JP2016525097A5 - - Google Patents
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- Publication number
- JP2016525097A5 JP2016525097A5 JP2016524936A JP2016524936A JP2016525097A5 JP 2016525097 A5 JP2016525097 A5 JP 2016525097A5 JP 2016524936 A JP2016524936 A JP 2016524936A JP 2016524936 A JP2016524936 A JP 2016524936A JP 2016525097 A5 JP2016525097 A5 JP 2016525097A5
- Authority
- JP
- Japan
- Prior art keywords
- melanoma
- pharmaceutical composition
- composition according
- braf
- inhibitor
- 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.)
- Granted
Links
- 201000001441 melanoma Diseases 0.000 claims 26
- 239000008194 pharmaceutical composition Substances 0.000 claims 26
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 10
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 10
- 229940125431 BRAF inhibitor Drugs 0.000 claims 7
- 229940124647 MEK inhibitor Drugs 0.000 claims 6
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 6
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 claims 5
- 239000003112 inhibitor Substances 0.000 claims 5
- 102200055464 rs113488022 Human genes 0.000 claims 5
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 claims 4
- 102220197820 rs121913227 Human genes 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- 230000001394 metastastic effect Effects 0.000 claims 3
- 206010061289 metastatic neoplasm Diseases 0.000 claims 3
- -1 2-chloro-4-trifluoromethylphenyl Chemical group 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229960002465 dabrafenib Drugs 0.000 claims 2
- BFSMGDJOXZAERB-UHFFFAOYSA-N dabrafenib Chemical compound S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 BFSMGDJOXZAERB-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229960004066 trametinib Drugs 0.000 claims 2
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 229960003862 vemurafenib Drugs 0.000 claims 2
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 2
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical compound N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims 1
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims 1
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 claims 1
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- DEZZLWQELQORIU-RELWKKBWSA-N GDC-0879 Chemical compound N=1N(CCO)C=C(C=2C=C3CCC(/C3=CC=2)=N\O)C=1C1=CC=NC=C1 DEZZLWQELQORIU-RELWKKBWSA-N 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 1
- HHCBMISMPSAZBF-UHFFFAOYSA-N LY3009120 Chemical compound CC1=NC2=NC(NC)=NC=C2C=C1C1=CC(NC(=O)NCCC(C)(C)C)=C(F)C=C1C HHCBMISMPSAZBF-UHFFFAOYSA-N 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 1
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 1
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 1
- VIUAUNHCRHHYNE-JTQLQIEISA-N N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide Chemical compound OC[C@@H](O)CNC(=O)C1=CC=NC=C1NC1=CC=C(I)C=C1F VIUAUNHCRHHYNE-JTQLQIEISA-N 0.000 claims 1
- SUDAHWBOROXANE-VIFPVBQESA-N PD 0325901-Cl Chemical compound OC[C@H](O)CONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F SUDAHWBOROXANE-VIFPVBQESA-N 0.000 claims 1
- YZDJQTHVDDOVHR-UHFFFAOYSA-N PLX-4720 Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(Cl)=CN=C3NC=2)=C1F YZDJQTHVDDOVHR-UHFFFAOYSA-N 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102000009516 Protein Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010009341 Protein Serine-Threonine Kinases Proteins 0.000 claims 1
- 229950003054 binimetinib Drugs 0.000 claims 1
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims 1
- FQUXBVQTVWLTDK-UHFFFAOYSA-N chromen-4-one;hydrochloride Chemical compound Cl.C1=CC=C2C(=O)C=COC2=C1 FQUXBVQTVWLTDK-UHFFFAOYSA-N 0.000 claims 1
- 229960002271 cobimetinib Drugs 0.000 claims 1
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims 1
- HXINDCTZKGGRDE-JPKZNVRTSA-L disodium;[3-[5-[2-[[(3r)-1-(1-methylpyrazol-3-yl)sulfonylpiperidin-3-yl]amino]pyrimidin-4-yl]imidazo[2,1-b][1,3]oxazol-6-yl]phenoxy]methyl phosphate Chemical compound [Na+].[Na+].CN1C=CC(S(=O)(=O)N2C[C@@H](CCC2)NC=2N=C(C=CN=2)C=2N3C=COC3=NC=2C=2C=C(OCOP([O-])([O-])=O)C=CC=2)=N1 HXINDCTZKGGRDE-JPKZNVRTSA-L 0.000 claims 1
- CMJCXYNUCSMDBY-ZDUSSCGKSA-N lgx818 Chemical compound COC(=O)N[C@@H](C)CNC1=NC=CC(C=2C(=NN(C=2)C(C)C)C=2C(=C(NS(C)(=O)=O)C=C(Cl)C=2)F)=N1 CMJCXYNUCSMDBY-ZDUSSCGKSA-N 0.000 claims 1
- 208000021039 metastatic melanoma Diseases 0.000 claims 1
- 239000003226 mitogen Substances 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 229950002592 pimasertib Drugs 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 229950008933 refametinib Drugs 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361845749P | 2013-07-12 | 2013-07-12 | |
| US61/845,749 | 2013-07-12 | ||
| PCT/IB2014/063022 WO2015004636A1 (en) | 2013-07-12 | 2014-07-11 | A pharmaceutical combination for the treatment of melanoma |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019141995A Division JP2019206565A (ja) | 2013-07-12 | 2019-08-01 | 黒色腫の治療のための組合せ医薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016525097A JP2016525097A (ja) | 2016-08-22 |
| JP2016525097A5 true JP2016525097A5 (https=) | 2017-08-10 |
| JP6568060B2 JP6568060B2 (ja) | 2019-08-28 |
Family
ID=52279411
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016524936A Active JP6568060B2 (ja) | 2013-07-12 | 2014-07-11 | 黒色腫の治療のための組合せ医薬 |
| JP2019141995A Pending JP2019206565A (ja) | 2013-07-12 | 2019-08-01 | 黒色腫の治療のための組合せ医薬 |
| JP2020152028A Pending JP2021001186A (ja) | 2013-07-12 | 2020-09-10 | 黒色腫の治療のための組合せ医薬 |
| JP2022026851A Active JP7799508B2 (ja) | 2013-07-12 | 2022-02-24 | 黒色腫の治療のための組合せ医薬 |
| JP2023210858A Pending JP2024037891A (ja) | 2013-07-12 | 2023-12-14 | 黒色腫の治療のための組合せ医薬 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019141995A Pending JP2019206565A (ja) | 2013-07-12 | 2019-08-01 | 黒色腫の治療のための組合せ医薬 |
| JP2020152028A Pending JP2021001186A (ja) | 2013-07-12 | 2020-09-10 | 黒色腫の治療のための組合せ医薬 |
| JP2022026851A Active JP7799508B2 (ja) | 2013-07-12 | 2022-02-24 | 黒色腫の治療のための組合せ医薬 |
| JP2023210858A Pending JP2024037891A (ja) | 2013-07-12 | 2023-12-14 | 黒色腫の治療のための組合せ医薬 |
Country Status (12)
| Country | Link |
|---|---|
| US (4) | US11007174B2 (https=) |
| EP (1) | EP3019166B1 (https=) |
| JP (5) | JP6568060B2 (https=) |
| CN (3) | CN111053768B (https=) |
| AR (1) | AR096892A1 (https=) |
| AU (1) | AU2014288857B2 (https=) |
| CA (1) | CA2917742C (https=) |
| DK (1) | DK3019166T3 (https=) |
| ES (1) | ES2733929T3 (https=) |
| IL (1) | IL243572B (https=) |
| TW (4) | TW202031253A (https=) |
| WO (1) | WO2015004636A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111053768B (zh) | 2013-07-12 | 2023-12-12 | 皮拉马尔企业有限公司 | 用于治疗黑素瘤的药物组合 |
| IL256111B2 (en) * | 2015-06-05 | 2023-09-01 | Univ Illinois | Treatment of pac combinations |
| SI3881833T1 (sl) * | 2015-06-30 | 2024-03-29 | Genentech, Inc., | Tablete s takojšnjim sproščanjem, ki vsebujejo zdravilo in postopek za oblikovanje tablet |
| US10821112B2 (en) * | 2016-03-16 | 2020-11-03 | Dicerna Pharmaceuticals, Inc. | Compositions and methods for the treatment of a beta-catenin-associated disease or disorder |
| ES2928773T3 (es) | 2017-01-17 | 2022-11-22 | Heparegenix Gmbh | Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos |
| EP3624896A4 (en) * | 2017-05-16 | 2021-03-31 | Biomed Valley Discoveries, Inc. | COMPOSITIONS AND METHODS OF TREATMENT OF CANCER WITH ATYPICAL BRAF MUTATIONS |
| AU2018368453B2 (en) | 2017-11-17 | 2024-05-30 | The Board Of Trustees Of The University Of Illinois | Cancer therapy by degrading dual MEK signaling |
| CN107827726B (zh) * | 2017-11-28 | 2020-09-15 | 辽宁中医药大学 | 马齿苋中化合物Oleracone E及其提取分离方法 |
| CN108591464B (zh) * | 2018-06-28 | 2020-06-23 | 宁波奥克斯高科技有限公司 | 一种气体绝缘开关柜用密封结构 |
| CA3114385A1 (en) * | 2018-10-05 | 2020-04-09 | The Board Of Trustees Of The University Of Illinois | Combination therapy for the treatment of uveal melanoma |
| MX2021012248A (es) * | 2019-04-11 | 2022-03-11 | Mei Pharma Inc | Polimorfos de voruciclib y metodos de elaboracion y uso de los mismos. |
| US20240000789A1 (en) * | 2020-05-12 | 2024-01-04 | Novartis Ag | Therapeutic combinations comprising a craf inhibitor |
| CN112168821B (zh) * | 2020-11-09 | 2022-10-14 | 中南大学湘雅医院 | 一种治疗维罗非尼耐药的黑色素瘤的联合用药物及其应用 |
| MX2023005806A (es) * | 2020-11-19 | 2023-07-31 | Mei Pharma Inc | Tratamiento de cánceres con mutación en oncogen homologo al virus kirsten de sarcoma de rata (kras). |
| CN117043159A (zh) * | 2020-11-19 | 2023-11-10 | 梅制药公司 | Kras突变型癌症的治疗 |
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| USH1427H (en) | 1988-04-06 | 1995-04-04 | Briet; Phillipe | Substituted flavonoid compounds, their salts, their manufacture and their use in combination with interleukin-2 |
| US5284856A (en) | 1988-10-28 | 1994-02-08 | Hoechst Aktiengesellschaft | Oncogene-encoded kinases inhibition using 4-H-1-benzopyran-4-one derivatives |
| US5723313A (en) | 1995-09-27 | 1998-03-03 | St. Jude Children's Research Hospital | ARF-p19, a novel regulator of the mammalian cell cycle |
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| US5849733A (en) | 1996-05-10 | 1998-12-15 | Bristol-Myers Squibb Co. | 2-thio or 2-oxo flavopiridol analogs |
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| JP2006508184A (ja) | 2002-11-06 | 2006-03-09 | サイクラセル・リミテッド | Ｃｄｋ阻害剤及びゲムシタビンを含む医薬組成物 |
| GB0328180D0 (en) | 2003-12-04 | 2004-01-07 | Cyclacel Ltd | Combination |
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| ATE517892T1 (de) | 2006-07-07 | 2011-08-15 | Piramal Life Sciences Ltd | Enantioselektive synthese pyrrolidinsubstituierter flavone |
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| CN101841463B (zh) * | 2010-03-05 | 2012-05-16 | 清华大学 | 基于sctp的多路径并发传输方法 |
| JP5903433B2 (ja) * | 2010-08-26 | 2016-04-13 | ノバルティス アーゲー | 癌の治療に有用なｖｅｇｆｒ阻害剤およびｍｅｋ阻害剤の医薬的組み合わせ |
| AU2011330733A1 (en) | 2010-11-19 | 2013-06-06 | Piramal Enterprises Limited | Pharmaceutical combination of paclitaxel and a CDK inhibitor |
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| TW201242597A (en) | 2011-03-14 | 2012-11-01 | Piramal Life Sciences Ltd | A synergistic pharmaceutical combination for the treatment of pancreatic cancer |
| TW201300105A (zh) | 2011-05-31 | 2013-01-01 | Piramal Life Sciences Ltd | 治療頭頸鱗狀細胞癌之相乘藥物組合物 |
| US20120321637A1 (en) * | 2011-06-20 | 2012-12-20 | The Board Of Regents Of The University Of Texas System | Combination cancer therapy with herv inhibition |
| AU2012274990A1 (en) | 2011-06-24 | 2014-02-06 | Piramal Enterprises Limited | Compounds for the treatment of cancers associated with human papillomavirus |
| EP2802323B1 (en) | 2012-01-13 | 2016-08-10 | Piramal Enterprises Limited | Pyrrolidine-substituted flavone derivatives for prevention or treatment of oral mucositis |
| WO2014049515A1 (en) | 2012-09-25 | 2014-04-03 | Piramal Enterprises Limited | Pyrrolidine substituted flavones for treatment of renal cystic diseases |
| WO2014128523A1 (en) | 2013-02-19 | 2014-08-28 | Piramal Enterprises Limited | A process for preparation of an intermediate of the pyrrolidine substituted flavones |
| CN111053768B (zh) | 2013-07-12 | 2023-12-12 | 皮拉马尔企业有限公司 | 用于治疗黑素瘤的药物组合 |
| US10555931B2 (en) | 2014-05-28 | 2020-02-11 | Piramal Enterprises Limited | Pharmaceutical combination for the treatment of cancer |
-
2014
- 2014-07-11 CN CN201911007262.XA patent/CN111053768B/zh active Active
- 2014-07-11 TW TW108142557A patent/TW202031253A/zh unknown
- 2014-07-11 ES ES14822283T patent/ES2733929T3/es active Active
- 2014-07-11 AU AU2014288857A patent/AU2014288857B2/en active Active
- 2014-07-11 WO PCT/IB2014/063022 patent/WO2015004636A1/en not_active Ceased
- 2014-07-11 CN CN202311581824.8A patent/CN117731786A/zh active Pending
- 2014-07-11 AR ARP140102577A patent/AR096892A1/es not_active Application Discontinuation
- 2014-07-11 DK DK14822283.9T patent/DK3019166T3/da active
- 2014-07-11 TW TW111106633A patent/TWI839690B/zh active
- 2014-07-11 TW TW103123951A patent/TWI680760B/zh active
- 2014-07-11 US US14/904,407 patent/US11007174B2/en active Active
- 2014-07-11 JP JP2016524936A patent/JP6568060B2/ja active Active
- 2014-07-11 CN CN201480050507.6A patent/CN105530931B/zh active Active
- 2014-07-11 EP EP14822283.9A patent/EP3019166B1/en active Active
- 2014-07-11 TW TW113110009A patent/TW202502325A/zh unknown
- 2014-07-11 CA CA2917742A patent/CA2917742C/en active Active
-
2016
- 2016-01-11 IL IL24357216A patent/IL243572B/en active IP Right Grant
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2018
- 2018-12-13 US US16/218,576 patent/US20190282544A1/en not_active Abandoned
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2019
- 2019-08-01 JP JP2019141995A patent/JP2019206565A/ja active Pending
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2020
- 2020-09-10 JP JP2020152028A patent/JP2021001186A/ja active Pending
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2021
- 2021-02-05 US US17/168,876 patent/US11839591B2/en active Active
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2022
- 2022-02-24 JP JP2022026851A patent/JP7799508B2/ja active Active
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2023
- 2023-10-30 US US18/497,653 patent/US12383530B2/en active Active
- 2023-12-14 JP JP2023210858A patent/JP2024037891A/ja active Pending
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