ZA201408452B - 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof - Google Patents
5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereofInfo
- Publication number
- ZA201408452B ZA201408452B ZA2014/08452A ZA201408452A ZA201408452B ZA 201408452 B ZA201408452 B ZA 201408452B ZA 2014/08452 A ZA2014/08452 A ZA 2014/08452A ZA 201408452 A ZA201408452 A ZA 201408452A ZA 201408452 B ZA201408452 B ZA 201408452B
- Authority
- ZA
- South Africa
- Prior art keywords
- carbonitrile
- morpholin
- pyrazine
- methylamino
- pyridyl
- Prior art date
Links
- YBYYWUUUGCNAHQ-UHFFFAOYSA-N 5-[[4-(morpholin-2-ylmethylamino)-5-(trifluoromethyl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Chemical compound C1=C(NCC2OCCNC2)C(C(F)(F)F)=CN=C1NC1=CN=C(C#N)C=N1 YBYYWUUUGCNAHQ-UHFFFAOYSA-N 0.000 title 1
- 230000001225 therapeutic effect Effects 0.000 title 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261647200P | 2012-05-15 | 2012-05-15 | |
| PCT/GB2013/051233 WO2013171470A1 (en) | 2012-05-15 | 2013-05-14 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA201408452B true ZA201408452B (en) | 2016-08-31 |
Family
ID=48468659
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA2014/08452A ZA201408452B (en) | 2012-05-15 | 2014-11-18 | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US9663503B2 (enExample) |
| EP (2) | EP3210980B1 (enExample) |
| JP (2) | JP6027230B2 (enExample) |
| KR (6) | KR102090792B1 (enExample) |
| CN (2) | CN104302635B (enExample) |
| AU (2) | AU2013261605B2 (enExample) |
| BR (1) | BR112014026801B1 (enExample) |
| CA (1) | CA2870837C (enExample) |
| DK (1) | DK2855448T3 (enExample) |
| ES (2) | ES2624307T3 (enExample) |
| IL (1) | IL235133A (enExample) |
| IN (1) | IN2014DN09221A (enExample) |
| MX (1) | MX358819B (enExample) |
| NZ (1) | NZ702050A (enExample) |
| PL (1) | PL2855448T3 (enExample) |
| RU (1) | RU2659786C2 (enExample) |
| SG (1) | SG11201407238VA (enExample) |
| WO (1) | WO2013171470A1 (enExample) |
| ZA (1) | ZA201408452B (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2776417B1 (en) | 2011-11-09 | 2018-10-31 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| CA2870837C (en) | 2012-05-15 | 2022-05-10 | Cancer Research Technology Limited | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
| PL3808749T3 (pl) | 2012-12-07 | 2023-07-10 | Vertex Pharmaceuticals Incorporated | Pirazolo[1,5-a]pirymidyny użyteczne jako inhibitory kinazy atr do leczenia chorób nowotworowych |
| JP2016512815A (ja) | 2013-03-15 | 2016-05-09 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体 |
| PL3077397T3 (pl) | 2013-12-06 | 2020-04-30 | Vertex Pharmaceuticals Inc. | Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne |
| SG10201902206QA (en) | 2014-06-05 | 2019-04-29 | Vertex Pharma | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof |
| PT3157566T (pt) * | 2014-06-17 | 2019-07-11 | Vertex Pharma | Método para tratamento de cancro utilizando uma combinação de inibidores chk1 e atr |
| RU2768621C1 (ru) | 2015-09-30 | 2022-03-24 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr |
| WO2018094325A1 (en) * | 2016-11-18 | 2018-05-24 | The Trustees Of Columbia University In The City Of New York | Therapeutic modulation of oncogenes by pharmacologic top2 targeting for cancer |
| KR20190130621A (ko) * | 2017-03-31 | 2019-11-22 | 시애틀 지네틱스, 인크. | Chk1 저해제와 wee1 저해제의 조합물 |
| US11596637B2 (en) | 2017-04-10 | 2023-03-07 | Sierra Oncology, Inc. | CHK1 (SRA737)/PARPi combination methods of inhibiting tumor growth |
| WO2018191299A1 (en) * | 2017-04-10 | 2018-10-18 | Sierra Oncology, Inc. | Chk1(sra737)wee1 inhibitor combination methods of inhibiting tumor growth |
| AU2018278336A1 (en) * | 2017-06-01 | 2020-01-16 | Crt Pioneer Fund Lp | Biomarkers and patient selection strategies |
| CN107266897B (zh) * | 2017-08-04 | 2019-05-14 | 上海跃贝新材料科技股份有限公司 | 一种低粘度矿物增强pc/pet合金材料及其制备方法 |
| CA3092079A1 (en) * | 2018-02-26 | 2019-08-29 | Sierra Oncology, Inc. | Methods of treatment of cancer comprising chk1 inhibitors |
| CN113631179A (zh) * | 2019-01-25 | 2021-11-09 | 努梅迪公司 | 用于治疗特发性肺纤维化的方法 |
| CA3135165A1 (en) * | 2019-03-28 | 2020-10-01 | Sierra Oncology, Inc. | Methods of treating cancer with chk1 inhibitors |
| CA3140123A1 (en) * | 2019-05-14 | 2020-11-19 | Sierra Oncology, Inc. | Methods of treating cancer using chk1 inhibitors |
| CN110872277B (zh) * | 2019-11-14 | 2021-06-04 | 浙江大学 | N-取代芳环-2-氨基嘧啶类化合物及用途 |
| CN110684083B (zh) * | 2019-12-06 | 2020-05-15 | 北京诺赛启研再生医学研究院有限公司 | 抑制黑色素合成的偶联物ii及其在药品和化妆品中的应用 |
| CN110680928B (zh) * | 2019-12-06 | 2020-04-28 | 深圳前海港影生物科技有限公司 | 抑制黑色素合成的偶联物及其在药品和化妆品中的应用 |
| TW202204348A (zh) * | 2020-04-07 | 2022-02-01 | 美商西爾拉癌症醫學公司 | Ｃｈｋ１抑制劑之合成方法 |
| EP4387959A4 (en) * | 2021-08-17 | 2025-07-02 | Glaxosmithkline Intellectual Property No 3 Ltd | PREPARATION OF A P2X3 ANTAGONIST |
| TW202519226A (zh) | 2023-11-08 | 2025-05-16 | 美商艾克塞里克斯公司 | 使用抑制ｐｋｍｙｔ１之化合物治療癌症之方法 |
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| US3773778A (en) | 1972-01-24 | 1973-11-20 | Squibb & Sons Inc | Sulfur derivatives of pyrazolo (3,4-b)pyridines |
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| JP2005515173A (ja) | 2001-10-31 | 2005-05-26 | バイエル・ヘルスケア・アクチェンゲゼルシャフト | ピリミド［４，５−ｂ］インドール誘導体 |
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| AU2003243318A1 (en) * | 2002-05-29 | 2003-12-19 | Millennium Pharmaceuticals, Inc. | Diarylurea compounds and derivatives as chk-1 inhibitors for the treatment of cancer |
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| ATE437872T1 (de) | 2003-10-14 | 2009-08-15 | Univ Arizona | Proteinkinaseinhibitoren |
| CA2542329A1 (en) | 2003-10-16 | 2005-04-28 | Chiron Corporation | 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines as inhibitors of raf kinase for treatment of cancer |
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| BRPI0609956A2 (pt) | 2005-04-28 | 2010-05-18 | Supergen Inc | inibidores de proteìna quinase |
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| US7776865B2 (en) | 2005-10-06 | 2010-08-17 | Schering Corporation | Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| GB0616747D0 (en) * | 2006-08-24 | 2006-10-04 | Astrazeneca Ab | Novel compounds |
| EP2125746B1 (en) | 2006-12-27 | 2012-04-18 | Sanofi | Cycloalkylamine substituted isoquinoline derivatives |
| EP2727909A1 (en) * | 2007-03-16 | 2014-05-07 | The Scripps Research Institute | Inhibitors of focal adhesion kinase |
| WO2008117050A1 (en) | 2007-03-27 | 2008-10-02 | Astrazeneca Ab | Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer |
| US8618121B2 (en) | 2007-07-02 | 2013-12-31 | Cancer Research Technology Limited | 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors |
| GB0719644D0 (en) | 2007-10-05 | 2007-11-14 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB0803018D0 (en) | 2008-02-19 | 2008-03-26 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| EP2776417B1 (en) | 2011-11-09 | 2018-10-31 | Cancer Research Technology Limited | 5-(pyridin-2-yl-amino)-pyrazine-2-carbonitrile compounds and their therapeutic use |
| CA2870837C (en) | 2012-05-15 | 2022-05-10 | Cancer Research Technology Limited | 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile and therapeutic uses thereof |
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2013
- 2013-05-14 CA CA2870837A patent/CA2870837C/en active Active
- 2013-05-14 KR KR1020147031572A patent/KR102090792B1/ko active Active
- 2013-05-14 KR KR1020207007411A patent/KR102246265B1/ko active Active
- 2013-05-14 RU RU2014147105A patent/RU2659786C2/ru active
- 2013-05-14 JP JP2015512120A patent/JP6027230B2/ja active Active
- 2013-05-14 WO PCT/GB2013/051233 patent/WO2013171470A1/en not_active Ceased
- 2013-05-14 CN CN201380025541.3A patent/CN104302635B/zh active Active
- 2013-05-14 KR KR1020227037439A patent/KR102635954B1/ko active Active
- 2013-05-14 DK DK13723910.9T patent/DK2855448T3/en active
- 2013-05-14 PL PL13723910T patent/PL2855448T3/pl unknown
- 2013-05-14 SG SG11201407238VA patent/SG11201407238VA/en unknown
- 2013-05-14 EP EP17152400.2A patent/EP3210980B1/en active Active
- 2013-05-14 ES ES13723910.9T patent/ES2624307T3/es active Active
- 2013-05-14 US US14/396,338 patent/US9663503B2/en active Active
- 2013-05-14 KR KR1020247004407A patent/KR20240023685A/ko not_active Withdrawn
- 2013-05-14 NZ NZ702050A patent/NZ702050A/en unknown
- 2013-05-14 ES ES17152400T patent/ES2981584T3/es active Active
- 2013-05-14 BR BR112014026801-0A patent/BR112014026801B1/pt active IP Right Grant
- 2013-05-14 CN CN201610652725.8A patent/CN106279142B/zh active Active
- 2013-05-14 AU AU2013261605A patent/AU2013261605B2/en active Active
- 2013-05-14 KR KR1020217012299A patent/KR102341637B1/ko active Active
- 2013-05-14 KR KR1020217041302A patent/KR20210156333A/ko not_active Ceased
- 2013-05-14 EP EP13723910.9A patent/EP2855448B1/en active Active
- 2013-05-14 IN IN9221DEN2014 patent/IN2014DN09221A/en unknown
- 2013-05-14 MX MX2014012881A patent/MX358819B/es active IP Right Grant
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2014
- 2014-10-19 IL IL235133A patent/IL235133A/en active IP Right Grant
- 2014-11-18 ZA ZA2014/08452A patent/ZA201408452B/en unknown
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2016
- 2016-10-13 JP JP2016201383A patent/JP6362652B2/ja active Active
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2017
- 2017-05-04 US US15/587,270 patent/US10259806B2/en active Active
- 2017-11-28 AU AU2017268508A patent/AU2017268508C1/en active Active
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2020
- 2020-12-17 US US17/124,606 patent/US11787792B2/en active Active
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