JP2019527230A - 大環状キナーゼ阻害剤 - Google Patents
大環状キナーゼ阻害剤 Download PDFInfo
- Publication number
- JP2019527230A JP2019527230A JP2019504675A JP2019504675A JP2019527230A JP 2019527230 A JP2019527230 A JP 2019527230A JP 2019504675 A JP2019504675 A JP 2019504675A JP 2019504675 A JP2019504675 A JP 2019504675A JP 2019527230 A JP2019527230 A JP 2019527230A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- nhc
- nhs
- aryl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- QOLDCHQHOOFRGQ-UHFFFAOYSA-N CC(C)c1n[n](C)cc1 Chemical compound CC(C)c1n[n](C)cc1 QOLDCHQHOOFRGQ-UHFFFAOYSA-N 0.000 description 1
- UQFQONCQIQEYPJ-UHFFFAOYSA-N C[n]1nccc1 Chemical compound C[n]1nccc1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 description 1
- NODLZCJDRXTSJO-UHFFFAOYSA-N Cc1n[n](C)cc1 Chemical compound Cc1n[n](C)cc1 NODLZCJDRXTSJO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- A61P37/02—Immunomodulators
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662367886P | 2016-07-28 | 2016-07-28 | |
| US62/367,886 | 2016-07-28 | ||
| PCT/US2017/044214 WO2018022911A1 (en) | 2016-07-28 | 2017-07-27 | Macrocycle kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019527230A true JP2019527230A (ja) | 2019-09-26 |
| JP2019527230A5 JP2019527230A5 (OSRAM) | 2020-09-03 |
Family
ID=61016718
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019504675A Pending JP2019527230A (ja) | 2016-07-28 | 2017-07-27 | 大環状キナーゼ阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10689400B2 (OSRAM) |
| EP (1) | EP3490564A4 (OSRAM) |
| JP (1) | JP2019527230A (OSRAM) |
| KR (1) | KR20190034225A (OSRAM) |
| CN (1) | CN109715165A (OSRAM) |
| AU (1) | AU2017302019A1 (OSRAM) |
| BR (1) | BR112019001607A2 (OSRAM) |
| CA (1) | CA3031100A1 (OSRAM) |
| IL (1) | IL264395A (OSRAM) |
| MX (1) | MX2019001125A (OSRAM) |
| RU (1) | RU2019105587A (OSRAM) |
| SG (1) | SG11201900163PA (OSRAM) |
| TW (1) | TW201815799A (OSRAM) |
| WO (1) | WO2018022911A1 (OSRAM) |
| ZA (1) | ZA201901034B (OSRAM) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3636649T (lt) | 2014-01-24 | 2024-04-10 | Turning Point Therapeutics, Inc. | Diarilo makrociklai kaip proteinkinazių moduliatoriai |
| US10316044B2 (en) | 2015-07-02 | 2019-06-11 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| ES2818528T3 (es) | 2015-07-21 | 2021-04-13 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral y uso del mismo en el tratamiento del cáncer |
| EP3490564A4 (en) | 2016-07-28 | 2020-02-26 | Turning Point Therapeutics, Inc. | MACRO CYCLE Kinase Inhibitors |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| EP3658148B1 (en) | 2017-07-28 | 2024-07-10 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
| CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
| MX2020006490A (es) | 2017-12-19 | 2020-08-17 | Turning Point Therapeutics Inc | Compuestos macrociclicos para tratar enfermedades. |
| CN111971287B (zh) | 2018-03-28 | 2023-06-02 | 重庆复尚源创医药技术有限公司 | 作为trk激酶抑制剂的大环化合物 |
| PL3786167T3 (pl) | 2018-04-25 | 2024-11-25 | Primegene (Beijing) Co., Ltd. | Diarylowy związek makrocykliczny i kompozycja farmaceutyczna oraz ich zastosowanie |
| CA3224945C (en) | 2018-07-31 | 2025-11-18 | Loxo Oncology, Inc. | SPRAY DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPAN-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE |
| FI3870579T3 (fi) | 2018-10-22 | 2025-01-02 | Alumis Inc | Tyk2-inhibiittoreita ja niiden käyttöjä |
| BR112021019070A2 (pt) * | 2019-03-26 | 2022-02-15 | Ventyx Biosciences Inc | Ligantes de pseudoquinase tyk2 |
| US12410191B2 (en) | 2019-05-21 | 2025-09-09 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Macrolide derivatives, preparation method and application thereof |
| CN112110938B (zh) * | 2019-06-21 | 2021-11-09 | 成都海博为药业有限公司 | 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途 |
| WO2021027503A1 (zh) * | 2019-08-12 | 2021-02-18 | 罗欣药业(上海)有限公司 | 三环类化合物、其制备方法、中间体及应用 |
| KR20220088699A (ko) | 2019-09-27 | 2022-06-28 | 디스크 메디슨, 인크. | 골수섬유증 및 관련 상태의 치료 방법 |
| EP4114530A4 (en) * | 2020-03-02 | 2024-04-17 | Turning Point Therapeutics, Inc. | Therapeutic uses of macrocyclic compounds |
| JP2023528223A (ja) | 2020-05-13 | 2023-07-04 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症を処置するための抗ヘモジュベリン(hjv)抗体 |
| WO2021244609A1 (zh) * | 2020-06-04 | 2021-12-09 | 成都倍特药业股份有限公司 | 具有大环结构的化合物及其用途 |
| CN116829562B (zh) * | 2021-02-10 | 2025-04-01 | 深圳国顺康医药科技有限公司 | 一种巨环化合物、药物组合物以及其用途 |
| CN113354548A (zh) * | 2021-04-12 | 2021-09-07 | 常熟耐素生物材料科技有限公司 | 一种基于六亚甲基四胺的植物多烯酚醛胺环氧固化剂及其制备方法 |
| WO2023078267A1 (zh) * | 2021-11-02 | 2023-05-11 | 赛诺哈勃药业(成都)有限公司 | 作为蛋白激酶调节剂的含氨基大环化合物 |
| WO2023208244A1 (zh) * | 2022-04-29 | 2023-11-02 | 南京明德新药研发有限公司 | 大环类化合物及其应用 |
| WO2025010294A2 (en) * | 2023-07-03 | 2025-01-09 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds and use as tyk2 inhibitors |
Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010503690A (ja) * | 2006-09-18 | 2010-02-04 | ポラリス・グループ | タンパク質キナーゼ阻害剤として有用なピラゾロ(1,5−a)(1,3,5)トリアジン及びピラゾロ(1,5−a)ピリミジン誘導体 |
| JP2013530142A (ja) * | 2010-05-20 | 2013-07-25 | アレイ バイオファーマ、インコーポレイテッド | Trkキナーゼ阻害剤としてのマクロ環化合物 |
| JP2014515346A (ja) * | 2011-05-19 | 2014-06-30 | セントロ ナシオナル デ インベスティガシオネス オンコロヒカス(セエネイオ) | タンパク質キナーゼ阻害剤としての大環状化合物 |
| JP2014528405A (ja) * | 2011-09-30 | 2014-10-27 | イプセン ファルマ ソシエテ パール アクシオン サンプリフィエIpsen Pharma S.A.S. | マクロ環状lrrk2キナーゼ阻害剤 |
| WO2015050989A2 (en) * | 2013-10-01 | 2015-04-09 | Cs Therapeutics Inc. | Macrocyclic compounds for the treatment of proliferative diseases |
| WO2015112806A2 (en) * | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| JP2016510796A (ja) * | 2013-03-15 | 2016-04-11 | オンコデザイン エス.ア. | 大環状rip2キナーゼ阻害剤 |
| JP6871903B2 (ja) * | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE195935T1 (de) | 1993-03-25 | 2000-09-15 | Upjohn Co | Formyl- oder cyano- substituierte indolderivate mit dopaminergischer wirkung |
| GB9800569D0 (en) | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| CN102143750B (zh) * | 2008-09-08 | 2014-04-02 | 默克专利有限公司 | 用作蛋白激酶抑制剂的大环嘧啶 |
| US8450322B2 (en) | 2008-09-22 | 2013-05-28 | Array Biopharma Inc. | Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors |
| TR201807039T4 (tr) | 2008-10-22 | 2018-06-21 | Array Biopharma Inc | Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri. |
| JP5769199B2 (ja) | 2008-10-31 | 2015-08-26 | ジェネンテック, インコーポレイテッド | ピラゾロピリミジンjak阻害剤化合物と方法 |
| US8757434B2 (en) * | 2010-07-01 | 2014-06-24 | The Coca-Cola Company | Merchandiser |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| EP2508607A1 (en) | 2011-04-07 | 2012-10-10 | Helmholtz-Zentrum für Infektionsforschung GmbH | Medicament for liver regeneration and for treatment of liver failure |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| KR20140053330A (ko) | 2011-08-19 | 2014-05-07 | 머크 샤프 앤드 돔 코포레이션 | 마크로락탐의 제조를 위한 방법 및 중간체 |
| JP6046728B2 (ja) | 2011-09-30 | 2016-12-21 | オンコデザイン エス.ア. | 大環状flt3キナーゼ阻害剤 |
| PT2822953T (pt) | 2012-03-06 | 2017-04-06 | Pfizer | Derivados macrocíclicos para o tratamento de doenças proliferativas |
| CA2866164C (en) | 2012-03-09 | 2020-07-07 | Lexicon Pharmaceuticals, Inc. | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
| IN2014DN07384A (OSRAM) | 2012-03-09 | 2015-04-24 | Lexicon Pharmaceuticals Inc | |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| SMT202400213T1 (it) | 2015-07-06 | 2024-07-09 | Turning Point Therapeutics Inc | Polimorfo di diaril macrociclo |
| ES2818528T3 (es) | 2015-07-21 | 2021-04-13 | Turning Point Therapeutics Inc | Macrociclo de diarilo quiral y uso del mismo en el tratamiento del cáncer |
| EP3490564A4 (en) | 2016-07-28 | 2020-02-26 | Turning Point Therapeutics, Inc. | MACRO CYCLE Kinase Inhibitors |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| EP3658148B1 (en) | 2017-07-28 | 2024-07-10 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
-
2017
- 2017-07-27 EP EP17835284.5A patent/EP3490564A4/en not_active Withdrawn
- 2017-07-27 SG SG11201900163PA patent/SG11201900163PA/en unknown
- 2017-07-27 AU AU2017302019A patent/AU2017302019A1/en not_active Abandoned
- 2017-07-27 MX MX2019001125A patent/MX2019001125A/es unknown
- 2017-07-27 WO PCT/US2017/044214 patent/WO2018022911A1/en not_active Ceased
- 2017-07-27 KR KR1020197003927A patent/KR20190034225A/ko not_active Ceased
- 2017-07-27 BR BR112019001607-4A patent/BR112019001607A2/pt not_active Application Discontinuation
- 2017-07-27 CA CA3031100A patent/CA3031100A1/en active Pending
- 2017-07-27 JP JP2019504675A patent/JP2019527230A/ja active Pending
- 2017-07-27 TW TW106125249A patent/TW201815799A/zh unknown
- 2017-07-27 US US16/320,589 patent/US10689400B2/en active Active
- 2017-07-27 RU RU2019105587A patent/RU2019105587A/ru not_active Application Discontinuation
- 2017-07-27 CN CN201780056515.5A patent/CN109715165A/zh active Pending
-
2019
- 2019-01-22 IL IL264395A patent/IL264395A/en unknown
- 2019-02-18 ZA ZA2019/01034A patent/ZA201901034B/en unknown
Patent Citations (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010503690A (ja) * | 2006-09-18 | 2010-02-04 | ポラリス・グループ | タンパク質キナーゼ阻害剤として有用なピラゾロ(1,5−a)(1,3,5)トリアジン及びピラゾロ(1,5−a)ピリミジン誘導体 |
| JP2013530142A (ja) * | 2010-05-20 | 2013-07-25 | アレイ バイオファーマ、インコーポレイテッド | Trkキナーゼ阻害剤としてのマクロ環化合物 |
| JP2014515346A (ja) * | 2011-05-19 | 2014-06-30 | セントロ ナシオナル デ インベスティガシオネス オンコロヒカス(セエネイオ) | タンパク質キナーゼ阻害剤としての大環状化合物 |
| JP2014528405A (ja) * | 2011-09-30 | 2014-10-27 | イプセン ファルマ ソシエテ パール アクシオン サンプリフィエIpsen Pharma S.A.S. | マクロ環状lrrk2キナーゼ阻害剤 |
| JP2016510796A (ja) * | 2013-03-15 | 2016-04-11 | オンコデザイン エス.ア. | 大環状rip2キナーゼ阻害剤 |
| WO2015050989A2 (en) * | 2013-10-01 | 2015-04-09 | Cs Therapeutics Inc. | Macrocyclic compounds for the treatment of proliferative diseases |
| WO2015112806A2 (en) * | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| JP6871903B2 (ja) * | 2015-07-02 | 2021-05-19 | ターニング・ポイント・セラピューティクス・インコーポレイテッドTurning Point Therapeutics,Inc. | プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子 |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112019001607A2 (pt) | 2019-04-30 |
| EP3490564A1 (en) | 2019-06-05 |
| IL264395A (en) | 2019-02-28 |
| TW201815799A (zh) | 2018-05-01 |
| KR20190034225A (ko) | 2019-04-01 |
| US10689400B2 (en) | 2020-06-23 |
| CN109715165A (zh) | 2019-05-03 |
| US20190169208A1 (en) | 2019-06-06 |
| SG11201900163PA (en) | 2019-02-27 |
| WO2018022911A1 (en) | 2018-02-01 |
| ZA201901034B (en) | 2021-06-30 |
| MX2019001125A (es) | 2019-06-12 |
| RU2019105587A (ru) | 2020-08-28 |
| CA3031100A1 (en) | 2018-02-01 |
| EP3490564A4 (en) | 2020-02-26 |
| AU2017302019A1 (en) | 2019-02-07 |
| RU2019105587A3 (OSRAM) | 2020-11-18 |
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Legal Events
| Date | Code | Title | Description |
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