JP2007521340A5 - - Google Patents
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- Publication number
- JP2007521340A5 JP2007521340A5 JP2006552303A JP2006552303A JP2007521340A5 JP 2007521340 A5 JP2007521340 A5 JP 2007521340A5 JP 2006552303 A JP2006552303 A JP 2006552303A JP 2006552303 A JP2006552303 A JP 2006552303A JP 2007521340 A5 JP2007521340 A5 JP 2007521340A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- formula
- compound according
- cancer
- ethanol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 17
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 8
- 210000004027 cell Anatomy 0.000 claims 5
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- 150000004682 monohydrates Chemical class 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 229910016523 CuKa Inorganic materials 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 239000012830 cancer therapeutic Substances 0.000 claims 1
- 239000003183 carcinogenic agent Substances 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000008585 mastocytosis Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 230000000771 oncological effect Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US54249004P | 2004-02-06 | 2004-02-06 | |
| US60/542,490 | 2004-02-06 | ||
| US62493704P | 2004-11-04 | 2004-11-04 | |
| US60/624,937 | 2004-11-04 | ||
| PCT/US2005/003728 WO2005077945A2 (en) | 2004-02-06 | 2005-02-04 | Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012129253A Division JP2012188446A (ja) | 2004-02-06 | 2012-06-06 | キナーゼ阻害薬の２−アミノチアゾール−５−芳香族カルボキサミド化合物の製造法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007521340A JP2007521340A (ja) | 2007-08-02 |
| JP2007521340A5 true JP2007521340A5 (enExample) | 2008-03-06 |
| JP5148115B2 JP5148115B2 (ja) | 2013-02-20 |
Family
ID=34864498
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006552303A Expired - Lifetime JP5148115B2 (ja) | 2004-02-06 | 2005-02-04 | キナーゼ阻害薬の２−アミノチアゾール−５−芳香族カルボキサミド化合物の製造法 |
| JP2012129253A Pending JP2012188446A (ja) | 2004-02-06 | 2012-06-06 | キナーゼ阻害薬の２−アミノチアゾール−５−芳香族カルボキサミド化合物の製造法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012129253A Pending JP2012188446A (ja) | 2004-02-06 | 2012-06-06 | キナーゼ阻害薬の２−アミノチアゾール−５−芳香族カルボキサミド化合物の製造法 |
Country Status (26)
| Country | Link |
|---|---|
| EP (1) | EP1711481B2 (enExample) |
| JP (2) | JP5148115B2 (enExample) |
| KR (2) | KR101310427B1 (enExample) |
| AR (1) | AR047533A1 (enExample) |
| AT (1) | ATE453630T1 (enExample) |
| AU (1) | AU2005212405B2 (enExample) |
| BR (1) | BRPI0507476B8 (enExample) |
| CA (1) | CA2555291C (enExample) |
| CY (1) | CY1109907T1 (enExample) |
| DE (1) | DE602005018601D1 (enExample) |
| DK (1) | DK1711481T4 (enExample) |
| ES (1) | ES2337272T5 (enExample) |
| GE (1) | GEP20094804B (enExample) |
| HR (1) | HRP20100166T4 (enExample) |
| IL (1) | IL177280A (enExample) |
| IN (1) | IN2014DN06567A (enExample) |
| NO (1) | NO338049B1 (enExample) |
| NZ (1) | NZ548613A (enExample) |
| PE (1) | PE20050691A1 (enExample) |
| PL (1) | PL1711481T5 (enExample) |
| PT (1) | PT1711481E (enExample) |
| RU (1) | RU2382039C2 (enExample) |
| SI (1) | SI1711481T2 (enExample) |
| TW (1) | TWI338004B (enExample) |
| WO (1) | WO2005077945A2 (enExample) |
| ZA (1) | ZA200606242B (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1523991A (zh) | 2001-08-10 | 2004-08-25 | ��˹��ŵ�� | 单独的c-Src抑制剂或其与STI571的组合用于治疗白血病的用途 |
| AU2004236240C1 (en) | 2003-05-01 | 2010-11-04 | Bristol-Myers Squibb Company | Aryl-substituted pyrazole compounds useful as kinase inhibitors |
| US7652146B2 (en) | 2004-02-06 | 2010-01-26 | Bristol-Myers Squibb Company | Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors |
| TWI338004B (en) * | 2004-02-06 | 2011-03-01 | Bristol Myers Squibb Co | Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors |
| TW200600513A (en) | 2004-06-30 | 2006-01-01 | Bristol Myers Squibb Co | A method for preparing pyrrolotriazine compounds |
| PT1885339E (pt) * | 2005-05-05 | 2015-10-12 | Bristol Myers Squibb Holdings Ireland | Formulações de um inibidor src/abl |
| DE602006014001D1 (de) | 2005-08-05 | 2010-06-10 | Bristol Myers Squibb Co | Herstellung von 2-aminothiazol-5-carbonsäurederivaten |
| EP1937270A1 (en) * | 2005-09-21 | 2008-07-02 | Brystol-Myers Squibb Company | Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof |
| US20070219370A1 (en) * | 2006-03-15 | 2007-09-20 | Bristol-Myers Squibb Company | Process for preparing n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino] -5-thiazolecarboxamide and related metabolites thereof |
| CN101534831B (zh) | 2006-09-11 | 2013-07-17 | 柯瑞斯公司 | 包含锌结合基团的取代的酪氨酸抑制剂 |
| AR062927A1 (es) | 2006-10-11 | 2008-12-17 | Bayer Healthcare Ag | 4- [4-( [ [ 4- cloro-3-( trifluorometil) fenil) carbamoil] amino] -3- fluorofenoxi) -n- metilpiridin-2- carboxamida monohidratada |
| JP5528806B2 (ja) | 2006-10-12 | 2014-06-25 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
| JP5528807B2 (ja) | 2006-10-12 | 2014-06-25 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
| EP1992344A1 (en) | 2007-05-18 | 2008-11-19 | Institut Curie | P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation |
| US8067423B2 (en) | 2007-10-23 | 2011-11-29 | Teva Pharmaceutical Industries Ltd. | Polymorphs of dasatinib isopropyl alcohol and process for preparation thereof |
| WO2010062715A2 (en) * | 2008-11-03 | 2010-06-03 | Teva Pharmaceutical Industries Ltd. | Polymorphs of dasatinib and process for preparation thereof |
| WO2010067374A2 (en) * | 2008-12-08 | 2010-06-17 | Hetero Research Foundation | Polymorphs of dasatinib |
| AU2010245072B2 (en) * | 2009-05-05 | 2013-11-28 | Merck Sharp & Dohme Corp. | p38 kinase inhibiting agents |
| CN101812060B (zh) * | 2010-02-02 | 2011-08-17 | 南京卡文迪许生物工程技术有限公司 | 一种简捷制备高纯度达沙替尼的新方法以及中间体化合物 |
| EP2359813A1 (en) | 2010-02-04 | 2011-08-24 | Ratiopharm GmbH | Pharmaceutical composition comprising N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamid |
| CN102250084A (zh) * | 2010-02-08 | 2011-11-23 | 南京卡文迪许生物工程技术有限公司 | 达沙替尼多晶型物及其制备方法和药用组合物 |
| JP5589097B2 (ja) * | 2010-02-08 | 2014-09-10 | 南京▲か▼文迪許生物工程技術有限公司 | ダサチニブ多結晶体、並びにその調製方法及び薬物組成物 |
| WO2013065063A1 (en) | 2011-11-03 | 2013-05-10 | Cadila Healthcare Limited | Anhydrous form of dasatinib, process for its preparation and its use |
| AU2013276138B2 (en) | 2012-06-15 | 2017-02-23 | Basf Se | Multicomponent crystals comprising Dasatinib and selected cocrystal formers |
| CN102827156A (zh) * | 2012-09-11 | 2012-12-19 | 湖南欧亚生物有限公司 | 一种达沙替尼的新的工业合成方法 |
| CN103819469A (zh) * | 2012-11-16 | 2014-05-28 | 重庆医药工业研究院有限责任公司 | 一种达沙替尼的晶型及其制备方法 |
| CZ306598B6 (cs) | 2012-12-06 | 2017-03-22 | Zentiva, K.S. | Způsob přípravy a čištění nových i známých polymorfů a solvátů dasatinibu |
| CN103880833B (zh) * | 2012-12-19 | 2018-04-06 | 北京本草天源药物研究院 | 达沙替尼一水合物的新晶形及其制备方法和药物组合物 |
| WO2014102759A2 (en) | 2012-12-31 | 2014-07-03 | Ranbaxy Laboratories Limited | Process for the preparation of dasatinib and its intermediates |
| CN103319476B (zh) * | 2013-06-13 | 2015-12-02 | 济南德爱医药技术有限公司 | 一种激酶抑制剂 |
| CA2917183C (en) * | 2013-07-25 | 2019-01-29 | Basf Se | Salts of dasatinib in crystalline form |
| CA2917209A1 (en) | 2013-07-25 | 2015-01-29 | Basf Se | Salts of dasatinib in amorphous form |
| CN104341410A (zh) * | 2013-08-09 | 2015-02-11 | 上海科胜药物研发有限公司 | 一种达沙替尼新晶型及其制备方法 |
| CN103483289B (zh) * | 2013-09-06 | 2016-01-27 | 浙江科源化工有限公司 | 一种2-氨基-n-(2-氯-6-甲基苯基)噻唑-5-甲酰胺的合成方法 |
| IN2013MU03610A (enExample) | 2013-12-18 | 2015-04-24 | Dharmesh Mahendrabhai Shah | |
| CZ306732B6 (cs) * | 2013-12-19 | 2017-05-31 | Zentiva, K.S. | Způsob přípravy bezvodé polymorfní formy N-6 Dasatinibu |
| AU2015200822A1 (en) | 2014-03-11 | 2015-10-01 | Cerbios-Pharma Sa | Process and intermediates for the preparation of dasatinib |
| RU2567537C1 (ru) * | 2014-04-23 | 2015-11-10 | Олег Ростиславович Михайлов | Кристаллическая безводная дельта-модификация n-(2-хлор-6-метилфенил)-2-[[6-[4-(2-гидроксиэтил)-1-пиперазинил]-2-метил-4-пиримидинил]амино]-5-тиазолкарбоксамида, способ ее получения и фармацевтическая композиция на ее основе |
| HU231013B1 (hu) | 2014-05-26 | 2019-11-28 | Egis Gyógyszergyár Zrt. | Dasatinib sók |
| WO2017002131A1 (en) * | 2015-06-29 | 2017-01-05 | Msn Laboratories Private Limited | Crystalline forms of n-(2-chloro-6-methy]phenvn-2-[f6-[4-(2-hvdroxvethvl)-l- piperazinvil-2-methvl-4-pvrimidinvllaminol-5-thiazolecarboxamide and their process thereof |
| WO2017098391A1 (en) * | 2015-12-11 | 2017-06-15 | Shilpa Medicare Limited | Process for the preparation of dasatinib |
| WO2017108605A1 (en) | 2015-12-22 | 2017-06-29 | Synthon B.V. | Pharmaceutical composition comprising amorphous dasatinib |
| CN105503854A (zh) * | 2015-12-31 | 2016-04-20 | 哈药集团技术中心 | 一种达沙替尼无水合物的新晶型物及其制备方法 |
| JP2019504090A (ja) | 2016-02-03 | 2019-02-14 | ドクター レディズ ラボラトリーズ リミテッド | ダサチニブの固体状態形態およびそれらの調製プロセス |
| EP3419605A1 (en) | 2016-02-25 | 2019-01-02 | Remedica Ltd | Dasatinib formulation |
| GB201608587D0 (en) | 2016-05-16 | 2016-06-29 | Univ Dundee | Treatment of opiod tolerance |
| CN106117195A (zh) * | 2016-06-09 | 2016-11-16 | 青岛辰达生物科技有限公司 | 一种用于治疗白血病的药物达沙替尼的合成方法 |
| IT201700006157A1 (it) * | 2017-01-20 | 2018-07-20 | Cerbios Pharma Sa | Co-cristalli di un composto antitumorale |
| IT201700006145A1 (it) | 2017-01-20 | 2018-07-20 | Cerbios Pharma Sa | Co-cristallo di un composto antitumorale |
| JP6597727B2 (ja) | 2017-05-11 | 2019-10-30 | 東洋インキＳｃホールディングス株式会社 | 表面保護用粘着剤および粘着シート |
| CA3069107A1 (en) * | 2017-07-07 | 2019-01-10 | Biocon Limited | Polymorphic forms of dasatinib |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| JP2021501130A (ja) | 2017-10-05 | 2021-01-14 | フルクラム セラピューティクス，インコーポレイテッド | ＤＵＸ４の発現を低減するためのｐ３８阻害剤の使用 |
| AU2019285066B2 (en) | 2018-06-15 | 2024-06-13 | Handa Pharmaceuticals, Inc. | Kinase inhibitor salts and compositions thereof |
| EP3643713B1 (en) | 2018-10-23 | 2025-07-30 | iOmx Therapeutics AG | Heterocyclic kinase inhibitors and uses thereof |
| CN109369638B (zh) * | 2018-11-21 | 2020-07-07 | 山东罗欣药业集团股份有限公司 | 一种达沙替尼的制备工艺 |
| CN109503568B (zh) * | 2018-12-29 | 2020-08-07 | 山东罗欣药业集团股份有限公司 | 一种达沙替尼的制备方法 |
| US20220298126A1 (en) * | 2019-08-15 | 2022-09-22 | Bayer Aktiengesellschaft | Process of preparing 2-(phenylimino)-3-alkyl-1,3-thiazolidin-4-ones |
| CN112409349A (zh) * | 2019-08-20 | 2021-02-26 | 湖南华纳大药厂股份有限公司 | 激酶抑制剂及其制备、药物组合物和用途 |
| CA3168667A1 (en) | 2020-01-24 | 2021-07-29 | Nanocopoeia, Llc | Amorphous solid dispersions of dasatinib and uses thereof |
| GB2592680A (en) | 2020-03-06 | 2021-09-08 | Zentiva Ks | Pharmaceutical compositions comprising dasatinib anhydrous and uses thereof |
| EP4071248A1 (en) | 2021-04-07 | 2022-10-12 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Means and methods for enhancing receptor-targeted gene transfer |
| US11980619B2 (en) | 2021-07-28 | 2024-05-14 | Nanocopoeia, Llc | Pharmaceutical compositions and crushable tablets including amorphous solid dispersions of dasatinib and uses |
| CN114634421A (zh) * | 2022-02-24 | 2022-06-17 | 济宁晟泰药业有限公司 | 一种达沙替尼中间体的制备方法 |
| US12384773B2 (en) | 2023-11-02 | 2025-08-12 | Arcus Biosciences, Inc. | Thiazole compounds and methods of use thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3547917A (en) * | 1966-12-07 | 1970-12-15 | Uniroyal Inc | 2-amino-4-methylthiazole-5-carboxamides |
| US5514643A (en) * | 1993-08-16 | 1996-05-07 | Lucky Ltd. | 2-aminothiazolecarboxamide derivatives, processes for preparing the same and use thereof for controlling phytopathogenic organisms |
| CZ296266B6 (cs) * | 1997-06-24 | 2006-02-15 | Janssen Pharmaceutica N. V. | 5-Substituovaný 1,2,4-thiadiazolylový derivát, zpusob a meziprodukt pro jeho prípravu, jeho pouzitía farmaceutická kompozice s jeho obsahem |
| PT1169038E (pt) * | 1999-04-15 | 2012-10-26 | Bristol Myers Squibb Co | Inibidores cíclicos da proteína tirosina cinase |
| ATE479667T1 (de) * | 2003-02-06 | 2010-09-15 | Bristol Myers Squibb Co | Als kinaseinhibitoren geeignete verbindungen auf thiazolylbasis |
| EP2260849A1 (en) * | 2004-01-21 | 2010-12-15 | Emory University | Compositions and methods of use for tyrosine kinase inhibitors to treat pathogenic infection |
| TWI338004B (en) * | 2004-02-06 | 2011-03-01 | Bristol Myers Squibb Co | Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors |
-
2005
- 2005-02-01 TW TW094103090A patent/TWI338004B/zh not_active IP Right Cessation
- 2005-02-04 AU AU2005212405A patent/AU2005212405B2/en not_active Expired
- 2005-02-04 ES ES05722772T patent/ES2337272T5/es not_active Expired - Lifetime
- 2005-02-04 WO PCT/US2005/003728 patent/WO2005077945A2/en not_active Ceased
- 2005-02-04 PE PE2005000128A patent/PE20050691A1/es active IP Right Grant
- 2005-02-04 AT AT05722772T patent/ATE453630T1/de active
- 2005-02-04 GE GEAP20059607A patent/GEP20094804B/en unknown
- 2005-02-04 AR ARP050100427A patent/AR047533A1/es not_active Application Discontinuation
- 2005-02-04 DE DE602005018601T patent/DE602005018601D1/de not_active Expired - Lifetime
- 2005-02-04 KR KR1020067015839A patent/KR101310427B1/ko not_active Expired - Lifetime
- 2005-02-04 HR HRP20100166TT patent/HRP20100166T4/hr unknown
- 2005-02-04 JP JP2006552303A patent/JP5148115B2/ja not_active Expired - Lifetime
- 2005-02-04 PT PT05722772T patent/PT1711481E/pt unknown
- 2005-02-04 KR KR1020127021611A patent/KR20120097424A/ko not_active Ceased
- 2005-02-04 SI SI200530905T patent/SI1711481T2/sl unknown
- 2005-02-04 IN IN6567DEN2014 patent/IN2014DN06567A/en unknown
- 2005-02-04 EP EP05722772.0A patent/EP1711481B2/en not_active Expired - Lifetime
- 2005-02-04 BR BRPI0507476A patent/BRPI0507476B8/pt not_active IP Right Cessation
- 2005-02-04 PL PL05722772T patent/PL1711481T5/pl unknown
- 2005-02-04 CA CA2555291A patent/CA2555291C/en not_active Expired - Lifetime
- 2005-02-04 RU RU2006131591/04A patent/RU2382039C2/ru active
- 2005-02-04 NZ NZ548613A patent/NZ548613A/en not_active IP Right Cessation
- 2005-02-04 DK DK05722772.0T patent/DK1711481T4/da active
-
2006
- 2006-07-27 ZA ZA2006/06242A patent/ZA200606242B/en unknown
- 2006-08-03 IL IL177280A patent/IL177280A/en active IP Right Grant
- 2006-08-24 NO NO20063780A patent/NO338049B1/no unknown
-
2010
- 2010-03-19 CY CY20101100253T patent/CY1109907T1/el unknown
-
2012
- 2012-06-06 JP JP2012129253A patent/JP2012188446A/ja active Pending
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