AR083213A1 - Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos - Google Patents
Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlosInfo
- Publication number
- AR083213A1 AR083213A1 ARP110103595A ARP110103595A AR083213A1 AR 083213 A1 AR083213 A1 AR 083213A1 AR P110103595 A ARP110103595 A AR P110103595A AR P110103595 A ARP110103595 A AR P110103595A AR 083213 A1 AR083213 A1 AR 083213A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- formula
- compound
- hydrogen
- Prior art date
Links
Classifications
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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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
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- 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
- C07D213/72—Nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
Se refiere además a procesos de elaboración para formas sólidas específicas del compuesto de fórmula (4) y sus sales, a estas formas sólidas, y al uso de tales formas sólidas para el tratamiento terapéutico de animales de sangre caliente.Reivindicación 1: Un proceso para la elaboración de un compuesto de la formula (1) o un estereoisómero, tautómero, o una sal del mismo, en donde: W es CRw o N, en donde Rw se selecciona a partir del grupo que consiste en hidrógeno, ciano, halógeno, metilo, trifluorometilo, sulfonamido; R1 se selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, alquilo sustituido e insustituido, alquenilo sustituido e insustituido, alquinilo sustituido e insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, cicloalquilo sustituido e insustituido, -COR1a, -CO2R1a, -CONR1aR1b, -NR1aR1b, -NR1aSO2R1b, -OCOR1a, -OR1a, -SOR1a, en donde R1a y R1b se seleccionan independientemente a partir del grupo que consiste en hidrógeno, alquilo sustituido o insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, y cicloalquilo sustituido e insustituido; R2 selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, hidroxilo, amino, alquilo sustituido e insustituido, -COR2a y -NR2aCOR2b, en donde R2a y R2b se seleccionan independientemente a partir del grupo que consiste en hidrógeno, y alquilo sustituido o insustituido; R3 se selecciona a partir del grupo que consiste en hidrógeno, ciano, nitro, halógeno, alquilo sustituido e insustituido, alquenilo sustituido e insustituido, alquinilo sustituido e insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, cicloalquilo sustituido e insustituido, -COR3a, -NR3aR3b, -NR3aCOR3b, -NR3aSO2R3b, -OR3a, -SR3a, -SOR3a, -SO2R3a, y en donde R3a y R3b se seleccionan independientemente a partir del .grupo que consiste en hidrógeno, alquilo sustituido o insustituido, arilo sustituido e insustituido, heteroarilo sustituido e insustituido, heterociclilo sustituido e insustituido, y cicloalquilo sustituido e insustituido; y R4 se selecciona a partir del grupo que consiste en hidrógeno, y halógeno; el cual comprende el paso de hacer reaccionar un compuesto de la fórmula (2) en donde Y2B- representa un ácido borónico acíclico, un éster borónico acíclico o un éster borónico cíclico, R1 y R2 son como se definen para la fórmula (1), con un compuesto de la fórmula (3) en donde Hal representa halógeno, W, R3 y R4 son como se definen para un compuesto de la fórmula (1); bajo condiciones de Suzuki, para obtener un compuesto de la fórmula (1); opcionalmente seguido por una reacción de formación de sal. Reivindicación 7: Una forma cristalina del compuesto de la fórmula (4) o de un hidrato o solvato del compuesto de la fórmula (4), o de una sal del compuesto de la fórmula (4), o de un hidrato o solvato de una sal del compuesto de la fórmula (4). Reivindicación 9: Una forma cristalina del compuesto de fórmula (4) de acuerdo con la reivindicación 7, en la forma polimorfa A anhidra, en donde la forma cristalina del compuesto de fórmula (4) muestra, en la difracción de rayos-X, un pico en un ángulo de difracción 2q de 14.8 ± 0.3º y 10.2 ± 0.3º.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38872110P | 2010-10-01 | 2010-10-01 | |
US201161494915P | 2011-06-09 | 2011-06-09 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR083213A1 true AR083213A1 (es) | 2013-02-06 |
Family
ID=44773179
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110103595A AR083213A1 (es) | 2010-10-01 | 2011-09-29 | Proceso de preparacion de derivados pirimidinicos, compuestos intermediarios y proceso para prepararlos |
Country Status (31)
Country | Link |
---|---|
US (3) | US9181215B2 (es) |
EP (2) | EP3040333B1 (es) |
JP (3) | JP5998145B2 (es) |
KR (2) | KR20180123586A (es) |
CN (3) | CN104945373A (es) |
AR (1) | AR083213A1 (es) |
AU (4) | AU2011308856B2 (es) |
BR (1) | BR112013007123B1 (es) |
CA (1) | CA2813333C (es) |
CL (2) | CL2013000850A1 (es) |
CO (1) | CO6700837A2 (es) |
DK (1) | DK3040333T3 (es) |
EC (1) | ECSP13012596A (es) |
ES (1) | ES2699951T3 (es) |
GT (1) | GT201300080A (es) |
HK (1) | HK1220686A1 (es) |
HU (1) | HUE041326T2 (es) |
IL (3) | IL225113A (es) |
LT (1) | LT3040333T (es) |
MX (1) | MX354482B (es) |
MY (1) | MY160785A (es) |
NZ (1) | NZ608285A (es) |
PE (1) | PE20140002A1 (es) |
PH (1) | PH12015501585A1 (es) |
PL (1) | PL3040333T3 (es) |
PT (1) | PT3040333T (es) |
RU (2) | RU2015150728A (es) |
SG (1) | SG188439A1 (es) |
SI (1) | SI3040333T1 (es) |
TW (1) | TWI540133B (es) |
WO (1) | WO2012044727A2 (es) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2676180T3 (es) | 2011-07-01 | 2018-07-17 | Novartis Ag | Terapia de combinación que comprende un inhibidor de CDK4/6 y un inhibidor de PI3K para el uso en el tratamiento de cáncer |
KR20140069235A (ko) | 2011-09-27 | 2014-06-09 | 노파르티스 아게 | 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
KR102128127B1 (ko) * | 2012-10-23 | 2020-06-30 | 노파르티스 아게 | 5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법 |
US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
EA028033B1 (ru) | 2013-03-14 | 2017-09-29 | Новартис Аг | 3-пиримидин-4-ил-оксазолидин-2-оны в качестве ингибиторов мутантного idh |
US9318944B2 (en) | 2013-04-29 | 2016-04-19 | Rockwell Automation Technologies, Inc. | Methods and apparatus for active front end filter capacitor degradation detection |
US9294005B2 (en) | 2013-10-01 | 2016-03-22 | Rockwell Automation Technologies, Inc. | Method and apparatus for detecting AFE filter capacitor degradation |
RU2663999C2 (ru) * | 2013-10-16 | 2018-08-14 | Шанхай Инли Фармасьютикал Ко., Лтд | Конденсированное гетероциклическое соединение, способ его получения, его фармацевтическая композиция и применения |
US10100031B2 (en) * | 2014-04-22 | 2018-10-16 | Universitaet Basel | Manufacturing process for triazine, pyrimidine and pyridine derivatives |
CN105085476B (zh) * | 2014-11-24 | 2018-03-09 | 苏州晶云药物科技有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法 |
CA2971118C (en) | 2014-12-17 | 2020-07-14 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof |
US9481665B2 (en) * | 2015-03-13 | 2016-11-01 | Yong Xu | Process for preparing PI3K inhibitor buparsilib |
JP2018509448A (ja) | 2015-03-25 | 2018-04-05 | ノバルティス アーゲー | 組合せ医薬 |
CN105001151B (zh) * | 2015-08-28 | 2017-07-14 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
CN106543140A (zh) * | 2015-09-21 | 2017-03-29 | 苏州晶云药物科技有限公司 | 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法 |
DK3389662T3 (da) * | 2015-12-16 | 2022-02-28 | Genentech Inc | Fremgangsmåde til fremstilling af tricykliske PI3K-inhibitorforbindelser og fremgangsmåder til anvendelse af disse til behandling af cancer |
CN106905294A (zh) * | 2016-07-08 | 2017-06-30 | 苏州科睿思制药有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法 |
CN107793394A (zh) * | 2017-08-03 | 2018-03-13 | 上海厚璞生物科技有限公司 | 一种生产选择性pi3k抑制剂的系列关键中间体 |
CN110016142B (zh) * | 2019-04-30 | 2021-08-03 | 合肥工业大学 | 一种含嘧啶硼酸结构的硅油及其制备方法 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6124476A (en) | 1998-04-17 | 2000-09-26 | Symyx Technologies, Inc. | Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates |
CN1735598A (zh) * | 2002-11-11 | 2006-02-15 | 拜耳医药保健股份公司 | 作为ip受体拮抗剂的苯基或杂芳基氨基烷烃衍生物 |
DK2316831T3 (da) | 2002-11-21 | 2013-06-10 | Novartis Ag | 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer |
JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
KR101435231B1 (ko) | 2006-08-24 | 2014-10-02 | 아스트라제네카 아베 | 증식성 질환의 치료에 유용한 모르폴리노 피리미딘 유도체 |
ATE551334T1 (de) | 2007-02-06 | 2012-04-15 | Novartis Ag | Pi3-kinase-hemmer und verfahren zu ihrer verwendung |
WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
BRPI1010979A2 (pt) * | 2009-05-15 | 2018-03-06 | Novartis Ag | "combinação de um inibidor de fosfoinositídeo 3- quinase e de uma composto antidiabético" |
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2011
- 2011-09-29 AU AU2011308856A patent/AU2011308856B2/en active Active
- 2011-09-29 KR KR1020187032263A patent/KR20180123586A/ko not_active Application Discontinuation
- 2011-09-29 EP EP16151719.8A patent/EP3040333B1/en active Active
- 2011-09-29 LT LTEP16151719.8T patent/LT3040333T/lt unknown
- 2011-09-29 PE PE2013000654A patent/PE20140002A1/es active IP Right Grant
- 2011-09-29 KR KR1020137011172A patent/KR20130119928A/ko active Application Filing
- 2011-09-29 DK DK16151719.8T patent/DK3040333T3/da active
- 2011-09-29 CN CN201510157366.4A patent/CN104945373A/zh active Pending
- 2011-09-29 PT PT16151719T patent/PT3040333T/pt unknown
- 2011-09-29 CN CN201180047753.2A patent/CN103140479B/zh active Active
- 2011-09-29 HU HUE16151719A patent/HUE041326T2/hu unknown
- 2011-09-29 PL PL16151719T patent/PL3040333T3/pl unknown
- 2011-09-29 AR ARP110103595A patent/AR083213A1/es unknown
- 2011-09-29 SI SI201131619T patent/SI3040333T1/sl unknown
- 2011-09-29 MX MX2013003507A patent/MX354482B/es active IP Right Grant
- 2011-09-29 JP JP2013531796A patent/JP5998145B2/ja active Active
- 2011-09-29 BR BR112013007123-0A patent/BR112013007123B1/pt active IP Right Grant
- 2011-09-29 WO PCT/US2011/053808 patent/WO2012044727A2/en active Application Filing
- 2011-09-29 CA CA2813333A patent/CA2813333C/en active Active
- 2011-09-29 RU RU2015150728A patent/RU2015150728A/ru unknown
- 2011-09-29 RU RU2013120326/04A patent/RU2576619C2/ru active
- 2011-09-29 SG SG2013016837A patent/SG188439A1/en unknown
- 2011-09-29 NZ NZ608285A patent/NZ608285A/en not_active IP Right Cessation
- 2011-09-29 ES ES16151719T patent/ES2699951T3/es active Active
- 2011-09-29 CN CN201510156027.4A patent/CN104987321A/zh active Pending
- 2011-09-29 EP EP11767362.4A patent/EP2621908A2/en not_active Withdrawn
- 2011-09-29 US US13/825,880 patent/US9181215B2/en active Active
- 2011-09-29 MY MYPI2013000811A patent/MY160785A/en unknown
- 2011-09-30 TW TW100135673A patent/TWI540133B/zh active
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2013
- 2013-03-07 IL IL225113A patent/IL225113A/en unknown
- 2013-03-22 GT GT201300080A patent/GT201300080A/es unknown
- 2013-03-22 CO CO13057091A patent/CO6700837A2/es unknown
- 2013-03-28 CL CL2013000850A patent/CL2013000850A1/es unknown
- 2013-04-30 EC ECSP13012596 patent/ECSP13012596A/es unknown
- 2013-09-24 HK HK16108618.7A patent/HK1220686A1/zh unknown
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2014
- 2014-06-19 IL IL233282A patent/IL233282A/en unknown
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2015
- 2015-02-24 AU AU2015200938A patent/AU2015200938B2/en not_active Ceased
- 2015-02-24 AU AU2015200936A patent/AU2015200936A1/en not_active Abandoned
- 2015-03-30 IL IL238046A patent/IL238046A/en not_active IP Right Cessation
- 2015-04-27 CL CL2015001088A patent/CL2015001088A1/es unknown
- 2015-05-06 US US14/705,013 patent/US9359326B2/en not_active Expired - Fee Related
- 2015-07-20 PH PH12015501585A patent/PH12015501585A1/en unknown
- 2015-10-23 AU AU2015246141A patent/AU2015246141B2/en not_active Ceased
- 2015-12-17 JP JP2015246501A patent/JP2016128414A/ja active Pending
- 2015-12-17 JP JP2015246502A patent/JP2016106091A/ja active Pending
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2016
- 2016-05-06 US US15/147,986 patent/US9452994B2/en not_active Expired - Fee Related
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