CN101809002B - 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物 - Google Patents
用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物 Download PDFInfo
- Publication number
- CN101809002B CN101809002B CN2008801062258A CN200880106225A CN101809002B CN 101809002 B CN101809002 B CN 101809002B CN 2008801062258 A CN2008801062258 A CN 2008801062258A CN 200880106225 A CN200880106225 A CN 200880106225A CN 101809002 B CN101809002 B CN 101809002B
- Authority
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- China
- Prior art keywords
- alkyl
- amino
- alkoxy
- group
- phenyl
- 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.)
- Expired - Fee Related
Links
- 0 **C1=*C(N2[C@](*)COCC2)=C(C2)C2C(*)=N1 Chemical compound **C1=*C(N2[C@](*)COCC2)=C(C2)C2C(*)=N1 0.000 description 9
- NWCWFNJUARWJTI-HNNXBMFYSA-O C[C@@H](COCC1)N1c1nc(-c2ccc(CNC(NC3CC3)=S)cc2)nc(C[SH+]C)c1 Chemical compound C[C@@H](COCC1)N1c1nc(-c2ccc(CNC(NC3CC3)=S)cc2)nc(C[SH+]C)c1 NWCWFNJUARWJTI-HNNXBMFYSA-O 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94853907P | 2007-07-09 | 2007-07-09 | |
| US60/948539 | 2007-07-09 | ||
| PCT/GB2008/050548 WO2009007750A1 (en) | 2007-07-09 | 2008-07-08 | Morpholino pyrimidine derivatives used in diseases linked to mtor kinase and/or pi3k |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101809002A CN101809002A (zh) | 2010-08-18 |
| CN101809002B true CN101809002B (zh) | 2013-03-27 |
Family
ID=39791229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008801062258A Expired - Fee Related CN101809002B (zh) | 2007-07-09 | 2008-07-08 | 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8138183B2 (OSRAM) |
| EP (1) | EP2176238B1 (OSRAM) |
| JP (1) | JP5508260B2 (OSRAM) |
| KR (1) | KR20100042280A (OSRAM) |
| CN (1) | CN101809002B (OSRAM) |
| AR (1) | AR070079A1 (OSRAM) |
| AT (1) | ATE554075T1 (OSRAM) |
| AU (1) | AU2008273891B2 (OSRAM) |
| BR (1) | BRPI0814688A2 (OSRAM) |
| CA (1) | CA2692720A1 (OSRAM) |
| CL (1) | CL2008003940A1 (OSRAM) |
| CO (1) | CO6251364A2 (OSRAM) |
| CR (1) | CR11200A (OSRAM) |
| DO (1) | DOP2010000012A (OSRAM) |
| EA (1) | EA018708B1 (OSRAM) |
| EC (1) | ECSP109935A (OSRAM) |
| ES (1) | ES2385692T3 (OSRAM) |
| NI (1) | NI201000002A (OSRAM) |
| PE (1) | PE20100138A1 (OSRAM) |
| WO (1) | WO2009007750A1 (OSRAM) |
| ZA (1) | ZA200909224B (OSRAM) |
Families Citing this family (53)
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| AU2008273889B2 (en) * | 2007-07-09 | 2012-03-08 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| MX315904B (es) | 2008-05-30 | 2013-11-29 | Amgen Inc | Inhibidores de fosfoinosituro-3 cinasa. |
| US8785457B2 (en) | 2009-03-13 | 2014-07-22 | Cellzome Limited | Pyrimidine derivatives as mTOR inhibitors |
| UY32582A (es) | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| AR077628A1 (es) | 2009-07-02 | 2011-09-14 | Sanofi Aventis | Derivados de 6-(morfolin-4-il)-pirimidin-4(3h)-ona, su preparacion y su utilizacion farmaceutica como inhibidores de la fosforilacion de akt(pkb) |
| JP5680638B2 (ja) | 2009-07-02 | 2015-03-04 | サノフイ | 新規な（６−オキソ−１，６−ジヒドロピリミジン−２−イル）アミド誘導体、この調製およびａｋｔ（ｐｋｂ）リン酸化インヒビターとしてのこの医薬的な使用 |
| MX2012005023A (es) | 2009-10-30 | 2012-06-19 | Ariad Pharma Inc | Metodos y composiciones para tratar cancer. |
| EP2992878A1 (en) | 2010-02-03 | 2016-03-09 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| ES2535116T3 (es) | 2010-03-04 | 2015-05-05 | Cellzome Limited | Derivados de urea sustituida con morfolino como inhibidores de mtor |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| ES2612492T3 (es) | 2010-12-28 | 2017-05-17 | Sanofi | Nuevos derivados de piridiminas, su preparación y su utilización farmacéutica como inhibidores de fosforilación de AKT (PKB) |
| US20140163023A1 (en) | 2011-04-04 | 2014-06-12 | Cellzome Limited | Dihydropyrrolo pyrimidine derivatives as mtor inhibitors |
| MX373641B (es) | 2011-04-29 | 2020-05-04 | Selecta Biosciences Inc | Nanoportadores sintéticos tolerogénicos para la terapia contra alergias. |
| AU2012290056B2 (en) | 2011-08-03 | 2015-03-19 | Signal Pharmaceuticals, Llc | Identification of gene expression profile as a predictive biomarker for LKB1 status |
| RU2616619C2 (ru) | 2011-09-21 | 2017-04-18 | Селлзоум Лимитед | Морфолино-замещенные производные мочевины или карбамата в качестве ингибиторов mtor |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| BR112014008241A2 (pt) | 2011-10-07 | 2017-04-18 | Cellzome Ltd | composto, composição farmacêutica, métodos para tratar, controlar, retardar ou prevenir doenças e distúrbios, e para preparar um composto, e, uso de um composto |
| CA2871112C (en) | 2012-07-04 | 2020-05-12 | F. Hoffmann-La Roche Ag | Covalently linked antigen-antibody conjugates |
| FR2994572B1 (fr) * | 2012-08-17 | 2015-04-17 | Centre Nat Rech Scient | Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| JP6417338B2 (ja) * | 2013-02-19 | 2018-11-07 | アムジエン・インコーポレーテツド | 癌の治療のためのｍｄｍ２阻害剤としてのシス−モルホリノン及び他の化合物 |
| EP2970237B1 (en) | 2013-03-14 | 2017-09-27 | Amgen Inc. | Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| JP6382945B2 (ja) | 2013-04-17 | 2018-08-29 | シグナル ファーマシューティカルズ，エルエルシー | ジヒドロピラジノ−ピラジンによる癌治療 |
| KR102459285B1 (ko) | 2013-04-17 | 2022-10-27 | 시그날 파마소티칼 엘엘씨 | 1-에틸-7-(2-메틸-6-(1H-1,2,4-트리아졸-3-일)피리딘-3-일)-3,4-디하이드로피라지노[2,3-b]피라진-2(1H)-온에 관한 약학 제제, 제조방법, 고체 형태 및 사용 방법 |
| TWI654979B (zh) | 2013-04-17 | 2019-04-01 | 美商標誌製藥公司 | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| KR102221029B1 (ko) | 2013-04-17 | 2021-02-26 | 시그날 파마소티칼 엘엘씨 | 디하이드로피라지노-피라진을 사용한 암의 치료 |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| WO2014172431A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer |
| CN105283175A (zh) | 2013-05-03 | 2016-01-27 | 西莱克塔生物科技公司 | 用于降低的或增强的药效学作用的致耐受性合成纳米载体和治疗性大分子 |
| CN113831345A (zh) | 2013-05-29 | 2021-12-24 | 西格诺药品有限公司 | 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途 |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| EP3089996B1 (en) | 2014-01-03 | 2021-07-28 | F. Hoffmann-La Roche AG | Bispecific anti-hapten/anti-blood brain barrier receptor antibodies, complexes thereof and their use as blood brain barrier shuttles |
| EP3131551A4 (en) | 2014-04-16 | 2017-09-20 | Signal Pharmaceuticals, LLC | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| CA2947504A1 (en) * | 2014-06-26 | 2015-12-30 | F. Hoffmann-La Roche Ag | Anti-brdu antibodies and methods of use |
| WO2016020288A1 (en) | 2014-08-04 | 2016-02-11 | Nuevolution A/S | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| KR20170045344A (ko) | 2014-09-07 | 2017-04-26 | 셀렉타 바이오사이언시즈, 인크. | 항-바이러스 전달 벡터 면역 반응을 약화시키기 위한 방법 및 조성물 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| JP7523909B2 (ja) | 2017-03-11 | 2024-07-29 | セレクタ バイオサイエンシーズ インコーポレーテッド | 抗炎症剤および免疫抑制剤を含む合成ナノキャリアによる組み合わせ処置に関連する方法および組成物 |
| WO2018218197A2 (en) | 2017-05-26 | 2018-11-29 | Board Of Regents, The University Of Texas System | Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase |
| SG11201912403SA (en) | 2017-06-22 | 2020-01-30 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| LT3651768T (lt) | 2017-07-13 | 2024-04-25 | Board Of Regents, The University Of Texas System | Heterocikliniai atr kinazės inhibitoriai |
| EP3668839B1 (en) | 2017-08-17 | 2023-04-12 | Board of Regents, The University of Texas System | Heterocyclic inhibitors of atr kinase |
| WO2019178590A1 (en) | 2018-03-16 | 2019-09-19 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of atr kinase |
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| EP4076657A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| MX2022012259A (es) | 2020-03-31 | 2022-12-08 | Nuevolution As | Compuestos activos frente a receptores nucleares. |
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| JPWO2007114323A1 (ja) | 2006-04-04 | 2009-08-20 | 大正製薬株式会社 | アミノピロリジン化合物 |
| KR20080110912A (ko) | 2006-04-19 | 2008-12-19 | 노파르티스 아게 | 인다졸 화합물 및 ｃｄｃ７의 억제 방법 |
| WO2007126043A1 (ja) | 2006-04-27 | 2007-11-08 | Mitsubishi Tanabe Pharma Corporation | チアゾール環を含むカルボン酸誘導体の医薬用途 |
| GB0610909D0 (en) | 2006-06-05 | 2006-07-12 | Merck Sharp & Dohme | Therapeutic treatment |
| US8222256B2 (en) | 2006-07-05 | 2012-07-17 | Exelixis, Inc. | Methods of using IGFIR and ABL kinase modulators |
| WO2008023159A1 (en) | 2006-08-24 | 2008-02-28 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| EP2057129A1 (en) * | 2006-08-24 | 2009-05-13 | AstraZeneca AB | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| KR20100016431A (ko) | 2007-04-12 | 2010-02-12 | 에프. 호프만-라 로슈 아게 | 약학적 화합물 |
| AU2008273892A1 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
-
2008
- 2008-07-08 EP EP08776183A patent/EP2176238B1/en active Active
- 2008-07-08 KR KR1020107002942A patent/KR20100042280A/ko not_active Ceased
- 2008-07-08 US US12/668,056 patent/US8138183B2/en not_active Expired - Fee Related
- 2008-07-08 AU AU2008273891A patent/AU2008273891B2/en not_active Ceased
- 2008-07-08 ES ES08776183T patent/ES2385692T3/es active Active
- 2008-07-08 EA EA201000091A patent/EA018708B1/ru not_active IP Right Cessation
- 2008-07-08 CN CN2008801062258A patent/CN101809002B/zh not_active Expired - Fee Related
- 2008-07-08 CA CA 2692720 patent/CA2692720A1/en not_active Abandoned
- 2008-07-08 BR BRPI0814688A patent/BRPI0814688A2/pt not_active IP Right Cessation
- 2008-07-08 JP JP2010515602A patent/JP5508260B2/ja not_active Expired - Fee Related
- 2008-07-08 AT AT08776183T patent/ATE554075T1/de active
- 2008-07-08 WO PCT/GB2008/050548 patent/WO2009007750A1/en not_active Ceased
- 2008-12-19 PE PE2008002157A patent/PE20100138A1/es not_active Application Discontinuation
- 2008-12-30 CL CL2008003940A patent/CL2008003940A1/es unknown
- 2008-12-30 AR ARP080105784A patent/AR070079A1/es unknown
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2009
- 2009-12-23 ZA ZA2009/09224A patent/ZA200909224B/en unknown
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2010
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- 2010-01-08 CR CR11200A patent/CR11200A/es not_active Application Discontinuation
- 2010-01-08 DO DO2010000012A patent/DOP2010000012A/es unknown
- 2010-02-03 EC EC2010009935A patent/ECSP109935A/es unknown
- 2010-02-09 CO CO10014081A patent/CO6251364A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EA018708B1 (ru) | 2013-10-30 |
| JP5508260B2 (ja) | 2014-05-28 |
| AU2008273891A1 (en) | 2009-01-15 |
| ZA200909224B (en) | 2011-05-25 |
| ECSP109935A (es) | 2010-03-31 |
| BRPI0814688A2 (pt) | 2017-06-06 |
| EP2176238B1 (en) | 2012-04-18 |
| CO6251364A2 (es) | 2011-02-21 |
| ES2385692T3 (es) | 2012-07-30 |
| AR070079A1 (es) | 2010-03-10 |
| CN101809002A (zh) | 2010-08-18 |
| NI201000002A (es) | 2010-10-12 |
| HK1142906A1 (en) | 2010-12-17 |
| AU2008273891B2 (en) | 2012-01-12 |
| CA2692720A1 (en) | 2009-01-15 |
| CR11200A (es) | 2010-06-17 |
| JP2010533160A (ja) | 2010-10-21 |
| ATE554075T1 (de) | 2012-05-15 |
| DOP2010000012A (es) | 2010-01-31 |
| CL2008003940A1 (es) | 2010-09-24 |
| US8138183B2 (en) | 2012-03-20 |
| EA201000091A1 (ru) | 2010-06-30 |
| PE20100138A1 (es) | 2010-03-20 |
| US20100249131A1 (en) | 2010-09-30 |
| EP2176238A1 (en) | 2010-04-21 |
| WO2009007750A1 (en) | 2009-01-15 |
| KR20100042280A (ko) | 2010-04-23 |
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