PE133799A1 - Antagonistas del receptor de trombina - Google Patents
Antagonistas del receptor de trombinaInfo
- Publication number
- PE133799A1 PE133799A1 PE1998001140A PE00114098A PE133799A1 PE 133799 A1 PE133799 A1 PE 133799A1 PE 1998001140 A PE1998001140 A PE 1998001140A PE 00114098 A PE00114098 A PE 00114098A PE 133799 A1 PE133799 A1 PE 133799A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- alcoxi
- compound
- link
- Prior art date
Links
- 239000003856 thrombin receptor antagonist Substances 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 201000006474 Brain Ischemia Diseases 0.000 abstract 1
- 208000003174 Brain Neoplasms Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- 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
- C07D405/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D405/14—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 three or more hetero rings
-
- 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A UN COMPUESTO I, DONDE n ES 0-2; Q ES UN GRUPO a; n1 Y n2 SON 0-2; SI NO EXISTE ENLACE DOBLE Q ES HETEROARILO R-SUSTITUIDO, ARILO R-SUSTITUIDO FUSIONADO; R ES H, ALQUILO C1-C6, -NR16CONR4R5, ENTRE OTROS; R1 Y R2 SON H, ALQUILO C1-C6, FLUOROALQUILO C1-C6, ENTRE OTROS O R1 Y R2 FORMAN JUNTOS =O; R3 ES H, ALCOXI C1-C6, -SOR16, SO2R17, CONR18R19, ENTRE OTROS; HET ES ANILLO HETEROAROMATICO DE 5 A 14 MIEMBROS; R4 Y R5 SON H, ALQUILO C1-C6, FENILO, ENTRE OTROS; O R4 Y R5 FORMAN -(CH2)4-, -(CH2)5-, -(CH2)2NR7-(CH2)2-; R7 ES H o ALQUILO C1-C6; R8, R10, R11 SON R1, OR1; R9 ES H, OH, ALCOXI C1-C6, ENTRE OTROS; B ES -(CH2)n3, -CH2-O-, -CH2NR6-, ENTRE OTROS; n3 ES 0-5; R6 ES H, ALQUILO C1-C6, FENILO; CUANDO EXISTE ENLACE SIMPLE X ES -O-, NR6; Y ES =O, =S, (H,H), (H,OH), (H,ALCOXI C1-C6); CUANDO EL ENLACE SIMPLE NO EXISTE X ES OH, NHR2O; Y ES =O, (H,H), (H,OH), (H,SH), (H,ALCOXI C1-C6); R16 ES ALQUILO C1-C6, FENILO; R17, R18, R19 SON H, ALQUILO C1-C6, FENILO; Z ES -CH2-, -O-, -S(O)(0-2), -CO-, -C(=NOR17)-, ENTRE OTROS; R20 ES H, ALQUILO C1-C6, FENILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN COMPUESTO PREFERIDO DE FORMULA Ia. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR TROMBINA Y PUEDE SER UTIL PARA EL TRATAMIENTO DE TROMBOSIS, ATEROSCLEROSIS, RESTENOSIS, HIPERTENSION, ARRITMIA, INSUFICIENCIA CARDIACA, ISQUEMIA CEREBRAL Y CANCER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97797997A | 1997-11-25 | 1997-11-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE133799A1 true PE133799A1 (es) | 2000-01-10 |
Family
ID=25525702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1998001140A PE133799A1 (es) | 1997-11-25 | 1998-11-23 | Antagonistas del receptor de trombina |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP1036072B1 (es) |
| JP (2) | JP3449620B2 (es) |
| KR (1) | KR100393492B1 (es) |
| CN (2) | CN1290265A (es) |
| AR (1) | AR017189A1 (es) |
| AT (1) | ATE266025T1 (es) |
| AU (1) | AU747204B2 (es) |
| BR (1) | BR9812793A (es) |
| CA (1) | CA2309352C (es) |
| CO (1) | CO4990946A1 (es) |
| CZ (1) | CZ298578B6 (es) |
| DE (1) | DE69823694T2 (es) |
| DK (1) | DK1036072T3 (es) |
| ES (1) | ES2219919T3 (es) |
| HU (1) | HUP0100607A3 (es) |
| ID (1) | ID24726A (es) |
| IL (1) | IL135797A (es) |
| MY (1) | MY140887A (es) |
| NO (1) | NO322022B1 (es) |
| NZ (1) | NZ504218A (es) |
| PE (1) | PE133799A1 (es) |
| PL (1) | PL195027B1 (es) |
| PT (1) | PT1036072E (es) |
| RU (1) | RU2204557C2 (es) |
| SA (1) | SA99190972B1 (es) |
| SK (1) | SK285153B6 (es) |
| TR (1) | TR200001480T2 (es) |
| TW (1) | TWI236476B (es) |
| WO (1) | WO1999026943A1 (es) |
| ZA (1) | ZA9810685B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000229961A (ja) | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト［２，３−ｃ］フラン誘導体およびその製造方法 |
| WO2001017968A1 (en) * | 1999-09-02 | 2001-03-15 | Shionogi & Co., Ltd. | Integrase inhibitors containing aromatic heterocycle derivatives |
| US7235567B2 (en) | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| US7488742B2 (en) * | 2000-06-15 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
| EP1294714B1 (en) * | 2000-06-15 | 2007-08-01 | Schering Corporation | Thrombin receptor antagonists |
| EP1764366A3 (en) * | 2000-06-15 | 2007-10-03 | Schering Corporation | Thrombin receptor antagonists |
| RU2270192C2 (ru) | 2001-04-19 | 2006-02-20 | Эйсай Ко., Лтд. | Производные 2-иминопирролидина |
| CN100369917C (zh) * | 2001-10-18 | 2008-02-20 | 先灵公司 | 作为凝血酶受体拮抗剂的喜巴辛类似物 |
| DE60317493T3 (de) * | 2002-04-16 | 2018-07-12 | Merck Sharp & Dohme Corp. | Trizyklische thrombin rezeptor antagonisten |
| ES2211315B1 (es) * | 2002-11-12 | 2005-10-16 | Almirall Prodesfarma, S.A. | Nuevos compuestos triciclicos. |
| WO2004078721A1 (ja) | 2003-02-19 | 2004-09-16 | Eisai Co., Ltd. | 環状ベンズアミジン誘導体の製造方法 |
| JPWO2005108370A1 (ja) | 2004-04-16 | 2008-03-21 | 味の素株式会社 | ベンゼン化合物 |
| EP1751144B1 (en) * | 2004-05-28 | 2008-08-27 | Schering Corporation | Constrained himbacine analogs as thrombin receptor antagonists |
| RU2408594C2 (ru) * | 2004-10-08 | 2011-01-10 | Шеринг Корпорейшн | Антагонисты рецептора тромбина |
| JP4775971B2 (ja) * | 2005-01-14 | 2011-09-21 | シェーリング コーポレイション | ヒンバシンアナログのエキソ−選択的合成 |
| CN102757423B (zh) * | 2005-01-14 | 2016-04-20 | 先灵公司 | 喜巴辛类似物的外型和非对映立体选择合成 |
| CA2594741A1 (en) * | 2005-01-14 | 2006-07-20 | Schering Corporation | Synthesis of himbacine analogs |
| TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
| EP2069326B1 (en) * | 2006-10-04 | 2015-03-18 | Merck Sharp & Dohme Corp. | Bicyclic and tricyclic derivatives as thrombin receptor antagonists |
| WO2011128421A1 (de) | 2010-04-16 | 2011-10-20 | Sanofi | Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren |
| ES2527535T3 (es) | 2010-04-16 | 2015-01-26 | Sanofi | Piridil-vinil-pirazolo-quinolinas como inhibidores de PAR1 |
| CN108658910B (zh) * | 2017-03-29 | 2020-11-03 | 北京新领先医药科技发展有限公司 | 一种沃拉帕沙中间体1-α的制备方法 |
| CN113387947B (zh) * | 2021-07-12 | 2022-07-01 | 中国科学院成都生物研究所 | 调节雌激素受体合成活性的吡唑并吡啶衍生物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773792A (en) | 1968-03-08 | 1973-11-20 | Itt Rayonier Inc | Acetates of plicatic acid and processes for the preparation thereof |
| US4486445A (en) | 1983-01-12 | 1984-12-04 | E. I. Du Pont De Nemours And Company | Justicidin insecticidal and antiviral compounds |
| CA2008116C (en) * | 1989-02-23 | 2001-11-20 | Thomas Weller | Glycine derivatives |
| IL106197A (en) * | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
-
1998
- 1998-11-23 WO PCT/US1998/024523 patent/WO1999026943A1/en not_active Ceased
- 1998-11-23 CO CO98068933A patent/CO4990946A1/es unknown
- 1998-11-23 EP EP98958039A patent/EP1036072B1/en not_active Expired - Lifetime
- 1998-11-23 AT AT98958039T patent/ATE266025T1/de not_active IP Right Cessation
- 1998-11-23 ID IDW20000993A patent/ID24726A/id unknown
- 1998-11-23 ZA ZA9810685A patent/ZA9810685B/xx unknown
- 1998-11-23 PL PL98341114A patent/PL195027B1/pl not_active IP Right Cessation
- 1998-11-23 PE PE1998001140A patent/PE133799A1/es not_active Application Discontinuation
- 1998-11-23 AR ARP980105935A patent/AR017189A1/es active IP Right Grant
- 1998-11-23 KR KR10-2000-7005679A patent/KR100393492B1/ko not_active Expired - Fee Related
- 1998-11-23 IL IL13579798A patent/IL135797A/xx not_active IP Right Cessation
- 1998-11-23 HU HU0100607A patent/HUP0100607A3/hu unknown
- 1998-11-23 PT PT98958039T patent/PT1036072E/pt unknown
- 1998-11-23 DE DE69823694T patent/DE69823694T2/de not_active Expired - Lifetime
- 1998-11-23 CZ CZ20001856A patent/CZ298578B6/cs not_active IP Right Cessation
- 1998-11-23 JP JP2000522101A patent/JP3449620B2/ja not_active Expired - Fee Related
- 1998-11-23 TR TR2000/01480T patent/TR200001480T2/xx unknown
- 1998-11-23 CN CN98813307A patent/CN1290265A/zh active Pending
- 1998-11-23 BR BR9812793-4A patent/BR9812793A/pt not_active Application Discontinuation
- 1998-11-23 CA CA002309352A patent/CA2309352C/en not_active Expired - Fee Related
- 1998-11-23 RU RU2000116548/04A patent/RU2204557C2/ru not_active IP Right Cessation
- 1998-11-23 AU AU14158/99A patent/AU747204B2/en not_active Ceased
- 1998-11-23 SK SK759-2000A patent/SK285153B6/sk not_active IP Right Cessation
- 1998-11-23 NZ NZ504218A patent/NZ504218A/en unknown
- 1998-11-23 TW TW087119396A patent/TWI236476B/zh not_active IP Right Cessation
- 1998-11-23 DK DK98958039T patent/DK1036072T3/da active
- 1998-11-23 CN CNA2008100835852A patent/CN101274929A/zh active Pending
- 1998-11-23 ES ES98958039T patent/ES2219919T3/es not_active Expired - Lifetime
- 1998-11-24 MY MYPI98005330A patent/MY140887A/en unknown
-
1999
- 1999-01-10 SA SA99190972A patent/SA99190972B1/ar unknown
-
2000
- 2000-05-24 NO NO20002659A patent/NO322022B1/no not_active IP Right Cessation
-
2002
- 2002-10-29 JP JP2002315015A patent/JP2003128670A/ja not_active Withdrawn
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