JP2010510215A5 - - Google Patents
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- Publication number
- JP2010510215A5 JP2010510215A5 JP2009537199A JP2009537199A JP2010510215A5 JP 2010510215 A5 JP2010510215 A5 JP 2010510215A5 JP 2009537199 A JP2009537199 A JP 2009537199A JP 2009537199 A JP2009537199 A JP 2009537199A JP 2010510215 A5 JP2010510215 A5 JP 2010510215A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- group
- aliphatic
- fluoro
- cancer
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 41
- 125000001931 aliphatic group Chemical group 0.000 claims description 24
- -1 N-methylpyrrolidinyl Chemical group 0.000 claims description 13
- 102000003989 Aurora kinases Human genes 0.000 claims description 11
- 108090000433 Aurora kinases Proteins 0.000 claims description 11
- 125000000623 heterocyclic group Chemical group 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 9
- 229910052739 hydrogen Inorganic materials 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 125000001153 fluoro group Chemical group F* 0.000 claims description 7
- 125000002541 furyl group Chemical group 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000001544 thienyl group Chemical group 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 230000001404 mediated effect Effects 0.000 claims description 5
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 3
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 3
- 125000003944 tolyl group Chemical group 0.000 claims description 3
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 2
- 102000004000 Aurora Kinase A Human genes 0.000 claims description 2
- 108090000461 Aurora Kinase A Proteins 0.000 claims description 2
- 101150065749 Churc1 gene Proteins 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 102100038239 Protein Churchill Human genes 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 description 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- SRFVRJILPIASPG-UHFFFAOYSA-N 4-[[7-(2-fluoro-6-methoxyphenyl)-9-(1-methylpyrrol-2-yl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C=2N(C=CC=2)C)=C1 SRFVRJILPIASPG-UHFFFAOYSA-N 0.000 description 1
- ZLHFILGSQDJULK-UHFFFAOYSA-N 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 ZLHFILGSQDJULK-UHFFFAOYSA-N 0.000 description 1
- NRJOLMQQQLDIPP-UHFFFAOYSA-N 4-[[9-ethynyl-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C#C)=C1 NRJOLMQQQLDIPP-UHFFFAOYSA-N 0.000 description 1
- 101100167062 Caenorhabditis elegans chch-3 gene Proteins 0.000 description 1
- AIUYVPGHBMKGAC-UHFFFAOYSA-M sodium;4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoate Chemical compound [Na+].C1=C(C([O-])=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 AIUYVPGHBMKGAC-UHFFFAOYSA-M 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85934006P | 2006-11-16 | 2006-11-16 | |
| US60/859,340 | 2006-11-16 | ||
| PCT/US2007/023948 WO2008063525A1 (en) | 2006-11-16 | 2007-11-14 | Compounds for inhibiting mitotic progression |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011187930A Division JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010510215A JP2010510215A (ja) | 2010-04-02 |
| JP2010510215A5 true JP2010510215A5 (OSRAM) | 2011-10-20 |
| JP5102839B2 JP5102839B2 (ja) | 2012-12-19 |
Family
ID=39315133
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009537199A Active JP5102839B2 (ja) | 2006-11-16 | 2007-11-14 | 有糸分裂進行を阻害するための化合物 |
| JP2011187930A Active JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
| JP2013236439A Pending JP2014055166A (ja) | 2006-11-16 | 2013-11-15 | 有糸分裂進行を阻害するための化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011187930A Active JP5452811B2 (ja) | 2006-11-16 | 2011-08-30 | 有糸分裂進行を阻害するための化合物 |
| JP2013236439A Pending JP2014055166A (ja) | 2006-11-16 | 2013-11-15 | 有糸分裂進行を阻害するための化合物 |
Country Status (34)
| Country | Link |
|---|---|
| US (7) | US8026246B2 (OSRAM) |
| EP (4) | EP2086981B1 (OSRAM) |
| JP (3) | JP5102839B2 (OSRAM) |
| KR (2) | KR101342014B1 (OSRAM) |
| CN (2) | CN101547924B (OSRAM) |
| AR (1) | AR064246A1 (OSRAM) |
| AT (1) | ATE556076T1 (OSRAM) |
| AU (1) | AU2007322046B2 (OSRAM) |
| BR (1) | BRPI0718803B8 (OSRAM) |
| CA (1) | CA2669680C (OSRAM) |
| CL (1) | CL2007003244A1 (OSRAM) |
| CR (3) | CR10782A (OSRAM) |
| CY (1) | CY1112828T1 (OSRAM) |
| DK (2) | DK2497772T3 (OSRAM) |
| EA (1) | EA015779B1 (OSRAM) |
| ES (3) | ES2537451T3 (OSRAM) |
| GE (1) | GEP20125459B (OSRAM) |
| HR (2) | HRP20120490T1 (OSRAM) |
| IL (1) | IL198690A0 (OSRAM) |
| MA (1) | MA30988B1 (OSRAM) |
| MX (3) | MX2009004670A (OSRAM) |
| MY (1) | MY153243A (OSRAM) |
| NO (1) | NO343338B1 (OSRAM) |
| NZ (3) | NZ611898A (OSRAM) |
| PH (1) | PH12012502057B1 (OSRAM) |
| PL (2) | PL2497772T3 (OSRAM) |
| PT (2) | PT2497772E (OSRAM) |
| RS (2) | RS53788B1 (OSRAM) |
| SG (2) | SG176443A1 (OSRAM) |
| SI (2) | SI2086981T1 (OSRAM) |
| TW (1) | TWI401255B (OSRAM) |
| UA (1) | UA94129C2 (OSRAM) |
| WO (1) | WO2008063525A1 (OSRAM) |
| ZA (1) | ZA200903279B (OSRAM) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104193750B (zh) | 2004-05-14 | 2018-04-27 | 千禧药品公司 | 通过抑制极光激酶抑制有丝分裂的化合物和方法 |
| CL2007003244A1 (es) * | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| WO2010065134A1 (en) * | 2008-12-05 | 2010-06-10 | Millennium Pharmaceuticals, Inc. | 5, 7-dihydro- 6h-pyrimido [ 5, 4-d] [ 1 ] benzazepin-6-thiones as plk inhibitors |
| MX2011006725A (es) | 2008-12-22 | 2011-09-15 | Millennium Pharm Inc | Combinacion de inhibidores de aurora cinasa y anticuerpos anti-cd20. |
| JO3635B1 (ar) * | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
| JO3434B1 (ar) * | 2009-07-31 | 2019-10-20 | Millennium Pharm Inc | مركبات صيدلانية لمعالجة السرطان وامراض واضطرابات اخري |
| CN104031049A (zh) * | 2010-02-19 | 2014-09-10 | 米伦纽姆医药公司 | 极光激酶抑制剂的结晶形式 |
| US20120107304A1 (en) | 2010-04-27 | 2012-05-03 | Boehringer Ingelheim International Gmbh | Combination therapy in treatment of oncological and fibrotic diseases |
| WO2011161031A1 (en) * | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| AR086656A1 (es) * | 2011-06-03 | 2014-01-15 | Millennium Pharm Inc | Combinacion de inhibidores de mek e inhibidores selectivos de la quinasa aurora a |
| US20130303519A1 (en) * | 2012-03-20 | 2013-11-14 | Millennium Pharmaceuticals, Inc. | Methods of treating cancer using aurora kinase inhibitors |
| CN103772391A (zh) * | 2012-10-23 | 2014-05-07 | 杨子娇 | 一类治疗房角狭窄的化合物及其用途 |
| US9724354B2 (en) | 2013-03-22 | 2017-08-08 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mTORC1/2 inhibitors and selective inhibitors of Aurora A kinase |
| WO2015085289A1 (en) | 2013-12-06 | 2015-06-11 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd30 antibodies |
| CA2972076A1 (en) * | 2014-12-23 | 2016-06-30 | Millennium Pharmaceuticals, Inc. | Combination of raf inhibitors and aurora kinase inhibitors |
| JP2018524292A (ja) | 2015-07-21 | 2018-08-30 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | オーロラキナーゼインヒビターと化学療法剤の投与 |
| CA2997769A1 (en) | 2015-09-09 | 2017-03-16 | Icahn School Of Medicine At Mount Sinai | Heterocyclic constrained tricyclic sulfonamides as anti-cancer agents |
| CN108349961B (zh) | 2015-09-09 | 2022-02-18 | 西奈山伊坎医学院 | 杂环受限三环磺酰胺作为抗癌试剂 |
| US11340215B2 (en) | 2016-02-26 | 2022-05-24 | Japanese Foundation For Cancer Research | Screening method of anticancer agent focused on function of HP1 and evaluation system |
| CN109195593A (zh) | 2016-03-15 | 2019-01-11 | 奥莱松基因组股份有限公司 | 用于治疗实体瘤的lsd1抑制剂的组合 |
| JP6188986B1 (ja) * | 2017-03-23 | 2017-08-30 | 株式会社ノエビア | 時計遺伝子発現量調整剤及びエラスチン産生促進剤 |
| WO2019195658A1 (en) | 2018-04-05 | 2019-10-10 | Dana-Farber Cancer Institute, Inc. | Sting levels as a biomarker for cancer immunotherapy |
| WO2020049208A1 (es) | 2018-09-09 | 2020-03-12 | Fundacio Privada Institut De Recerca De La Sida - Caixa | Aurora cinasa como diana para tratar, prevenir o curar una infección por vih o sida |
| US20220305048A1 (en) | 2019-08-26 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| WO2023196959A1 (en) | 2022-04-07 | 2023-10-12 | Eli Lilly And Company | Process for making a kras g12c inhibitor |
| WO2023196887A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | Method of treatment including kras g12c inhibitors and aurora a inhibitors |
| IL317823A (en) | 2022-06-30 | 2025-02-01 | Lilly Co Eli | KRAS G12C inhibitor for cancer treatment |
| WO2025075211A1 (en) | 2023-10-03 | 2025-04-10 | Takeda Pharmaceutical Company Limited | Alisertib and paclitaxel for treating small cell lung cancer |
| WO2025245045A1 (en) | 2024-05-21 | 2025-11-27 | The Regents Of The University Of California | Methods of treating lung cancer |
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| CN104193750B (zh) * | 2004-05-14 | 2018-04-27 | 千禧药品公司 | 通过抑制极光激酶抑制有丝分裂的化合物和方法 |
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| US20100160324A1 (en) | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| ES2408318T3 (es) | 2005-12-23 | 2013-06-20 | Glaxosmithkline Llc | Inhibidores de azaindol de las cinasas Aurora |
| JP2010500352A (ja) | 2006-08-09 | 2010-01-07 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | 有糸分裂の進行を阻止するためのピリドベンゾアゼピン化合物および方法 |
| CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
| JO3635B1 (ar) | 2009-05-18 | 2020-08-27 | Millennium Pharm Inc | مركبات صيدلانية صلبة وطرق لانتاجها |
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2007
- 2007-11-09 CL CL200703244A patent/CL2007003244A1/es unknown
- 2007-11-14 NZ NZ611898A patent/NZ611898A/en not_active IP Right Cessation
- 2007-11-14 RS RS20150047A patent/RS53788B1/sr unknown
- 2007-11-14 MX MX2009004670A patent/MX2009004670A/es active IP Right Grant
- 2007-11-14 EA EA200970486A patent/EA015779B1/ru unknown
- 2007-11-14 TW TW096143087A patent/TWI401255B/zh active
- 2007-11-14 EP EP07867449A patent/EP2086981B1/en active Active
- 2007-11-14 CN CN2007800423837A patent/CN101547924B/zh active Active
- 2007-11-14 SG SG2011080652A patent/SG176443A1/en unknown
- 2007-11-14 DK DK12153131.3T patent/DK2497772T3/en active
- 2007-11-14 SI SI200730975T patent/SI2086981T1/sl unknown
- 2007-11-14 US US11/985,277 patent/US8026246B2/en active Active
- 2007-11-14 GE GEAP200711309A patent/GEP20125459B/en unknown
- 2007-11-14 KR KR1020117022355A patent/KR101342014B1/ko active Active
- 2007-11-14 PL PL12153131T patent/PL2497772T3/pl unknown
- 2007-11-14 JP JP2009537199A patent/JP5102839B2/ja active Active
- 2007-11-14 DK DK07867449.6T patent/DK2086981T3/da active
- 2007-11-14 EP EP15155821.0A patent/EP2944639B1/en active Active
- 2007-11-14 BR BRPI0718803A patent/BRPI0718803B8/pt active IP Right Grant
- 2007-11-14 EP EP12153134.7A patent/EP2497773B1/en active Active
- 2007-11-14 CA CA2669680A patent/CA2669680C/en active Active
- 2007-11-14 AT AT07867449T patent/ATE556076T1/de active
- 2007-11-14 PL PL07867449T patent/PL2086981T3/pl unknown
- 2007-11-14 HR HRP20120490TT patent/HRP20120490T1/hr unknown
- 2007-11-14 KR KR1020097012501A patent/KR101110458B1/ko active Active
- 2007-11-14 ZA ZA200903279A patent/ZA200903279B/xx unknown
- 2007-11-14 RS RS20120247A patent/RS52313B/sr unknown
- 2007-11-14 MX MX2012011398A patent/MX343391B/es unknown
- 2007-11-14 ES ES12153134.7T patent/ES2537451T3/es active Active
- 2007-11-14 NZ NZ577042A patent/NZ577042A/en unknown
- 2007-11-14 ES ES12153131.3T patent/ES2528793T3/es active Active
- 2007-11-14 SG SG10201503350TA patent/SG10201503350TA/en unknown
- 2007-11-14 SI SI200731591T patent/SI2497772T1/sl unknown
- 2007-11-14 MX MX2012011396A patent/MX348568B/es unknown
- 2007-11-14 EP EP12153131.3A patent/EP2497772B1/en active Active
- 2007-11-14 WO PCT/US2007/023948 patent/WO2008063525A1/en not_active Ceased
- 2007-11-14 NZ NZ597252A patent/NZ597252A/xx unknown
- 2007-11-14 ES ES07867449T patent/ES2384123T3/es active Active
- 2007-11-14 PT PT121531313T patent/PT2497772E/pt unknown
- 2007-11-14 CN CN201310367332.9A patent/CN103483343B/zh active Active
- 2007-11-14 AU AU2007322046A patent/AU2007322046B2/en active Active
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- 2007-11-16 AR ARP070105104A patent/AR064246A1/es unknown
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2009
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- 2009-05-11 IL IL198690A patent/IL198690A0/en active IP Right Grant
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2011
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2012
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2013
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2014
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2015
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2018
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