BRPI0408704A - benzil-piridazinonas como inibidores de transcriptase reversa - Google Patents
benzil-piridazinonas como inibidores de transcriptase reversaInfo
- Publication number
- BRPI0408704A BRPI0408704A BRPI0408704-6A BRPI0408704A BRPI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A BR PI0408704 A BRPI0408704 A BR PI0408704A
- Authority
- BR
- Brazil
- Prior art keywords
- reverse transcriptase
- formula
- compounds
- transcriptase inhibitors
- pyridazinones
- Prior art date
Links
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 title abstract 2
- GZVJKNAPQDHVHH-UHFFFAOYSA-N 5-benzyl-1h-pyridazin-6-one Chemical class O=C1NN=CC=C1CC1=CC=CC=C1 GZVJKNAPQDHVHH-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 3
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical class OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- 108010092799 RNA-directed DNA polymerase Proteins 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 239000003981 vehicle Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/14—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/22—Nitrogen and oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
"BENZIL-PIRIDAZINONAS COMO INIBIDORES DE TRANSCRIPTASE REVERSA". Esta invenção refere-se a derivados de piridazinonas inusitados, da fórmula I, onde R¬ 1¬-R¬ 4¬, R¬ 7¬, R¬ 8¬ e X¬ 1¬ são como definidos no sumário, e seus sais e solvatos farmaceuticamente aceitáveis, e métodos para inibir ou modular a trasncriptase reversa do Vírus da Imunodeficiência Humana (HIV) com compostos da fórmula I, composições farmacêuticas que contêm os compostos da fórmula I misturados com pelo menos um solvente, veículo ou excipiente, e processos para preparar compostos da fórmula I. Os compostos são úteis para tratar distúrbios nos quais HIV e vírus geneticamente relacionados estão implicados.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45714403P | 2003-03-24 | 2003-03-24 | |
| PCT/EP2004/002736 WO2004085406A1 (en) | 2003-03-24 | 2004-03-17 | Benzyl-pyridazinons as reverse transcriptase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0408704A true BRPI0408704A (pt) | 2006-03-07 |
Family
ID=33098202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0408704-6A BRPI0408704A (pt) | 2003-03-24 | 2004-03-17 | benzil-piridazinonas como inibidores de transcriptase reversa |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US7189718B2 (pt) |
| EP (1) | EP1608629A1 (pt) |
| JP (1) | JP4485520B2 (pt) |
| KR (1) | KR20050119652A (pt) |
| CN (1) | CN100469769C (pt) |
| AR (1) | AR043674A1 (pt) |
| AU (1) | AU2004224191A1 (pt) |
| BR (1) | BRPI0408704A (pt) |
| CA (1) | CA2518823A1 (pt) |
| MX (1) | MXPA05010081A (pt) |
| RU (1) | RU2344128C2 (pt) |
| TW (1) | TW200505453A (pt) |
| WO (1) | WO2004085406A1 (pt) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0102299D0 (sv) | 2001-06-26 | 2001-06-26 | Astrazeneca Ab | Compounds |
| SE0102764D0 (sv) | 2001-08-17 | 2001-08-17 | Astrazeneca Ab | Compounds |
| ES2232306B1 (es) * | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
| WO2005090317A1 (en) * | 2004-03-23 | 2005-09-29 | F.Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| WO2005100323A1 (en) * | 2004-04-15 | 2005-10-27 | F. Hoffmann-La Roche Ag | Process for preparing pyridazinone compounds |
| US7700640B2 (en) * | 2004-10-16 | 2010-04-20 | Astrazeneca Ab | Process for making phenoxy benzamide compounds |
| GB0423042D0 (en) * | 2004-10-16 | 2004-11-17 | Astrazeneca Ab | Chemical process |
| EP1863777A1 (en) * | 2005-03-24 | 2007-12-12 | F.Hoffmann-La Roche Ag | 1,2,4 -triazole-5-one compounds as heterocyclic reverse transcriptase inhibitors |
| JP4651714B2 (ja) | 2005-07-09 | 2011-03-16 | アストラゼネカ アクチボラグ | 糖尿病の治療においてglk活性化剤として使用するためのヘテロアリールベンズアミド誘導体 |
| CN101228135B (zh) * | 2005-07-21 | 2011-08-31 | 霍夫曼-拉罗奇有限公司 | 作为甲状腺激素受体激动剂的哒嗪酮衍生物 |
| AR057455A1 (es) | 2005-07-22 | 2007-12-05 | Merck & Co Inc | Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica |
| EP1937651B1 (en) * | 2005-09-30 | 2008-12-24 | F.Hoffmann-La Roche Ag | Nnrt inhibitors |
| CA2625047A1 (en) | 2005-10-19 | 2007-04-26 | F. Hoffmann-La Roche Ag | Phenyl-acetamide nnrt inhibitors |
| JO2769B1 (en) | 2005-10-26 | 2014-03-15 | جانسين فارماسوتيكا ان. في | Rapid decomposition of physiologically antagonistic agents of the 2-dopamine receptor |
| GB0610680D0 (en) * | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
| CL2007002105A1 (es) * | 2006-07-21 | 2008-02-22 | Hoffmann La Roche | Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u |
| WO2008019968A1 (en) * | 2006-08-16 | 2008-02-21 | F. Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| JO2849B1 (en) | 2007-02-13 | 2015-03-15 | جانسين فارماسوتيكا ان. في | Dopamine 2 receptor antagonists are rapidly hydrolyzed |
| BRPI0809617A2 (pt) * | 2007-03-29 | 2014-09-16 | Hoffmann La Roche | Inibidores não-nucleosídicos da transcriptase reversa |
| MX2009010932A (es) * | 2007-04-09 | 2009-10-29 | Hoffmann La Roche | Inhibidores no nucleosidos de transcriptasa inversa. |
| CN101663292A (zh) | 2007-04-23 | 2010-03-03 | 詹森药业有限公司 | 作为快速解离的多巴胺2受体拮抗剂的4-烷氧基哒嗪衍生物 |
| MX2009011416A (es) | 2007-04-23 | 2009-11-05 | Janssen Pharmaceutica Nv | Tia(di)azoles como antagonistas del receptor de dopamina 2 de disociacion rapida. |
| AU2008257771B2 (en) | 2007-05-30 | 2015-02-19 | F. Hoffmann-La Roche Ag | Non-nucleoside reverse transcriptase inhibitors |
| JP2010530863A (ja) * | 2007-06-22 | 2010-09-16 | エフ.ホフマン−ラ ロシュ アーゲー | 非ヌクレオシド逆転写酵素阻害剤としての尿素及びカルバマート誘導体 |
| AU2008322676B9 (en) | 2007-11-15 | 2014-03-27 | Msd Italia S.R.L. | Pyridazinone derivatives as PARP inhibitors |
| MX2010005483A (es) | 2007-11-20 | 2010-06-11 | Merck Sharp & Dohme | Inhibidores de transcriptasa inversa no nucleosidos. |
| WO2009067597A1 (en) * | 2007-11-21 | 2009-05-28 | Decode Genetics Ehf | 4- (or 5-) substituted catechol derivatives |
| EP2225239B1 (en) * | 2007-12-21 | 2014-10-22 | F. Hoffmann-La Roche AG | Heterocyclic antiviral compounds |
| AU2009275887B2 (en) | 2008-07-31 | 2013-06-20 | Janssen Pharmaceutica Nv | Piperazin-1-yl-trifluoromethyl-substituted-pyridines as fast dissociating dopamine 2 receptor antagonists |
| AU2009298981B2 (en) | 2008-10-02 | 2012-09-27 | Asahi Kasei Pharma Corporation | 8-substituted isoquinoline derivative and use thereof |
| ME02181B (me) | 2010-03-30 | 2015-10-20 | Merck Canada Inc | Ne-nukleozidni inhibitori reverzne transkriptaze |
| CN102731410B (zh) * | 2012-07-06 | 2014-07-30 | 山东大学 | 一种哒嗪类hiv-1逆转录酶抑制剂的制备与应用 |
| ES2907926T3 (es) | 2012-09-17 | 2022-04-27 | Madrigal Pharmaceuticals Inc | Procedimiento para sintetizar análogos de hormonas tiroideas y polimorfos de los mismos |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| LT3125894T (lt) | 2014-04-01 | 2020-12-10 | Merck Sharp & Dohme Corp. | Živ atvirkštinės transkriptazės inhibitorių provaistai |
| DE102015011861B4 (de) | 2015-09-10 | 2018-03-01 | Rudolf Schindler | Neue cyclische Carboxamide als NMDA NR2B Rezeptor Inhibitoren |
| CN110167557A (zh) | 2016-10-18 | 2019-08-23 | 马德里加尔制药公司 | 用thr-beta兴奋剂治疗肝脏疾病或脂质疾病的方法 |
| CN109053693B (zh) * | 2018-09-20 | 2021-02-05 | 顺毅股份有限公司 | 哒嗪胺类化合物的制备及其应用 |
| MA54549A (fr) | 2018-12-18 | 2022-03-30 | Merck Sharp & Dohme | Dérivés de pyrimidone en tant qu'agents cytotoxiques sélectifs contre des cellules infectées par le vih |
| US20220251021A1 (en) * | 2019-07-01 | 2022-08-11 | Ascentawits Pharmaceuticals, Ltd. | Akr1c3 inhibitor and medical use |
| CN116003253A (zh) * | 2022-12-31 | 2023-04-25 | 上海试四化学品有限公司 | 一种三氟苯嘧啶中间体2-[3-(三氟甲基)苯基]丙二酸二甲酯的制备方法 |
| US12377104B1 (en) | 2024-02-06 | 2025-08-05 | Madrigal Pharmaceuticals, Inc. | Methods for treating a fatty liver disease |
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| US4949314A (en) | 1966-08-16 | 1990-08-14 | The United States Of America As Represented By The Secretary Of The Navy | Method and means for increasing echo-ranging-search rate |
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| US4518584A (en) | 1983-04-15 | 1985-05-21 | Cetus Corporation | Human recombinant interleukin-2 muteins |
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| GB8327880D0 (en) | 1983-10-18 | 1983-11-16 | Ajinomoto Kk | Saccharomyces cerevisiae |
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| US4604377A (en) | 1984-03-28 | 1986-08-05 | Cetus Corporation | Pharmaceutical compositions of microbially produced interleukin-2 |
| US4569790A (en) | 1984-03-28 | 1986-02-11 | Cetus Corporation | Process for recovering microbially produced interleukin-2 and purified recombinant interleukin-2 compositions |
| IL76360A0 (en) | 1984-09-26 | 1986-01-31 | Takeda Chemical Industries Ltd | Mutual separation of proteins |
| GB8501372D0 (en) | 1985-01-18 | 1985-02-20 | Smith Kline French Lab | Chemical compounds |
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| US5204466A (en) | 1990-02-01 | 1993-04-20 | Emory University | Method and compositions for the synthesis of bch-189 and related compounds |
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| US5464933A (en) | 1993-06-07 | 1995-11-07 | Duke University | Synthetic peptide inhibitors of HIV transmission |
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| EP0809490A4 (en) | 1995-02-10 | 1999-10-20 | Smithkline Beecham Corp | USE OF LCK SH2 SPECIFIC COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASES AND ALLOPLASTIC STOPPING REACTIONS |
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| IL117574A0 (en) | 1995-04-03 | 1996-07-23 | Bristol Myers Squibb Co | Processes for the preparation of cyclobutanone derivatives |
| EP0871436A4 (en) | 1995-06-30 | 1999-10-20 | Smithkline Beecham Corp | USE OF STAT 6 SH2 DOMAINE-SPECIFIC COMPOUNDS FOR TREATING ALLERGIC REACTIONS |
| JPH10512585A (ja) | 1995-06-30 | 1998-12-02 | スミスクライン・ビーチャム・コーポレイション | 赤血球形成を増強するためのstat 5 sh2領域特異性化合物の使用 |
| CN1136197C (zh) | 1996-05-30 | 2004-01-28 | 霍夫曼-拉罗奇有限公司 | 新的哒嗪酮衍生物 |
| CN1303378A (zh) * | 1998-04-27 | 2001-07-11 | 国家科研中心 | 3-(氨基-或氨基烷基)吡啶酮衍生物和它们在hiv相关疾病治疗中的用途 |
| WO2001085670A1 (en) | 2000-05-12 | 2001-11-15 | Kissei Pharmaceutical Co., Ltd. | Malonanilic acid derivatives, medicinal compositions containing the same and use thereof |
| GB0024795D0 (en) | 2000-10-10 | 2000-11-22 | Hoffmann La Roche | Pyrazole derivatives for the treatment of viral diseases |
| BRPI0208811B8 (pt) | 2001-04-10 | 2021-05-25 | Pfizer | derivados de pirazol, seu uso e processo de preparação, bem como composição farmacêutica compreendendo os mesmos |
| US7199147B2 (en) | 2001-06-12 | 2007-04-03 | Dainippon Sumitomo Pharma Co., Ltd. | Rho kinase inhibitors |
-
2004
- 2004-03-17 KR KR1020057017745A patent/KR20050119652A/ko not_active Withdrawn
- 2004-03-17 CA CA002518823A patent/CA2518823A1/en not_active Abandoned
- 2004-03-17 BR BRPI0408704-6A patent/BRPI0408704A/pt not_active IP Right Cessation
- 2004-03-17 EP EP04721167A patent/EP1608629A1/en not_active Withdrawn
- 2004-03-17 JP JP2006504704A patent/JP4485520B2/ja not_active Expired - Fee Related
- 2004-03-17 WO PCT/EP2004/002736 patent/WO2004085406A1/en not_active Ceased
- 2004-03-17 RU RU2005132630/04A patent/RU2344128C2/ru active
- 2004-03-17 AU AU2004224191A patent/AU2004224191A1/en not_active Abandoned
- 2004-03-17 MX MXPA05010081A patent/MXPA05010081A/es active IP Right Grant
- 2004-03-17 CN CNB2004800081215A patent/CN100469769C/zh not_active Expired - Fee Related
- 2004-03-18 TW TW093107263A patent/TW200505453A/zh unknown
- 2004-03-22 AR ARP040100938A patent/AR043674A1/es unknown
- 2004-03-23 US US10/807,993 patent/US7189718B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1608629A1 (en) | 2005-12-28 |
| TW200505453A (en) | 2005-02-16 |
| RU2005132630A (ru) | 2006-07-27 |
| AU2004224191A1 (en) | 2004-10-07 |
| JP4485520B2 (ja) | 2010-06-23 |
| RU2344128C2 (ru) | 2009-01-20 |
| US7189718B2 (en) | 2007-03-13 |
| JP2006521310A (ja) | 2006-09-21 |
| KR20050119652A (ko) | 2005-12-21 |
| CA2518823A1 (en) | 2004-10-07 |
| CN1764649A (zh) | 2006-04-26 |
| MXPA05010081A (es) | 2005-11-23 |
| WO2004085406A1 (en) | 2004-10-07 |
| AR043674A1 (es) | 2005-08-03 |
| CN100469769C (zh) | 2009-03-18 |
| US20040198736A1 (en) | 2004-10-07 |
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