENTRE OTROS; n ES DE 0-5. SON COMPUESTOS SELECCIONADOS: 2-(2-AMINO-1,3-TIAZOL-4-IL)-N-[4-({(5R)-[(R)-HIDROXI(FENIL)METIL]PIRROLIDINIL}METIL)FENIL]ACETAMIDA; 2-(2-AMINO-1,3-TIAZOL-4-IL)-N-[4-({(2S,5R)-[(R)-HIDROXI(FENIL)METIL]PIRROLIDINIL}METIL)FENIL]ACETAMIDA; N-(4-(((2S,5R)-5-((R)-HIDROXI(FENIL)METIL)PIRROLIDIN-2-IL)METIL)FENIL)-2-(3-METIL-1H-1,2,4-TRIAZOL-1-IL)PROPANAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON AGONISTAS DEL RECEPTOR ADRENERGICO BETA 3 SIENDO UTILES EN EL TRATAMIENTO DE VEJIGA SOBREACTIVA, INCONTINENCIA URINARIA, URGENCIA URINARIA, ENTRE OTROS
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12306308P | 2008-04-04 | 2008-04-04 | |
| US20604309P | 2009-01-27 | 2009-01-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091825A1 true PE20091825A1 (es) | 2009-12-04 |
Family
ID=40671093
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2009000460A PE20091825A1 (es) | 2008-04-04 | 2009-03-27 | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
Country Status (41)
Families Citing this family (66)
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| US4891872A (en) | 1988-05-09 | 1990-01-09 | Sussman Martin V | Apparatus for incrementally drawing fibers |
| PE20091825A1 (es) * | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
| BR112012004333A2 (pt) * | 2009-08-27 | 2015-09-08 | Merck Sharp & Dohme | composto, composição farmacêutica, e, método para o tratamento ou a prevenção de uma doença ou um distúrbio. |
| US20120202819A1 (en) * | 2009-10-07 | 2012-08-09 | Merck Sharp & Dohme Corporation | Combination therapy using a beta 3 adrenergic receptor agonists and an antimuscarinic agent |
| US8748433B2 (en) * | 2010-04-30 | 2014-06-10 | Merck Sharp & Dohme Corp. | β3 adrenergic receptor agonists |
| WO2012012314A1 (en) * | 2010-07-23 | 2012-01-26 | Merck Sharp & Dohme Corp. | Novel pyrrolidine derived beta 3 adrenergic receptor agonists |
| US9522129B2 (en) | 2010-08-03 | 2016-12-20 | Velicept Therapeutics, Inc. | Pharmaceutical Combination |
| US9907767B2 (en) | 2010-08-03 | 2018-03-06 | Velicept Therapeutics, Inc. | Pharmaceutical compositions and the treatment of overactive bladder |
| EP2600859A1 (en) * | 2010-08-03 | 2013-06-12 | Altherx Inc. | Combinations of beta - 3 adrenergic receptor agonists and muscarinic receptor antagonists for treating overactive bladder |
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| JP6088535B2 (ja) * | 2011-10-27 | 2017-03-08 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | ベータ3アゴニストおよび中間体を製造するプロセス |
| WO2013062881A1 (en) * | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| CN106479990B (zh) | 2011-11-18 | 2020-09-18 | 科德克希思公司 | 用于制备羟基取代的氨基甲酸酯的生物催化剂 |
| KR20150020160A (ko) | 2012-02-09 | 2015-02-25 | 앨씨알엑스, 인크. | 과민성 방광의 치료를 위한 무스카린 수용체 길항제 및 베타―3 아드레날린 수용체 작용제의 조합물 |
| JP2015178458A (ja) * | 2012-07-25 | 2015-10-08 | 杏林製薬株式会社 | ベンゼン環縮合含窒素5員複素環式化合物、またはその薬理学的に許容される塩 |
| WO2014108449A1 (en) | 2013-01-08 | 2014-07-17 | Atrogi Ab | A screening method, a kit, a method of treatment and a compound for use in a method of treatment |
| NZ712180A (en) | 2013-03-13 | 2017-01-27 | Flatley Discovery Lab Llc | Pyridazinone compounds and methods for the treatment of cystic fibrosis |
| ES2746801T3 (es) | 2013-03-15 | 2020-03-06 | Merck Sharp & Dohme | Proceso de preparación de agonistas beta-3 y productos intermedios |
| CN103232352B (zh) * | 2013-05-11 | 2015-12-23 | 苏州永健生物医药有限公司 | (r)-4-(2-(2-羟基-2-苯乙胺基)乙基)苯胺基甲酸叔丁基酯 |
| CN103760286A (zh) * | 2014-01-14 | 2014-04-30 | 北京万全德众医药生物技术有限公司 | 一种用高效液相色谱法测定琥珀酸索非那新中间体光学纯度的方法 |
| EP3882252B1 (en) | 2014-06-11 | 2025-11-19 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| HK1245117A1 (zh) | 2014-12-03 | 2018-08-24 | Velicept Therapeutics, Inc. | 使用调节释放索拉贝隆用於下尿路症状的组合物和方法 |
| EP3247354B1 (en) * | 2015-01-20 | 2019-08-07 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| FI3365321T3 (fi) | 2015-10-23 | 2024-01-02 | B3Ar Therapeutics Inc | Solabegron-Zwitterioni ja sen käyttöjä |
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| US12173018B2 (en) | 2018-05-25 | 2024-12-24 | VenatoRx Pharmaceuticals, Inc. | Penicillin-binding protein inhibitors |
| EP4545072A3 (en) * | 2018-12-05 | 2025-07-02 | Urovant Sciences GmbH | Use of vibegron to treat overactive bladder symptoms in men with benign prostatic hyperplasia |
| CN109503500A (zh) * | 2018-12-17 | 2019-03-22 | 天津药明康德新药开发有限公司 | 一种2-(2-氧代吡嗪-1(2h)-基)乙酸的合成方法 |
| CN109734712B (zh) * | 2019-01-30 | 2020-10-20 | 广东东阳光药业有限公司 | 芳基或杂芳基取代的吡咯烷酰胺衍生物及其用途 |
| CA3129024A1 (en) | 2019-03-18 | 2020-09-24 | Urovant Sciences Gmbh | Use of vibegron to treat overactive bladder |
| GB201903832D0 (en) | 2019-03-20 | 2019-05-01 | Atrogi Ab | New compounds and methods |
| WO2021003383A1 (en) | 2019-07-02 | 2021-01-07 | Reald Spark, Llc | Directional display apparatus |
| WO2021041202A1 (en) | 2019-08-23 | 2021-03-04 | Reald Spark, Llc | Directional illumination apparatus and privacy display |
| WO2021050967A1 (en) | 2019-09-11 | 2021-03-18 | Reald Spark, Llc | Directional illumination apparatus and privacy display |
| WO2021050918A1 (en) | 2019-09-11 | 2021-03-18 | Reald Spark, Llc | Switchable illumination apparatus and privacy display |
| US11162661B2 (en) | 2019-10-03 | 2021-11-02 | Reald Spark, Llc | Illumination apparatus comprising passive optical nanostructures |
| JP7604471B2 (ja) | 2019-10-03 | 2024-12-23 | リアルディー スパーク エルエルシー | 照射装置を製造する方法 |
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| ES3048448T3 (en) | 2020-07-22 | 2025-12-10 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
| EP4267143A1 (en) | 2020-12-22 | 2023-11-01 | Urovant Sciences GmbH | Methods of monitoring digoxin with concomitant use of vibegron to treat overactive bladder |
| WO2022175848A1 (en) | 2021-02-16 | 2022-08-25 | Urovant Sciences Gmbh | Methods of treating heart failure with vibegron |
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| JP2025535162A (ja) * | 2022-10-18 | 2025-10-22 | ボナファイド・ヘルス,エルエルシー | βアドレナリン作動及びムスカリン拮抗組成物並びに使用方法 |
| CN115850286B (zh) * | 2022-12-05 | 2023-08-22 | 奥锐特药业(天津)有限公司 | 一种维贝格龙中间体及其制备方法 |
| CN117756809A (zh) * | 2023-12-21 | 2024-03-26 | 苏州莱克施德药业有限公司 | (6s)4,6,7,8-四氢-4-氧代吡咯并[1,2-a]嘧啶-6-羧酸甲酯的合成方法 |
| WO2025262600A1 (en) | 2024-06-17 | 2025-12-26 | Urovant Sciences Gmbh | Crystalline form of vibegron hemihydrate |
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| US6525202B2 (en) * | 2000-07-17 | 2003-02-25 | Wyeth | Cyclic amine phenyl beta-3 adrenergic receptor agonists |
| DOP2003000587A (es) | 2002-02-27 | 2003-08-30 | Pfizer Prod Inc | AGONISTAS DEL RECEPTOR ß3-ADRENERGICO |
| NZ539577A (en) * | 2002-11-07 | 2007-06-29 | Astellas Pharma Inc | Remedy for overactive bladder comprising acetic acid anilide derivative as the active ingredient |
| FR2874011B1 (fr) * | 2004-08-03 | 2007-06-15 | Sanofi Synthelabo | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| PE20091825A1 (es) | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
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2009
- 2009-03-27 PE PE2009000460A patent/PE20091825A1/es active IP Right Grant
- 2009-03-30 AR ARP090101127A patent/AR072043A1/es active IP Right Grant
- 2009-04-02 EP EP09726601A patent/EP2276756B9/en active Active
- 2009-04-02 RS RS20120042A patent/RS52175B/sr unknown
- 2009-04-02 WO PCT/US2009/039249 patent/WO2009124166A1/en not_active Ceased
- 2009-04-02 CN CN200980121149.2A patent/CN102056917B/zh active Active
- 2009-04-02 MX MX2010010929A patent/MX2010010929A/es active IP Right Grant
- 2009-04-02 PL PL09726601T patent/PL2276756T3/pl unknown
- 2009-04-02 EA EA201071169A patent/EA020135B1/ru not_active IP Right Cessation
- 2009-04-02 KR KR1020127015876A patent/KR101288798B1/ko not_active Expired - Fee Related
- 2009-04-02 SI SI200930188T patent/SI2276756T1/sl unknown
- 2009-04-02 ME MEP-2012-549A patent/ME01988B/me unknown
- 2009-04-02 US US12/417,239 patent/US8247415B2/en active Active
- 2009-04-02 JP JP2010543320A patent/JP4783867B2/ja active Active
- 2009-04-02 WO PCT/US2009/039253 patent/WO2009124167A1/en not_active Ceased
- 2009-04-02 KR KR1020127026256A patent/KR20120118086A/ko not_active Withdrawn
- 2009-04-02 HR HRP20120129AT patent/HRP20120129T2/hr unknown
- 2009-04-02 SG SG2013017736A patent/SG188883A1/en unknown
- 2009-04-02 CN CN201110265670.2A patent/CN102391255B/zh active Active
- 2009-04-02 US US12/936,221 patent/US8399480B2/en active Active
- 2009-04-02 ES ES09726601T patent/ES2376278T3/es active Active
- 2009-04-02 GE GEAP200911992A patent/GEP20125666B/en unknown
- 2009-04-02 PT PT09726601T patent/PT2276756E/pt unknown
- 2009-04-02 NZ NZ588266A patent/NZ588266A/en unknown
- 2009-04-02 AU AU2009231714A patent/AU2009231714B2/en active Active
- 2009-04-02 CA CA2719876A patent/CA2719876C/en active Active
- 2009-04-02 KR KR1020107024750A patent/KR101331771B1/ko active Active
- 2009-04-02 AT AT09726601T patent/ATE535521T1/de active
- 2009-04-02 BR BRPI0909768-6A patent/BRPI0909768B1/pt active IP Right Grant
- 2009-04-03 TW TW098111302A patent/TWI378098B/zh active
- 2009-04-03 CL CL2009000815A patent/CL2009000815A1/es unknown
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2010
- 2010-07-14 JP JP2010159938A patent/JP5432846B2/ja active Active
- 2010-09-16 IL IL208215A patent/IL208215A/en active IP Right Grant
- 2010-09-20 ZA ZA2010/06720A patent/ZA201006720B/en unknown
- 2010-09-30 HN HN2010002030A patent/HN2010002030A/es unknown
- 2010-09-30 SV SV2010003687A patent/SV2010003687A/es unknown
- 2010-10-01 DO DO2010000294A patent/DOP2010000294A/es unknown
- 2010-10-01 NI NI201000164A patent/NI201000164A/es unknown
- 2010-10-04 CO CO10122821A patent/CO6331440A2/es active IP Right Grant
- 2010-10-04 EC EC2010010518A patent/ECSP10010518A/es unknown
- 2010-10-22 CR CR11751A patent/CR11751A/es unknown
- 2010-10-29 MA MA33292A patent/MA32257B1/fr unknown
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2011
- 2011-05-13 JP JP2011107738A patent/JP4783870B1/ja active Active
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2012
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- 2012-06-20 US US13/527,934 patent/US8653260B2/en active Active
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2013
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2024
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