PE20230114A1 - Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinas - Google Patents
Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinasInfo
- Publication number
- PE20230114A1 PE20230114A1 PE2022001313A PE2022001313A PE20230114A1 PE 20230114 A1 PE20230114 A1 PE 20230114A1 PE 2022001313 A PE2022001313 A PE 2022001313A PE 2022001313 A PE2022001313 A PE 2022001313A PE 20230114 A1 PE20230114 A1 PE 20230114A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- compound
- preparation
- application
- protein degradation
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title 1
- 230000017854 proteolysis Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 102000001307 androgen receptors Human genes 0.000 abstract 2
- 108010080146 androgen receptors Proteins 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 230000003287 optical effect Effects 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 230000015556 catabolic process Effects 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 238000006731 degradation reaction Methods 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
Referida a un compuesto representado por la formula (I), un isomero optico del mismo o una sal farmacologicamente aceptable del mismo, caracterizado porque X es C(R) o N; T1, T2, T3 y T4 son C(R) o N; T5 es -(C=O)- o -CH2-; R1, R2, R3 y R4 son CN, halogeno, alquilo de C1-6, alcoxi de C1-6, entre otros; L1, L2 y L3 son O, S, NH, C(=O), entre otros. Tambien se refiere a un compuesto representado por la formula (II), un isomero optico del mismo o una sal farmacologicamente aceptable del mismo, caracterizado porque el anillo A y el anillo B son un heterocicloalquilo 5 de 3 a 8 miembros, heteroarilo de 5 a 6 miembros o ausente, y el heterocicloalquilo de 3 a 8 miembros o el heteroarilo de 5 a 6 miembros es opcionalmente sustituido por 1, 2 o 3 R; R1, R2, R3 y R4 son CN, halogeno, alquilo de C1-6, alcoxi de C1-6, entre otros; X es C(R) o N; T1, T2, T3 y T4 son C(R) o N; T5 es -(C=O)- o -CH2-; L2 es un enlace sencillo, O, S, NH, C(=O), S(=O), entre otros; R es H, F, Cl, Br, I, OH o alquilo de C1-6; R5 es H, halogeno o alquilo de C1-6. Dichos compuestos son utiles en la degradacion del receptor de androgenos (AR).
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201911342649 | 2019-12-23 | ||
CN202010200682 | 2020-03-20 | ||
CN202010496353 | 2020-06-03 | ||
CN202011486334 | 2020-12-16 | ||
PCT/CN2020/138572 WO2021129653A1 (zh) | 2019-12-23 | 2020-12-23 | 一种蛋白降解剂化合物的制备方法和应用 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20230114A1 true PE20230114A1 (es) | 2023-01-27 |
Family
ID=76573691
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022001313A PE20230114A1 (es) | 2019-12-23 | 2020-12-23 | Metodo y aplicacion de preparacion de compuesto como agente de degradacion de proteinas |
Country Status (18)
Country | Link |
---|---|
US (1) | US20230111119A1 (es) |
EP (1) | EP4083020A4 (es) |
JP (1) | JP2023508097A (es) |
KR (1) | KR20220120629A (es) |
CN (2) | CN113087704B (es) |
AU (1) | AU2020414151A1 (es) |
BR (1) | BR112022012385A2 (es) |
CA (1) | CA3162523A1 (es) |
CL (1) | CL2022001724A1 (es) |
CO (1) | CO2022010305A2 (es) |
EC (1) | ECSP22056811A (es) |
IL (1) | IL294225A (es) |
JO (1) | JOP20220159A1 (es) |
MX (1) | MX2022007885A (es) |
PE (1) | PE20230114A1 (es) |
TW (1) | TWI755992B (es) |
WO (1) | WO2021129653A1 (es) |
ZA (1) | ZA202208051B (es) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US11883393B2 (en) | 2019-12-19 | 2024-01-30 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
BR112022025057A2 (pt) | 2020-06-12 | 2023-01-31 | Shanghai Jemincare Pharmaceuticals Co Ltd | Composto de ftalazinona e método de preparação do mesmo e uso médico do mesmo |
IL309666A (en) | 2021-07-09 | 2024-02-01 | Plexium Inc | Aryl compounds and pharmaceutical preparations that modulate IKZF2 |
WO2024002205A1 (en) * | 2022-06-30 | 2024-01-04 | Anhorn Medicines Co., Ltd. | Bifunctional compound and pharmaceutical composition comprising the bifunctional compound, and method for treating androgen receptor related disease by using the same |
WO2024012570A1 (zh) * | 2022-07-15 | 2024-01-18 | 西藏海思科制药有限公司 | 一种含氮杂环衍生物及其组合物和药学上的应用 |
US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20180228907A1 (en) * | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
KR20200052995A (ko) * | 2015-01-20 | 2020-05-15 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
DK3660004T3 (da) * | 2016-10-11 | 2023-05-08 | Arvinas Operations Inc | Forbindelser og fremgangsmåder til målrettet degradering af androgenreceptor |
AU2017363257B2 (en) * | 2016-11-22 | 2021-08-19 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with E3 ligase ligand and methods of use |
CA3042297A1 (en) * | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
-
2020
- 2020-12-23 CN CN202011545626.2A patent/CN113087704B/zh active Active
- 2020-12-23 CA CA3162523A patent/CA3162523A1/en active Pending
- 2020-12-23 TW TW109145818A patent/TWI755992B/zh active
- 2020-12-23 IL IL294225A patent/IL294225A/en unknown
- 2020-12-23 CN CN202080087926.2A patent/CN114829342A/zh active Pending
- 2020-12-23 PE PE2022001313A patent/PE20230114A1/es unknown
- 2020-12-23 AU AU2020414151A patent/AU2020414151A1/en active Pending
- 2020-12-23 US US17/788,154 patent/US20230111119A1/en active Pending
- 2020-12-23 BR BR112022012385A patent/BR112022012385A2/pt unknown
- 2020-12-23 MX MX2022007885A patent/MX2022007885A/es unknown
- 2020-12-23 EP EP20908128.0A patent/EP4083020A4/en active Pending
- 2020-12-23 KR KR1020227025429A patent/KR20220120629A/ko active Search and Examination
- 2020-12-23 WO PCT/CN2020/138572 patent/WO2021129653A1/zh unknown
- 2020-12-23 JP JP2022539058A patent/JP2023508097A/ja active Pending
- 2020-12-23 JO JOP/2022/0159A patent/JOP20220159A1/ar unknown
-
2022
- 2022-06-22 CL CL2022001724A patent/CL2022001724A1/es unknown
- 2022-07-19 ZA ZA2022/08051A patent/ZA202208051B/en unknown
- 2022-07-20 EC ECSENADI202256811A patent/ECSP22056811A/es unknown
- 2022-07-21 CO CONC2022/0010305A patent/CO2022010305A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
ZA202208051B (en) | 2023-11-29 |
JP2023508097A (ja) | 2023-02-28 |
CN114829342A (zh) | 2022-07-29 |
JOP20220159A1 (ar) | 2023-01-30 |
EP4083020A4 (en) | 2024-01-24 |
CA3162523A1 (en) | 2021-07-01 |
CL2022001724A1 (es) | 2023-02-24 |
CO2022010305A2 (es) | 2022-08-09 |
CN113087704A (zh) | 2021-07-09 |
US20230111119A1 (en) | 2023-04-13 |
TWI755992B (zh) | 2022-02-21 |
EP4083020A1 (en) | 2022-11-02 |
IL294225A (en) | 2022-08-01 |
KR20220120629A (ko) | 2022-08-30 |
TW202128662A (zh) | 2021-08-01 |
MX2022007885A (es) | 2022-09-19 |
CN113087704B (zh) | 2023-09-08 |
AU2020414151A1 (en) | 2022-08-25 |
ECSP22056811A (es) | 2022-12-30 |
BR112022012385A2 (pt) | 2022-08-30 |
WO2021129653A1 (zh) | 2021-07-01 |
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