HUP0101407A2 - Eljárás ciklooxigenáz -2-gátló hatású piridinszármazékok előállítására és az eljárás intermedierjei - Google Patents
Eljárás ciklooxigenáz -2-gátló hatású piridinszármazékok előállítására és az eljárás intermedierjeiInfo
- Publication number
- HUP0101407A2 HUP0101407A2 HU0101407A HUP0101407A HUP0101407A2 HU P0101407 A2 HUP0101407 A2 HU P0101407A2 HU 0101407 A HU0101407 A HU 0101407A HU P0101407 A HUP0101407 A HU P0101407A HU P0101407 A2 HUP0101407 A2 HU P0101407A2
- Authority
- HU
- Hungary
- Prior art keywords
- alkyl
- amino
- carbon atoms
- groups
- aryl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 229940111134 coxibs Drugs 0.000 title 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 150000003222 pyridines Chemical class 0.000 title 1
- 230000002194 synthesizing effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 3
- -1 nitro- Chemical class 0.000 abstract 3
- 102000010907 Cyclooxygenase 2 Human genes 0.000 abstract 2
- 108010037462 Cyclooxygenase 2 Proteins 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- C07D213/61—Halogen atoms or nitro radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
- C07C251/02—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
- C07C251/30—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having nitrogen atoms of imino groups quaternised
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
A találmány tárgya eljárás az (I) általános képletű vegyületekelőállítására - ahol O-2 R csoportok vannak jelen, és aszubsztituensek főbb jelentései a következők: mindegyik R, R' és R"jelentése egymástól függetlenül 1-10 szénatomos alkil-, 6-10szénatomos aril- vagy aralkilcsoport; halogénatom; nitro-, amino-, (1-6 szénatomos alkil)amino-, di(1-6 szénatomos alkil)amino- vagycianocsoport; az alkil- és arilcsoportok, valamint az aralkil-, (1-6szénatomos alkil)amino- és di(1-6 szénatomos alkil)amino-csoportokalkil- és arilegységei adott esetben szubsztituálva lehetnek; Yjelentése szén- vagy nitrogénatom; és m értéke 0, 1 vagy 2. Atalálmány szerinti hatóanyagok szelektíven gátolják a ciklooxigenáz-2indukálható enzimet, és így alkalmasak a ciklooxigenáz-2 enzimmelközvetített betegségek megelőzésére vagy kezelésére. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US8288898P | 1998-04-24 | 1998-04-24 | |
US8566898P | 1998-05-15 | 1998-05-15 | |
PCT/US1999/008645 WO1999055830A2 (en) | 1998-04-24 | 1999-04-20 | Process for synthesizing cox-2 inhibitors |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0101407A2 true HUP0101407A2 (hu) | 2001-09-28 |
HUP0101407A3 HUP0101407A3 (en) | 2002-12-28 |
HU227627B1 HU227627B1 (en) | 2011-10-28 |
Family
ID=26767964
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0101407A HU227627B1 (en) | 1998-04-24 | 1999-04-20 | Process for synthesizing pyridine derivatives as cox-2 inhibitors and the intermediates |
Country Status (28)
Country | Link |
---|---|
US (2) | US6040319A (hu) |
EP (1) | EP1071745B1 (hu) |
JP (2) | JP3325264B2 (hu) |
KR (1) | KR100414998B1 (hu) |
CN (1) | CN1178658C (hu) |
AR (1) | AR015279A1 (hu) |
AT (1) | ATE272613T1 (hu) |
AU (1) | AU759469B2 (hu) |
BR (2) | BRPI9917739B8 (hu) |
CA (1) | CA2329193C (hu) |
CZ (1) | CZ292515B6 (hu) |
DE (1) | DE69919151T2 (hu) |
DK (1) | DK1071745T3 (hu) |
EA (1) | EA002975B1 (hu) |
ES (1) | ES2226378T3 (hu) |
HK (1) | HK1031399A1 (hu) |
HR (1) | HRP20000722B1 (hu) |
HU (1) | HU227627B1 (hu) |
IL (2) | IL139127A0 (hu) |
NZ (1) | NZ507597A (hu) |
PL (1) | PL193248B1 (hu) |
PT (1) | PT1071745E (hu) |
RS (1) | RS49945B (hu) |
SI (1) | SI1071745T1 (hu) |
SK (1) | SK284805B6 (hu) |
TW (1) | TW474934B (hu) |
UA (1) | UA57143C2 (hu) |
WO (1) | WO1999055830A2 (hu) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5861419A (en) | 1996-07-18 | 1999-01-19 | Merck Frosst Canad, Inc. | Substituted pyridines as selective cyclooxygenase-2 inhibitors |
EP1159270B1 (de) * | 1999-01-14 | 2003-11-05 | Lonza AG | Verfahren zur herstellung von 1-(6-methylpyridin-3-yl)-2- 4-(methylsulfonyl phenyl)ethanon |
US7141673B1 (en) | 1999-01-14 | 2006-11-28 | Lonza Ag | 1-(6-methylpyridine-3-yl)-2-[4-(methylsulphonyl) phenyl] ethanone and method for its preparation |
JP2001115963A (ja) | 1999-10-13 | 2001-04-27 | Daikin Ind Ltd | 圧縮機 |
CA2391650C (en) * | 1999-11-29 | 2011-01-25 | Merck & Co., Inc. | Polymorphic, amorphous and hydrated forms of 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl-[2,3']bipyridinyl |
US6858631B1 (en) | 1999-11-29 | 2005-02-22 | Merck & Co., Inc. | Polymorphic, amorphous and hydrated forms of 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridinyl |
ATE283048T1 (de) * | 1999-12-08 | 2004-12-15 | Pharmacia Corp | Cyclooxygenase-2 hemmer enthaltende zusammensetzungen mit schnellem wirkungseintritt |
JP2001261653A (ja) * | 2000-03-17 | 2001-09-26 | Sankio Chemical Co Ltd | ピリジン誘導体の合成法 |
US6800647B2 (en) | 2000-05-26 | 2004-10-05 | Merck & Co., Inc. | 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl-[2,3]bipyridinyl in pure crystalline form and process for synthesis |
PH12001001175B1 (en) * | 2000-05-26 | 2006-08-10 | Merck Sharp & Dohme | 5-chloro-3-(4-methanesulfonylphenyl)-6'-methyl- (2,3')bipyridinyl in pure crystalline form and process for synthesis |
US6521642B2 (en) | 2000-05-26 | 2003-02-18 | Merck & Co., Inc. | 5-chloro-3-(4-methanesulfonylphenyl)-6′-methyl-[2,3′]bipyridinyl in pure crystalline form and process for synthesis |
CA2414674A1 (en) * | 2000-07-13 | 2002-01-24 | Pharmacia Corporation | Use of cox-2 inhibitors in the treatment and prevention of ocular cox-2 mediated disorders |
PE20020146A1 (es) * | 2000-07-13 | 2002-03-31 | Upjohn Co | Formulacion oftalmica que comprende un inhibidor de ciclooxigenasa-2 (cox-2) |
US7115565B2 (en) * | 2001-01-18 | 2006-10-03 | Pharmacia & Upjohn Company | Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability |
MY137736A (en) | 2001-04-03 | 2009-03-31 | Pharmacia Corp | Reconstitutable parenteral composition |
US20040132780A1 (en) * | 2001-05-04 | 2004-07-08 | Allen Christopher P. | Method and compositions for treating migraines |
UA80682C2 (en) * | 2001-08-06 | 2007-10-25 | Pharmacia Corp | Orally deliverable stabilized oral suspension formulation and process for the incresaing physical stability of thixotropic pharmaceutical composition |
JP4700916B2 (ja) * | 2004-02-02 | 2011-06-15 | 富士フイルムファインケミカルズ株式会社 | ピリジン誘導体の製造方法 |
US7271383B2 (en) * | 2004-08-11 | 2007-09-18 | Lexmark International, Inc. | Scanning system with feedback for a MEMS oscillating scanner |
EP2494992A1 (en) | 2004-08-24 | 2012-09-05 | Merck Sharp & Dohme Corp. | Combination therapy for treating cyclooxygenase-2 mediated diseases or conditions in patients at risk of thrombotic cardiovascular events |
CA2676413A1 (en) * | 2007-01-19 | 2008-07-31 | Mallinckrodt Inc. | Diagnostic and therapeutic cyclooxygenase-2 binding ligands |
MY163020A (en) | 2009-02-27 | 2017-07-31 | Cadila Healthcare Ltd | A process for the preparation of etoricoxib |
WO2011158250A1 (en) | 2010-06-16 | 2011-12-22 | Glenmark Generics Limited | Process for preparation of 2, 3-diaryl-5-substituted pyridines and their intermediates |
US8841457B2 (en) | 2010-11-15 | 2014-09-23 | Virdev Intermediates Pvt. Ltd. | Process for cyclooxygenase-2 selective inhibitor |
ITMI20110362A1 (it) | 2011-03-09 | 2012-09-10 | F I S Fabbrica Italiana Sint P A | Procedimento per la preparazione di 1-(6-metilpiridin-3-il)-2-[4-(metilsolfonil)fenil]etanone, un intermedio dell'etoricoxib. |
EP2714676B1 (en) | 2011-05-27 | 2019-04-24 | Farma GRS, d.o.o. | A process for the preparation of polymorphic form i of etoricoxib |
ITMI20111455A1 (it) | 2011-07-29 | 2013-01-30 | Italiana Sint Spa | Nuovo procedimento per la preparazione di 1-(6-metilpiridin-3-il)-2-[4-(metilsolfonil)fenil]etanone, un intermedio dell'etoricoxib. |
CN103204803A (zh) | 2012-01-13 | 2013-07-17 | 阿尔弗雷德·E·蒂芬巴赫尔有限责任两合公司 | 用于合成依托考昔的方法 |
ITMI20120394A1 (it) | 2012-03-14 | 2013-09-15 | Zach System Spa | Processo di sintesi di un chetosolfone derivato |
EP2831045A2 (en) | 2012-03-30 | 2015-02-04 | Mylan Laboratories, Limited | An improved process for the preparation of etoricoxib |
GR1007973B (el) * | 2012-06-26 | 2013-09-12 | Φαρματεν Αβεε, | Νεα ν-οξοιμινο παραγωγα ως ενδιαμεσα μιας βελτιωμενης μεθοδου παρασκευης 2,3-διαρυλο-5-υποκατεστημενων πυριδινων |
WO2014033526A1 (en) | 2012-08-27 | 2014-03-06 | Cadila Healthcare Limited | Pharmaceutical compositions of etoricoxib |
ITVI20130014A1 (it) | 2013-01-22 | 2014-07-23 | Italiana Sint Spa | Procedimento molto efficiente per preparare un intermedio di etoricoxib |
WO2014114352A1 (en) * | 2013-01-25 | 2014-07-31 | Synthon Bv | Process for making etoricoxib |
CN104418799A (zh) * | 2013-09-03 | 2015-03-18 | 天津药物研究院 | 一种依托考昔的晶型及其制备方法和应用 |
WO2015036550A1 (en) | 2013-09-13 | 2015-03-19 | Synthon B.V. | Process for making etoricoxib |
WO2016149126A1 (en) | 2015-03-13 | 2016-09-22 | The Board Of Trustees Of The Leland Stanford Junior University | Ltb4 inhibition to prevent and treat human lymphedema |
CN104817473A (zh) * | 2015-03-27 | 2015-08-05 | 南京大学 | 1-二甲氨基-3-二甲亚胺基-2-氯丙烯高氯酸盐在制备依托考昔中的应用 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA988522A (en) * | 1972-05-05 | 1976-05-04 | Haydn W.R. Williams | 1,8-naphthyridine compounds |
DE3842062A1 (de) * | 1988-12-14 | 1990-06-28 | Hoechst Ag | Explosionssichere 1-dimethylamino-3-dimethylimino-2-arylpropen-1-salze, verfahren zu ihrer herstellung und ihre verwendung |
DK0912518T3 (da) * | 1996-07-18 | 2003-12-08 | Merck Frosst Canada Inc | Substituerede pyridiner som selektive cyclooxygenase-2 inhibitorer |
US5861419A (en) * | 1996-07-18 | 1999-01-19 | Merck Frosst Canad, Inc. | Substituted pyridines as selective cyclooxygenase-2 inhibitors |
-
1999
- 1999-04-20 UA UA2000116652A patent/UA57143C2/uk unknown
- 1999-04-20 SK SK1589-2000A patent/SK284805B6/sk not_active IP Right Cessation
- 1999-04-20 HU HU0101407A patent/HU227627B1/hu unknown
- 1999-04-20 CN CNB998075507A patent/CN1178658C/zh not_active Expired - Lifetime
- 1999-04-20 WO PCT/US1999/008645 patent/WO1999055830A2/en active IP Right Grant
- 1999-04-20 PL PL344108A patent/PL193248B1/pl unknown
- 1999-04-20 EP EP99918706A patent/EP1071745B1/en not_active Expired - Lifetime
- 1999-04-20 AU AU36557/99A patent/AU759469B2/en not_active Expired
- 1999-04-20 SI SI9930632T patent/SI1071745T1/xx unknown
- 1999-04-20 KR KR10-2000-7011764A patent/KR100414998B1/ko active Protection Beyond IP Right Term
- 1999-04-20 JP JP2000545976A patent/JP3325264B2/ja not_active Expired - Lifetime
- 1999-04-20 NZ NZ507597A patent/NZ507597A/xx not_active IP Right Cessation
- 1999-04-20 AT AT99918706T patent/ATE272613T1/de active
- 1999-04-20 ES ES99918706T patent/ES2226378T3/es not_active Expired - Lifetime
- 1999-04-20 DK DK99918706T patent/DK1071745T3/da active
- 1999-04-20 RS YUP-641/00A patent/RS49945B/sr unknown
- 1999-04-20 CZ CZ20003940A patent/CZ292515B6/cs not_active IP Right Cessation
- 1999-04-20 EA EA200001102A patent/EA002975B1/ru not_active IP Right Cessation
- 1999-04-20 DE DE69919151T patent/DE69919151T2/de not_active Expired - Lifetime
- 1999-04-20 IL IL13912799A patent/IL139127A0/xx active IP Right Grant
- 1999-04-20 BR BRPI9917739A patent/BRPI9917739B8/pt not_active IP Right Cessation
- 1999-04-20 CA CA002329193A patent/CA2329193C/en not_active Expired - Lifetime
- 1999-04-20 PT PT99918706T patent/PT1071745E/pt unknown
- 1999-04-20 BR BRPI9909844-0A patent/BR9909844B1/pt not_active IP Right Cessation
- 1999-04-23 US US09/298,127 patent/US6040319A/en not_active Expired - Lifetime
- 1999-04-23 AR ARP990101884A patent/AR015279A1/es active IP Right Grant
- 1999-04-23 TW TW088106545A patent/TW474934B/zh active
-
2000
- 2000-01-21 US US09/488,774 patent/US6252116B1/en not_active Expired - Fee Related
- 2000-10-18 IL IL139127A patent/IL139127A/en not_active IP Right Cessation
- 2000-10-24 HR HR20000722A patent/HRP20000722B1/xx not_active IP Right Cessation
-
2001
- 2001-03-26 HK HK01102195A patent/HK1031399A1/xx not_active IP Right Cessation
-
2002
- 2002-05-22 JP JP2002147700A patent/JP3834263B2/ja not_active Expired - Lifetime
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