AR052269A1 - Analogos de rapamicina, un proceso para su elaboracion y los usos de los mismos en la preparacion de un medicamento para el tratamiento de trastornos neurologicos, proliferativos e inflamatorios. - Google Patents
Analogos de rapamicina, un proceso para su elaboracion y los usos de los mismos en la preparacion de un medicamento para el tratamiento de trastornos neurologicos, proliferativos e inflamatorios.Info
- Publication number
- AR052269A1 AR052269A1 ARP050105290A ARP050105290A AR052269A1 AR 052269 A1 AR052269 A1 AR 052269A1 AR P050105290 A ARP050105290 A AR P050105290A AR P050105290 A ARP050105290 A AR P050105290A AR 052269 A1 AR052269 A1 AR 052269A1
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- AR
- Argentina
- Prior art keywords
- substituted
- group
- aryl
- alkyl
- preparation
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged 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
- A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
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- 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
- A61P17/06—Antipsoriatics
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- 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
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- 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
- A61P25/08—Antiepileptics; Anticonvulsants
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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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
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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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- A61P9/06—Antiarrhythmics
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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
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Estos compuestos son utiles en el tratamiento de los trastornos neurologicos o complicaciones debidas a accidentes cerebrovascular o lesion cefálica, enfermedad neoplásica benigna o maligna, carcinomas y adenocarcinomas. Reivindicacion 1: Un compuesto de la formula (1) en la cual R1 y R2 son grupos independientes diferentes y son seleccionados del grupo constituido por OR3 y N(R3')(R3ö) o R1 y R2 son diferentes, están conectados a través de un enlace simple y son seleccionados del grupo constituido por O y NR3; R3, R3' y R3ö son independientemente seleccionados del grupo constituido por H, alquilo C1-6, alquilo sustituido C1-6, cicloalquilo C3-8, cicloalquilo sustituido C3-8, arilo, arilo sustituido, heteroarilo y heteroarilo sustituido; R4 y R4' son (a) independientemente seleccionados entre H, OH, O(alquilo C1-6), O(alquilo sustituido C1-6), O(acilo), O(arilo), O(arilo sustituido) y halogeno; o (b) tomados en conjunto para formar un enlace doble a O; R5, R6 y R7 son independientemente seleccionados del grupo formado por H, OH y OCH3; R8 y R9 están conectados a través de (i) un enlace simple y son CH2 o (ii) un enlace doble y son CH; R15 es seleccionado del grupo constituido por C=O, CHOH y CH2; n es 1 o 2; o una sal farmacéuticamente aceptable del mismo. Reivindicacion 34: Un método para la preparacion de un compuesto de acuerdo con lo definido en cualquiera de las reivindicaciones 1 a 27, que comprende los siguientes pasos: (i) la combinacion de rapamicina o un análogo de la misma con un nitrosobenceno sustituido y (ii) el aislamiento del producto (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63766604P | 2004-12-20 | 2004-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR052269A1 true AR052269A1 (es) | 2007-03-07 |
Family
ID=36087657
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050105290A AR052269A1 (es) | 2004-12-20 | 2005-12-15 | Analogos de rapamicina, un proceso para su elaboracion y los usos de los mismos en la preparacion de un medicamento para el tratamiento de trastornos neurologicos, proliferativos e inflamatorios. |
Country Status (27)
| Country | Link |
|---|---|
| US (5) | US7276498B2 (es) |
| EP (1) | EP1828202B1 (es) |
| JP (1) | JP5094406B2 (es) |
| KR (1) | KR20070090913A (es) |
| CN (1) | CN101084227B (es) |
| AR (1) | AR052269A1 (es) |
| AT (1) | ATE549342T1 (es) |
| AU (1) | AU2005319454B2 (es) |
| BR (1) | BRPI0519495A2 (es) |
| CA (1) | CA2590155A1 (es) |
| CR (1) | CR9148A (es) |
| DK (1) | DK1828202T3 (es) |
| ES (1) | ES2380779T3 (es) |
| GT (1) | GT200500368A (es) |
| HK (1) | HK1108442A1 (es) |
| HN (1) | HN2005035605A (es) |
| IL (1) | IL183664A (es) |
| MX (1) | MX2007007408A (es) |
| NI (1) | NI200700157A (es) |
| NO (1) | NO20072664L (es) |
| NZ (1) | NZ574663A (es) |
| PE (1) | PE20060765A1 (es) |
| RU (1) | RU2394036C2 (es) |
| SG (1) | SG158143A1 (es) |
| TW (1) | TW200628152A (es) |
| UA (1) | UA94034C2 (es) |
| WO (1) | WO2006068932A2 (es) |
Families Citing this family (50)
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| CA2493878C (en) | 2002-07-30 | 2013-07-23 | Wyeth | Parenteral formulations containing a rapamycin hydroxyester |
| AU2005219822A1 (en) * | 2004-03-02 | 2005-09-15 | Wyeth | Macrolides and methods for producing same |
| JP2008501342A (ja) * | 2004-06-03 | 2008-01-24 | ワイス | 複合ポリケチドを生成するための生合成遺伝子クラスター |
| US7273874B2 (en) * | 2004-12-20 | 2007-09-25 | Wyeth | Rapamycin derivatives and the uses thereof in the treatment of neurological disorders |
| DK1828202T3 (da) * | 2004-12-20 | 2012-05-07 | Wyeth Llc | Rapamycinanaloge samt deres anvendelse ved behandling af neurologiske, proliferative og inflammatoriske lidelser |
| CA2630645A1 (en) * | 2005-12-07 | 2007-06-14 | Wyeth | Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate |
| WO2007067566A2 (en) * | 2005-12-07 | 2007-06-14 | Wyeth | Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry |
| RU2008121240A (ru) * | 2005-12-07 | 2010-01-20 | Вайет (Us) | Способ получения очищенного кристаллического cci-779 |
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| RU2010104916A (ru) * | 2006-08-16 | 2011-08-20 | Михаил В. Благосклонный (US) | Способ профилактики и лечения возрастных заболеваний |
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| JP2008305262A (ja) * | 2007-06-08 | 2008-12-18 | Konica Minolta Business Technologies Inc | サーバ及びシンクライアント環境でのプリンタ紹介方法 |
| CA2715080C (en) | 2007-09-28 | 2021-09-28 | Intrexon Corporation | Therapeutic gene-switch constructs and bioreactors for the expression of biotherapeutic molecules, and uses thereof |
| US8653045B2 (en) * | 2008-02-05 | 2014-02-18 | The Johns Hopkins University | Induction of thyroid iodide-handling gene expression in human cancers |
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| CN102292078A (zh) | 2008-11-11 | 2011-12-21 | 得克萨斯大学体系董事会 | 哺乳动物雷帕霉素靶蛋白的抑制 |
| DE102008060549A1 (de) | 2008-12-04 | 2010-06-10 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Wirkstoff-Peptid-Konstrukt zur extrazellulären Anreicherung |
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| WO2014059295A1 (en) | 2012-10-12 | 2014-04-17 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
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2005
- 2005-12-15 DK DK05849447.7T patent/DK1828202T3/da active
- 2005-12-15 MX MX2007007408A patent/MX2007007408A/es active IP Right Grant
- 2005-12-15 RU RU2007119584/04A patent/RU2394036C2/ru not_active IP Right Cessation
- 2005-12-15 CA CA002590155A patent/CA2590155A1/en not_active Abandoned
- 2005-12-15 WO PCT/US2005/045551 patent/WO2006068932A2/en active Application Filing
- 2005-12-15 HN HN2005035605A patent/HN2005035605A/es unknown
- 2005-12-15 AT AT05849447T patent/ATE549342T1/de active
- 2005-12-15 CN CN2005800437154A patent/CN101084227B/zh not_active Expired - Fee Related
- 2005-12-15 EP EP05849447A patent/EP1828202B1/en not_active Not-in-force
- 2005-12-15 ES ES05849447T patent/ES2380779T3/es active Active
- 2005-12-15 TW TW094144448A patent/TW200628152A/zh unknown
- 2005-12-15 SG SG200908383-3A patent/SG158143A1/en unknown
- 2005-12-15 AR ARP050105290A patent/AR052269A1/es not_active Application Discontinuation
- 2005-12-15 BR BRPI0519495-4A patent/BRPI0519495A2/pt not_active IP Right Cessation
- 2005-12-15 PE PE2005001466A patent/PE20060765A1/es not_active Application Discontinuation
- 2005-12-15 US US11/300,839 patent/US7276498B2/en not_active Expired - Fee Related
- 2005-12-15 GT GT200500368A patent/GT200500368A/es unknown
- 2005-12-15 NZ NZ574663A patent/NZ574663A/en not_active IP Right Cessation
- 2005-12-15 KR KR1020077013082A patent/KR20070090913A/ko not_active Application Discontinuation
- 2005-12-15 JP JP2007546925A patent/JP5094406B2/ja not_active Expired - Fee Related
- 2005-12-15 AU AU2005319454A patent/AU2005319454B2/en not_active Expired - Fee Related
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2007
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- 2007-05-24 CR CR9148A patent/CR9148A/es not_active Application Discontinuation
- 2007-05-25 NO NO20072664A patent/NO20072664L/no not_active Application Discontinuation
- 2007-06-04 IL IL183664A patent/IL183664A/en not_active IP Right Cessation
- 2007-06-18 NI NI200700157A patent/NI200700157A/es unknown
- 2007-08-14 US US11/893,090 patent/US7470682B2/en not_active Expired - Fee Related
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2008
- 2008-03-04 HK HK08102453.8A patent/HK1108442A1/xx not_active IP Right Cessation
- 2008-11-24 US US12/276,668 patent/US20090203682A1/en not_active Abandoned
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2009
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