ECSP22011086A - Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina - Google Patents
Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazinaInfo
- Publication number
- ECSP22011086A ECSP22011086A ECSENADI202211086A ECDI202211086A ECSP22011086A EC SP22011086 A ECSP22011086 A EC SP22011086A EC SENADI202211086 A ECSENADI202211086 A EC SENADI202211086A EC DI202211086 A ECDI202211086 A EC DI202211086A EC SP22011086 A ECSP22011086 A EC SP22011086A
- Authority
- EC
- Ecuador
- Prior art keywords
- pyrazolo
- pyrazine
- phosphatase inhibitors
- shp2 phosphatase
- type shp2
- Prior art date
Links
- 102000007607 Non-Receptor Type 11 Protein Tyrosine Phosphatase Human genes 0.000 title 1
- 108010032107 Non-Receptor Type 11 Protein Tyrosine Phosphatase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003216 pyrazines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La invención proporciona nuevos derivados de pirazina de fórmula (I): (conforme a figura constante en resumen de memoria técnica) (I) o un tautómero o un solvato o una sal farmacéuticamente aceptable del mismo, en donde los sustituyentes son como se definen en la presente descripción. La invención también proporciona composiciones farmacéuticas que comprenden dichos compuestos y el uso de dichos compuestos en el tratamiento de enfermedades, por ejemplo, el cáncer.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1911928.8A GB201911928D0 (en) | 2019-08-20 | 2019-08-20 | Pharmaceutical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP22011086A true ECSP22011086A (es) | 2022-03-31 |
Family
ID=68099585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI202211086A ECSP22011086A (es) | 2019-08-20 | 2022-02-11 | Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US12458640B2 (es) |
| EP (1) | EP4017855A1 (es) |
| JP (1) | JP7698629B2 (es) |
| KR (1) | KR102933621B1 (es) |
| CN (1) | CN114206885B (es) |
| AU (1) | AU2020333251B2 (es) |
| BR (1) | BR112022003184A2 (es) |
| CA (1) | CA3148312A1 (es) |
| CL (1) | CL2022000271A1 (es) |
| CO (1) | CO2022001357A2 (es) |
| CR (1) | CR20220062A (es) |
| DO (1) | DOP2022000039A (es) |
| EC (1) | ECSP22011086A (es) |
| GB (1) | GB201911928D0 (es) |
| GE (2) | GEAP202515878A (es) |
| IL (1) | IL289462B2 (es) |
| MX (1) | MX2022001908A (es) |
| PE (1) | PE20220931A1 (es) |
| PH (1) | PH12021553238A1 (es) |
| TN (1) | TN2022000039A1 (es) |
| TW (1) | TWI900489B (es) |
| WO (1) | WO2021033153A1 (es) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA52421A (fr) | 2018-03-02 | 2021-01-06 | Otsuka Pharma Co Ltd | Composés pharmaceutiques |
| MA53395A (fr) | 2018-07-24 | 2021-06-02 | Otsuka Pharma Co Ltd | Composés hétérobicycliques pour inhiber l'activité de shp2 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| CN115916194A (zh) | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
| TW202216151A (zh) | 2020-07-15 | 2022-05-01 | 日商大鵬藥品工業股份有限公司 | 含有使用於腫瘤之治療之嘧啶化合物之組合 |
| EP4208261A1 (en) | 2020-09-03 | 2023-07-12 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| PE20240088A1 (es) | 2021-05-05 | 2024-01-16 | Revolution Medicines Inc | Inhibidores de ras |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| IL308195A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors for cancer treatment |
| TW202313041A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商諾華公司 | 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合 |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途 |
| TWI843142B (zh) * | 2021-07-07 | 2024-05-21 | 大陸商浙江同源康醫藥股份有限公司 | 用作shp2抑制劑的化合物及其應用 |
| US20240374571A1 (en) | 2021-09-01 | 2024-11-14 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| WO2023051648A1 (zh) * | 2021-09-28 | 2023-04-06 | 甘李药业股份有限公司 | 可用作shp2抑制剂的化合物及其制备方法和用途 |
| CN118119622A (zh) * | 2021-09-29 | 2024-05-31 | 微境生物医药科技(上海)有限公司 | 作为shp2抑制剂的稠环化合物 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| CN117659049A (zh) * | 2022-08-23 | 2024-03-08 | 苏州泽璟生物制药股份有限公司 | 取代桥环类抑制剂及其制备方法和应用 |
| CN116947867B (zh) * | 2022-04-18 | 2025-12-30 | 上海茂晟康慧科技有限公司 | 一种嘧啶-4(3h)-酮类杂环化合物的重要中间体的制备方法 |
| CN119768393A (zh) | 2022-05-25 | 2025-04-04 | 医肯纳肿瘤学公司 | Mek抑制剂和其用途 |
| EP4536364A1 (en) | 2022-06-10 | 2025-04-16 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN117384187B (zh) * | 2022-09-30 | 2026-01-30 | 轩竹生物科技股份有限公司 | 泛素特异性蛋白酶1抑制剂 |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| CN121487951A (zh) | 2023-04-07 | 2026-02-06 | 锐新医药公司 | 大环ras抑制剂 |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| AU2024251341A1 (en) | 2023-04-14 | 2025-10-16 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| EP4695261A1 (en) | 2023-04-14 | 2026-02-18 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| KR102928747B1 (ko) | 2023-07-21 | 2026-02-26 | 대한민국 | 피라졸로[1,5-에이]퀴나졸린 유도체 화합물을 포함하는 인간면역결핍바이러스 억제용 조성물 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| KR20260042550A (ko) | 2023-08-24 | 2026-03-31 | 다이호야쿠힌고교 가부시키가이샤 | 세다주리딘 및 아자시티딘의 고정 용량 조합물 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
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| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| CN119039223B (zh) * | 2024-10-31 | 2025-02-25 | 江苏豪森药业集团有限公司 | 一种含氮杂芳类衍生物的制备方法及其中间体 |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
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| PT3468972T (pt) | 2016-06-14 | 2020-08-21 | Novartis Ag | Compostos e composições para inibir a atividade da shp2 |
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| TW202500565A (zh) | 2016-10-24 | 2025-01-01 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| CN110730678B (zh) | 2017-01-10 | 2022-07-15 | 诺华股份有限公司 | 包含alk抑制剂和shp2抑制剂的药物组合 |
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| TWI852912B (zh) | 2017-09-07 | 2024-08-21 | 美商銳新醫藥公司 | Shp2抑制劑組合物以及治療癌症的方法 |
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| TW202140024A (zh) | 2020-01-24 | 2021-11-01 | 日商大鵬藥品工業股份有限公司 | Shp2抑制劑嘧啶酮與新穎癌症醫藥併用於癌症之抗腫瘤活性之增強 |
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2019
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| US12458640B2 (en) | 2025-11-04 |
| TW202124383A (zh) | 2021-07-01 |
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| MX2022001908A (es) | 2022-04-18 |
| US20260102394A1 (en) | 2026-04-16 |
| CA3148312A1 (en) | 2021-02-25 |
| WO2021033153A1 (en) | 2021-02-25 |
| IL289462A (en) | 2022-02-01 |
| GEP20257767B (en) | 2025-05-27 |
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| AU2020333251B2 (en) | 2026-02-19 |
| KR102933621B1 (ko) | 2026-03-03 |
| AU2020333251A1 (en) | 2022-02-17 |
| BR112022003184A2 (pt) | 2022-05-17 |
| PH12021553238A1 (en) | 2023-02-20 |
| CO2022001357A2 (es) | 2022-03-18 |
| PE20220931A1 (es) | 2022-05-31 |
| TN2022000039A1 (en) | 2023-10-09 |
| EP4017855A1 (en) | 2022-06-29 |
| CN114206885B (zh) | 2025-05-02 |
| GEAP202515878A (en) | 2025-01-17 |
| KR20220049518A (ko) | 2022-04-21 |
| IL289462B1 (en) | 2026-04-01 |
| CN114206885A (zh) | 2022-03-18 |
| TWI900489B (zh) | 2025-10-11 |
| CL2022000271A1 (es) | 2022-10-28 |
| GB201911928D0 (en) | 2019-10-02 |
| JP2022546213A (ja) | 2022-11-04 |
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