CA3200006A1 - Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors - Google Patents

Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Info

Publication number
CA3200006A1
CA3200006A1 CA3200006A CA3200006A CA3200006A1 CA 3200006 A1 CA3200006 A1 CA 3200006A1 CA 3200006 A CA3200006 A CA 3200006A CA 3200006 A CA3200006 A CA 3200006A CA 3200006 A1 CA3200006 A1 CA 3200006A1
Authority
CA
Canada
Prior art keywords
independently selected
heteroatoms
alkyl
ring
substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3200006A
Other languages
English (en)
French (fr)
Inventor
Paul A. Barsanti
Hilary Plake Beck
Melissa Fleury
Brian Thomas Jones
Ethan DeNardo MCSPADDEN
Zhonghua Pei
Chenbo WANG
Firoz Ali JAIPURI
Daniel Lee Severance
Kevin J. Duffy
Brian Lawhorn
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline Intellectual Property No 4 Ltd
Ideaya Biosciences Inc
Original Assignee
GlaxoSmithKline Intellectual Property No 4 Ltd
Ideaya Biosciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GlaxoSmithKline Intellectual Property No 4 Ltd, Ideaya Biosciences Inc filed Critical GlaxoSmithKline Intellectual Property No 4 Ltd
Publication of CA3200006A1 publication Critical patent/CA3200006A1/en
Pending legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA3200006A 2020-12-02 2021-12-01 Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors Pending CA3200006A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063120410P 2020-12-02 2020-12-02
US63/120,410 2020-12-02
US202163232749P 2021-08-13 2021-08-13
US63/232,749 2021-08-13
PCT/IB2021/061173 WO2022118210A1 (en) 2020-12-02 2021-12-01 Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Publications (1)

Publication Number Publication Date
CA3200006A1 true CA3200006A1 (en) 2022-06-09

Family

ID=78824758

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3200006A Pending CA3200006A1 (en) 2020-12-02 2021-12-01 Substituted thiadiazolyl derivatives as dna polymerase theta inhibitors

Country Status (7)

Country Link
US (1) US20250325552A1 (https=)
EP (1) EP4255573A1 (https=)
JP (1) JP2023552764A (https=)
AU (1) AU2021390194B2 (https=)
CA (1) CA3200006A1 (https=)
TW (1) TW202237595A (https=)
WO (1) WO2022118210A1 (https=)

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TW202315618A (zh) * 2021-06-11 2023-04-16 美商愛德亞生物科學公司 作為DNA聚合酶θ抑制劑之O-聯結噻二唑基化合物
WO2023202623A1 (zh) * 2022-04-20 2023-10-26 南京再明医药有限公司 Polq抑制剂化合物及其应用
CA3257870A1 (en) * 2022-06-01 2023-12-07 Ideaya Biosciences, Inc. THIADIAZOLYL DERIVATIVES USED AS DNA POLYMERASE THETA INHIBITORS AND THEIR USES
AU2023352129A1 (en) * 2022-09-29 2025-05-01 Repare Therapeutics Inc. N-(5-substituted-[(1,3,4-thiadiazolyl) or (1,3-thiazolyl)](substituted)carboxamide compounds, pharmaceutical compositions, and methods of preparing the amide compounds and of their use
CN117946138A (zh) * 2022-10-28 2024-04-30 杭州圣域生物医药科技有限公司 并环含氮化合物、其中间体、制备方法和应用
WO2024099336A1 (en) * 2022-11-10 2024-05-16 Danatlas Pharmaceuticals Co., Ltd. Thiadiazolyl derivatives, compositions and uses thereof
CN120077028A (zh) * 2022-11-10 2025-05-30 北京丹擎医药科技有限公司 噻二唑衍生物及其组合物和应用
JP2025541823A (ja) * 2022-12-09 2025-12-23 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー4)、リミテッド Dnaポリメラーゼシータ阻害剤としてのチアジアゾリル誘導体およびその使用
WO2024149349A1 (zh) * 2023-01-14 2024-07-18 西藏海思科制药有限公司 靶向Polθ的化合物及其用途
KR20250153866A (ko) 2023-03-10 2025-10-27 브레이크포인트 테라퓨틱스 게엠베하 Dna 중합효소 세타 억제제
WO2024211836A2 (en) * 2023-04-05 2024-10-10 Moma Therapeutics, Inc. Semi-saturated bicyclic derivatives and related uses
AU2024254066A1 (en) * 2023-04-05 2025-10-16 Moma Therapeutics, Inc. Biaryl derivatives and related uses
WO2024213082A1 (en) * 2023-04-13 2024-10-17 Danatlas Pharmaceuticals Co., Ltd. Thiadiazolone derivatives, compositions and uses thereof
CN121712768A (zh) * 2023-05-30 2026-03-20 宁波新湾科技发展有限公司 噻唑基或噻二唑基酰胺衍生物及其用途
CN121399118A (zh) * 2023-06-02 2026-01-23 成都微芯药业有限公司 Polθ抑制剂及其制备方法和用途
WO2025011617A1 (zh) * 2023-07-12 2025-01-16 杭州圣域生物医药科技有限公司 并环杂芳环类化合物、其中间体、制备方法和应用
WO2025016391A1 (zh) * 2023-07-18 2025-01-23 南京再明医药有限公司 噻唑并吡嗪类化合物及其应用
CN121773109A (zh) * 2023-07-27 2026-03-31 北京丹擎医药科技有限公司 PolQ降解剂及其组合物和应用
WO2025036490A1 (zh) * 2023-08-17 2025-02-20 海思科医药集团股份有限公司 一种DNA聚合酶θ抑制剂及其用途
WO2025165092A1 (en) * 2024-01-30 2025-08-07 Daewoong Pharmaceutical Co., Ltd. Novel heterocyclic compounds and pharmaceutical composition comprising the same as dna polymerase theta inhibitors for the prevention or treatment of cancer
CN120829441A (zh) * 2024-04-24 2025-10-24 杭州圣域生物医药科技有限公司 一种并环含氮化合物及其中间体的制备方法
CN120829442A (zh) * 2024-04-24 2025-10-24 杭州圣域生物医药科技有限公司 一种并环含氮化合物及其中间体的制备方法
WO2025223483A1 (zh) * 2024-04-24 2025-10-30 杭州圣域生物医药科技有限公司 并环含氮化合物、其晶型及其制备方法和用途

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EP3034500A1 (en) * 2014-12-17 2016-06-22 Genkyotex Sa Amido thiazole derivatives as NADPH oxidase inhibitors
WO2019028104A1 (en) * 2017-08-02 2019-02-07 Alphala Co., Ltd. NOVEL COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
BR112021014977A2 (pt) * 2019-01-30 2021-10-05 Ideaya Biosciences, Inc. Derivados de acetamido como inibidores de dna polimerase teta
JP2022519535A (ja) * 2019-01-31 2022-03-24 イデアヤ、バイオサイエンシズ、インコーポレイテッド Dnaポリメラーゼシータ阻害剤としてのヘテロアリールメチレン誘導体
AU2020282768B2 (en) * 2019-05-31 2023-09-14 Ideaya Biosciences, Inc. Thiadiazolyl derivatives as DNA Polymerase Theta inhibitors

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JP2023552764A (ja) 2023-12-19
EP4255573A1 (en) 2023-10-11
AU2021390194B2 (en) 2025-06-26
AU2021390194A1 (en) 2023-06-22
WO2022118210A1 (en) 2022-06-09
TW202237595A (zh) 2022-10-01
US20250325552A1 (en) 2025-10-23

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