JPWO2020177653A5 - - Google Patents
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- JPWO2020177653A5 JPWO2020177653A5 JP2021551865A JP2021551865A JPWO2020177653A5 JP WO2020177653 A5 JPWO2020177653 A5 JP WO2020177653A5 JP 2021551865 A JP2021551865 A JP 2021551865A JP 2021551865 A JP2021551865 A JP 2021551865A JP WO2020177653 A5 JPWO2020177653 A5 JP WO2020177653A5
- Authority
- JP
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- Prior art keywords
- membered
- alkyl
- halogen
- alkoxy
- alkylamino
- Prior art date
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- 125000000623 heterocyclic group Chemical group 0.000 claims 59
- 229910052736 halogen Inorganic materials 0.000 claims 49
- 150000002367 halogens Chemical class 0.000 claims 49
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 43
- 125000004093 cyano group Chemical group *C#N 0.000 claims 39
- 125000000753 cycloalkyl group Chemical group 0.000 claims 38
- 125000003282 alkyl amino group Chemical group 0.000 claims 36
- 125000003118 aryl group Chemical group 0.000 claims 35
- 125000000217 alkyl group Chemical group 0.000 claims 34
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 32
- 150000001875 compounds Chemical class 0.000 claims 27
- -1 —NH 2 Chemical group 0.000 claims 24
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 23
- 229920006395 saturated elastomer Polymers 0.000 claims 22
- 150000002148 esters Chemical class 0.000 claims 21
- 239000000651 prodrug Substances 0.000 claims 21
- 229940002612 prodrug Drugs 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 21
- 239000012453 solvate Substances 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 229910052805 deuterium Inorganic materials 0.000 claims 17
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 17
- 125000005842 heteroatom Chemical group 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 239000000126 substance Substances 0.000 claims 9
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical compound O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims 9
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 8
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 6
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 5
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 5
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 5
- YEJRWHAVMIAJKC-UHFFFAOYSA-N 4-Butyrolactone Chemical compound O=C1CCCO1 YEJRWHAVMIAJKC-UHFFFAOYSA-N 0.000 claims 4
- OZJPLYNZGCXSJM-UHFFFAOYSA-N 5-valerolactone Chemical compound O=C1CCCCO1 OZJPLYNZGCXSJM-UHFFFAOYSA-N 0.000 claims 4
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 238000006467 substitution reaction Methods 0.000 claims 4
- 229960002317 succinimide Drugs 0.000 claims 4
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 3
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000003554 tetrahydropyrrolyl group Chemical group 0.000 claims 3
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical group C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 2
- 125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 claims 2
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims 2
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims 2
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims 2
- DDZGQYREBDXECY-UHFFFAOYSA-N 1h-pyrazolo[3,4-b]pyrazine Chemical compound C1=CN=C2C=NNC2=N1 DDZGQYREBDXECY-UHFFFAOYSA-N 0.000 claims 2
- IAAQUOVTPAMQCR-UHFFFAOYSA-N 1h-pyrido[3,2-d]pyrimidin-2-one Chemical compound C1=CC=C2NC(=O)N=CC2=N1 IAAQUOVTPAMQCR-UHFFFAOYSA-N 0.000 claims 2
- HFTVJMFWJUFBNO-UHFFFAOYSA-N 5h-pyrrolo[2,3-b]pyrazine Chemical compound C1=CN=C2NC=CC2=N1 HFTVJMFWJUFBNO-UHFFFAOYSA-N 0.000 claims 2
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 2
- 102000002727 Protein Tyrosine Phosphatase Human genes 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000004069 aziridinyl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 229930188620 butyrolactone Natural products 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 108020000494 protein-tyrosine phosphatase Proteins 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 2
- PAPBSGBWRJIAAV-UHFFFAOYSA-N ε-Caprolactone Chemical compound O=C1CCCCCO1 PAPBSGBWRJIAAV-UHFFFAOYSA-N 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical group C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910160960.7 | 2019-03-04 | ||
| CN201910160960.7A CN111647000B (zh) | 2019-03-04 | 2019-03-04 | 吡嗪类衍生物及其在抑制shp2中的应用 |
| PCT/CN2020/077391 WO2020177653A1 (zh) | 2019-03-04 | 2020-03-02 | 吡嗪类衍生物及其在抑制shp2中的应用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022523786A JP2022523786A (ja) | 2022-04-26 |
| JPWO2020177653A5 true JPWO2020177653A5 (enExample) | 2022-11-02 |
Family
ID=72337672
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021551865A Pending JP2022523786A (ja) | 2019-03-04 | 2020-03-02 | ピラジン誘導体およびｓｈｐ２の阻害の際のその適用 |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US12338246B2 (enExample) |
| EP (1) | EP3936502A4 (enExample) |
| JP (1) | JP2022523786A (enExample) |
| KR (1) | KR20210135561A (enExample) |
| CN (2) | CN111647000B (enExample) |
| AU (1) | AU2020233038B2 (enExample) |
| BR (1) | BR112021017495A2 (enExample) |
| CA (1) | CA3132395A1 (enExample) |
| CL (1) | CL2021002308A1 (enExample) |
| CO (1) | CO2021013140A2 (enExample) |
| IL (1) | IL286069B2 (enExample) |
| MX (1) | MX2021010625A (enExample) |
| NZ (1) | NZ780509A (enExample) |
| PH (1) | PH12021552134A1 (enExample) |
| SG (1) | SG11202109603SA (enExample) |
| WO (1) | WO2020177653A1 (enExample) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| CN120208856A (zh) | 2018-09-29 | 2025-06-27 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物的制造 |
| CN111647000B (zh) * | 2019-03-04 | 2021-10-12 | 勤浩医药（苏州）有限公司 | 吡嗪类衍生物及其在抑制shp2中的应用 |
| WO2021178488A1 (en) | 2020-03-03 | 2021-09-10 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| AU2021293228A1 (en) | 2020-06-18 | 2023-02-09 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors |
| JP2023530838A (ja) * | 2020-06-22 | 2023-07-20 | スーチュアン・コールン－バイオテック・バイオファーマシューティカル・カンパニー・リミテッド | 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用 |
| KR20230038197A (ko) | 2020-07-08 | 2023-03-17 | 노파르티스 아게 | Shp2의 활성 억제를 위한 화합물 및 조성물의 제조 |
| WO2022006780A1 (en) * | 2020-07-08 | 2022-01-13 | Novartis Ag | Manufacture of compounds and compositions for inhibiting activity of shp2 |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | 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 |
| WO2022063190A1 (zh) * | 2020-09-23 | 2022-03-31 | 南京明德新药研发有限公司 | 吡嗪硫联苯基类化合物及其应用 |
| CA3217084A1 (en) * | 2021-05-05 | 2022-11-10 | Farbod Shojaei | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
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| WO2022235815A1 (en) * | 2021-05-05 | 2022-11-10 | Huabio International, Llc | Combination therapies comprising shp2 inhibitors and egfr tyrosine kinase inhibitors |
| EP4334324A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| US12390469B2 (en) * | 2021-05-05 | 2025-08-19 | Huyabio International, Llc | SHP2 inhibitor monotherapy and uses thereof |
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| TW202244049A (zh) * | 2021-05-12 | 2022-11-16 | 大陸商藥雅科技（上海）有限公司 | Shp2磷酸酶抑制劑的製備及其應用 |
| CN115340561A (zh) * | 2021-05-14 | 2022-11-15 | 药雅科技(上海)有限公司 | Shp2磷酸酶稠环类抑制剂的制备及其应用 |
| EP4328228A4 (en) * | 2021-05-13 | 2025-04-30 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | Heterocyclic compound for inhibiting SHP2 activity, method of preparation therefor and use thereof |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| 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 |
| US20240383908A1 (en) * | 2021-07-07 | 2024-11-21 | Hinova Pharmaceuticals Inc. | Synthesis and application of phosphatase degrader |
| CN118103368A (zh) | 2021-08-25 | 2024-05-28 | 皮克医疗公司 | Eif4e抑制剂及其用途 |
| US12157732B2 (en) | 2021-08-25 | 2024-12-03 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN116063307B (zh) * | 2021-10-29 | 2025-08-19 | 中国药科大学 | Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用 |
| WO2023122938A1 (en) * | 2021-12-28 | 2023-07-06 | Js Innomed Holdings Ltd. | Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof |
| WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| KR20250022133A (ko) | 2022-06-10 | 2025-02-14 | 레볼루션 메디슨즈, 인크. | 거대고리 ras 억제제 |
| CN115521305B (zh) * | 2022-09-20 | 2024-11-08 | 中国药科大学 | Shp2&nampt双靶向化合物及其药物组合物和用途 |
| WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| CN115677661B (zh) * | 2022-10-27 | 2024-04-19 | 中国药科大学 | 杂环硫醚类化合物及其用途和药物组合物 |
| CN118206550A (zh) * | 2022-12-15 | 2024-06-18 | 江苏威凯尔医药科技有限公司 | Shp2抑制剂及其应用 |
| CN120826403A (zh) * | 2023-02-24 | 2025-10-21 | 深圳真实生物医药科技有限公司 | Shp2抑制剂化合物及其应用 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| AU2024243852A1 (en) | 2023-04-07 | 2025-11-06 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| KR20250169290A (ko) | 2023-04-14 | 2025-12-02 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형, 이를 함유하는 조성물 및 이의 사용 방법 |
| KR20250172857A (ko) | 2023-04-14 | 2025-12-09 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025011568A1 (zh) * | 2023-07-11 | 2025-01-16 | 勤浩医药（苏州）有限公司 | 用作shp2抑制剂的杂环化合物、包含其的药物组合物及其制备方法和用途 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025067459A2 (en) | 2023-09-29 | 2025-04-03 | D3 Bio (Wuxi) Co., Ltd. | Therapies for the treatment of cancer |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| CN118108707A (zh) * | 2024-02-04 | 2024-05-31 | 中国药科大学 | 吡嗪类化合物及其制备方法、药物组合物和应用 |
| 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 |
| WO2025242126A1 (zh) * | 2024-05-22 | 2025-11-27 | 上海正大天晴医药科技开发有限公司 | 一种药物组合及其应用 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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| CN107922388B (zh) * | 2015-06-19 | 2020-12-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
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| AU2019239658A1 (en) | 2018-03-21 | 2020-11-12 | Suzhou Puhe BioPharma Co., Ltd. | SHP2 inhibitors and uses thereof |
| TW201946627A (zh) | 2018-04-10 | 2019-12-16 | 美商銳新醫藥公司 | 治療癌症的ｓｈｐ２抑制劑組合物和方法 |
| CN111647000B (zh) * | 2019-03-04 | 2021-10-12 | 勤浩医药（苏州）有限公司 | 吡嗪类衍生物及其在抑制shp2中的应用 |
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2019
- 2019-03-04 CN CN201910160960.7A patent/CN111647000B/zh active Active
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2020
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- 2020-03-02 JP JP2021551865A patent/JP2022523786A/ja active Pending
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