CR20160352A - 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer - Google Patents
2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimerInfo
- Publication number
- CR20160352A CR20160352A CR20160352A CR20160352A CR20160352A CR 20160352 A CR20160352 A CR 20160352A CR 20160352 A CR20160352 A CR 20160352A CR 20160352 A CR20160352 A CR 20160352A CR 20160352 A CR20160352 A CR 20160352A
- Authority
- CR
- Costa Rica
- Prior art keywords
- alzheimer
- disease
- tetrahydropiridins
- trifluoro
- amino
- Prior art date
Links
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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D227/00—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
- C07D227/02—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D227/06—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D227/10—Nitrogen atoms not forming part of a nitro radical
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
- C07D417/12—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 chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400086 | 2014-02-19 | ||
| DKPA201400349 | 2014-07-01 | ||
| PCT/EP2015/053327 WO2015124576A1 (en) | 2014-02-19 | 2015-02-17 | 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20160352A true CR20160352A (es) | 2016-10-20 |
Family
ID=59009438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20160352A CR20160352A (es) | 2014-02-19 | 2015-02-17 | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20170066741A1 (Direct) |
| EP (1) | EP3107897A1 (Direct) |
| JP (1) | JP6483146B2 (Direct) |
| KR (1) | KR20160115936A (Direct) |
| CN (1) | CN106029639B (Direct) |
| AP (1) | AP2016009370A0 (Direct) |
| AR (1) | AR099489A1 (Direct) |
| AU (1) | AU2015220873A1 (Direct) |
| CA (1) | CA2940028A1 (Direct) |
| CL (1) | CL2016002072A1 (Direct) |
| CR (1) | CR20160352A (Direct) |
| DO (1) | DOP2016000194A (Direct) |
| EA (1) | EA031132B1 (Direct) |
| EC (1) | ECSP16072941A (Direct) |
| GE (1) | GEP20186892B (Direct) |
| IL (1) | IL246875A0 (Direct) |
| MA (1) | MA39225A1 (Direct) |
| MX (1) | MX2016010777A (Direct) |
| PE (1) | PE20161225A1 (Direct) |
| PH (1) | PH12016501600A1 (Direct) |
| RU (1) | RU2016133626A (Direct) |
| SG (1) | SG11201606812WA (Direct) |
| TW (1) | TW201609700A (Direct) |
| UA (1) | UA117695C2 (Direct) |
| WO (1) | WO2015124576A1 (Direct) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20160352A (es) | 2014-02-19 | 2016-10-20 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| MA40941A (fr) * | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| MX2018001699A (es) * | 2015-08-12 | 2018-05-07 | H Lundbeck As | 2-amino-3-fluoro-3-(fluorometil)-6-meti-6-fenil-3,4,5,6-tetrahidr opiridinas como inhibidores de bace1. |
| EP3702470A3 (en) * | 2015-09-09 | 2020-10-07 | The Trustees of Columbia University in the City of New York | Reduction of er-mam-localized app-c99 and methods of treating alzheimer's disease |
| TW201726651A (zh) * | 2015-09-23 | 2017-08-01 | 健生藥品公司 | ２，３，４，５－四氫吡啶－６－胺衍生物 |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| JP2019536762A (ja) | 2016-10-28 | 2019-12-19 | ハー・ルンドベック・アクチエゼルスカベット | 精神疾患及び／又は認知障害の治療のためのイミダゾピラジノンを含む併用療法 |
| KR20190077349A (ko) | 2016-10-28 | 2019-07-03 | 하. 룬드벡 아크티에셀스카브 | 이미다조피라지논의 투여를 포함하는 병용 치료 |
| WO2018114910A1 (en) | 2016-12-21 | 2018-06-28 | H. Lundbeck A/S | 6-amino-5-fluoro-5-(fluoromethyl)-2,3,4,5-tetrahydropyridin-2-yl-phenyl-5-(methoxy-d3)-pyrazine-2-carboxamides and fluorinated derivatives thereof as bace1 inhibitors |
| CN114748622B (zh) | 2017-10-05 | 2024-09-24 | 弗尔康医疗公司 | P38激酶抑制剂降低dux4和下游基因表达以用于治疗fshd |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| HRP20211784T1 (hr) | 2017-12-14 | 2022-02-18 | H. Lundbeck A/S | Kombinacijski tretmani koji se sastoje od primjene 1h-pirazolo[4,3-b]piridina |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| EP3728250A1 (en) | 2017-12-20 | 2020-10-28 | H. Lundbeck A/S | PYRAZOLO[3,4-beta]PYRIDINES AND IMIDAZO[1,5-beta]PYRIDAZINES AS PDE1 INHIBITORS |
| KR102507861B1 (ko) | 2018-04-19 | 2023-03-09 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
| KR102510077B1 (ko) | 2018-04-24 | 2023-03-14 | 삼성에스디에스 주식회사 | 부채널 공격에 안전한 연산 장치 및 방법 |
| US12042492B2 (en) | 2020-10-09 | 2024-07-23 | Texas Tech University System | BACE1 inhibitory ligand molecules against amyloid beta-induced synaptic and mitochondrial toxicities |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005505506A (ja) * | 2001-06-12 | 2005-02-24 | イーラン ファーマスーティカルズ、インコーポレイテッド | アルツハイマー病の治療に有用な大環状分子 |
| GB0124928D0 (en) * | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| EP1474395B1 (en) * | 2002-02-12 | 2007-10-17 | Smithkline Beecham Corporation | Nicotinamide derivates useful as p38 inhibitors |
| TWI431004B (zh) * | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Ｂａｃｅ抑制劑 |
| EA021240B1 (ru) * | 2010-06-09 | 2015-05-29 | Янссен Фармацевтика Нв | Производные 5,6-дигидро-2h-[1,4]оксазин-3-иламина в качестве ингибиторов бета-секретазы (bace) |
| CA2816285A1 (en) * | 2010-10-29 | 2012-05-03 | Shionogi & Co., Ltd. | Naphthyridine derivative |
| US20130281449A1 (en) * | 2011-01-12 | 2013-10-24 | Novartis Ag | Oxazine Derivatives and their Use in the Treatment of Neurological Disorders |
| CA2824220C (en) * | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| WO2012147763A1 (ja) * | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| JP2014516063A (ja) * | 2011-06-07 | 2014-07-07 | エフ．ホフマン−ラ ロシュ アーゲー | Ｂａｃｅ１及び／又はｂａｃｅ２阻害剤としてのハロゲン−アルキル−１，３オキサジン |
| UY34278A (es) * | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US8338413B1 (en) * | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| EP2827857A4 (en) | 2012-03-20 | 2016-03-30 | Elan Pharm Inc | SPIROCYCLIC DIHYDRO-THIAZINE AND INHIBITORS OF BACE DIHYDRO-OXAZINE AND COMPOSITIONS AND USES THEREOF |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| US9540359B2 (en) | 2012-10-24 | 2017-01-10 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| CR20160352A (es) | 2014-02-19 | 2016-10-20 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物 |
-
2015
- 2015-02-17 CR CR20160352A patent/CR20160352A/es unknown
- 2015-02-17 CA CA2940028A patent/CA2940028A1/en not_active Abandoned
- 2015-02-17 AP AP2016009370A patent/AP2016009370A0/en unknown
- 2015-02-17 WO PCT/EP2015/053327 patent/WO2015124576A1/en not_active Ceased
- 2015-02-17 SG SG11201606812WA patent/SG11201606812WA/en unknown
- 2015-02-17 MA MA39225A patent/MA39225A1/fr unknown
- 2015-02-17 CN CN201580009034.XA patent/CN106029639B/zh not_active Expired - Fee Related
- 2015-02-17 US US15/119,639 patent/US20170066741A1/en not_active Abandoned
- 2015-02-17 EP EP15707304.0A patent/EP3107897A1/en not_active Withdrawn
- 2015-02-17 AU AU2015220873A patent/AU2015220873A1/en not_active Abandoned
- 2015-02-17 MX MX2016010777A patent/MX2016010777A/es unknown
- 2015-02-17 UA UAA201608414A patent/UA117695C2/uk unknown
- 2015-02-17 PE PE2016001299A patent/PE20161225A1/es not_active Application Discontinuation
- 2015-02-17 EA EA201691447A patent/EA031132B1/ru not_active IP Right Cessation
- 2015-02-17 KR KR1020167021930A patent/KR20160115936A/ko not_active Withdrawn
- 2015-02-17 RU RU2016133626A patent/RU2016133626A/ru not_active Application Discontinuation
- 2015-02-17 GE GEAP201514248A patent/GEP20186892B/en unknown
- 2015-02-17 JP JP2016551851A patent/JP6483146B2/ja not_active Expired - Fee Related
- 2015-02-17 TW TW104105281A patent/TW201609700A/zh unknown
- 2015-02-18 AR ARP150100475A patent/AR099489A1/es unknown
- 2015-02-19 US US14/625,658 patent/US9353084B2/en not_active Expired - Fee Related
-
2016
- 2016-07-21 IL IL246875A patent/IL246875A0/en unknown
- 2016-07-28 DO DO2016000194A patent/DOP2016000194A/es unknown
- 2016-08-11 PH PH12016501600A patent/PH12016501600A1/en unknown
- 2016-08-17 CL CL2016002072A patent/CL2016002072A1/es unknown
- 2016-09-09 EC ECIEPI201672941A patent/ECSP16072941A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20170066741A1 (en) | 2017-03-09 |
| CN106029639A (zh) | 2016-10-12 |
| WO2015124576A1 (en) | 2015-08-27 |
| AU2015220873A1 (en) | 2016-08-11 |
| US9353084B2 (en) | 2016-05-31 |
| DOP2016000194A (es) | 2016-09-30 |
| GEP20186892B (en) | 2018-09-10 |
| MA39225A1 (fr) | 2017-04-28 |
| AP2016009370A0 (en) | 2016-08-31 |
| MX2016010777A (es) | 2016-10-26 |
| RU2016133626A3 (Direct) | 2018-09-25 |
| EP3107897A1 (en) | 2016-12-28 |
| IL246875A0 (en) | 2016-08-31 |
| EA031132B1 (ru) | 2018-11-30 |
| JP2017506237A (ja) | 2017-03-02 |
| PE20161225A1 (es) | 2016-12-04 |
| US20150232449A1 (en) | 2015-08-20 |
| CN106029639B (zh) | 2019-01-08 |
| AR099489A1 (es) | 2016-07-27 |
| RU2016133626A (ru) | 2018-03-20 |
| CL2016002072A1 (es) | 2017-01-20 |
| SG11201606812WA (en) | 2016-09-29 |
| KR20160115936A (ko) | 2016-10-06 |
| TW201609700A (zh) | 2016-03-16 |
| ECSP16072941A (es) | 2017-02-24 |
| CA2940028A1 (en) | 2015-08-27 |
| EA201691447A1 (ru) | 2016-12-30 |
| JP6483146B2 (ja) | 2019-03-13 |
| UA117695C2 (uk) | 2018-09-10 |
| PH12016501600A1 (en) | 2017-02-06 |
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