HRP20000722B1 - Process for synthesizing cox-2 inhibitors - Google Patents
Process for synthesizing cox-2 inhibitorsInfo
- Publication number
- HRP20000722B1 HRP20000722B1 HR20000722A HRP20000722A HRP20000722B1 HR P20000722 B1 HRP20000722 B1 HR P20000722B1 HR 20000722 A HR20000722 A HR 20000722A HR P20000722 A HRP20000722 A HR P20000722A HR P20000722 B1 HRP20000722 B1 HR P20000722B1
- Authority
- HR
- Croatia
- Prior art keywords
- 6alkyl
- alkyl
- aryl
- compound
- formula
- 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
- 230000002194 synthesizing effect Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 3
- -1 -S (O) maryl Chemical group 0.000 abstract 3
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Pulmonology (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)
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 (fr) | 1998-04-24 | 1999-04-20 | Procede de synthese d'inhibiteurs de cox-2 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20000722A2 HRP20000722A2 (en) | 2001-06-30 |
| HRP20000722B1 true HRP20000722B1 (en) | 2009-07-31 |
Family
ID=26767964
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20000722A HRP20000722B1 (en) | 1998-04-24 | 2000-10-24 | Process for synthesizing cox-2 inhibitors |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US6040319A (fr) |
| EP (1) | EP1071745B1 (fr) |
| JP (2) | JP3325264B2 (fr) |
| KR (1) | KR100414998B1 (fr) |
| CN (1) | CN1178658C (fr) |
| AR (1) | AR015279A1 (fr) |
| AT (1) | ATE272613T1 (fr) |
| AU (1) | AU759469B2 (fr) |
| BR (2) | BRPI9917739B8 (fr) |
| CA (1) | CA2329193C (fr) |
| CZ (1) | CZ292515B6 (fr) |
| DE (1) | DE69919151T2 (fr) |
| DK (1) | DK1071745T3 (fr) |
| EA (1) | EA002975B1 (fr) |
| ES (1) | ES2226378T3 (fr) |
| HK (1) | HK1031399A1 (fr) |
| HR (1) | HRP20000722B1 (fr) |
| HU (1) | HU227627B1 (fr) |
| IL (2) | IL139127A0 (fr) |
| NZ (1) | NZ507597A (fr) |
| PL (1) | PL193248B1 (fr) |
| PT (1) | PT1071745E (fr) |
| RS (1) | RS49945B (fr) |
| SI (1) | SI1071745T1 (fr) |
| SK (1) | SK284805B6 (fr) |
| TW (1) | TW474934B (fr) |
| UA (1) | UA57143C2 (fr) |
| WO (1) | WO1999055830A2 (fr) |
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 |
| ATE253559T1 (de) * | 1999-01-14 | 2003-11-15 | 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 |
| DE60026877T2 (de) * | 1999-11-29 | 2006-11-23 | Merck Frosst Canada Ltd., Kirkland | Polymorphe, amorphe und hydratisierte formen von 5-chlor-3-(methansulfonylphenyl)-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 |
| BR0008060A (pt) * | 1999-12-08 | 2002-02-05 | Pharmacia Corp | Composições inibidoras de ciclooxigenase-2 tendo rápido inìcio de eficácia terapêutica |
| 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 |
| PE20020146A1 (es) * | 2000-07-13 | 2002-03-31 | Upjohn Co | Formulacion oftalmica que comprende un inhibidor de ciclooxigenasa-2 (cox-2) |
| WO2002005848A2 (fr) * | 2000-07-13 | 2002-01-24 | Pharmacia Corporation | Utilisation d'inhibiteurs de cox-2 pour le traitement et la prevention de troubles oculaires a mediation cox-2 |
| US7115565B2 (en) * | 2001-01-18 | 2006-10-03 | Pharmacia & Upjohn Company | Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability |
| PE20021017A1 (es) | 2001-04-03 | 2002-11-24 | Pharmacia Corp | Composicion parenteral reconstituible |
| 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 |
| EP1784179A4 (fr) | 2004-08-24 | 2010-03-31 | Merck Sharp & Dohme | Pluritherapie pour traiter des maladies ou des troubles medies par la cyclo-oxygenase 2 chez des patients presentant un risque d'evenement cardio-vasculaire thrombotique |
| WO2008091530A2 (fr) * | 2007-01-19 | 2008-07-31 | Mallinckrodt Inc. | Ligands de liaison à la cycloxygénase-2 diagnostiques et thérapeutiques |
| DK2479166T3 (da) | 2009-02-27 | 2014-09-01 | Cadila Healthcare Ltd | Fremgangsmåde til fremstilling af etoricoxib |
| ES2683125T3 (es) | 2010-06-16 | 2018-09-25 | Glenmark Generics Limited | Proceso para la preparación de piridinas 2,3-diaril-5-sustituidas y sus compuestos intermedios |
| BR112013012008B1 (pt) | 2010-11-15 | 2021-10-13 | Virdev Intermediates Pvt. Ltd | Processo para o inibidor seletivo da ciclo-oxigenase-2 |
| 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. |
| WO2012163839A1 (fr) | 2011-05-27 | 2012-12-06 | Farma Grs, D.O.O. | Procédé pour la préparation de la forme polymorphe i de l'étoricoxib |
| 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 (fr) | 2012-03-30 | 2015-02-04 | Mylan Laboratories, Limited | Procédé amélioré pour la préparation d'étoricoxib |
| 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 |
| ES2630051T3 (es) | 2012-08-27 | 2017-08-17 | Cadila Healthcare Limited | Composición farmacéutica de etoricoxib |
| ITVI20130014A1 (it) | 2013-01-22 | 2014-07-23 | Italiana Sint Spa | Procedimento molto efficiente per preparare un intermedio di etoricoxib |
| WO2014114352A1 (fr) * | 2013-01-25 | 2014-07-31 | Synthon Bv | Procédé de préparation d'étoricoxib |
| 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 (fr) | 2013-09-13 | 2015-03-19 | Synthon B.V. | Procédé pour la préparation d'étoricoxib |
| EP3268085A4 (fr) | 2015-03-13 | 2018-10-31 | The Board of Trustees of The Leland Stanford Junior University | Inhibition de ltb4 pour prévenir et traiter le lymphoedème humain |
| 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 |
Citations (1)
| 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 |
Family Cites Families (3)
| 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 |
| PL187848B1 (pl) * | 1996-07-18 | 2004-10-29 | Merck Frosst Canada Inc | Podstawione pirydyny, kompozycja farmaceutyczna, podstawione pirydyny jako selektywne inhibitory cyklooksygenazy-2 oraz zastosowanie podstawionych pirydyn |
-
1999
- 1999-04-20 SK SK1589-2000A patent/SK284805B6/sk not_active IP Right Cessation
- 1999-04-20 BR BRPI9917739A patent/BRPI9917739B8/pt not_active IP Right Cessation
- 1999-04-20 CZ CZ20003940A patent/CZ292515B6/cs not_active IP Right Cessation
- 1999-04-20 WO PCT/US1999/008645 patent/WO1999055830A2/fr active IP Right Grant
- 1999-04-20 CN CNB998075507A patent/CN1178658C/zh not_active Expired - Lifetime
- 1999-04-20 IL IL13912799A patent/IL139127A0/xx active IP Right Grant
- 1999-04-20 DE DE69919151T patent/DE69919151T2/de not_active Expired - Lifetime
- 1999-04-20 ES ES99918706T patent/ES2226378T3/es not_active Expired - Lifetime
- 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 HU HU0101407A patent/HU227627B1/hu unknown
- 1999-04-20 KR KR10-2000-7011764A patent/KR100414998B1/ko active Protection Beyond IP Right Term
- 1999-04-20 UA UA2000116652A patent/UA57143C2/uk unknown
- 1999-04-20 EP EP99918706A patent/EP1071745B1/fr not_active Expired - Lifetime
- 1999-04-20 SI SI9930632T patent/SI1071745T1/xx unknown
- 1999-04-20 DK DK99918706T patent/DK1071745T3/da active
- 1999-04-20 BR BRPI9909844-0A patent/BR9909844B1/pt not_active IP Right Cessation
- 1999-04-20 CA CA002329193A patent/CA2329193C/fr not_active Expired - Lifetime
- 1999-04-20 PT PT99918706T patent/PT1071745E/pt unknown
- 1999-04-20 EA EA200001102A patent/EA002975B1/ru not_active IP Right Cessation
- 1999-04-20 RS YUP-641/00A patent/RS49945B/sr unknown
- 1999-04-20 PL PL344108A patent/PL193248B1/pl unknown
- 1999-04-20 AU AU36557/99A patent/AU759469B2/en not_active Expired
- 1999-04-23 TW TW088106545A patent/TW474934B/zh active
- 1999-04-23 AR ARP990101884A patent/AR015279A1/es active IP Right Grant
- 1999-04-23 US US09/298,127 patent/US6040319A/en not_active Expired - Lifetime
-
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
Patent Citations (1)
| 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 |
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