IL293797A - Bifunctional compounds for btk degradation via the ubiquitin proteosome pathway - Google Patents
Bifunctional compounds for btk degradation via the ubiquitin proteosome pathwayInfo
- Publication number
- IL293797A IL293797A IL293797A IL29379722A IL293797A IL 293797 A IL293797 A IL 293797A IL 293797 A IL293797 A IL 293797A IL 29379722 A IL29379722 A IL 29379722A IL 293797 A IL293797 A IL 293797A
- Authority
- IL
- Israel
- Prior art keywords
- membered
- alkyl
- compound
- heterocycloalkyl
- pct
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (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)
- Heat Sensitive Colour Forming Recording (AREA)
- Luminescent Compositions (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962943720P | 2019-12-04 | 2019-12-04 | |
| US202063010524P | 2020-04-15 | 2020-04-15 | |
| PCT/US2020/063176 WO2021113557A1 (en) | 2019-12-04 | 2020-12-03 | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL293797A true IL293797A (en) | 2022-08-01 |
Family
ID=74004152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL293797A IL293797A (en) | 2019-12-04 | 2020-12-03 | Bifunctional compounds for btk degradation via the ubiquitin proteosome pathway |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11820781B2 (https=) |
| EP (2) | EP4069237B1 (https=) |
| JP (2) | JP2023504147A (https=) |
| KR (1) | KR20220112273A (https=) |
| CN (1) | CN115003304A (https=) |
| AU (1) | AU2020397920A1 (https=) |
| BR (1) | BR112022010349A2 (https=) |
| CA (1) | CA3160713A1 (https=) |
| DK (1) | DK4069237T3 (https=) |
| ES (1) | ES3033520T3 (https=) |
| FI (1) | FI4069237T3 (https=) |
| HU (1) | HUE072392T2 (https=) |
| IL (1) | IL293797A (https=) |
| MX (1) | MX2022006672A (https=) |
| PL (1) | PL4069237T3 (https=) |
| WO (1) | WO2021113557A1 (https=) |
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|---|---|---|---|---|
| MX2021004191A (es) | 2018-10-15 | 2021-05-27 | Nurix Therapeutics Inc | Compuestos bifuncionales para degradar la tirosina cinasa de bruton (btk) mediante la trayectoria de ubiquitina proteosoma. |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3877371A4 (en) | 2018-11-07 | 2022-07-27 | Dana-Farber Cancer Institute, Inc. | IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF |
| US12522583B2 (en) | 2018-11-07 | 2026-01-13 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof |
| EP3917916A4 (en) | 2019-01-30 | 2022-12-14 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| US12582722B2 (en) | 2019-02-13 | 2026-03-24 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading BTK via ubiquitin proteosome pathway |
| CN111606883B (zh) | 2019-02-25 | 2023-05-09 | 上海科技大学 | 基于戊二酰亚胺骨架的含硫化合物及其应用 |
| CA3136348A1 (en) | 2019-04-09 | 2020-10-15 | Nurix Therapeutics, Inc. | 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus |
| AU2020278592B2 (en) | 2019-05-17 | 2024-10-10 | Nurix Therapeutics, Inc. | Cyano cyclobutyl compounds for Cbl-b inhibition and uses thereof |
| MX2021015675A (es) | 2019-06-26 | 2022-02-03 | Nurix Therapeutics Inc | Compuestos de bencil-triazol sustituidos para la inhibicion de cbl-b y otros usos de los mismos. |
| WO2021023233A1 (zh) | 2019-08-05 | 2021-02-11 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
| EP4034140A1 (en) | 2019-09-24 | 2022-08-03 | Nurix Therapeutics, Inc. | Cbl inhibitors and compositions for use in adoptive cell therapy |
| WO2021113557A1 (en) | 2019-12-04 | 2021-06-10 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| WO2021168197A1 (en) | 2020-02-19 | 2021-08-26 | Nurix Therapeutics, Inc. | Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof |
| AU2021226514B2 (en) * | 2020-02-25 | 2023-10-19 | Shanghaitech University | Glutarimide skeleton-based compounds and application thereof |
| US11691963B2 (en) | 2020-05-06 | 2023-07-04 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| US12043632B2 (en) | 2020-12-23 | 2024-07-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| WO2022217123A2 (en) | 2021-04-08 | 2022-10-13 | Nurix Therapeutics, Inc. | Combination therapies with cbl-b inhibitor compounds |
| AU2022270089A1 (en) * | 2021-05-03 | 2023-11-16 | Nurix Therapeutics, Inc. | Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| KR20240026946A (ko) * | 2021-06-25 | 2024-02-29 | 셀진 코포레이션 | 세레블론 결합 화합물, 이의 조성물, 및 이에 의한 치료 방법 |
| JP2024524480A (ja) * | 2021-07-01 | 2024-07-05 | ハンチョウ、ヘルズン、セラピューティクス、カンパニー、リミテッド | ブルトン型チロシンキナーゼ及びその突然変異体の分解剤、組成物並びにそれらの応用 |
| AU2022310182A1 (en) | 2021-07-14 | 2024-02-01 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk with diminished imid activity |
| CN118019539A (zh) | 2021-07-23 | 2024-05-10 | 纽力克斯治疗公司 | 用于降解BTK并具有增强的IMiD活性的双官能化合物 |
| WO2023009709A1 (en) * | 2021-07-29 | 2023-02-02 | Ajax Therapeutics, Inc. | Pyrazolo piperazines as jak2 inhibitors |
| CN117813307A (zh) * | 2021-08-18 | 2024-04-02 | 新锐思生物制药股份有限公司 | 白介素-1受体相关激酶的双官能降解物及其治疗用途 |
| WO2023039081A2 (en) * | 2021-09-08 | 2023-03-16 | Memorial Sloan-Kettering Cancer Center | Ink4 tumor suppressor proteins mediate resistance to cdk4/6 kinase inhibitors |
| US20240317734A1 (en) * | 2021-09-13 | 2024-09-26 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2023059582A1 (en) * | 2021-10-04 | 2023-04-13 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and their use in treating disease |
| CA3236073A1 (en) | 2021-10-26 | 2023-05-04 | Robert J. Brown | Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| WO2023086319A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| WO2023088406A1 (zh) * | 2021-11-18 | 2023-05-25 | 正大天晴药业集团股份有限公司 | 稠合酰亚胺类衍生物 |
| CN116143757B (zh) * | 2021-11-22 | 2024-07-05 | 杭州和正医药有限公司 | 一种可降解btk激酶的多功能化合物、组合物及应用 |
| EP4446324A4 (en) * | 2021-12-08 | 2026-05-06 | Gluetacs Therapeutics Shanghai Co Ltd | Ligand compounds for e3 ubiquitin ligase, protein degraders developed on basis of ligand compounds, and uses thereof |
| AU2023278399A1 (en) | 2022-06-02 | 2024-12-19 | Xizang Haisco Pharmaceutical Co., Ltd. | Compound for inhibiting or degrading bcl6 and use thereof in pharmaceutics |
| WO2023239629A1 (en) | 2022-06-06 | 2023-12-14 | Plexium, Inc. | Compounds and pharmaceutical compositions that degrade cdk2 |
| CN117384161A (zh) * | 2022-07-04 | 2024-01-12 | 华东理工大学 | 靶向降解cdk蛋白的化合物及其应用 |
| CN119630667A (zh) * | 2022-07-25 | 2025-03-14 | 细胞基因公司 | 经取代的咪唑并吡嗪化合物作为irak3的配体定向降解剂 |
| EP4578849A4 (en) * | 2022-08-26 | 2025-11-26 | Fujifilm Corp | NEW PIPERAZINE DERIVATIVE OR SALT THEREOF AND PHARMACEUTICAL COMPOSITION |
| WO2024102970A1 (en) * | 2022-11-11 | 2024-05-16 | Kronos Bio, Inc. | Compounds for modulating syk activity and e3 ubiquitin ligase activity |
| CN121816348A (zh) | 2023-08-11 | 2026-04-07 | 深圳众格生物科技有限公司 | 一种降解irak4的蛋白降解靶向嵌合体化合物及其应用 |
| WO2025090535A2 (en) * | 2023-10-23 | 2025-05-01 | Nurix Therapeutics, Inc. | Salts and free bases of bifunctional compound and polymorph forms thereof |
| WO2025162210A1 (zh) * | 2024-02-04 | 2025-08-07 | 上海超阳药业有限公司 | 一种具备降解酪氨酸蛋白激酶btk活性的化合物及其制备方法和用途 |
| WO2025174220A1 (ko) * | 2024-02-14 | 2025-08-21 | 주식회사 유빅스테라퓨틱스 | Shp2 단백질 분해 활성을 갖는 화합물 및 이들의 의약 용도 |
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| EP4570320A3 (en) | 2025-08-27 |
| DK4069237T3 (da) | 2025-06-23 |
| US12600732B2 (en) | 2026-04-14 |
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