FI4013755T3 - Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä - Google Patents
Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä Download PDFInfo
- Publication number
- FI4013755T3 FI4013755T3 FIEP20757967.3T FI20757967T FI4013755T3 FI 4013755 T3 FI4013755 T3 FI 4013755T3 FI 20757967 T FI20757967 T FI 20757967T FI 4013755 T3 FI4013755 T3 FI 4013755T3
- Authority
- FI
- Finland
- Prior art keywords
- alkyl
- alkoxy
- hydrogen
- alkylene
- pharmaceutically acceptable
- Prior art date
Links
- 102100029234 Histone-lysine N-methyltransferase NSD2 Human genes 0.000 title 1
- 101000634048 Homo sapiens Histone-lysine N-methyltransferase NSD2 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 (i) — hydrogen Chemical class 0.000 claims 25
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 18
- 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 claims 17
- 239000000203 mixture Substances 0.000 claims 17
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 14
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 229960000643 adenine Drugs 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 125000001359 1,2,3-triazol-4-yl group Chemical group [H]N1N=NC([*])=C1[H] 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 229930024421 Adenine Natural products 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000004212 difluorophenyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004284 isoxazol-3-yl group Chemical group [H]C1=C([H])C(*)=NO1 0.000 claims 1
- 125000004287 oxazol-2-yl group Chemical group [H]C1=C([H])N=C(*)O1 0.000 claims 1
- 125000000369 oxido group Chemical group [*]=O 0.000 claims 1
- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical compound OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 229920001935 styrene-ethylene-butadiene-styrene Polymers 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2019/100542 WO2021026803A1 (en) | 2019-08-14 | 2019-08-14 | Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents |
| PCT/IB2020/057602 WO2021028854A1 (en) | 2019-08-14 | 2020-08-12 | Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| FI4013755T3 true FI4013755T3 (fi) | 2025-04-02 |
Family
ID=72145436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FIEP20757967.3T FI4013755T3 (fi) | 2019-08-14 | 2020-08-12 | Piperidinyylimetyylipuriiniamiineja nsd2:n estäjinä ja syöpälääkkeinä |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US11420970B1 (https=) |
| EP (2) | EP4013755B1 (https=) |
| JP (2) | JP7638960B2 (https=) |
| KR (1) | KR102946008B1 (https=) |
| CN (1) | CN114585622B (https=) |
| AU (1) | AU2020328919A1 (https=) |
| BR (1) | BR112022002520A2 (https=) |
| CO (1) | CO2022002804A2 (https=) |
| DK (1) | DK4013755T3 (https=) |
| EC (1) | ECSP22019360A (https=) |
| ES (1) | ES3023540T3 (https=) |
| FI (1) | FI4013755T3 (https=) |
| IL (2) | IL289754B2 (https=) |
| MX (1) | MX2022001784A (https=) |
| MY (1) | MY209614A (https=) |
| PH (1) | PH12022550343A1 (https=) |
| PL (1) | PL4013755T3 (https=) |
| PT (1) | PT4013755T (https=) |
| WO (2) | WO2021026803A1 (https=) |
| ZA (1) | ZA202200519B (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021026803A1 (en) * | 2019-08-14 | 2021-02-18 | Novartis Ag | Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents |
| DK4013756T3 (da) * | 2019-09-20 | 2024-05-27 | Novartis Ag | MLL1-inhibitorer og anticancermidler |
| JP2025504379A (ja) * | 2022-01-05 | 2025-02-12 | ケイ３６・セラピューティクス・インコーポレイテッド | 重水素濃縮ピペリジニル－メチル－プリンアミン及び関連化合物、ならびに疾患及び状態の治療におけるそれらの使用 |
| IL314895A (en) * | 2022-02-16 | 2024-10-01 | Duke Street Bio Ltd | Pharmaceutical compound |
| WO2023225150A1 (en) * | 2022-05-18 | 2023-11-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine fumaric acid salts, crystalline forms, and their use in treating medical diseases and conditions |
| US20250326752A1 (en) * | 2022-05-18 | 2025-10-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions |
| AU2023273656A1 (en) * | 2022-05-18 | 2024-11-28 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine d-tartaric acid salts, crystalline forms, and their use in treating medical diseases and conditions |
| WO2023225144A1 (en) * | 2022-05-18 | 2023-11-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions |
| WO2023230038A1 (en) * | 2022-05-23 | 2023-11-30 | K36 Therapeutics, Inc. | Piperidinyl-methylpurine pyrimidines and related compounds and their use in treating diseases and conditions |
| US20250361235A1 (en) * | 2022-05-23 | 2025-11-27 | K36 Therapeutics, Inc. | Piperidinyl-methylpurine benzenes and related compounds and their use in treating diseases and conditions |
| WO2024073283A1 (en) * | 2022-09-26 | 2024-04-04 | Board Of Regents, The University Of Texas System | Heterocycles as modulators of nsd activity |
| JP2025530501A (ja) * | 2022-09-26 | 2025-09-11 | ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム | Ｎｓｄ活性の修飾物質としての複素環 |
| KR20250129690A (ko) * | 2022-12-12 | 2025-08-29 | 케이36 테라퓨틱스, 인크. | 피페리딘일-메틸-푸린 아민을 함유하는 약학적 조성물과 질환 및 병태 치료에서 이의 용도 |
| WO2025106786A1 (en) * | 2023-11-17 | 2025-05-22 | K36 Therapeutics, Inc. | Deuterium-enriched piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions |
| CN117720550A (zh) * | 2023-12-14 | 2024-03-19 | 深圳市华先医药科技有限公司 | (s)-3-甲基-4-氧代-2-氧杂-8-氮杂螺[4.5]癸烷-8-甲酸叔丁酯合成方法 |
| CN117843641B (zh) * | 2023-12-28 | 2025-04-25 | 和径医药科技（上海）有限公司 | Nsd3抑制剂及其制备方法和应用 |
| WO2025147514A1 (en) * | 2024-01-02 | 2025-07-10 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purineamine nsd2 inhibitor therapeutic methods and compositions for treating cancer |
| CN118459395A (zh) * | 2024-05-10 | 2024-08-09 | 南通大学 | 一种5-(叔丁氧羰基氨基)哌啶-3-羧酸甲酯的合成方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7157465B2 (en) | 2001-04-17 | 2007-01-02 | Dainippon Simitomo Pharma Co., Ltd. | Adenine derivatives |
| US7332486B2 (en) * | 2002-08-08 | 2008-02-19 | Memory Pharmaceuticals Corp. | Phosphodiesterase 4 inhibitors |
| MXPA05003193A (es) * | 2002-09-27 | 2005-06-08 | Sumitomo Pharma | Compuesto de adenina novedoso y uso del mismo. |
| JP2004137157A (ja) * | 2002-10-16 | 2004-05-13 | Sumitomo Pharmaceut Co Ltd | 新規アデニン誘導体を有効成分として含有する医薬 |
| JP2007269629A (ja) | 2004-06-21 | 2007-10-18 | Astellas Pharma Inc | キナゾリン誘導体 |
| AR065784A1 (es) | 2007-03-20 | 2009-07-01 | Dainippon Sumitomo Pharma Co | Derivados de 8-oxo adenina,medicamentos que los contienen y usos como agentes terapeuticos para enfermedades alergicas, antivirales o antibacterianas. |
| JP5694345B2 (ja) * | 2009-10-22 | 2015-04-01 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔｏｌｌ様受容体の調節因子 |
| GB201204985D0 (en) | 2012-03-21 | 2012-05-02 | Genentech Inc | Compounds |
| WO2019196918A1 (zh) | 2018-04-13 | 2019-10-17 | 罗欣药业(上海)有限公司 | 五元杂环并嘧啶类化合物、药物组合物及用途 |
| CN109223794B (zh) * | 2018-08-24 | 2020-07-28 | 江苏理工学院 | 一种化合物c6作为组蛋白甲基转移酶nsd3活性抑制剂及其应用 |
| CN108853110B (zh) | 2018-08-24 | 2020-07-28 | 江苏理工学院 | 一种化合物a8作为组蛋白甲基转移酶nsd3活性抑制剂及其应用 |
| WO2021026803A1 (en) * | 2019-08-14 | 2021-02-18 | Novartis Ag | Piperidinyl-methyl-purineamines as nsd2 inhibitors and anti-cancer agents |
| JP2025504379A (ja) | 2022-01-05 | 2025-02-12 | ケイ３６・セラピューティクス・インコーポレイテッド | 重水素濃縮ピペリジニル－メチル－プリンアミン及び関連化合物、ならびに疾患及び状態の治療におけるそれらの使用 |
| AU2023273656A1 (en) | 2022-05-18 | 2024-11-28 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine d-tartaric acid salts, crystalline forms, and their use in treating medical diseases and conditions |
| WO2023225144A1 (en) | 2022-05-18 | 2023-11-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions |
| US20250326752A1 (en) | 2022-05-18 | 2025-10-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine salts, crystalline forms, and their use in treating medical diseases and conditions |
| WO2023225150A1 (en) | 2022-05-18 | 2023-11-23 | K36 Therapeutics, Inc. | Piperidinyl-methyl-purine amine fumaric acid salts, crystalline forms, and their use in treating medical diseases and conditions |
-
2019
- 2019-08-14 WO PCT/CN2019/100542 patent/WO2021026803A1/en not_active Ceased
-
2020
- 2020-08-12 MY MYPI2022000244A patent/MY209614A/en unknown
- 2020-08-12 WO PCT/IB2020/057602 patent/WO2021028854A1/en not_active Ceased
- 2020-08-12 CN CN202080069611.5A patent/CN114585622B/zh active Active
- 2020-08-12 KR KR1020227008255A patent/KR102946008B1/ko active Active
- 2020-08-12 ES ES20757967T patent/ES3023540T3/es active Active
- 2020-08-12 PT PT207579673T patent/PT4013755T/pt unknown
- 2020-08-12 BR BR112022002520A patent/BR112022002520A2/pt unknown
- 2020-08-12 EP EP20757967.3A patent/EP4013755B1/en active Active
- 2020-08-12 PH PH1/2022/550343A patent/PH12022550343A1/en unknown
- 2020-08-12 IL IL289754A patent/IL289754B2/en unknown
- 2020-08-12 FI FIEP20757967.3T patent/FI4013755T3/fi active
- 2020-08-12 JP JP2022509034A patent/JP7638960B2/ja active Active
- 2020-08-12 AU AU2020328919A patent/AU2020328919A1/en active Pending
- 2020-08-12 EP EP25150251.4A patent/EP4559915A1/en active Pending
- 2020-08-12 DK DK20757967.3T patent/DK4013755T3/da active
- 2020-08-12 MX MX2022001784A patent/MX2022001784A/es unknown
- 2020-08-12 PL PL20757967.3T patent/PL4013755T3/pl unknown
- 2020-08-12 IL IL320143A patent/IL320143A/en unknown
-
2021
- 2021-05-21 US US17/327,226 patent/US11420970B1/en active Active
-
2022
- 2022-01-11 ZA ZA2022/00519A patent/ZA202200519B/en unknown
- 2022-03-10 CO CONC2022/0002804A patent/CO2022002804A2/es unknown
- 2022-03-14 EC ECSENADI202219360A patent/ECSP22019360A/es unknown
- 2022-05-09 US US17/739,855 patent/US12312353B2/en active Active
-
2025
- 2025-02-19 JP JP2025024756A patent/JP2025081505A/ja active Pending
- 2025-05-20 US US19/213,478 patent/US20250276971A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| BR112022002520A2 (pt) | 2022-05-10 |
| KR20220047330A (ko) | 2022-04-15 |
| US20230002388A1 (en) | 2023-01-05 |
| AU2020328919A1 (en) | 2022-02-17 |
| EP4013755A1 (en) | 2022-06-22 |
| EP4013755B1 (en) | 2025-01-08 |
| IL289754A (en) | 2022-03-01 |
| CN114585622B (zh) | 2024-08-09 |
| KR102946008B1 (ko) | 2026-04-01 |
| CN114585622A (zh) | 2022-06-03 |
| CA3144542A1 (en) | 2021-02-18 |
| US11420970B1 (en) | 2022-08-23 |
| IL320143A (en) | 2025-06-01 |
| DK4013755T3 (da) | 2025-03-31 |
| ECSP22019360A (es) | 2022-04-29 |
| MY209614A (en) | 2025-07-24 |
| IL289754B2 (en) | 2025-09-01 |
| PH12022550343A1 (en) | 2023-03-13 |
| WO2021026803A1 (en) | 2021-02-18 |
| US12312353B2 (en) | 2025-05-27 |
| JP2022544946A (ja) | 2022-10-24 |
| JP2025081505A (ja) | 2025-05-27 |
| MX2022001784A (es) | 2022-04-18 |
| CO2022002804A2 (es) | 2022-04-08 |
| ES3023540T3 (en) | 2025-06-02 |
| JP7638960B2 (ja) | 2025-03-04 |
| PL4013755T3 (pl) | 2025-05-12 |
| WO2021028854A1 (en) | 2021-02-18 |
| IL289754B1 (en) | 2025-05-01 |
| PT4013755T (pt) | 2025-05-02 |
| US20250276971A1 (en) | 2025-09-04 |
| EP4559915A1 (en) | 2025-05-28 |
| ZA202200519B (en) | 2024-08-28 |
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