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PE20110924A1 - Derivados de 2, 4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3 - Google Patents

Derivados de 2, 4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3

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Publication number
PE20110924A1
PE20110924A1 PE2011001374A PE2011001374A PE20110924A1 PE 20110924 A1 PE20110924 A1 PE 20110924A1 PE 2011001374 A PE2011001374 A PE 2011001374A PE 2011001374 A PE2011001374 A PE 2011001374A PE 20110924 A1 PE20110924 A1 PE 20110924A1
Authority
PE
Peru
Prior art keywords
alkyl
pyrimidine
diamine
disustituted
derivatives
Prior art date
Application number
PE2011001374A
Other languages
English (en)
Inventor
Hui Li
Thilo J Heckrodt
Yan Chen
Darren John Mcmurtrie
Vanessa Taylor
Rajinder Singh
Pingyu Ding
Sambaiah Thota
Rose Yen
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42091548&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110924(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of PE20110924A1 publication Critical patent/PE20110924A1/es

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    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINA DE FORMULA (I) DONDE X E Y SON CADA UNO O, S, S(O), ENTRE OTROS; EL ANILLO A ES ARILO(C6-C10) O HETEROARILO DE 5 A 10 MIEMBROS; R2 ES H, Re, Rb, ENTRE OTROS, EN DONDE Re ES ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ARILO(C6-C10), ENTRE OTROS; Ra ES H, ALQUILO(C1-C6), HETEROARILO DE 5 A 15 MIEMBROS; p ES DE 0 A 4; Z1 Y Z2 SON CADA UNO CH, CR2 O N; R3 Y R4 SON CADA UNO H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO, ENTRE OTROS; R5 ES HALO, CN, ALQUILO(C1-C6), NITRO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N4-(1,3-DIMETILBENZIMIDAZOLIN-2-ON-5-IL)-N2-((4-METILSULFONILAMINO)FENIL)-5-FLUOROPIRIMIDINA-2,4-DIAMINA; 5-[2-(2,4-DIFLUORO-5-METOXI-FENILAMINO)-5-METIL-PIRIMIDIN-4-ILAMINO]-3H-BENZOXAZOL-2-ONA; 5-(2-(4-(1-(CICLOPROPILAMINO)ETIL)FENILAMINO)-5-METILPIRIMIDIN-4-ILAMINO)BENZO[d]OXAZOL-2(3H)-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE JAK QUINASAS SIENDO UTILES EN EL TRATAMIENTO DE UNA ENFERMEDAD AUTOINMUNE MEDIADA POR CELULAS T, RECHAZO AL TRANSPLANTE DE ALOINJERTO
PE2011001374A 2009-01-23 2010-01-22 Derivados de 2, 4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3 PE20110924A1 (es)

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Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CN105348203B (zh) 2005-06-08 2018-09-18 里格尔药品股份有限公司 抑制jak途径的组合物和方法
MX2011007750A (es) * 2009-01-23 2011-09-29 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la ruta jak.
AU2010266040B2 (en) * 2009-06-25 2015-01-15 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
EP3309151B1 (en) 2009-06-25 2025-03-19 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
DK2598500T3 (da) * 2010-07-28 2021-07-26 Rigel Pharmaceuticals Inc Sammensætninger og fremgangsmåder til hæmning af jak-reaktionsvejen
CA2812608C (en) 2010-10-06 2020-07-14 Glaxosmithkline Llc Benzimidazole derivatives as pi3 kinase inhibitors
EP2688890B1 (en) 2011-03-22 2017-08-30 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
US8703767B2 (en) 2011-04-01 2014-04-22 University Of Utah Research Foundation Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
EP3628665B1 (en) 2011-04-01 2022-11-02 University of Utah Research Foundation Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase
CA2832611C (en) * 2011-04-12 2019-05-14 Rigel Pharmaceuticals, Inc. Methods for inhibiting allograft rejection
EP2554544A1 (en) * 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
NZ722096A (en) 2011-12-15 2016-11-25 Alkermes Pharma Ireland Ltd Prodrugs of secondary amine compounds
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
US9540367B2 (en) 2012-08-17 2017-01-10 Concert Pharmaceuticals, Inc. Deuterated baricitinib
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
KR102194611B1 (ko) 2012-10-04 2020-12-23 유니버시티 오브 유타 리서치 파운데이션 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체
CA2887465A1 (en) 2012-10-04 2014-04-10 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
CN103788066A (zh) * 2012-10-31 2014-05-14 韩冰 一类保护移植器官的化合物及其用途
WO2014116973A1 (en) 2013-01-25 2014-07-31 Rigel Pharmaceuticals, Inc. Compounds and methods for treating inflammatory bowel diseases
KR102334260B1 (ko) 2013-03-14 2021-12-02 스미토모 다이니폰 파마 온콜로지, 인크. Ｊａｋ2 및 ａｌｋ2 억제제 및 이들의 사용 방법
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
US9549988B2 (en) 2013-06-09 2017-01-24 RJS Biologics Pharmaceutical compounds targeted by MIF affinity-tethered moieties
HUE033448T2 (en) 2013-08-07 2017-11-28 Cadila Healthcare Ltd Janus kinase inhibitor N-cyanomethylamides
CN105017159B (zh) * 2014-04-28 2019-05-17 四川大学 5-氟-2,4-二取代氨基嘧啶衍生物及其制备方法和用途
US10314942B2 (en) * 2014-06-30 2019-06-11 Bacterin International, Inc. Manufacture of biomaterial implants via three-dimensional printing technology
WO2016100452A2 (en) * 2014-12-17 2016-06-23 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2017007658A1 (en) * 2015-07-07 2017-01-12 Rigel Pharmaceuticals, Inc. A combination for immune mediated cancer treatment
LT3380465T (lt) 2015-11-26 2020-11-10 Novartis Ag Diamino piridino dariniai
KR20230156174A (ko) 2016-07-12 2023-11-13 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
US20200039998A1 (en) * 2016-12-19 2020-02-06 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
CN110431134A (zh) 2017-01-23 2019-11-08 锐新医药公司 作为变构shp2抑制剂的吡啶化合物
CN118021814A (zh) 2017-04-21 2024-05-14 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
KR102628675B1 (ko) * 2017-05-26 2024-01-25 캔써 리서치 테크놀로지 리미티드 벤즈이미다졸론 유래된 bcl6의 저해제
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構ｓｈｐ２抑制劑的吡啶、吡嗪和三嗪化合物
WO2019099311A1 (en) * 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
WO2019173230A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
AU2019247498A1 (en) 2018-04-05 2020-11-26 Sumitomo Pharma Oncology, Inc. AXL kinase inhibitors and use of the same
JP2021524458A (ja) 2018-05-24 2021-09-13 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ ５−（（５−メチル−２−（（３，４，５−トリメチルフェニル）アミノ）ピリミジン−４−イル）アミノ）−ベンゾ［ｄ］オキサゾール−２（３Ｈ）−オンのフマル酸塩
AU2019310590A1 (en) 2018-07-26 2021-01-14 Sumitomo Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
WO2021026451A1 (en) 2019-08-08 2021-02-11 Rigel Pharmaceuticals, Inc. Compounds and method for treating cytokine release syndrome
TW202207934A (zh) 2020-03-27 2022-03-01 瑞典商阿斯特捷利康公司 用於肺遞送的乾粉配製物及使用方法
CN113549018B (zh) * 2020-04-24 2024-02-27 中国药科大学 蛋白激酶抑制剂及其衍生物，制备方法、药物组合物和应用
WO2021239133A1 (zh) * 2020-05-29 2021-12-02 南京正大天晴制药有限公司 作为axl抑制剂的嘧啶类化合物
WO2022188735A1 (en) * 2021-03-08 2022-09-15 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as hpk1 inhibitors
CN116178434A (zh) * 2021-11-26 2023-05-30 南京正大天晴制药有限公司 Axl激酶抑制剂的单对甲苯磺酸盐及其晶型
CN116178433A (zh) * 2021-11-26 2023-05-30 南京正大天晴制药有限公司 Axl激酶抑制剂的盐及其制备方法和用途

Family Cites Families (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4166452A (en) 1976-05-03 1979-09-04 Generales Constantine D J Jr Apparatus for testing human responses to stimuli
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US4738851A (en) 1985-09-27 1988-04-19 University Of Iowa Research Foundation, Inc. Controlled release ophthalmic gel formulation
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US4882150A (en) 1988-06-03 1989-11-21 Kaufman Herbert E Drug delivery system
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
CA2058764A1 (en) 1989-04-28 1990-10-29 Peter D. Hodson Dry powder inhalation device
US5521222A (en) 1989-09-28 1996-05-28 Alcon Laboratories, Inc. Topical ophthalmic pharmaceutical vehicles
DE69009946T2 (de) 1989-12-04 1994-11-03 Searle & Co System zur transdermalen Albuterol Applikation.
US5364833A (en) 1990-05-09 1994-11-15 Basf Aktiengesellschaft Cyclohexenone oxime ethers, their preparation and their use as herbicides
US5077033A (en) 1990-08-07 1991-12-31 Mediventures Inc. Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
US5404871A (en) 1991-03-05 1995-04-11 Aradigm Delivery of aerosol medications for inspiration
US5327883A (en) 1991-05-20 1994-07-12 Dura Pharmaceuticals, Inc. Apparatus for aerosolizing powdered medicine and process and using
US6060069A (en) 1991-05-20 2000-05-09 Dura Pharmaceuticals, Inc. Pulmonary delivery of pharmaceuticals
US5492112A (en) 1991-05-20 1996-02-20 Dura Pharmaceuticals, Inc. Dry powder inhaler
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
IL104068A (en) 1991-12-12 1998-10-30 Glaxo Group Ltd Pharmaceutical preparations in a spray without surfactant containing 1, 1, 1, 2 tetrafluoroethane or 1,1,2,3,3 petafluor N propane as propellant
DE69228827T2 (de) 1991-12-18 1999-10-21 Minnesota Mining And Mfg. Co., Saint Paul Mehrschichtige sperrstrukturen
US5320094A (en) 1992-01-10 1994-06-14 The Johns Hopkins University Method of administering insulin
ATE132381T1 (de) 1992-01-29 1996-01-15 Voelkl Franz Ski Ballspielschläger, insbesondere tennisschläger
US5277195A (en) 1992-02-03 1994-01-11 Dura Pharmaceuticals, Inc. Portable spirometer
US6582728B1 (en) 1992-07-08 2003-06-24 Inhale Therapeutic Systems, Inc. Spray drying of macromolecules to produce inhaleable dry powders
KR0177265B1 (ko) 1992-10-19 1999-04-01 미첼 알. 우드베리 건분말 흡입기
US5558085A (en) 1993-01-29 1996-09-24 Aradigm Corporation Intrapulmonary delivery of peptide drugs
US6131567A (en) 1993-01-29 2000-10-17 Aradigm Corporation Method of use of monomeric insulin as a means for improving the reproducibility of inhaled insulin
ES2154673T3 (es) 1993-01-29 2001-04-16 Aradigm Corp Suministro intrapulmonar de hormonas.
US5672581A (en) 1993-01-29 1997-09-30 Aradigm Corporation Method of administration of insulin
US5364838A (en) 1993-01-29 1994-11-15 Miris Medical Corporation Method of administration of insulin
US5743250A (en) 1993-01-29 1998-04-28 Aradigm Corporation Insulin delivery enhanced by coached breathing
TW402506B (en) 1993-06-24 2000-08-21 Astra Ab Therapeutic preparation for inhalation
US5661130A (en) 1993-06-24 1997-08-26 The Uab Research Foundation Absorption enhancers for drug administration
US5506203C1 (en) 1993-06-24 2001-02-06 Astra Ab Systemic administration of a therapeutic preparation
WO1995024183A1 (en) 1994-03-07 1995-09-14 Inhale Therapeutic Systems Methods and compositions for pulmonary delivery of insulin
IL114193A (en) 1994-06-20 2000-02-29 Teva Pharma Ophthalmic pharmaceutical compositions based on sodium alginate
ES2094688B1 (es) 1994-08-08 1997-08-01 Cusi Lab Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion.
US5780014A (en) 1995-04-14 1998-07-14 Inhale Therapeutic Systems Method and apparatus for pulmonary administration of dry powder alpha 1-antitrypsin
US5645051A (en) 1995-04-21 1997-07-08 Dura Pharmaceuticals, Inc. Unit dose dry powder inhaler
US5622166A (en) 1995-04-24 1997-04-22 Dura Pharmaceuticals, Inc. Dry powder inhaler delivery system
US5700904A (en) 1995-06-07 1997-12-23 Eli Lilly And Company Preparation of an acylated protein powder
US5654007A (en) 1995-06-07 1997-08-05 Inhale Therapeutic Systems Methods and system for processing dispersible fine powders
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
IT1283911B1 (it) 1996-02-05 1998-05-07 Farmigea Spa Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo
US5800807A (en) 1997-01-29 1998-09-01 Bausch & Lomb Incorporated Ophthalmic compositions including glycerin and propylene glycol
ZA989744B (en) 1997-10-31 2000-04-26 Lilly Co Eli Method for administering acylated insulin.
KR20010033811A (ko) 1997-12-31 2001-04-25 토마스 안 빅토리아 2차 및 3차 아민을 함유하는 약제의 물에 용해가능한프로드럭 및 그것의 제조방법
US6261547B1 (en) 1998-04-07 2001-07-17 Alcon Manufacturing, Ltd. Gelling ophthalmic compositions containing xanthan gum
US6197934B1 (en) 1998-05-22 2001-03-06 Collagenesis, Inc. Compound delivery using rapidly dissolving collagen film
US6241969B1 (en) 1998-06-26 2001-06-05 Elan Corporation Plc Aqueous compositions containing corticosteroids for nasal and pulmonary delivery
US20020006901A1 (en) 1999-02-05 2002-01-17 Aldo T. Iacono Use of aerosolized cyclosporine for prevention and treatment of pulmonary disease
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
US7678364B2 (en) 1999-08-25 2010-03-16 Alkermes, Inc. Particles for inhalation having sustained release properties
AU2001226029A1 (en) 2000-01-10 2001-07-24 Dura Pharmaceuticals, Inc. Pharmaceutical formulation and method for pulmonary and oral delivery
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
JP2006514989A (ja) 2002-07-29 2006-05-18 ライジェル ファーマシューティカルズ ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
DK2287156T3 (da) 2003-08-15 2013-08-26 Novartis Ag 2,4-Di(phenylamino)-pyrimidiner egnede i behandling af neoplastiske sygdomme, inflammatoriske lidelser og lidelser i immunsystemet
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
SI1856135T1 (sl) 2005-01-19 2010-04-30 Rigel Pharmaceuticals Inc Predzdravila 2,4-pirimidindiaminskih spojin in njihove uporabe
CN105348203B (zh) 2005-06-08 2018-09-18 里格尔药品股份有限公司 抑制jak途径的组合物和方法
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
KR20090031787A (ko) * 2006-07-21 2009-03-27 노파르티스 아게 Ｊａｋ 키나제 억제제로서의 ２,４-디(아릴아미노)-피리미딘-５-카르복스아미드 화합물
GB0615619D0 (en) * 2006-08-05 2006-09-13 Astrazeneca Ab Chemical process for preparation of intermediates
DE602007012363D1 (de) * 2006-10-19 2011-03-17 Rigel Pharmaceuticals Inc 2,4-pyridimediamon-derivate als hemmer von jak-kinasen zur behandlung von autoimmunerkrankungen
WO2008118822A1 (en) * 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2009063240A1 (en) * 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
MX2011007750A (es) * 2009-01-23 2011-09-29 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la ruta jak.
TW201107329A (en) * 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
DK2598500T3 (da) * 2010-07-28 2021-07-26 Rigel Pharmaceuticals Inc Sammensætninger og fremgangsmåder til hæmning af jak-reaktionsvejen

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