AU2012299223A1 - Process and intermediates for preparing macrolactams - Google Patents
Process and intermediates for preparing macrolactams Download PDFInfo
- Publication number
- AU2012299223A1 AU2012299223A1 AU2012299223A AU2012299223A AU2012299223A1 AU 2012299223 A1 AU2012299223 A1 AU 2012299223A1 AU 2012299223 A AU2012299223 A AU 2012299223A AU 2012299223 A AU2012299223 A AU 2012299223A AU 2012299223 A1 AU2012299223 A1 AU 2012299223A1
- Authority
- AU
- Australia
- Prior art keywords
- compound
- meo
- salt
- pct
- compounds
- 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.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C35/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
- C07C35/02—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic
- C07C35/04—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic containing a three or four-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C269/04—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/32—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
- C07C271/34—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/14—Preparation of carboxylic acid esters from carboxylic acid halides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/013—Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
- C07C69/12—Acetic acid esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D498/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
- C07K5/126—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Oncology (AREA)
- Veterinary Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Cephalosporin Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161525462P | 2011-08-19 | 2011-08-19 | |
| US61/525,462 | 2011-08-19 | ||
| US201161533439P | 2011-09-12 | 2011-09-12 | |
| US61/533,439 | 2011-09-12 | ||
| US201161533915P | 2011-09-13 | 2011-09-13 | |
| US61/533,915 | 2011-09-13 | ||
| US201161539540P | 2011-09-27 | 2011-09-27 | |
| US61/539,540 | 2011-09-27 | ||
| PCT/US2012/051177 WO2013028470A1 (en) | 2011-08-19 | 2012-08-16 | Process and intermediates for preparing macrolactams |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2012299223A1 true AU2012299223A1 (en) | 2014-02-27 |
Family
ID=47746773
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2012299223A Abandoned AU2012299223A1 (en) | 2011-08-19 | 2012-08-16 | Process and intermediates for preparing macrolactams |
| AU2012299218A Abandoned AU2012299218A1 (en) | 2011-08-19 | 2012-08-16 | Crystal forms of a HCV protease inhibitor |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2012299218A Abandoned AU2012299218A1 (en) | 2011-08-19 | 2012-08-16 | Crystal forms of a HCV protease inhibitor |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US9238604B2 (enExample) |
| EP (3) | EP2744336B1 (enExample) |
| JP (2) | JP2014521750A (enExample) |
| KR (2) | KR20140059236A (enExample) |
| CN (2) | CN103889439A (enExample) |
| AU (2) | AU2012299223A1 (enExample) |
| BR (2) | BR112014003802A2 (enExample) |
| CA (2) | CA2844386A1 (enExample) |
| MX (2) | MX2014001944A (enExample) |
| RU (2) | RU2014110399A (enExample) |
| WO (3) | WO2013028465A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8828930B2 (en) | 2009-07-30 | 2014-09-09 | Merck Sharp & Dohme Corp. | Hepatitis C virus NS3 protease inhibitors |
| US8957203B2 (en) | 2011-05-05 | 2015-02-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| RU2014110399A (ru) | 2011-08-19 | 2015-09-27 | Мерк Шарп И Доум Корп. | Кристаллические формы вгс протеазного ингибитора |
| UA119315C2 (uk) | 2012-07-03 | 2019-06-10 | Гіліад Фармассет Елелсі | Інгібітори вірусу гепатиту с |
| HRP20161694T1 (hr) | 2012-10-19 | 2017-03-10 | Bristol-Myers Squibb Company | 9-metil supstituirani heksadekahidrociklopropa(e)pirolo (1,2-a)(1,4) diazaciklopentadecinil karbamat derivati kao ne-strukturalni 3 (ns3) proteazni inhibitori za liječenje infekcija virusom hepatitisa c |
| US9643999B2 (en) | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| WO2014070964A1 (en) | 2012-11-02 | 2014-05-08 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| EP2914598B1 (en) | 2012-11-02 | 2017-10-18 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
| US9409943B2 (en) | 2012-11-05 | 2016-08-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| US9580463B2 (en) | 2013-03-07 | 2017-02-28 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
| ES2735355T3 (es) | 2013-03-15 | 2019-12-18 | Gilead Sciences Inc | Inhibidores macrocíclicos y bicíclicos de virus de hepatitis C |
| EP3057926A4 (en) * | 2013-10-18 | 2017-07-12 | Merck Sharp & Dohme Corp. | Methods and intermediates for preparing macrolactams |
| WO2015095437A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Methods and intermediates for the preparation of macrolactams |
| PL3097107T3 (pl) * | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| CN106413736A (zh) * | 2014-06-06 | 2017-02-15 | 艾伯维公司 | 晶型 |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) * | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| KR102772574B1 (ko) * | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| EP4483875A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| 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 |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | 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 | 大環式化合物およびその使用 |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| CN111057045A (zh) * | 2019-12-18 | 2020-04-24 | 安徽红杉生物医药科技有限公司 | Hcv ns3/4a蛋白酶抑制剂中间体及其合成方法、应用 |
| CN112174982A (zh) * | 2020-09-10 | 2021-01-05 | 上海希迈医药科技有限公司 | 一种洛普替尼晶型及其制备方法 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4871868A (en) | 1987-03-11 | 1989-10-03 | Takeda Chemical Industries, Ltd. | Production of substituted acetylenic compounds |
| GB9207987D0 (en) | 1992-04-10 | 1992-05-27 | Smithkline Beecham Plc | Novel container and closure |
| US5716960A (en) * | 1995-01-13 | 1998-02-10 | U.S. Bioscience Inc. And Individuals | Crystalline trimetrexate salts and the process for making the same |
| NO317155B1 (no) | 1997-02-04 | 2004-08-30 | Ono Pharmaceutical Co | <omega>-cykloalkyl-prostagladin-E<N>2</N>-derivater |
| ZA98879B (en) * | 1997-02-04 | 1998-08-03 | Ono Pharmaceutical Co | Omega-cycloalkyl-prostaglandin e2 derivatives |
| EP2602259A3 (en) | 2005-02-18 | 2014-09-10 | Mitsubishi Tanabe Pharma Corporation | Salt of proline derivative, solvate thereof, and production method thereof |
| WO2006102087A2 (en) | 2005-03-22 | 2006-09-28 | Merck & Co., Inc. | Hcv protease substrates |
| US7879797B2 (en) | 2005-05-02 | 2011-02-01 | Merck Sharp & Dohme Corp. | HCV NS3 protease inhibitors |
| US7470664B2 (en) | 2005-07-20 | 2008-12-30 | Merck & Co., Inc. | HCV NS3 protease inhibitors |
| CN101228181B (zh) * | 2005-07-20 | 2013-09-18 | 默沙东公司 | Hcv ns3蛋白酶抑制剂 |
| AU2006275605B2 (en) | 2005-08-01 | 2011-01-06 | Merck Sharp & Dohme Corp. | Macrocyclic peptides as HCV NS3 protease inhibitors |
| AU2007224367A1 (en) | 2006-03-07 | 2007-09-13 | The Procter & Gamble Company | Compositions for oxidatively dyeing keratin fibers and methods for using such compositions |
| GB0609492D0 (en) | 2006-05-15 | 2006-06-21 | Angeletti P Ist Richerche Bio | Therapeutic agents |
| GB0612423D0 (en) | 2006-06-23 | 2006-08-02 | Angeletti P Ist Richerche Bio | Therapeutic agents |
| JP5345941B2 (ja) | 2006-10-24 | 2013-11-20 | メルク・シャープ・アンド・ドーム・コーポレーション | Ｈｃｖｎｓ３プロテアーゼ阻害剤 |
| CA2667165A1 (en) | 2006-10-24 | 2008-05-02 | Merck & Co., Inc. | Hcv ns3 protease inhibitors |
| US20100099695A1 (en) | 2006-10-27 | 2010-04-22 | Liverton Nigel J | HCV NS3 Protease Inhibitors |
| ES2444575T3 (es) | 2006-10-27 | 2014-02-25 | Merck Sharp & Dohme Corp. | Inhibidores de la proteasa NS3 del VHC |
| EP2160392A2 (en) * | 2007-05-03 | 2010-03-10 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
| WO2009010804A1 (en) | 2007-07-19 | 2009-01-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Macrocyclic compounds as antiviral agents |
| EP2268285B1 (en) | 2008-02-25 | 2018-06-27 | Merck Sharp & Dohme Corp. | Therapeutic compounds |
| EP2274288A2 (en) | 2008-04-24 | 2011-01-19 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| WO2009131196A1 (ja) * | 2008-04-24 | 2009-10-29 | 武田薬品工業株式会社 | 置換ピロリジン誘導体およびその用途 |
| US8461107B2 (en) | 2008-04-28 | 2013-06-11 | Merck Sharp & Dohme Corp. | HCV NS3 protease inhibitors |
| SI2310095T1 (sl) * | 2008-07-22 | 2013-01-31 | Merck Sharp & Dohme Corp. | Makrocikliäśne kuinoksalinske spojine kot hcv ns3 proteazni inhibitorji |
| US8828930B2 (en) | 2009-07-30 | 2014-09-09 | Merck Sharp & Dohme Corp. | Hepatitis C virus NS3 protease inhibitors |
| CA2770338A1 (en) * | 2009-08-27 | 2011-03-03 | Merck Sharp & Dohme Corp. | Processes for preparing protease inhibitors of hepatitis c virus |
| RU2014110399A (ru) | 2011-08-19 | 2015-09-27 | Мерк Шарп И Доум Корп. | Кристаллические формы вгс протеазного ингибитора |
-
2012
- 2012-08-16 RU RU2014110399/04A patent/RU2014110399A/ru not_active Application Discontinuation
- 2012-08-16 WO PCT/US2012/051168 patent/WO2013028465A1/en not_active Ceased
- 2012-08-16 BR BR112014003802A patent/BR112014003802A2/pt not_active IP Right Cessation
- 2012-08-16 KR KR1020147006888A patent/KR20140059236A/ko not_active Withdrawn
- 2012-08-16 MX MX2014001944A patent/MX2014001944A/es unknown
- 2012-08-16 KR KR1020147006858A patent/KR20140053330A/ko not_active Withdrawn
- 2012-08-16 MX MX2014001945A patent/MX2014001945A/es unknown
- 2012-08-16 CN CN201280050382.8A patent/CN103889439A/zh active Pending
- 2012-08-16 RU RU2014110400/04A patent/RU2014110400A/ru not_active Application Discontinuation
- 2012-08-16 US US14/239,393 patent/US9238604B2/en active Active
- 2012-08-16 JP JP2014526217A patent/JP2014521750A/ja active Pending
- 2012-08-16 CN CN201280050361.6A patent/CN103874414A/zh active Pending
- 2012-08-16 CA CA2844386A patent/CA2844386A1/en not_active Abandoned
- 2012-08-16 AU AU2012299223A patent/AU2012299223A1/en not_active Abandoned
- 2012-08-16 WO PCT/US2012/051182 patent/WO2013028471A1/en not_active Ceased
- 2012-08-16 AU AU2012299218A patent/AU2012299218A1/en not_active Abandoned
- 2012-08-16 WO PCT/US2012/051177 patent/WO2013028470A1/en not_active Ceased
- 2012-08-16 EP EP12826404.1A patent/EP2744336B1/en not_active Not-in-force
- 2012-08-16 US US14/239,391 patent/US9073825B2/en active Active
- 2012-08-16 BR BR112014003798A patent/BR112014003798A2/pt not_active IP Right Cessation
- 2012-08-16 US US14/239,389 patent/US9242917B2/en active Active
- 2012-08-16 EP EP12825726.8A patent/EP2744331A4/en not_active Withdrawn
- 2012-08-16 EP EP12825540.3A patent/EP2744507A4/en not_active Withdrawn
- 2012-08-16 JP JP2014526215A patent/JP2014524442A/ja active Pending
- 2012-08-16 CA CA2844388A patent/CA2844388A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN103874414A (zh) | 2014-06-18 |
| JP2014521750A (ja) | 2014-08-28 |
| KR20140053330A (ko) | 2014-05-07 |
| WO2013028465A1 (en) | 2013-02-28 |
| CA2844386A1 (en) | 2013-02-28 |
| RU2014110400A (ru) | 2015-09-27 |
| EP2744507A1 (en) | 2014-06-25 |
| AU2012299218A1 (en) | 2014-02-20 |
| JP2014524442A (ja) | 2014-09-22 |
| RU2014110399A (ru) | 2015-09-27 |
| EP2744507A4 (en) | 2015-01-28 |
| US9242917B2 (en) | 2016-01-26 |
| US9073825B2 (en) | 2015-07-07 |
| US20140200343A1 (en) | 2014-07-17 |
| MX2014001945A (es) | 2014-03-27 |
| KR20140059236A (ko) | 2014-05-15 |
| US9238604B2 (en) | 2016-01-19 |
| EP2744331A1 (en) | 2014-06-25 |
| MX2014001944A (es) | 2014-03-27 |
| CN103889439A (zh) | 2014-06-25 |
| EP2744336A1 (en) | 2014-06-25 |
| EP2744336B1 (en) | 2017-07-05 |
| EP2744331A4 (en) | 2015-01-21 |
| CA2844388A1 (en) | 2013-02-28 |
| US20140206605A1 (en) | 2014-07-24 |
| WO2013028471A1 (en) | 2013-02-28 |
| EP2744336A4 (en) | 2014-12-31 |
| WO2013028470A1 (en) | 2013-02-28 |
| BR112014003802A2 (pt) | 2017-06-13 |
| BR112014003798A2 (pt) | 2017-03-01 |
| US20140243519A1 (en) | 2014-08-28 |
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