BR112022010349A2 - Compostos bifuncionais para degradar btk por meio de via da ubiquitina-proteossoma - Google Patents
Compostos bifuncionais para degradar btk por meio de via da ubiquitina-proteossomaInfo
- Publication number
- BR112022010349A2 BR112022010349A2 BR112022010349A BR112022010349A BR112022010349A2 BR 112022010349 A2 BR112022010349 A2 BR 112022010349A2 BR 112022010349 A BR112022010349 A BR 112022010349A BR 112022010349 A BR112022010349 A BR 112022010349A BR 112022010349 A2 BR112022010349 A2 BR 112022010349A2
- Authority
- BR
- Brazil
- Prior art keywords
- ubiquitin
- pathway
- proteosoma
- btk
- bifunctional compounds
- 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
-
- 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
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Luminescent Compositions (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 |
|---|---|
| BR112022010349A2 true BR112022010349A2 (pt) | 2022-08-16 |
Family
ID=74004152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022010349A BR112022010349A2 (pt) | 2019-12-04 | 2020-12-03 | Compostos bifuncionais para degradar btk por meio de via da ubiquitina-proteossoma |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11820781B2 (enExample) |
| EP (2) | EP4069237B1 (enExample) |
| JP (2) | JP2023504147A (enExample) |
| KR (1) | KR20220112273A (enExample) |
| CN (1) | CN115003304A (enExample) |
| AU (1) | AU2020397920A1 (enExample) |
| BR (1) | BR112022010349A2 (enExample) |
| CA (1) | CA3160713A1 (enExample) |
| DK (1) | DK4069237T3 (enExample) |
| ES (1) | ES3033520T3 (enExample) |
| FI (1) | FI4069237T3 (enExample) |
| HU (1) | HUE072392T2 (enExample) |
| IL (1) | IL293797A (enExample) |
| MX (1) | MX2022006672A (enExample) |
| PL (1) | PL4069237T3 (enExample) |
| WO (1) | WO2021113557A1 (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113412259B (zh) | 2018-10-15 | 2024-07-16 | 紐力克斯治疗公司 | 通过泛素蛋白酶体途径降解btk的双官能化合物 |
| EP3876930A4 (en) | 2018-11-07 | 2022-07-20 | Dana-Farber Cancer Institute, Inc. | BENZIMIDAZOLE DERIVATIVES AND AZA-BENZIMIDAZOLE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF |
| WO2020097400A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| 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 |
| WO2020160295A1 (en) | 2019-01-30 | 2020-08-06 | Montelino Therapeutics, Llc | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2020167518A1 (en) | 2019-02-13 | 2020-08-20 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk via ubiquitin proteosome pathway |
| US12582641B2 (en) | 2019-02-25 | 2026-03-24 | Shanghaitech University | Sulfur-containing compound based on glutarimide skeleton and application thereof |
| AU2020272937B2 (en) | 2019-04-09 | 2024-09-26 | 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 |
| JP7587528B2 (ja) | 2019-05-17 | 2024-11-20 | ニューリックス セラピューティクス，インコーポレイテッド | Ｃｂｌ－ｂ阻害のためのシアノシクロブチル化合物及びその使用 |
| CA3144450A1 (en) | 2019-06-26 | 2020-12-30 | Nurix Therapeutics, Inc. | Substituted benzyl-triazole compounds for cbl-b inhibition, and further uses thereof |
| CN112321566B (zh) | 2019-08-05 | 2022-06-10 | 上海科技大学 | Egfr蛋白降解剂及其抗肿瘤应用 |
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| MX2022006672A (es) | 2019-12-04 | 2022-08-08 | Nurix Therapeutics Inc | Compuestos bifuncionales para la degradacion de btk a traves de la via de proteosomas de ubiquitina. |
| US12528814B2 (en) | 2020-02-19 | 2026-01-20 | Nurix Therapeutics, Inc. | Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof |
| CN113372327B (zh) * | 2020-02-25 | 2023-07-18 | 上海科技大学 | 基于戊二酰亚胺骨架的化合物及其应用 |
| BR112022022409A2 (pt) | 2020-05-06 | 2023-02-07 | Ajax Therapeutics Inc | 6-heteroarilóxi benzimidazóis e azabenzimidazóis como inibidores de jak2 |
| WO2022140527A1 (en) | 2020-12-23 | 2022-06-30 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| MX2023011883A (es) | 2021-04-08 | 2023-11-09 | Nurix Therapeutics Inc | Terapias combinadas con compuestos inhibidores de cbl-b. |
| CA3217892A1 (en) * | 2021-05-03 | 2022-11-10 | Joel Mcintosh | Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| JP2024526192A (ja) * | 2021-06-25 | 2024-07-17 | セルジーン コーポレーション | セレブロン結合化合物、その組成物及びそれによる治療方法 |
| CA3223769A1 (en) * | 2021-07-01 | 2023-01-05 | Xinglu ZHOU | Bruton's tyrosine kinase and mutant degrader, composition and application thereof |
| AU2022310182A1 (en) | 2021-07-14 | 2024-02-01 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk with diminished imid activity |
| EP4373493A1 (en) | 2021-07-23 | 2024-05-29 | Nurix Therapeutics, Inc. | Bifunctional compounds for degrading btk with enhanced imid activity |
| WO2023009709A1 (en) * | 2021-07-29 | 2023-02-02 | Ajax Therapeutics, Inc. | Pyrazolo piperazines as jak2 inhibitors |
| EP4367118B1 (en) * | 2021-08-18 | 2025-01-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof |
| US20250144099A1 (en) * | 2021-09-08 | 2025-05-08 | 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 |
| WO2023076303A1 (en) | 2021-10-26 | 2023-05-04 | Nurix Therapeutics, Inc. | Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| EP4434992A4 (en) * | 2021-11-18 | 2026-02-11 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | FUSIONIZED IMIDE DERIVATIVE |
| WO2023088477A1 (zh) | 2021-11-22 | 2023-05-25 | 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 |
| CA3240524A1 (en) * | 2021-12-08 | 2023-06-15 | Gluetacs Therapeutics (Shanghai) Co., Ltd. | E3 ubiquitin ligase ligand compound, protein degrader developed based thereon and their applications |
| JP2025518252A (ja) | 2022-06-02 | 2025-06-12 | シーザン ハイスーク ファーマシューティカル カンパニー リミテッド | Ｂｃｌ６を阻害又は分解する化合物及びその医薬的な応用 |
| 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 |
| US20260028343A1 (en) * | 2022-07-25 | 2026-01-29 | Celgene Corporation | Substituted Imidazopyrazine Compounds as Ligand Directed Degraders of IRAK3 |
| WO2024043334A1 (ja) * | 2022-08-26 | 2024-02-29 | 富士フイルム株式会社 | 新規なピペラジン誘導体又はその塩及び医薬組成物 |
| 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 |
| CN121335894A (zh) * | 2024-02-04 | 2026-01-13 | 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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| CN115003304A (zh) | 2022-09-02 |
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| US12600732B2 (en) | 2026-04-14 |
| MX2022006672A (es) | 2022-08-08 |
| HUE072392T2 (hu) | 2025-11-28 |
| PL4069237T3 (pl) | 2025-08-04 |
| WO2021113557A1 (en) | 2021-06-10 |
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