RU2011105768A - Производные пиперидина в качестве ингибиторов jakз - Google Patents
Производные пиперидина в качестве ингибиторов jakз Download PDFInfo
- Publication number
- RU2011105768A RU2011105768A RU2011105768/04A RU2011105768A RU2011105768A RU 2011105768 A RU2011105768 A RU 2011105768A RU 2011105768/04 A RU2011105768/04 A RU 2011105768/04A RU 2011105768 A RU2011105768 A RU 2011105768A RU 2011105768 A RU2011105768 A RU 2011105768A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- formula
- heteroaryl
- aryl
- lower alkyl
- Prior art date
Links
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical class C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title description 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 53
- 125000000217 alkyl group Chemical group 0.000 claims abstract 36
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 24
- 125000003118 aryl group Chemical group 0.000 claims abstract 22
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 20
- 125000001424 substituent group Chemical group 0.000 claims abstract 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 16
- 125000005843 halogen group Chemical group 0.000 claims abstract 9
- 150000003839 salts Chemical class 0.000 claims 15
- 241000124008 Mammalia Species 0.000 claims 6
- 230000004913 activation Effects 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 230000001575 pathological effect Effects 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 230000028993 immune response Effects 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000003993 interaction Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000002651 drug therapy Methods 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 0 C*(C)C1=C2C=C**2*C=C1 Chemical compound C*(C)C1=C2C=C**2*C=C1 0.000 description 6
- ANLQHFYDQPMDJY-UHFFFAOYSA-N N#CCC(N1CCCCC1)=O Chemical compound N#CCC(N1CCCCC1)=O ANLQHFYDQPMDJY-UHFFFAOYSA-N 0.000 description 2
- YMTHMOTWWHHUJA-XSSCSCGXSA-N CC(C)/C(/C/N=C\N)=C(/C(/N=C\C)=C)\S Chemical compound CC(C)/C(/C/N=C\N)=C(/C(/N=C\C)=C)\S YMTHMOTWWHHUJA-XSSCSCGXSA-N 0.000 description 1
- AWSQJBKYHBAHRH-KHPPLWFESA-N CC(C)/C(/C/N=C\N)=C(/C(SC=C)=C)\N Chemical compound CC(C)/C(/C/N=C\N)=C(/C(SC=C)=C)\N AWSQJBKYHBAHRH-KHPPLWFESA-N 0.000 description 1
- TVPBQWALLWZLPD-UHFFFAOYSA-N CC(C)c1nccc2c1cc[nH]2 Chemical compound CC(C)c1nccc2c1cc[nH]2 TVPBQWALLWZLPD-UHFFFAOYSA-N 0.000 description 1
- QDUJWHZMFYXBJJ-VJINBYIFSA-N CCCC(C)(C)/C(/C(N/C=C\N)=C)=N/C=N\C Chemical compound CCCC(C)(C)/C(/C(N/C=C\N)=C)=N/C=N\C QDUJWHZMFYXBJJ-VJINBYIFSA-N 0.000 description 1
- NBGVQJSFZBDTLK-UHFFFAOYSA-N CNc1c(cc[nH]2)c2nc(N)n1 Chemical compound CNc1c(cc[nH]2)c2nc(N)n1 NBGVQJSFZBDTLK-UHFFFAOYSA-N 0.000 description 1
- FCAZMSXDZZZZRX-UHFFFAOYSA-N CNc1c2OCCc2ncn1 Chemical compound CNc1c2OCCc2ncn1 FCAZMSXDZZZZRX-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8570508P | 2008-08-01 | 2008-08-01 | |
| US61/085,705 | 2008-08-01 | ||
| US9856208P | 2008-09-19 | 2008-09-19 | |
| US61/098,562 | 2008-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2011105768A true RU2011105768A (ru) | 2012-09-10 |
Family
ID=41170025
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2011105768/04A RU2011105768A (ru) | 2008-08-01 | 2009-07-31 | Производные пиперидина в качестве ингибиторов jakз |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20110165183A1 (enExample) |
| EP (1) | EP2324020A2 (enExample) |
| JP (1) | JP2011529918A (enExample) |
| KR (1) | KR20110050654A (enExample) |
| CN (1) | CN102171211A (enExample) |
| AU (1) | AU2009276420A1 (enExample) |
| BR (1) | BRPI0916931A2 (enExample) |
| CA (1) | CA2732628A1 (enExample) |
| IL (1) | IL210990A0 (enExample) |
| MX (1) | MX2011001259A (enExample) |
| NZ (1) | NZ590922A (enExample) |
| RU (1) | RU2011105768A (enExample) |
| WO (1) | WO2010014930A2 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2643371C2 (ru) * | 2012-11-20 | 2018-02-01 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Новые соединения |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013501003A (ja) | 2009-07-31 | 2013-01-10 | バイオクライスト ファーマシューティカルズ， インコーポレイテッド | ヤヌスキナーゼ阻害剤としてのピロロ［１，２−ｂ］ピリダジン誘導体 |
| US20130071415A1 (en) * | 2010-05-28 | 2013-03-21 | Biocryst Pharmaceuticals, Inc. | Heterocyclic Compounds as Janus Kinase Inhibitors |
| MX2013013331A (es) * | 2011-05-17 | 2014-10-17 | Principia Biopharma Inc | Derivados de azaindol como inhibidores de tirosina-cinasas. |
| IN2014DN07954A (enExample) | 2012-03-13 | 2015-05-01 | Basf Se | |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| EP2935216B1 (en) * | 2012-12-17 | 2018-06-27 | Sun Pharmaceutical Industries Limited | Process for the preparation of tofacitinib and intermediates thereof |
| EP2938616A4 (en) | 2012-12-28 | 2016-06-15 | Glenmark Pharmaceuticals Ltd | PROCESSING METHOD FOR THE PRODUCTION OF TOFACITINIB AND INTERMEDIATE PRODUCTS THEREOF |
| WO2015036059A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| CA2923101A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| EP3049086A4 (en) * | 2013-09-27 | 2017-02-22 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| ES2865058T3 (es) * | 2013-12-09 | 2021-10-14 | Unichem Lab Ltd | Un proceso mejorado para la preparación de (3R,4R)-(1-bencil-4-metilpiperidin-3-il)-metilamina |
| CN112353806A (zh) | 2014-02-21 | 2021-02-12 | 普林斯匹亚生物制药公司 | Btk抑制剂的盐和固体形式 |
| CN104860950A (zh) * | 2014-02-24 | 2015-08-26 | 重庆医药工业研究院有限责任公司 | 一种制备4-氯吡咯[2,3-d]并嘧啶的方法 |
| CN104059016A (zh) * | 2014-06-20 | 2014-09-24 | 湖南天地恒一制药有限公司 | 制备托法替布的中间体及所述中间体的制备方法 |
| KR101710127B1 (ko) * | 2014-08-29 | 2017-02-27 | 한화제약주식회사 | 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민 |
| SG11201704808VA (en) | 2014-12-18 | 2017-07-28 | Principia Biopharma Inc | Treatment of pemphigus |
| CN105732637B (zh) * | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| EP3078665A1 (en) * | 2015-04-10 | 2016-10-12 | OLON S.p.A. | Efficient method for the preparation of tofacitinib citrate |
| BR112017027951A2 (pt) * | 2015-06-22 | 2018-08-28 | Ono Pharmaceutical Co., Ltd. | composto inibitório de brk |
| US20180305350A1 (en) | 2015-06-24 | 2018-10-25 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN105622616A (zh) * | 2016-02-25 | 2016-06-01 | 上海雅本化学有限公司 | 一种4-氯吡咯并嘧啶的制备方法 |
| IL263815B (en) | 2016-06-29 | 2022-07-01 | Principia Biopharma Inc | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(Oxtan-3-yl)piperazin-1-yl)pent-2-ananitrile |
| GB201617758D0 (en) | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| CN109970745B (zh) * | 2018-04-16 | 2020-12-08 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡咯并三嗪类化合物及其药物组合物及其用途 |
| AU2020365951B2 (en) | 2019-10-14 | 2026-07-16 | Principia Biopharma Inc. | Methods for treating immune thrombocytopenia by administering (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| KR102993352B1 (ko) | 2019-12-20 | 2026-07-22 | 프린시피아 바이오파마, 인코퍼레이티드 | 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-에네니트릴의 고체 형태 |
| WO2021150723A1 (en) | 2020-01-22 | 2021-07-29 | Principia Biopharma Inc. | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN116768908B (zh) * | 2022-03-10 | 2025-11-18 | 石家庄迪斯凯威医药科技有限公司 | 一种含n多环化合物及其制备方法与用途 |
| CN117164519A (zh) * | 2023-08-18 | 2023-12-05 | 杭州小蓓医药科技有限公司 | 一种l-肌肽的合成方法 |
| CN117534603A (zh) * | 2023-11-10 | 2024-02-09 | 江苏海悦康医药科技有限公司 | 一种托法替布中间体的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU3951899A (en) * | 1998-06-19 | 2000-01-05 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| OA12118A (en) * | 1999-12-10 | 2006-05-04 | Pfizer Prod Inc | PyrroloÄ2,3-dÜpyrimidine compounds. |
| OA12292A (en) * | 2000-06-26 | 2003-11-11 | Pfizer Prod Inc | PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents. |
| US7301023B2 (en) * | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| WO2004047843A1 (en) * | 2002-11-26 | 2004-06-10 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| KR100824193B1 (ko) * | 2003-04-29 | 2008-04-21 | 화이자 인코포레이티드 | 고혈압 치료에 유용한5,7-디아미노피라졸로[4,3-ｄ]피리미딘 |
| CA2545192A1 (en) * | 2003-11-25 | 2005-06-09 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| AR054416A1 (es) * | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| JP5071374B2 (ja) * | 2005-07-14 | 2012-11-14 | アステラス製薬株式会社 | ヘテロ環ヤヌスキナーゼ３阻害剤 |
| NL2000291C2 (nl) * | 2005-11-10 | 2009-02-17 | Pfizer Prod Inc | 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H- pyrazool(4,3-d)pyrimidine-5-yl)piperidine-4-carbonzuur en zouten daarvan. |
| TW201111385A (en) * | 2009-08-27 | 2011-04-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
| RU2013120966A (ru) * | 2010-10-08 | 2014-11-20 | Эббви Инк. | ФУРО[3,2-d]ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ |
-
2009
- 2009-07-31 RU RU2011105768/04A patent/RU2011105768A/ru not_active Application Discontinuation
- 2009-07-31 EP EP09791064A patent/EP2324020A2/en not_active Withdrawn
- 2009-07-31 CN CN2009801396041A patent/CN102171211A/zh active Pending
- 2009-07-31 MX MX2011001259A patent/MX2011001259A/es unknown
- 2009-07-31 WO PCT/US2009/052449 patent/WO2010014930A2/en not_active Ceased
- 2009-07-31 KR KR1020117004724A patent/KR20110050654A/ko not_active Withdrawn
- 2009-07-31 CA CA2732628A patent/CA2732628A1/en not_active Abandoned
- 2009-07-31 JP JP2011521361A patent/JP2011529918A/ja active Pending
- 2009-07-31 NZ NZ590922A patent/NZ590922A/xx not_active IP Right Cessation
- 2009-07-31 AU AU2009276420A patent/AU2009276420A1/en not_active Abandoned
- 2009-07-31 BR BRPI0916931A patent/BRPI0916931A2/pt not_active IP Right Cessation
- 2009-07-31 US US13/057,100 patent/US20110165183A1/en not_active Abandoned
-
2011
- 2011-02-01 IL IL210990A patent/IL210990A0/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2643371C2 (ru) * | 2012-11-20 | 2018-02-01 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | Новые соединения |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20110050654A (ko) | 2011-05-16 |
| EP2324020A2 (en) | 2011-05-25 |
| AU2009276420A1 (en) | 2010-02-04 |
| BRPI0916931A2 (pt) | 2015-11-24 |
| JP2011529918A (ja) | 2011-12-15 |
| CN102171211A (zh) | 2011-08-31 |
| NZ590922A (en) | 2012-09-28 |
| IL210990A0 (en) | 2011-04-28 |
| US20110165183A1 (en) | 2011-07-07 |
| WO2010014930A3 (en) | 2010-07-29 |
| MX2011001259A (es) | 2011-03-15 |
| CA2732628A1 (en) | 2010-02-04 |
| WO2010014930A2 (en) | 2010-02-04 |
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