JP2006506352A - Hivインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−1,6−ジオン化合物 - Google Patents
Hivインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−1,6−ジオン化合物 Download PDFInfo
- Publication number
- JP2006506352A JP2006506352A JP2004536438A JP2004536438A JP2006506352A JP 2006506352 A JP2006506352 A JP 2006506352A JP 2004536438 A JP2004536438 A JP 2004536438A JP 2004536438 A JP2004536438 A JP 2004536438A JP 2006506352 A JP2006506352 A JP 2006506352A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- dione
- pyrido
- dihydroxy
- 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.)
- Withdrawn
Links
- 0 *C(C(*)(*)N(C1=C(C(O)=C2*)O)C2=O)NC1=O Chemical compound *C(C(*)(*)N(C1=C(C(O)=C2*)O)C2=O)NC1=O 0.000 description 8
- ZCJDYYGRHCAYGS-UHFFFAOYSA-N CC(N(C1)c(cccc2)c2NC1=O)=O Chemical compound CC(N(C1)c(cccc2)c2NC1=O)=O ZCJDYYGRHCAYGS-UHFFFAOYSA-N 0.000 description 1
- WDCUYDKTSTYREC-UHFFFAOYSA-N CC(N(C1)c2ccccc2N(Cc(cc2)ccc2F)C1=O)=O Chemical compound CC(N(C1)c2ccccc2N(Cc(cc2)ccc2F)C1=O)=O WDCUYDKTSTYREC-UHFFFAOYSA-N 0.000 description 1
- HARSCTXLBYAPHA-UHFFFAOYSA-N O=C(N(CCN1Cc2ccccc2)CC1=O)OCc1ccccc1 Chemical compound O=C(N(CCN1Cc2ccccc2)CC1=O)OCc1ccccc1 HARSCTXLBYAPHA-UHFFFAOYSA-N 0.000 description 1
- DODVUYJMSMYTCA-UHFFFAOYSA-N OC(C(O)=C1N2CCN(Cc(cc3)cc(Cl)c3Cl)C1=O)=CC2=O Chemical compound OC(C(O)=C1N2CCN(Cc(cc3)cc(Cl)c3Cl)C1=O)=CC2=O DODVUYJMSMYTCA-UHFFFAOYSA-N 0.000 description 1
- DMXMJVFXEJSXSO-UHFFFAOYSA-N OC(C(O)=C1N2CCN(Cc(cc3)ccc3F)C1=O)=C(CC1CN(CC3CC3)CCC1)C2=O Chemical compound OC(C(O)=C1N2CCN(Cc(cc3)ccc3F)C1=O)=C(CC1CN(CC3CC3)CCC1)C2=O DMXMJVFXEJSXSO-UHFFFAOYSA-N 0.000 description 1
- CBPWJNSTIAQAPD-UHFFFAOYSA-N OC(C(O)=C1N2CCN(Cc(cc3F)ccc3F)C1=O)=CC2=O Chemical compound OC(C(O)=C1N2CCN(Cc(cc3F)ccc3F)C1=O)=CC2=O CBPWJNSTIAQAPD-UHFFFAOYSA-N 0.000 description 1
- YWFZVOXGCWEKMX-UHFFFAOYSA-N OC(C(O)=C1N2c3ccccc3N(Cc(cc3)ccc3F)C1=O)=CC2=O Chemical compound OC(C(O)=C1N2c3ccccc3N(Cc(cc3)ccc3F)C1=O)=CC2=O YWFZVOXGCWEKMX-UHFFFAOYSA-N 0.000 description 1
- BTFLVNZODFQYRQ-UHFFFAOYSA-N OCC(CN(Cc(cc1)ccc1F)C1=O)N(C(C=C2O)=O)C1=C2O Chemical compound OCC(CN(Cc(cc1)ccc1F)C1=O)N(C(C=C2O)=O)C1=C2O BTFLVNZODFQYRQ-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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
-
- 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
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40974102P | 2002-09-11 | 2002-09-11 | |
| PCT/US2003/028366 WO2004024078A2 (en) | 2002-09-11 | 2003-09-10 | Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006506352A true JP2006506352A (ja) | 2006-02-23 |
| JP2006506352A5 JP2006506352A5 (enExample) | 2006-10-26 |
Family
ID=31993997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004536438A Withdrawn JP2006506352A (ja) | 2002-09-11 | 2003-09-10 | Hivインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−1,6−ジオン化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7517532B2 (enExample) |
| EP (1) | EP1549315A4 (enExample) |
| JP (1) | JP2006506352A (enExample) |
| AU (1) | AU2003267098B2 (enExample) |
| CA (1) | CA2498111A1 (enExample) |
| WO (1) | WO2004024078A2 (enExample) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005232103A (ja) * | 2004-02-20 | 2005-09-02 | Nagase & Co Ltd | 光学活性なビシナルジアミンおよびその製造方法 |
| WO2010147068A1 (ja) * | 2009-06-15 | 2010-12-23 | 塩野義製薬株式会社 | 置換された多環性カルバモイルピリドン誘導体 |
| JP2014510747A (ja) * | 2011-03-31 | 2014-05-01 | ファイザー・インク | 新規二環式ピリジノン |
| JP2015517517A (ja) * | 2012-05-16 | 2015-06-22 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | (特に)アルツハイマー病の治療に有用な置換3,4−ジヒドロ−2H−ピリド[1,2−a]ピラジン−1,6−ジオン誘導体 |
| JP2016531863A (ja) * | 2013-09-27 | 2016-10-13 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Hivインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
| JP2022500406A (ja) * | 2018-09-12 | 2022-01-04 | ノバルティス アーゲー | 抗ウイルス性ピリドピラジンジオン化合物 |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005538184A (ja) * | 2002-09-11 | 2005-12-15 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害剤として有用な8−ヒドロキシ−1−オキソ−テトラヒドロピロロピラジン化合物 |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| CA2568389A1 (en) | 2004-06-09 | 2005-12-22 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US7745459B2 (en) | 2004-09-21 | 2010-06-29 | Japan Tobacco Inc. | Quinolizinone compound and use thereof as HIV integrase inhibitor |
| EP1973906A1 (en) * | 2004-12-23 | 2008-10-01 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
| WO2006088173A1 (ja) * | 2005-02-21 | 2006-08-24 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有する2環性カルバモイルピリドン誘導体 |
| US7547516B2 (en) | 2005-03-10 | 2009-06-16 | Gen-Probe Incorporated | Method for reducing the presence of amplification inhibitors in a reaction receptacle |
| ES2567197T3 (es) * | 2005-04-28 | 2016-04-20 | Viiv Healthcare Company | Derivado de carbamoilpiridona policíclico que tiene actividad inhibidora de la integrasa del VIH |
| PH12012502411A1 (en) | 2005-05-10 | 2019-07-17 | Intermune Inc | Method of modulating stress-activated protein kinase system |
| KR20080064182A (ko) | 2005-10-27 | 2008-07-08 | 시오노기세야쿠 가부시키가이샤 | Hiv 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체 |
| AU2006306355A1 (en) * | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| CA2726588C (en) | 2008-06-03 | 2019-04-16 | Karl Kossen | Compounds and methods for treating inflammatory and fibrotic disorders |
| CN103951643B (zh) | 2008-07-25 | 2015-12-09 | 盐野义制药株式会社 | 用作hiv整合酶抑制剂的化合物 |
| EP2376453B1 (en) | 2008-12-11 | 2019-11-20 | VIIV Healthcare Company | Intermediates for carbamoylpyridone hiv integrase inhibitors |
| MX2011006241A (es) | 2008-12-11 | 2011-06-28 | Shionogi & Co | Sintesis de inhibidores de integrasa de vih de carbamoil-piridona e intermediarios. |
| TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
| PE20130010A1 (es) | 2010-02-26 | 2013-02-05 | Japan Tobacco Inc | Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina como inhibidor de la integrasa del vih |
| TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
| RU2608519C2 (ru) | 2010-09-24 | 2017-01-19 | Шионоги энд Ко. Лтд. | Пролекарственная форма замещенного полициклического производного карбамоилпиридона |
| US9359300B2 (en) | 2010-12-06 | 2016-06-07 | Confluence Life Sciences, Inc. | Methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds |
| PL2648516T3 (pl) | 2010-12-06 | 2019-04-30 | Aclaris Therapeutics Inc | Podstawione związki pirydynono-pirydynylowe |
| EP2670722B1 (en) * | 2011-01-31 | 2016-10-12 | Council of Scientific & Industrial Research | Chiral 1-(4-methylphenylmethyl)-5-oxo-{n-[(3-t-butoxycarbonyl-aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion |
| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| ES2608356T3 (es) | 2012-12-20 | 2017-04-10 | Janssen Pharmaceutica Nv | Novedosos derivados tricíclicos de 3,4-dihidro-2H-pirido[1,2-a]pirazin-1,6-diona como moduladores de la secretasa gamma |
| DK3067358T3 (da) | 2012-12-21 | 2019-11-04 | Gilead Sciences Inc | Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse |
| AU2014206834B2 (en) | 2013-01-17 | 2017-06-22 | Janssen Pharmaceutica Nv | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| WO2014172188A2 (en) * | 2013-04-16 | 2014-10-23 | Merck Sharp & Dohme Corp. | 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors |
| HRP20210813T1 (hr) | 2013-06-07 | 2021-06-25 | Aclaris Therapeutics, Inc. | Piridinonpiridinilni spojevi supstituirani s metil/fluorpiridinilmetoksi i piridinonpiridinilni spojevi supstituirani s fluorpirimidinilmetoksi |
| NO2865735T3 (enExample) | 2013-07-12 | 2018-07-21 | ||
| LT3019503T (lt) | 2013-07-12 | 2017-11-27 | Gilead Sciences, Inc. | Policikliniai karbamoilpiridono junginiai ir jų panaudojimas živ infekcijų gydymui |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| KR102373700B1 (ko) | 2014-04-02 | 2022-03-11 | 인터뮨, 인크. | 항섬유성 피리디논 |
| NO2717902T3 (enExample) | 2014-06-20 | 2018-06-23 | ||
| TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| EP3166951A1 (en) * | 2014-07-07 | 2017-05-17 | Savira Pharmaceuticals GmbH | Dihydropyridopyrazine-1,8-diones and their use in the treatment, amelioration or prevention of viral diseases |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| KR102000382B1 (ko) | 2015-02-03 | 2019-07-15 | 화이자 인코포레이티드 | 신규 시클로프로파벤조푸라닐 피리도피라진디온 |
| US9630978B2 (en) | 2015-04-02 | 2017-04-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| SI3346995T1 (sl) | 2015-11-09 | 2019-11-29 | Gilead Sciences Inc | Terapevtski sestavek za zdravljenje virusa človeške imunske pomanjkljivosti |
| EA202092921A1 (ru) | 2018-05-31 | 2021-04-07 | Сионоги Энд Ко., Лтд. | Полициклическое производное карбамоилпиридона |
| EA202092923A1 (ru) | 2018-05-31 | 2021-04-09 | Сионоги Энд Ко., Лтд. | Полициклическое производное пиридона |
| SG11202110045PA (en) * | 2019-03-20 | 2021-10-28 | Wave Life Sciences Ltd | Technologies useful for oligonucleotide preparation |
| CA3172088A1 (en) | 2020-03-27 | 2021-09-30 | Walter Smith | Oral compositions of mk2 pathway inhibitor for treatment of immune conditions |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1625192A (en) | 1991-05-31 | 1992-12-03 | Zeneca Limited | Heterocyclic derivatives |
| US5821241A (en) | 1994-02-22 | 1998-10-13 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| WO2000000478A1 (en) | 1998-06-26 | 2000-01-06 | Bristol-Myers Squibb Pharma Company | Substituted quinoxalin-2(1h)-ones useful as hiv reverse transcriptase inhibitors |
| EE200300145A (et) | 2000-10-12 | 2003-06-16 | Merck & Co., Inc. | Asa- ja polüasanaftalenüülkarboksamiidid ja farmatseutiline kompositsioon |
| CA2425625A1 (en) | 2000-10-12 | 2002-07-18 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| US20050010048A1 (en) | 2000-10-12 | 2005-01-13 | Linghang Zhuang | Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors |
| JP4287649B2 (ja) | 2000-10-12 | 2009-07-01 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類 |
| DE60218511T2 (de) | 2001-10-26 | 2007-10-25 | Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.P.A. | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| MXPA04003932A (es) | 2001-10-26 | 2004-06-18 | Angeletti P Ist Richerche Bio | Inhibidores de la hidroxipirimidinona carboxamida n-sustituida de la integrasa del virus de inmunodeficiencia humana. |
| JP2005538184A (ja) | 2002-09-11 | 2005-12-15 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害剤として有用な8−ヒドロキシ−1−オキソ−テトラヒドロピロロピラジン化合物 |
| EP1725102A4 (en) * | 2004-03-09 | 2009-04-29 | Merck & Co Inc | HIV integrase |
-
2003
- 2003-09-10 WO PCT/US2003/028366 patent/WO2004024078A2/en not_active Ceased
- 2003-09-10 US US10/526,275 patent/US7517532B2/en not_active Expired - Fee Related
- 2003-09-10 JP JP2004536438A patent/JP2006506352A/ja not_active Withdrawn
- 2003-09-10 AU AU2003267098A patent/AU2003267098B2/en not_active Ceased
- 2003-09-10 EP EP03749574A patent/EP1549315A4/en not_active Withdrawn
- 2003-09-10 CA CA002498111A patent/CA2498111A1/en not_active Abandoned
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005232103A (ja) * | 2004-02-20 | 2005-09-02 | Nagase & Co Ltd | 光学活性なビシナルジアミンおよびその製造方法 |
| WO2010147068A1 (ja) * | 2009-06-15 | 2010-12-23 | 塩野義製薬株式会社 | 置換された多環性カルバモイルピリドン誘導体 |
| JPWO2010147068A1 (ja) * | 2009-06-15 | 2012-12-06 | 塩野義製薬株式会社 | 置換された多環性カルバモイルピリドン誘導体 |
| JP2014510747A (ja) * | 2011-03-31 | 2014-05-01 | ファイザー・インク | 新規二環式ピリジノン |
| JP2015517517A (ja) * | 2012-05-16 | 2015-06-22 | ヤンセン ファーマシューティカルズ,インコーポレーテッド | (特に)アルツハイマー病の治療に有用な置換3,4−ジヒドロ−2H−ピリド[1,2−a]ピラジン−1,6−ジオン誘導体 |
| JP2016531863A (ja) * | 2013-09-27 | 2016-10-13 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Hivインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
| JP2017105793A (ja) * | 2013-09-27 | 2017-06-15 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Hivインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
| JP2022500406A (ja) * | 2018-09-12 | 2022-01-04 | ノバルティス アーゲー | 抗ウイルス性ピリドピラジンジオン化合物 |
| JP7273951B2 (ja) | 2018-09-12 | 2023-05-15 | ノバルティス アーゲー | 抗ウイルス性ピリドピラジンジオン化合物 |
| JP2024156974A (ja) * | 2018-09-12 | 2024-11-06 | ノバルティス アーゲー | 抗ウイルス性ピリドピラジンジオン化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20060024330A1 (en) | 2006-02-02 |
| US7517532B2 (en) | 2009-04-14 |
| WO2004024078A2 (en) | 2004-03-25 |
| AU2003267098A1 (en) | 2004-04-30 |
| CA2498111A1 (en) | 2004-03-25 |
| WO2004024078A3 (en) | 2004-05-13 |
| AU2003267098B2 (en) | 2008-11-20 |
| EP1549315A4 (en) | 2007-05-23 |
| EP1549315A2 (en) | 2005-07-06 |
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