AR076974A1 - Metodo para sintetizar pirfenidona - Google Patents
Metodo para sintetizar pirfenidonaInfo
- Publication number
- AR076974A1 AR076974A1 ARP100101971A ARP100101971A AR076974A1 AR 076974 A1 AR076974 A1 AR 076974A1 AR P100101971 A ARP100101971 A AR P100101971A AR P100101971 A ARP100101971 A AR P100101971A AR 076974 A1 AR076974 A1 AR 076974A1
- Authority
- AR
- Argentina
- Prior art keywords
- pirfenidone
- bromobenzene
- dibromobenzene
- butanol
- methyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
- C07D213/643—2-Phenoxypyridines; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered 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
- A61K31/33—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
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Environmental Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pyridine Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un proceso para sintetizar pirfenidona a partir de bromobenceno con menos de aproximadamente 0,15% en peso de dibromobenceno. También, procesos para sintetizar pirfenidona sin usar acetato de etilo o n-butanol, y pirfenidona con niveles controlados de acetato de etilo, n-butanol, di(5-metil-2-piridinona)bencenos, y otras impurezas con los tiempos de retencion que se especifican. También, formas de dosificacion que se formulan incluyendo la pirfenidona que se divulga. Reivindicacion 1: Un método para sintetizar pirfenidona caracterizado porque comprende mezclar bromobenceno, 5-metil-2-piridona, oxido cuproso, y un solvente orgánico en condiciones suficientes para formar pirfenidona, donde el bromobenceno comprende menos de aproximadamente 0,15% en peso o como proporcion molar, de dibromobenceno.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18358809P | 2009-06-03 | 2009-06-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076974A1 true AR076974A1 (es) | 2011-07-20 |
Family
ID=43298478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101971A AR076974A1 (es) | 2009-06-03 | 2010-06-03 | Metodo para sintetizar pirfenidona |
Country Status (35)
| Country | Link |
|---|---|
| US (6) | US20110003863A1 (es) |
| EP (1) | EP2440543B1 (es) |
| JP (2) | JP5848244B2 (es) |
| KR (1) | KR101734858B1 (es) |
| CN (1) | CN102482255A (es) |
| AP (1) | AP3630A (es) |
| AR (1) | AR076974A1 (es) |
| AU (1) | AU2010256693B2 (es) |
| BR (1) | BRPI1011015B8 (es) |
| CA (1) | CA2764043C (es) |
| CL (1) | CL2011003069A1 (es) |
| DK (1) | DK2440543T3 (es) |
| EA (1) | EA021826B1 (es) |
| ES (1) | ES2538103T3 (es) |
| GE (1) | GEP20156223B (es) |
| HN (1) | HN2011003187A (es) |
| HR (1) | HRP20150696T1 (es) |
| HU (1) | HUE026014T2 (es) |
| IL (1) | IL216565A (es) |
| MA (1) | MA33489B1 (es) |
| MX (1) | MX2011012654A (es) |
| MY (1) | MY162443A (es) |
| NI (1) | NI201100211A (es) |
| NZ (1) | NZ596872A (es) |
| PE (1) | PE20120398A1 (es) |
| PL (1) | PL2440543T3 (es) |
| PT (1) | PT2440543E (es) |
| RS (1) | RS54031B1 (es) |
| SG (1) | SG176648A1 (es) |
| SI (1) | SI2440543T1 (es) |
| TN (1) | TN2011000615A1 (es) |
| TW (1) | TWI434833B (es) |
| UA (1) | UA106759C2 (es) |
| WO (1) | WO2010141600A2 (es) |
| ZA (1) | ZA201108794B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2567283T3 (es) | 2008-06-03 | 2016-04-21 | Intermune, Inc. | Compuestos y métodos para tratar trastornos inflamatorios y fibróticos |
| CA2824432C (en) | 2011-01-31 | 2021-10-19 | Genoa Pharmaceuticals, Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
| US10105356B2 (en) | 2011-01-31 | 2018-10-23 | Avalyn Pharma Inc. | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
| MX2011007675A (es) | 2011-07-19 | 2012-07-11 | Cell Therapy And Technology S A De C V | Procedimiento para la fabricacion de una composicion farmaceutica en forma de tabletas de liberacion prolongada conteniendo pirfenidona y su aplicacion en la regresion de la insuficiencia renal cronica, contractura capsular mamaria y fibrosis hepatica humanas. |
| MX356551B (es) | 2012-08-23 | 2018-06-04 | Grupo Medifarma S A De C V Star | Composición antiséptica, antiseborreica y exfoliante para eliminar o prevenir el acné. |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| NZ760541A (en) | 2014-01-10 | 2022-08-26 | Avalyn Pharma Inc | Aerosol pirfenidone and pyridone analog compounds and uses thereof |
| CA2943363A1 (en) | 2014-04-02 | 2015-10-08 | Intermune, Inc. | Anti-fibrotic pyridinones |
| CA2958195A1 (en) * | 2014-08-15 | 2016-02-18 | PixarBio Corporation | Compositions for inhibiting inflammation in a subject with a spinal cord injury and methods of using the same |
| EP3307714A1 (en) | 2015-01-26 | 2018-04-18 | Ulkar Kimya Sanayii Ve Ticaret A. S. | An improved method for the synthesis and purification of pirfenidone |
| ITUB20154832A1 (it) | 2015-10-29 | 2017-04-29 | Procos Spa | Processo per la sintesi di pirfenidone |
| CN105315198A (zh) * | 2015-11-02 | 2016-02-10 | 重庆康乐制药有限公司 | 一种吡非尼酮的晶型及其制备方法 |
| CN105330598B (zh) * | 2015-12-02 | 2017-11-14 | 新发药业有限公司 | 一种吡非尼酮的制备方法 |
| WO2017122139A1 (en) * | 2016-01-14 | 2017-07-20 | Laurus Labs Limited | An improved process for the preparation of pirfenidone |
| US11066368B2 (en) | 2016-01-14 | 2021-07-20 | Laurus Labs Limited | Process for the preparation and particle size reduction of pirfenidone |
| WO2017130166A1 (en) * | 2016-01-31 | 2017-08-03 | Granules India Limited | An improved process for the preparation of highly pure anti-fibrotic drug |
| CA2937365C (en) | 2016-03-29 | 2018-09-18 | F. Hoffmann-La Roche Ag | Granulate formulation of 5-methyl-1-phenyl-2-(1h)-pyridone and method of making the same |
| IT201600071672A1 (it) * | 2016-07-08 | 2018-01-08 | Dipharma Francis Srl | Metodo per sintetizzare un farmaco immunosoppressore |
| US20180009753A1 (en) * | 2016-07-08 | 2018-01-11 | Dipharma Francis S.R.L. | Method for preparing an antifibrotic agent |
| IT201600108927A1 (it) * | 2016-10-27 | 2018-04-27 | Dipharma Francis Srl | Metodo per sintetizzare un farmaco antifibrotico |
| WO2018083709A1 (en) * | 2016-11-07 | 2018-05-11 | Msn Laboratories Private Limited, R&D Center | Improved process for the preparation of pure 5-methyl-1-phenyl-2-1 (h)-pyridone |
| WO2018178996A1 (en) * | 2017-03-28 | 2018-10-04 | Natco Pharma Limited | Improved process for the preparation of pirfenidone |
| WO2019028062A1 (en) | 2017-07-31 | 2019-02-07 | Washington University | PIRFENIDONE DERIVATIVES FOR MODULATION OF B-LYMPHOCYTE ACTIVITY AND PROTECTION OF ORGANS |
| ES2886152T3 (es) | 2017-12-11 | 2021-12-16 | Laurus Labs Ltd | Un procedimiento mejorado para la preparación de pirfenidona |
| CN112409246B (zh) * | 2019-08-21 | 2023-04-07 | 北京凯因科技股份有限公司 | 一种吡非尼酮的晶型及其制备方法 |
| US20230158004A1 (en) * | 2020-04-22 | 2023-05-25 | Yungjin Pharm. Co., Ltd. | Enteric-coated preparation comprising pirfenidone having improved safety and stability, and method for preparing same |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3839346A (en) * | 1972-12-18 | 1974-10-01 | Affiliated Med Res | N-substituted pyridone and general method for preparing pyridones |
| US5356898A (en) * | 1991-01-31 | 1994-10-18 | Warner-Lambert Company | Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines |
| WO2002085858A1 (fr) * | 2001-04-20 | 2002-10-31 | Asahi Glass Company, Limited | Procede de production d'un derive de piperidine purifie |
| JP4342940B2 (ja) * | 2001-08-06 | 2009-10-14 | 塩野義製薬株式会社 | ５−メチル−１−フェニル−２（１ｈ）ピリジノンの製造方法 |
| CN1218942C (zh) | 2002-06-11 | 2005-09-14 | 中南大学湘雅医学院 | 抗纤维化吡啶酮化合物及其生产工艺方法 |
| CN100396669C (zh) * | 2006-03-15 | 2008-06-25 | 浙江省医学科学院 | 一种抗纤维化药物吡非尼酮的制备方法 |
| MX2007006349A (es) * | 2007-05-29 | 2009-02-18 | Cell Therapy And Technology S | Nuevo proceso de sintesis para la obtencion de 5-metil-1-fenil-2-(ih)-piridona, composicion y uso de la misma. |
| JP5587184B2 (ja) | 2007-06-20 | 2014-09-10 | オースペックス・ファーマシューティカルズ・インコーポレイテッド | 繊維症阻害剤としての置換ｎ−アリールピリジノン |
| US20090131485A1 (en) * | 2007-09-10 | 2009-05-21 | Concert Pharmaceuticals, Inc. | Deuterated pirfenidone |
-
2010
- 2010-06-01 TW TW099117538A patent/TWI434833B/zh active
- 2010-06-02 MA MA34508A patent/MA33489B1/fr unknown
- 2010-06-02 JP JP2012514087A patent/JP5848244B2/ja active Active
- 2010-06-02 CA CA2764043A patent/CA2764043C/en active Active
- 2010-06-02 SI SI201030938T patent/SI2440543T1/sl unknown
- 2010-06-02 SG SG2011089455A patent/SG176648A1/en unknown
- 2010-06-02 EP EP10784021.7A patent/EP2440543B1/en active Active
- 2010-06-02 MY MYPI2011005818A patent/MY162443A/en unknown
- 2010-06-02 UA UAA201115405A patent/UA106759C2/uk unknown
- 2010-06-02 ES ES10784021.7T patent/ES2538103T3/es active Active
- 2010-06-02 PL PL10784021T patent/PL2440543T3/pl unknown
- 2010-06-02 RS RS20150376A patent/RS54031B1/en unknown
- 2010-06-02 US US12/792,387 patent/US20110003863A1/en not_active Abandoned
- 2010-06-02 HU HUE10784021A patent/HUE026014T2/en unknown
- 2010-06-02 PT PT107840217T patent/PT2440543E/pt unknown
- 2010-06-02 NZ NZ596872A patent/NZ596872A/en unknown
- 2010-06-02 PE PE2011002044A patent/PE20120398A1/es not_active Application Discontinuation
- 2010-06-02 EA EA201101695A patent/EA021826B1/ru not_active IP Right Cessation
- 2010-06-02 WO PCT/US2010/037090 patent/WO2010141600A2/en active Application Filing
- 2010-06-02 AP AP2012006052A patent/AP3630A/xx active
- 2010-06-02 KR KR1020117029855A patent/KR101734858B1/ko active IP Right Grant
- 2010-06-02 CN CN2010800245047A patent/CN102482255A/zh active Pending
- 2010-06-02 BR BRPI1011015A patent/BRPI1011015B8/pt active IP Right Grant
- 2010-06-02 GE GEAP201012512A patent/GEP20156223B/en unknown
- 2010-06-02 MX MX2011012654A patent/MX2011012654A/es active IP Right Grant
- 2010-06-02 AU AU2010256693A patent/AU2010256693B2/en not_active Revoked
- 2010-06-02 DK DK10784021.7T patent/DK2440543T3/en active
- 2010-06-03 AR ARP100101971A patent/AR076974A1/es active IP Right Grant
-
2011
- 2011-09-26 US US13/244,786 patent/US8519140B2/en active Active
- 2011-11-23 IL IL216565A patent/IL216565A/en active IP Right Grant
- 2011-11-30 ZA ZA2011/08794A patent/ZA201108794B/en unknown
- 2011-12-01 TN TNP2011000615A patent/TN2011000615A1/en unknown
- 2011-12-02 CL CL2011003069A patent/CL2011003069A1/es unknown
- 2011-12-05 HN HN2011003187A patent/HN2011003187A/es unknown
- 2011-12-05 NI NI201100211A patent/NI201100211A/es unknown
-
2013
- 2013-07-22 US US13/947,643 patent/US20130345430A1/en not_active Abandoned
-
2014
- 2014-04-08 US US14/247,357 patent/US20140221660A1/en not_active Abandoned
- 2014-11-11 US US14/538,426 patent/US20150065720A1/en not_active Abandoned
-
2015
- 2015-06-30 HR HRP20150696TT patent/HRP20150696T1/hr unknown
- 2015-08-20 US US14/830,999 patent/US20150368200A1/en not_active Abandoned
- 2015-10-15 JP JP2015203886A patent/JP2016026196A/ja active Pending
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