MX2017007748A - Compuestos de heteroarilo anulares fusionados y su uso como inhibidores del receptor de la tirocina cinasa (trk). - Google Patents
Compuestos de heteroarilo anulares fusionados y su uso como inhibidores del receptor de la tirocina cinasa (trk).Info
- Publication number
- MX2017007748A MX2017007748A MX2017007748A MX2017007748A MX2017007748A MX 2017007748 A MX2017007748 A MX 2017007748A MX 2017007748 A MX2017007748 A MX 2017007748A MX 2017007748 A MX2017007748 A MX 2017007748A MX 2017007748 A MX2017007748 A MX 2017007748A
- Authority
- MX
- Mexico
- Prior art keywords
- fused ring
- nr4r5
- ring heteroaryl
- heteroaryl compounds
- trk inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 208000035473 Communicable disease Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- -1 polymorph Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La descripción proporciona compuestos químicos novedosos representados por la Fórmula I o una sal, solvato, polimorfo, éster, tautómero o profármaco farmacéuticamente aceptable de los mismos. Los compuestos pueden utilizarse como un inhibidor del Trk y son útiles en el tratamiento del dolor, cáncer, inflamación, enfermedad neurodegenerativa y ciertas enfermedades infecciosas. (ver Fórmula). En algunos compuestos de la Fórmula I, Q es -CH=CR3C (O) NR4R5, -C?CC (O) NR4R5, o (ver Fórmula).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462092193P | 2014-12-15 | 2014-12-15 | |
| PCT/IB2015/002521 WO2016097869A1 (en) | 2014-12-15 | 2015-12-14 | Fused ring heteroaryl compounds and their use as trk inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017007748A true MX2017007748A (es) | 2018-01-30 |
| MX383885B MX383885B (es) | 2025-03-14 |
Family
ID=56110505
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017007748A MX383885B (es) | 2014-12-15 | 2015-12-14 | Compuestos de heteroarilo anulares fusionados y su uso como inhibidores del receptor de la tirosina cinasa (trk). |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US9701681B2 (es) |
| EP (2) | EP3233863B1 (es) |
| JP (1) | JP6609631B2 (es) |
| KR (2) | KR102659741B1 (es) |
| CN (1) | CN107207514B (es) |
| AU (1) | AU2015365587B2 (es) |
| BR (1) | BR112017012755B1 (es) |
| CA (1) | CA2971024C (es) |
| DK (1) | DK3233863T3 (es) |
| ES (1) | ES2983908T3 (es) |
| FI (1) | FI3233863T3 (es) |
| HR (1) | HRP20240937T1 (es) |
| HU (1) | HUE067779T2 (es) |
| MX (1) | MX383885B (es) |
| PL (1) | PL3233863T3 (es) |
| RU (1) | RU2708674C2 (es) |
| WO (1) | WO2016097869A1 (es) |
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| DK2350075T3 (da) | 2008-09-22 | 2014-05-26 | Array Biopharma Inc | Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer |
| PT3106463T (pt) | 2008-10-22 | 2018-05-18 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| RU2735545C2 (ru) | 2010-05-20 | 2020-11-03 | Эррэй Биофарма Инк. | Макроциклические соединения в качестве ингибиторов киназы trk |
| HRP20191283T1 (hr) | 2014-01-24 | 2019-10-18 | Turning Point Therapeutics, Inc. | Diaril makrocikli kao modulatori protein kinaze |
| EP3218380B1 (en) | 2014-11-16 | 2021-03-17 | Array Biopharma, Inc. | Preparation of a crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| EP4397665A3 (en) | 2015-07-06 | 2024-08-21 | Turning Point Therapeutics, Inc. | Diaryl macrocycle polymorph |
| BR112018003588A2 (pt) | 2015-08-26 | 2018-09-25 | Blueprint Medicines Corp | compostos e composições úteis para tratamento de distúrbios relacionados ao ntrk |
| TN2019000271A1 (en) | 2015-10-26 | 2021-01-07 | Univ Colorado Regents | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| RU2018122089A (ru) | 2015-11-19 | 2019-12-25 | Блюпринт Медсинс Корпорейшн | Соединения и композиции, подходящие для лечения расстройств, связанных с ntrk |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| IL304018A (en) | 2016-04-04 | 2023-08-01 | Loxo Oncology Inc | Liquid formulations of (S)-N-(5-((R)-2-(5,2-difluorophenyl)-pyrrolidine-1-yl)-pyrazolo[5,1-A]pyrimidin-3-yl)-3 -hydroxypyrrolidine-1-carboxamide |
| ES2952056T3 (es) | 2016-05-18 | 2023-10-26 | Loxo Oncology Inc | Preparación de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida |
| JOP20190092A1 (ar) * | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| JP7046940B2 (ja) * | 2016-10-28 | 2022-04-04 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | 神経栄養因子チロシンキナーゼ受容体阻害剤として用いられるアミノピラゾロピリミジン化合物 |
| WO2018152134A1 (en) * | 2017-02-14 | 2018-08-23 | Research Triangle Institute | Proline-based neuropeptide ff receptor modulators |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| US10738033B2 (en) | 2017-05-31 | 2020-08-11 | Nantbio, Inc. | Trk inhibition |
| US10800760B2 (en) | 2017-05-31 | 2020-10-13 | Nantbio, Inc. | Trk inhibition |
| US20190247398A1 (en) | 2017-10-26 | 2019-08-15 | Array Biopharma Inc. | Formulations of a macrocyclic trk kinase inhibitor |
| PL3724191T3 (pl) * | 2017-12-15 | 2022-04-25 | Pyramid Biosciences, Inc. | Pochodne 5-(2-(2,5-difluorofenylo)pirolidyn-1-ylo)-3-(1h-pirazol-1-ilo)pirazolo[1,5-a]pirymidyny i pokrewne związki jako inhibitory kinaz trk do leczenia nowotworu |
| CN108218754B (zh) * | 2018-01-23 | 2021-05-07 | 广东赛烽医药科技有限公司 | 一种2-(2,5-二氟苯基)吡咯烷的制备方法 |
| US11464780B2 (en) | 2018-02-28 | 2022-10-11 | Simcere Pharmaceutical Co. Ltd. | Pyrazolopyrimidine derivative and use thereof |
| JP7294677B2 (ja) | 2018-03-14 | 2023-06-20 | フォチョン・ファーマシューティカルズ・リミテッド | TRKキナーゼ阻害剤としての置換(2-アザビシクロ[3.1.0]ヘキサン-2-イル)ピラゾロ[1,5-a]ピリミジン化合物及び置換(2-アザビシクロ[3.1.0]ヘキサン-2-イル)イミダゾ[1,2-b]ピリダジン化合物 |
| US20210023086A1 (en) | 2018-03-29 | 2021-01-28 | Loxo Oncology, Inc. | Treatment of trk-associated cancers |
| CN108484361B (zh) * | 2018-05-11 | 2022-09-30 | 弈柯莱生物科技(上海)股份有限公司 | (s)-4-氯-1-(2,5)-二氟苯基丁-1-醇及其制备方法和应用 |
| CN110294761B (zh) * | 2018-06-08 | 2020-09-08 | 南京雷正医药科技有限公司 | 作为Trk激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物 |
| CN110577532B (zh) * | 2018-06-08 | 2022-06-03 | 江苏威凯尔医药科技有限公司 | 原肌球蛋白受体激酶抑制剂及其制备方法和应用 |
| WO2019233461A1 (zh) * | 2018-06-08 | 2019-12-12 | 江苏威凯尔医药科技有限公司 | 原肌球蛋白受体激酶抑制剂及其制备方法和应用 |
| GB201811825D0 (en) | 2018-07-19 | 2018-09-05 | Benevolentai Bio Ltd | Organic compounds |
| CN108794370A (zh) * | 2018-07-31 | 2018-11-13 | 上海弈柯莱生物医药科技有限公司 | 一种拉罗替尼中间体的制备方法 |
| CN110857304B (zh) * | 2018-08-24 | 2021-05-18 | 北京富龙康泰生物技术有限公司 | Trk抑制剂、其制备方法和用途 |
| CN109053525B (zh) * | 2018-09-25 | 2020-05-05 | 成都福柯斯医药技术有限公司 | 一种(r)-2-(2-取代-5-氟苯)吡咯烷的制备方法 |
| US11414431B2 (en) * | 2018-10-15 | 2022-08-16 | Nimbus Lakshmi, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors |
| CN111138333B (zh) * | 2018-11-02 | 2023-05-23 | 上海复星星泰医药科技有限公司 | 一种(r)-2-(2,5-二氟苯基)-吡咯烷的制备方法 |
| PH12021551304A1 (en) * | 2018-12-07 | 2022-05-16 | Betta Pharmaceuticals Co Ltd | Tyrosine kinase inhibitors, compositions and methods there of |
| CN111302995A (zh) * | 2018-12-12 | 2020-06-19 | 上海复星星泰医药科技有限公司 | 一种2-(2,5-二氟苯基)-吡咯烷消旋体的制备方法 |
| CN109593803A (zh) * | 2018-12-24 | 2019-04-09 | 上海健康医学院 | (r)-2-(2,5-二氟苯基)吡咯烷或其盐的制备方法 |
| CN111362946A (zh) * | 2018-12-25 | 2020-07-03 | 上海度德医药科技有限公司 | 一种药物化合物及其组合物和应用 |
| WO2020187291A1 (zh) * | 2019-03-19 | 2020-09-24 | 华中师范大学 | 吡唑并嘧啶化合物和药物组合物及其应用 |
| WO2020224626A1 (zh) * | 2019-05-08 | 2020-11-12 | 浙江同源康医药股份有限公司 | 用作激酶抑制剂的化合物及其应用 |
| CN114258394B (zh) * | 2019-08-28 | 2024-04-23 | 南京再明医药有限公司 | 一种致癌性融合激酶抑制剂的晶型及其应用 |
| CN114641478B (zh) * | 2019-10-30 | 2024-07-02 | 南京再明医药有限公司 | 吡唑并嘧啶类化合物的制备方法及其中间体 |
| CN112979654B (zh) * | 2019-12-16 | 2024-03-19 | 赛诺哈勃药业(成都)有限公司 | 杂芳基稠环化合物、其制备方法及应用 |
| WO2021148807A1 (en) | 2020-01-22 | 2021-07-29 | Benevolentai Bio Limited | Pharmaceutical compositions and their uses |
| CN111302997B (zh) * | 2020-04-15 | 2022-03-29 | 江苏恒沛药物科技有限公司 | “一锅法”制备拉罗替尼中间体的方法 |
| WO2021211882A1 (en) * | 2020-04-15 | 2021-10-21 | Pyramid Biosciences, Inc. | Methods for preparing tyrosine receptor kinase inhibitors |
| CN111393347B (zh) * | 2020-04-30 | 2020-11-17 | 安徽德信佳生物医药有限公司 | 一种拉洛替尼中间体的合成方法 |
| CN115551863A (zh) * | 2020-06-11 | 2022-12-30 | 贝达药业股份有限公司 | 酪氨酸激酶抑制剂的盐型、晶型、药物组合物及其用途 |
| CN114437075B (zh) * | 2020-11-03 | 2026-01-30 | 上海瑶琪生物科技有限公司 | 用作ntrk激酶抑制剂的化合物及其应用 |
| KR102541026B1 (ko) | 2020-11-11 | 2023-06-12 | 주식회사 한독 | Trk 억제제 화합물의 제조 방법 |
| CN116102464B (zh) * | 2021-11-10 | 2024-11-05 | 凯特立斯(深圳)科技有限公司 | 一种不对称氢化制备氨基醇的方法及其应用 |
| WO2025107298A1 (zh) * | 2023-11-24 | 2025-05-30 | 浙江同源康医药股份有限公司 | 晶体、药物组合物及其制备方法和应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA019507B1 (ru) | 2008-05-13 | 2014-04-30 | Айрм Ллк | Конденсированные азотсодержащие гетероциклы и содержащие их композиции в качестве ингибиторов киназы |
| PT3106463T (pt) | 2008-10-22 | 2018-05-18 | Array Biopharma Inc | Compostos de pirazolo[1,5-]pirimidina substituídos como inibidores de cinase trk |
| RU2539568C2 (ru) | 2008-10-31 | 2015-01-20 | Дженентек, Инк. | Пиразолопиримидиновые соединения-ингибиторы jak и способы |
| AR077468A1 (es) * | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| WO2011029027A1 (en) | 2009-09-03 | 2011-03-10 | Array Biopharma Inc. | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS |
| RU2735545C2 (ru) * | 2010-05-20 | 2020-11-03 | Эррэй Биофарма Инк. | Макроциклические соединения в качестве ингибиторов киназы trk |
| WO2012034095A1 (en) * | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| CN104302649B (zh) * | 2012-03-09 | 2017-06-23 | 莱西肯医药有限公司 | 基于吡唑并[1,5‑a]嘧啶的化合物、包含它们的组合物及其使用方法 |
-
2015
- 2015-12-14 CN CN201580075880.1A patent/CN107207514B/zh active Active
- 2015-12-14 BR BR112017012755-5A patent/BR112017012755B1/pt active IP Right Grant
- 2015-12-14 DK DK15869420.8T patent/DK3233863T3/da active
- 2015-12-14 AU AU2015365587A patent/AU2015365587B2/en active Active
- 2015-12-14 KR KR1020177018519A patent/KR102659741B1/ko active Active
- 2015-12-14 EP EP15869420.8A patent/EP3233863B1/en active Active
- 2015-12-14 JP JP2017533343A patent/JP6609631B2/ja active Active
- 2015-12-14 ES ES15869420T patent/ES2983908T3/es active Active
- 2015-12-14 MX MX2017007748A patent/MX383885B/es unknown
- 2015-12-14 RU RU2017125025A patent/RU2708674C2/ru active
- 2015-12-14 EP EP24169331.6A patent/EP4420732A3/en active Pending
- 2015-12-14 WO PCT/IB2015/002521 patent/WO2016097869A1/en not_active Ceased
- 2015-12-14 FI FIEP15869420.8T patent/FI3233863T3/fi active
- 2015-12-14 CA CA2971024A patent/CA2971024C/en active Active
- 2015-12-14 US US14/968,208 patent/US9701681B2/en active Active
- 2015-12-14 PL PL15869420.8T patent/PL3233863T3/pl unknown
- 2015-12-14 KR KR1020247012821A patent/KR20240055170A/ko active Pending
- 2015-12-14 HR HRP20240937TT patent/HRP20240937T1/hr unknown
- 2015-12-14 HU HUE15869420A patent/HUE067779T2/hu unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2017538766A (ja) | 2017-12-28 |
| AU2015365587B2 (en) | 2020-07-23 |
| BR112017012755B1 (pt) | 2023-11-14 |
| BR112017012755A2 (pt) | 2017-12-26 |
| ES2983908T3 (es) | 2024-10-28 |
| CA2971024A1 (en) | 2016-06-23 |
| RU2017125025A (ru) | 2019-01-17 |
| WO2016097869A4 (en) | 2016-08-04 |
| US20160168156A1 (en) | 2016-06-16 |
| CN107207514B (zh) | 2020-01-24 |
| EP4420732A2 (en) | 2024-08-28 |
| EP4420732A3 (en) | 2024-11-27 |
| CA2971024C (en) | 2023-09-26 |
| KR20170095919A (ko) | 2017-08-23 |
| EP3233863B1 (en) | 2024-04-10 |
| WO2016097869A1 (en) | 2016-06-23 |
| DK3233863T3 (da) | 2024-07-15 |
| CN107207514A (zh) | 2017-09-26 |
| AU2015365587A1 (en) | 2017-08-03 |
| RU2708674C2 (ru) | 2019-12-11 |
| HUE067779T2 (hu) | 2024-11-28 |
| PL3233863T3 (pl) | 2024-11-12 |
| FI3233863T3 (fi) | 2024-07-10 |
| KR20240055170A (ko) | 2024-04-26 |
| RU2017125025A3 (es) | 2019-06-21 |
| EP3233863A4 (en) | 2018-06-06 |
| EP3233863A1 (en) | 2017-10-25 |
| HRP20240937T1 (hr) | 2024-10-25 |
| US9701681B2 (en) | 2017-07-11 |
| KR102659741B1 (ko) | 2024-04-23 |
| MX383885B (es) | 2025-03-14 |
| JP6609631B2 (ja) | 2019-11-20 |
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