SG11201805838UA - Macrocyclic mcl1 inhibitors for treating cancer - Google Patents
Macrocyclic mcl1 inhibitors for treating cancerInfo
- Publication number
- SG11201805838UA SG11201805838UA SG11201805838UA SG11201805838UA SG11201805838UA SG 11201805838U A SG11201805838U A SG 11201805838UA SG 11201805838U A SG11201805838U A SG 11201805838UA SG 11201805838U A SG11201805838U A SG 11201805838UA SG 11201805838U A SG11201805838U A SG 11201805838UA
- Authority
- SG
- Singapore
- Prior art keywords
- astrazeneca
- waltham
- drive
- gatehouse
- international
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 201000011510 cancer Diseases 0.000 title abstract 3
- 102100026539 Induced myeloid leukemia cell differentiation protein Mcl-1 Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 101150094281 mcl1 gene Proteins 0.000 title 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 101001056180 Homo sapiens Induced myeloid leukemia cell differentiation protein Mcl-1 Proteins 0.000 abstract 1
- UVTJKLLUVOTSOB-UHFFFAOYSA-N etaqualone Chemical compound CCC1=CC=CC=C1N1C(=O)C2=CC=CC=C2N=C1C UVTJKLLUVOTSOB-UHFFFAOYSA-N 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002402 nanowire electron scattering Methods 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
- C07D497/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1 MI 11111 0 11101 HOE 010 1111 1 0 I OEM OH 1101 OHO 11110 MAMIE Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\"\" WO 2017/182625 Al 26 October 2017 (26.10.2017) WIPO I PCT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, C07D 515/22 (2006.01) A61P 35/00 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, A61K 31/395 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (21) International Application Number: HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, PCT/EP2017/059511 KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (22) International Filing Date: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 21 April 2017 (21.04.2017) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 62/326,156 22 April 2016 (22.04.2016) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (71) Applicant: ASTRAZENECA AB [SE/SE]; SE-151 85 TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, Sodertalje (SE). MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (72) Inventors: HIRD, Alexander; AstraZeneca 35 Gate- TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, house Drive, MA, Waltham 02451 (US). BELMONTE, KM, ML, MR, NE, SN, TD, TG). _ Matthew, Alan; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). YANG, Wenzhan; AstraZeneca Declarations under Rule 4.17: 35 Gatehouse Drive, MA, Waltham 02451 (US). SE- — as to applicant's entitlement to apply for and be granted a CRIST, John, Paul; AstraZeneca 35 Gatehouse Drive, patent (Rule 4.17(ii)) = MA, Waltham 02451 (US). ROBBINS, Daniel, William; Published: AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 — with international search report (Art. 21(3)) (US). KAZMIRSKI, Steven, Lee; AstraZeneca 35 Gate- — with sequence listing part of description (Rule 5.2(a)) house Drive, MA, Waltham 02451 (US). WU, Dedong; = — AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 = (US). PENG, Bo; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). JOHANNES, Jeffrey; AstraZeneca = 35 Gatehouse Drive, MA, Waltham 02451 (US). LAMB, Michelle, Laurae; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). YE, Oing; AstraZeneca 35 Gate- = = house Drive, MA, Waltham 02451 (US). ZHENG, Xi- _ aolan; AstraZeneca 35 Gatehouse Drive, MA, Waltham = 02451 (US). = (74) Agent: NESS, Mark; Milstein Building Granta Park, Cam- bridge Cambridgeshire CB21 6GH (GB). = (81) Designated States (unless otherwise indicated, for every = _ kind of national protection available): AE, AG, AL, AM, = Title: MACROCYCLIC MCL1 INHIBITORS FOR TREATING CANCER = (54) (57) : Disclosed is a compound which is 17-chloro-5,13,14,22-tetram- ethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo [27.7.1.14,7.011,15. _— 1-1 016,21.020,24.030,35]octatriaconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tride- fl caene-23-carboxylic acid (Formula I) and enantiomers and phar- in maceutically acceptable salts thereof. Also disclosed are phar- ei maceutical compositions of 17-chloro-5,13,14,22-tetramethy1-28-oxa-2,9- VZ+ ei ( 1 ) dithia- 5,6,12,13,22 -pentaazaheptacyclo [27.7.1.14,7.011,15.016,21.020,24.030,35]octatri- cc c OH aconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35 -tridecaene-23 -carboxylic acid, and 1-1 enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer IN S N with such compounds and compositions. 1-1 N—N ei 0 O
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326156P | 2016-04-22 | 2016-04-22 | |
| PCT/EP2017/059511 WO2017182625A1 (en) | 2016-04-22 | 2017-04-21 | Macrocyclic mcl1 inhibitors for treating cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201805838UA true SG11201805838UA (en) | 2018-11-29 |
Family
ID=58664658
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201805838UA SG11201805838UA (en) | 2016-04-22 | 2017-04-21 | Macrocyclic mcl1 inhibitors for treating cancer |
Country Status (37)
| Country | Link |
|---|---|
| US (4) | US9840518B2 (en) |
| EP (1) | EP3445767B1 (en) |
| JP (1) | JP6894449B2 (en) |
| KR (1) | KR102388208B1 (en) |
| CN (1) | CN109071566B (en) |
| AR (1) | AR108301A1 (en) |
| AU (1) | AU2017252222B2 (en) |
| BR (1) | BR112018070677B1 (en) |
| CL (1) | CL2018002410A1 (en) |
| CO (1) | CO2018008759A2 (en) |
| CR (1) | CR20180499A (en) |
| CY (1) | CY1123186T1 (en) |
| DK (1) | DK3445767T3 (en) |
| DO (1) | DOP2018000222A (en) |
| EA (1) | EA036551B1 (en) |
| ES (1) | ES2791319T3 (en) |
| HR (1) | HRP20200673T1 (en) |
| HU (1) | HUE049591T2 (en) |
| IL (1) | IL262237B (en) |
| LT (1) | LT3445767T (en) |
| MA (1) | MA44721B1 (en) |
| ME (1) | ME03729B (en) |
| MX (1) | MX386103B (en) |
| NI (1) | NI201800093A (en) |
| PE (1) | PE20181803A1 (en) |
| PH (1) | PH12018502227A1 (en) |
| PL (1) | PL3445767T3 (en) |
| PT (1) | PT3445767T (en) |
| RS (1) | RS60257B1 (en) |
| SG (1) | SG11201805838UA (en) |
| SI (1) | SI3445767T1 (en) |
| SM (1) | SMT202000249T1 (en) |
| SV (1) | SV2018005742A (en) |
| TN (1) | TN2018000319A1 (en) |
| TW (1) | TWI742074B (en) |
| WO (1) | WO2017182625A1 (en) |
| ZA (1) | ZA201807766B (en) |
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| CN109071566B (en) | 2016-04-22 | 2021-08-31 | 阿斯利康(瑞典)有限公司 | Macrocyclic MCL-1 Inhibitors for the Treatment of Cancer |
| CN109715632B (en) | 2016-05-19 | 2021-10-26 | 拜尔公开股份有限公司 | Macrocyclic indole derivatives |
| TWI781996B (en) * | 2017-03-31 | 2022-11-01 | 瑞典商阿斯特捷利康公司 | Methods of synthesizing an mcl-1 inhibitor |
| TW201904976A (en) * | 2017-03-31 | 2019-02-01 | 瑞典商阿斯特捷利康公司 | Mcl-1 inhibitors and methods of use thereof |
| SG11202001182QA (en) | 2017-08-15 | 2020-03-30 | Abbvie Inc | Macrocyclic mcl-1 inhibitors and methods of use |
| AU2018317836A1 (en) * | 2017-08-15 | 2020-03-19 | AbbVie Deutschland GmbH & Co. KG | Macrocyclic MCL-1 inhibitors and methods of use |
| WO2019096914A1 (en) * | 2017-11-17 | 2019-05-23 | Bayer Aktiengesellschaft | Macrocyclic chlorine substituted indole derivatives |
| WO2019096907A1 (en) * | 2017-11-17 | 2019-05-23 | Bayer Aktiengesellschaft | Aryl annulated macrocyclic indole derivatives |
| EP3710456B1 (en) | 2017-11-17 | 2022-09-21 | The Broad Institute, Inc. | Macrocyclic indole derivatives |
| US11478451B1 (en) | 2017-11-17 | 2022-10-25 | Bayer Aktiengesellschaft | Macrocyclic chlorine substituted indole derivatives |
| UY37971A (en) * | 2017-11-17 | 2019-06-28 | Bayer Ag | SUBSTITUTED MACROCYCLIC INDOL DERITATES |
| EP3710449B1 (en) | 2017-11-17 | 2022-07-06 | The Broad Institute, Inc. | Macrocyclic fluorine substituted indole derivatives as mcl-1 inhibitors, for use in the treatment of cancer |
| TW202014184A (en) * | 2018-04-30 | 2020-04-16 | 瑞典商阿斯特捷利康公司 | Combinations for treating cancer |
| US20220041623A1 (en) * | 2018-09-30 | 2022-02-10 | Jiangsu Hengrui Medicine Co., Ltd. | Indole macrocyclic derivative, preparation method thereof and application thereof in medicine |
| TWI810397B (en) | 2018-11-14 | 2023-08-01 | 瑞典商阿斯特捷利康公司 | Methods of treating cancer |
| CN111205309B (en) * | 2018-11-21 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | Indole macrocyclic derivatives, preparation method and medical application thereof |
| US11691989B2 (en) | 2018-11-22 | 2023-07-04 | Ascentage Pharma (Suzhou) Co., Ltd. | Macrocyclic indoles as Mcl-1 inhibitors |
| TWI760685B (en) * | 2019-01-23 | 2022-04-11 | 大陸商蘇州亞盛藥業有限公司 | Macrocyclic fused pyrrazoles as mcl-1 inhibitors |
| MX2021010321A (en) * | 2019-03-08 | 2021-11-17 | Zeno Man Inc | Macrocyclic compounds. |
| CN113574058B (en) * | 2019-04-30 | 2024-04-16 | 江苏恒瑞医药股份有限公司 | Indole macrocyclic derivatives, preparation methods and medical applications thereof |
| CN114127059B (en) | 2019-05-10 | 2024-09-24 | 詹森生物科技公司 | Macrocyclic chelating agents and methods of use thereof |
| CN114127079A (en) | 2019-05-17 | 2022-03-01 | 布罗德研究所有限公司 | Process for preparing macrocyclic indoles |
| UY38700A (en) | 2019-05-20 | 2020-12-31 | Novartis Ag | MCL-1 INHIBITORS ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE |
| US20220306653A1 (en) * | 2019-06-21 | 2022-09-29 | Janssen Pharmaceutica Nv | Macrocyclic inhibitors of mcl-1 |
| US20240067660A1 (en) | 2019-07-09 | 2024-02-29 | Janssen Pharmaceutica Nv | Macrocyclic spirocycle derivatives as mcl-1 inhibitors |
| US20220372014A1 (en) * | 2019-10-01 | 2022-11-24 | The Johns Hopkins University | Neuroprotective compounds and methods of use thereof |
| WO2021092053A1 (en) * | 2019-11-08 | 2021-05-14 | Unity Biotechnology, Inc. | Mcl-1 inhibitor macrocycle compounds for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer |
| WO2021092061A1 (en) * | 2019-11-08 | 2021-05-14 | Unity Biotechnology, Inc. | Combination treatment for senescence-associated diseases |
| KR20220103984A (en) * | 2019-11-21 | 2022-07-25 | 얀센 파마슈티카 엔.브이. | Macrocyclic indole derivatives as MCL-1 inhibitors |
| MX2022006180A (en) * | 2019-11-21 | 2022-06-14 | Janssen Pharmaceutica Nv | Macrocyclic sulfonyl derivatives as mcl-1 inhibitors. |
| AU2020409006A1 (en) * | 2019-12-18 | 2022-06-30 | Zeno Management, Inc. | Macrocyclic compounds |
| AU2021222332A1 (en) | 2020-02-21 | 2022-10-20 | Janssen Pharmaceutica Nv | Macrocyclic indole derivatives as inhibitors of MCL-1 |
| CN115335384B (en) * | 2020-03-30 | 2024-10-22 | 江苏恒瑞医药股份有限公司 | Crystal form of indole macrocyclic derivative and preparation method thereof |
| CN115605486A (en) * | 2020-05-29 | 2023-01-13 | 詹森药业有限公司(Be) | Macrocyclic 7-pyrazol-5-yl-indole derivatives as MCL-1 inhibitors |
| BR112022025631A2 (en) | 2020-06-19 | 2023-01-17 | Janssen Pharmaceutica Nv | N-LINKED MACROCYCLIC 4-(PYRAZOL-5-IL)-INDOLE DERIVATIVES AS MCL-1 INHIBITORS |
| WO2021255257A1 (en) | 2020-06-19 | 2021-12-23 | Janssen Pharmaceutica Nv | N-linked macrocyclic 7-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1 |
| JP2023532592A (en) | 2020-07-08 | 2023-07-28 | ヤンセン ファーマシューティカ エヌ.ベー. | Macrocyclic Ether-Containing Indole Derivatives as Inhibitors of MCL-1 |
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| US20240042051A1 (en) | 2020-11-24 | 2024-02-08 | Francesca Rocchetti | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| CA3200758A1 (en) | 2020-12-17 | 2022-06-23 | Janssen Pharmaceutica Nv | Branched macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1 |
| CN116848126A (en) | 2021-02-12 | 2023-10-03 | 詹森药业有限公司 | Macrocyclic 1,3-bridged 6-chloro-7-pyrazol-4-yl-1H-indole-2-carboxylate and 6-chloro-7-pyrimidin-5-yl-1H-indole- 2-carboxylate derivatives as MCL-1 inhibitors for cancer treatment |
| WO2022251247A1 (en) * | 2021-05-28 | 2022-12-01 | Zeno Management, Inc. | Macrocyclic compounds |
| AU2022291381B2 (en) | 2021-06-11 | 2025-04-24 | Gilead Sciences, Inc. | Combination mcl-1 inhibitors with anti-cancer agents |
| EP4351657A1 (en) | 2021-06-11 | 2024-04-17 | Gilead Sciences, Inc. | Combination mcl-1 inhibitors with anti-body drug conjugates |
| CN115490708B (en) * | 2021-06-18 | 2025-01-24 | 苏州亚盛药业有限公司 | Sulfonamide macrocyclic derivatives and preparation methods and uses thereof |
| WO2023057484A1 (en) | 2021-10-06 | 2023-04-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for predicting and improving the efficacy of mcl-1 inhibitor therapy |
| CR20240553A (en) | 2022-05-20 | 2025-05-02 | Servier Lab | Antibody-drug conjugates of antineoplastic compounds and methods of use thereof |
| WO2025111450A1 (en) | 2023-11-22 | 2025-05-30 | Les Laboratoires Servier | Anti-cd74 antibody-drug conjugates and methods of use thereof |
| WO2025111431A1 (en) | 2023-11-22 | 2025-05-30 | Les Laboratoires Servier | Anti-cd7 antibody-drug conjugates and methods of use thereof |
| WO2025126157A1 (en) | 2023-12-15 | 2025-06-19 | Advesya | Anti-il-1rap binding domains and antibody-drug conjugates thereof |
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2017
- 2017-04-21 CN CN201780022366.0A patent/CN109071566B/en active Active
- 2017-04-21 JP JP2018553226A patent/JP6894449B2/en active Active
- 2017-04-21 TN TNP/2018/000319A patent/TN2018000319A1/en unknown
- 2017-04-21 BR BR112018070677-9A patent/BR112018070677B1/en active IP Right Grant
- 2017-04-21 ES ES17720720T patent/ES2791319T3/en active Active
- 2017-04-21 PL PL17720720T patent/PL3445767T3/en unknown
- 2017-04-21 CO CONC2018/0008759A patent/CO2018008759A2/en unknown
- 2017-04-21 KR KR1020187033540A patent/KR102388208B1/en active Active
- 2017-04-21 SM SM20200249T patent/SMT202000249T1/en unknown
- 2017-04-21 US US15/493,210 patent/US9840518B2/en active Active
- 2017-04-21 MA MA44721A patent/MA44721B1/en unknown
- 2017-04-21 AU AU2017252222A patent/AU2017252222B2/en active Active
- 2017-04-21 EP EP17720720.6A patent/EP3445767B1/en active Active
- 2017-04-21 TW TW106113380A patent/TWI742074B/en active
- 2017-04-21 ME MEP-2020-99A patent/ME03729B/en unknown
- 2017-04-21 MX MX2018012711A patent/MX386103B/en unknown
- 2017-04-21 AR ARP170101026A patent/AR108301A1/en active IP Right Grant
- 2017-04-21 CR CR20180499A patent/CR20180499A/en unknown
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