JP6523461B2 - １７β−ＨＳＤ１−阻害剤のプロドラッグ - Google Patents
１７β−ＨＳＤ１−阻害剤のプロドラッグ Download PDFInfo
- Publication number
- JP6523461B2 JP6523461B2 JP2017533569A JP2017533569A JP6523461B2 JP 6523461 B2 JP6523461 B2 JP 6523461B2 JP 2017533569 A JP2017533569 A JP 2017533569A JP 2017533569 A JP2017533569 A JP 2017533569A JP 6523461 B2 JP6523461 B2 JP 6523461B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- methyl
- decahydro
- cyclopenta
- methylthiazol
- 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.)
- Active
Links
- AHOJHUQRRYNNQK-IPEDDGMGSA-N CC(CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CC3)C1=C(CC(Cl)=C1O)C3=C1Cl)/C2=N/OC Chemical compound CC(CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CC3)C1=C(CC(Cl)=C1O)C3=C1Cl)/C2=N/OC AHOJHUQRRYNNQK-IPEDDGMGSA-N 0.000 description 1
- LTOBWULSPQOODY-UKRYKFHKSA-N CC(CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3cc(Br)c4O)C2=O Chemical compound CC(CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3cc(Br)c4O)C2=O LTOBWULSPQOODY-UKRYKFHKSA-N 0.000 description 1
- MJISNQSHIYISHR-VZRRMLPQSA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3cc(N)c4O)C2=O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3cc(N)c4O)C2=O MJISNQSHIYISHR-VZRRMLPQSA-N 0.000 description 1
- SHENHPUEPSSUEQ-JDBGQIMMSA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3ccc4O)/C2=N/O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3ccc4O)/C2=N/O SHENHPUEPSSUEQ-JDBGQIMMSA-N 0.000 description 1
- QYFBVEIPJPOCKA-WJTCXCBESA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3ccc4OC(C1NCCC1)=O)/C2=N/OC Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4)C1c3ccc4OC(C1NCCC1)=O)/C2=N/OC QYFBVEIPJPOCKA-WJTCXCBESA-N 0.000 description 1
- KIPQOYJRWWGQTK-IGGGATHQSA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4Br)C1c3ccc4OP(O)(O)=O)C2=O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4Br)C1c3ccc4OP(O)(O)=O)C2=O KIPQOYJRWWGQTK-IGGGATHQSA-N 0.000 description 1
- MSWKAXLKIVADDA-MHNWBSPISA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4Cl)C1c3cc([N+]([O-])=O)c4O)C2=O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4Cl)C1c3cc([N+]([O-])=O)c4O)C2=O MSWKAXLKIVADDA-MHNWBSPISA-N 0.000 description 1
- JSSHTKVXODCHTG-MHNWBSPISA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4F)C1c3cc([N+]([O-])=O)c4O)C2=O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4F)C1c3cc([N+]([O-])=O)c4O)C2=O JSSHTKVXODCHTG-MHNWBSPISA-N 0.000 description 1
- XWDQEWFLKZSAOO-MHNWBSPISA-N C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4[N+]([O-])=O)C1c3cc([N+]([O-])=O)c4O)C2=O Chemical compound C[C@](CC1)(C([C@H](CCC(Nc2ncc(C)[s]2)=O)C2)C(CCc3c4[N+]([O-])=O)C1c3cc([N+]([O-])=O)c4O)C2=O XWDQEWFLKZSAOO-MHNWBSPISA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
- A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Ophthalmology & Optometry (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FI20146150 | 2014-12-23 | ||
| FI20146150 | 2014-12-23 | ||
| PCT/FI2015/050930 WO2016102776A1 (en) | 2014-12-23 | 2015-12-22 | Prodrugs of 17.beta.-hsd1 -inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018501266A JP2018501266A (ja) | 2018-01-18 |
| JP2018501266A5 JP2018501266A5 (enExample) | 2019-01-17 |
| JP6523461B2 true JP6523461B2 (ja) | 2019-06-05 |
Family
ID=55221442
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017533569A Active JP6523461B2 (ja) | 2014-12-23 | 2015-12-22 | １７β−ＨＳＤ１−阻害剤のプロドラッグ |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10413557B2 (enExample) |
| EP (1) | EP3237431B1 (enExample) |
| JP (1) | JP6523461B2 (enExample) |
| CN (1) | CN107207561B (enExample) |
| WO (1) | WO2016102776A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3237430B1 (en) * | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | PRODRUGS OF 17ß -HSD1 -INHIBITORS |
| LT3634975T (lt) | 2017-06-08 | 2024-06-25 | Organon R&D Finland Ltd | 15.beta.-[3-propanamido]-pakeisti estra-1,3,5(10)-trien-17-onų 17-oksimai, skirti 17.beta.-hidroksisteroidų dehidrogenazių slopinimui |
| WO2023122075A1 (en) * | 2021-12-20 | 2023-06-29 | Ohio State Innovation Foundation | Compositions comprising sterol-amino-phosphate compounds and methods of making and use thereof |
| WO2025185710A1 (zh) * | 2024-03-08 | 2025-09-12 | 长春金赛药业有限责任公司 | 17β-HSD1抑制剂化合物、药物组合物及其应用 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2000125533A (ru) | 1998-03-11 | 2002-10-20 | Эндорешерш, Инк. (Ca) | Ингибиторы 17-бета-гидроксистероиддегидрогеназ 5 и 3 типа и способы их применения |
| DE69935335T2 (de) | 1998-08-07 | 2007-11-22 | Novartis Vaccines and Diagnostics, Inc., Emeryville | Pyrazole als modulatoren des östrogenrezeptors |
| GB9929302D0 (en) | 1999-12-11 | 2000-02-02 | Univ Cardiff | Benzyl tetralins compositions and uses thereof |
| AU2002326823B2 (en) | 2001-09-06 | 2005-12-15 | Merck Sharp & Dohme Corp. | 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases |
| ES2347643T3 (es) | 2001-10-17 | 2010-11-03 | Schering Corporation | Piperin- y piperazinacetamidas como inhibidores de 17beta hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgenos. |
| US6750248B2 (en) | 2001-11-09 | 2004-06-15 | National University Of Singapore | Methods for preparing an estrogenic preparation and isolated estrogenic compounds from a plant and uses thereof |
| DE60332862D1 (de) | 2002-11-18 | 2010-07-15 | Schering Corp | 17beta-hydroxysteroid dehydrogenase typ-3 hemmer zur behandlung von androgen abhängigen erkrankungen |
| CN1744930A (zh) | 2002-12-17 | 2006-03-08 | 先灵公司 | 治疗雄激素依赖性疾病的3型17β－羟基类固醇脱氢酶抑制剂 |
| US7015211B2 (en) | 2003-03-21 | 2006-03-21 | Yale University | 15α-substituted estradiol carboxylic acid esters as locally active estrogens |
| GB0306718D0 (en) * | 2003-03-24 | 2003-04-30 | Sterix Ltd | Compound |
| US7465739B2 (en) | 2003-06-10 | 2008-12-16 | Solvay Pharmaceuticals B.V. | Compounds and their use in therapy |
| US7754709B2 (en) | 2003-06-10 | 2010-07-13 | Solvay Pharmaceuticals Bv | Tetracyclic thiophenepyrimidinone compounds as inhibitors of 17β hydroxysteroid dehydrogenase compounds |
| US8088758B2 (en) | 2003-11-12 | 2012-01-03 | Abbott Products Gmbh | 17β-hydroxysteroid dehydrogenase type I inhibitors |
| TWI331154B (en) | 2003-11-12 | 2010-10-01 | Solvay Pharm Gmbh | Novel 17-hydroxysteroid dehydrogenase type i inhibitors |
| US7378426B2 (en) | 2004-03-01 | 2008-05-27 | Bristol-Myers Squibb Company | Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3 |
| DE102004032673A1 (de) | 2004-07-02 | 2006-01-26 | Schering Ag | Neue 2-substituierte D-Homo-estra-1,3,5(10)-triene als Inhibitoren der 17ß-Hydroxysteroiddehydrogenase Typ 1 |
| DE102004032674A1 (de) | 2004-07-02 | 2006-01-26 | Schering Ag | Neue 2-substituierte Estra-1,3,5(10)-trien-17-one als Inhibitoren der 17β-Hydroxysteroiddehydrogenase Typ 1 |
| UA89964C2 (ru) | 2004-09-08 | 2010-03-25 | Н.В. Органон | 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ |
| AU2006251154B2 (en) | 2005-05-26 | 2012-06-28 | Solvay Pharmaceuticals Gmbh | 17beta-HSD1 and STS inhibitors |
| US8030298B2 (en) | 2005-05-26 | 2011-10-04 | Abbott Products Gmbh | 17β-HSD1 and STS inhibitors |
| RU2469042C2 (ru) | 2006-09-19 | 2012-12-10 | Зольвай Фармасьютиклз Гмбх | Терапевтически активные триазолы и их использование |
| CN101568547B (zh) | 2006-11-30 | 2014-06-25 | 索尔瓦药物有限公司 | 作为17βHSD抑制剂的被取代的雌三烯衍生物 |
| BR112015031846A8 (pt) * | 2013-06-25 | 2018-03-06 | Forendo Pharma Ltd | derivados de estratrientiazol, seus usos, e composição farmacêutica |
| US9850272B2 (en) | 2013-06-25 | 2017-12-26 | Forendo Pharma Ltd. | Therapeutically active estratrienthiazole derivatives as inhibitors of 17.beta-hydroxy-steroid dehydrogenase, type 1 |
| TW201512215A (zh) | 2013-06-25 | 2015-04-01 | Forendo Pharma Ltd | 治療活性雌三烯噻唑衍生物 |
| EP3237430B1 (en) * | 2014-12-23 | 2019-03-20 | Forendo Pharma Ltd | PRODRUGS OF 17ß -HSD1 -INHIBITORS |
-
2015
- 2015-12-22 US US15/539,184 patent/US10413557B2/en active Active
- 2015-12-22 JP JP2017533569A patent/JP6523461B2/ja active Active
- 2015-12-22 EP EP15828340.8A patent/EP3237431B1/en active Active
- 2015-12-22 WO PCT/FI2015/050930 patent/WO2016102776A1/en not_active Ceased
- 2015-12-22 CN CN201580074140.6A patent/CN107207561B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018501266A (ja) | 2018-01-18 |
| US10413557B2 (en) | 2019-09-17 |
| WO2016102776A1 (en) | 2016-06-30 |
| US20170354664A1 (en) | 2017-12-14 |
| CN107207561A (zh) | 2017-09-26 |
| EP3237431B1 (en) | 2019-03-20 |
| EP3237431A1 (en) | 2017-11-01 |
| CN107207561B (zh) | 2020-03-31 |
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