JP2020517734A5 - - Google Patents
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- JP2020517734A5 JP2020517734A5 JP2020507495A JP2020507495A JP2020517734A5 JP 2020517734 A5 JP2020517734 A5 JP 2020517734A5 JP 2020507495 A JP2020507495 A JP 2020507495A JP 2020507495 A JP2020507495 A JP 2020507495A JP 2020517734 A5 JP2020517734 A5 JP 2020517734A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound
- composition
- cancer
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 42
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 40
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 19
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 18
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 18
- 125000005842 heteroatom Chemical group 0.000 claims description 18
- 229910052760 oxygen Inorganic materials 0.000 claims description 18
- 239000001301 oxygen Chemical group 0.000 claims description 18
- 229910052717 sulfur Inorganic materials 0.000 claims description 18
- 239000011593 sulfur Chemical group 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 12
- 230000001404 mediated effect Effects 0.000 claims description 12
- 229920006395 saturated elastomer Polymers 0.000 claims description 10
- 239000002671 adjuvant Substances 0.000 claims description 8
- 239000003937 drug carrier Substances 0.000 claims description 8
- 239000003981 vehicle Substances 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 125000003118 aryl group Chemical group 0.000 claims description 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 229910052805 deuterium Inorganic materials 0.000 claims description 3
- 229910052736 halogen Inorganic materials 0.000 claims description 3
- 150000002367 halogens Chemical class 0.000 claims description 3
- 229910052739 hydrogen Inorganic materials 0.000 claims description 3
- 150000002431 hydrogen Chemical group 0.000 claims description 3
- 239000001257 hydrogen Substances 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 125000002950 monocyclic group Chemical group 0.000 claims description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 3
- 208000035475 disorder Diseases 0.000 claims 8
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 206010005003 Bladder cancer Diseases 0.000 claims 4
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 4
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 229940127089 cytotoxic agent Drugs 0.000 claims 4
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 4
- 201000005112 urinary bladder cancer Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 229940124060 PD-1 antagonist Drugs 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims 2
- 201000004101 esophageal cancer Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 0 C*1C(c2cc(*)cnc2)=Nc2c(*)cn[n]2C1NC(CC1)Cc2c1[n]cc2 Chemical compound C*1C(c2cc(*)cnc2)=Nc2c(*)cn[n]2C1NC(CC1)Cc2c1[n]cc2 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 3
- 239000012472 biological sample Substances 0.000 description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
- NYDZUYCYKKLQOB-UHFFFAOYSA-N C(C1)C1(CC1)Cc2c1[nH]cc2 Chemical compound C(C1)C1(CC1)Cc2c1[nH]cc2 NYDZUYCYKKLQOB-UHFFFAOYSA-N 0.000 description 1
- FGZKDSLCNWGBTO-UHFFFAOYSA-N CC(C)c1c2nc(-c3cc(F)cnc3)nc(NC(CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cc(F)cnc3)nc(NC(CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 FGZKDSLCNWGBTO-UHFFFAOYSA-N 0.000 description 1
- UMUUJFREWZYFON-UHFFFAOYSA-N CC(C)c1c2nc(-c3cc(F)cnc3)nc(NC(CC3)Cc4c3[nH]cc4)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cc(F)cnc3)nc(NC(CC3)Cc4c3[nH]cc4)[n]2nc1 UMUUJFREWZYFON-UHFFFAOYSA-N 0.000 description 1
- FGZKDSLCNWGBTO-INIZCTEOSA-N CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@@H](CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@@H](CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 FGZKDSLCNWGBTO-INIZCTEOSA-N 0.000 description 1
- FGZKDSLCNWGBTO-MRXNPFEDSA-N CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@H](CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@H](CC3)Cc(c4cc(F)c5)c3[nH]c4c5F)[n]2nc1 FGZKDSLCNWGBTO-MRXNPFEDSA-N 0.000 description 1
- UMUUJFREWZYFON-MRXNPFEDSA-N CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@H](CC3)Cc4c3[nH]cc4)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cc(F)cnc3)nc(N[C@H](CC3)Cc4c3[nH]cc4)[n]2nc1 UMUUJFREWZYFON-MRXNPFEDSA-N 0.000 description 1
- FUCRDFKNOZIVRC-UHFFFAOYSA-N CC(C)c1c2nc(-c3cncc(F)c3)nc(N)[n]2nc1 Chemical compound CC(C)c1c2nc(-c3cncc(F)c3)nc(N)[n]2nc1 FUCRDFKNOZIVRC-UHFFFAOYSA-N 0.000 description 1
- YMIIDPJLUFUSKS-UHFFFAOYSA-N Fc1cc(-c(nc(NCCc2c[nH]c3ccccc23)[n]2nc3)nc2c3Br)cnc1 Chemical compound Fc1cc(-c(nc(NCCc2c[nH]c3ccccc23)[n]2nc3)nc2c3Br)cnc1 YMIIDPJLUFUSKS-UHFFFAOYSA-N 0.000 description 1
- GGGMLOIGHLBDNF-UHFFFAOYSA-N OC(c(cn[n]1c(NCCc(c2ccc3)c[nH]c2c3O)c2)c1nc2-c1cc(F)cnc1)=O Chemical compound OC(c(cn[n]1c(NCCc(c2ccc3)c[nH]c2c3O)c2)c1nc2-c1cc(F)cnc1)=O GGGMLOIGHLBDNF-UHFFFAOYSA-N 0.000 description 1
- WTXGACVQWWAPKD-UHFFFAOYSA-N OCc(cn[n]1c(NCCc(c2ccc3)c[nH]c2c3O)c2)c1nc2-c1cncc(F)c1 Chemical compound OCc(cn[n]1c(NCCc(c2ccc3)c[nH]c2c3O)c2)c1nc2-c1cncc(F)c1 WTXGACVQWWAPKD-UHFFFAOYSA-N 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 125000001183 hydrocarbyl group Chemical group 0.000 description 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022091740A JP2022116319A (ja) | 2017-04-21 | 2022-06-06 | インドールahr阻害剤およびその使用 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762488476P | 2017-04-21 | 2017-04-21 | |
| US62/488,476 | 2017-04-21 | ||
| US201762592542P | 2017-11-30 | 2017-11-30 | |
| US62/592,542 | 2017-11-30 | ||
| US201862658454P | 2018-04-16 | 2018-04-16 | |
| US62/658,454 | 2018-04-16 | ||
| PCT/US2018/028532 WO2018195397A2 (en) | 2017-04-21 | 2018-04-20 | Indole ahr inhibitors and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022091740A Division JP2022116319A (ja) | 2017-04-21 | 2022-06-06 | インドールahr阻害剤およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020517734A JP2020517734A (ja) | 2020-06-18 |
| JP2020517734A5 true JP2020517734A5 (https=) | 2021-05-27 |
| JP7232244B2 JP7232244B2 (ja) | 2023-03-08 |
Family
ID=63856153
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020507495A Active JP7232244B2 (ja) | 2017-04-21 | 2018-04-20 | インドールahr阻害剤およびその使用 |
| JP2022091740A Withdrawn JP2022116319A (ja) | 2017-04-21 | 2022-06-06 | インドールahr阻害剤およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022091740A Withdrawn JP2022116319A (ja) | 2017-04-21 | 2022-06-06 | インドールahr阻害剤およびその使用 |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US10570138B2 (https=) |
| EP (2) | EP4710923A2 (https=) |
| JP (2) | JP7232244B2 (https=) |
| KR (1) | KR102668371B1 (https=) |
| CN (1) | CN110831600B (https=) |
| AU (1) | AU2018256459B2 (https=) |
| CA (1) | CA3059939A1 (https=) |
| CL (1) | CL2019003015A1 (https=) |
| CO (1) | CO2019011584A2 (https=) |
| FI (1) | FI3612030T3 (https=) |
| IL (1) | IL270025B2 (https=) |
| MX (1) | MX2019012431A (https=) |
| NZ (1) | NZ758243A (https=) |
| PT (1) | PT3612030T (https=) |
| SG (1) | SG11201909710XA (https=) |
| TW (1) | TWI778050B (https=) |
| WO (1) | WO2018195397A2 (https=) |
| ZA (1) | ZA201906822B (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| LT3555097T (lt) | 2016-12-16 | 2022-08-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pirolo[2,3-b]piridino junginiai kaip janus kinazės inhibitoriai |
| MX392743B (es) * | 2017-04-12 | 2025-03-12 | Magenta Therapeutics Inc | Antagonistas del receptor de hidrocarburo de arilo y sus usos. |
| WO2018195397A2 (en) | 2017-04-21 | 2018-10-25 | Kyn Therapeutics | Indole ahr inhibitors and uses thereof |
| FR3066761B1 (fr) * | 2017-05-23 | 2020-10-30 | Centre Nat Rech Scient | Nouveaux composes inhibiteurs des canaux ioniques |
| WO2019036657A1 (en) | 2017-08-17 | 2019-02-21 | Kyn Therapeutics | AHR INHIBITORS AND USES THEREOF |
| ES2946632T7 (es) | 2018-02-06 | 2025-03-04 | Ideaya Biosciences Inc | Moduladores de AhR |
| WO2019156989A1 (en) * | 2018-02-06 | 2019-08-15 | Ideaya Biosciences, Inc. | COMPOUNDS AND METHODS FOR THE MODULATION OF AhR |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Jak激酶家族之小分子抑制劑 |
| JP7448527B2 (ja) * | 2018-09-07 | 2024-03-12 | 大塚製薬株式会社 | ヘテロ環式化合物 |
| US20220144839A1 (en) * | 2018-10-16 | 2022-05-12 | Ikena Oncology, Inc. | Indole ahr inhibitors and uses thereof |
| WO2020081840A1 (en) * | 2018-10-17 | 2020-04-23 | Magenta Therapeutics Inc. | Methods of treating cancer with aryl hydrocarbon receptor antagonists |
| EA202191507A1 (ru) * | 2018-11-30 | 2021-08-20 | Селулэрити Инк. | Ароматические соединения для применения для активации кроветворных стволовых клеток и клеток-предшественников |
| CN113454207A (zh) * | 2018-11-30 | 2021-09-28 | 细胞结构公司 | 用新型芳香族化合物扩增自然杀伤细胞和ilc3细胞 |
| CN109813913B (zh) * | 2019-01-31 | 2021-11-09 | 中国医学科学院肿瘤医院 | 芳烃受体(AhR)在预测免疫治疗效果中的应用 |
| KR20210131316A (ko) | 2019-02-27 | 2021-11-02 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Sumo-활성화 효소 저해제 및 관문 저해제의 투여 |
| EP4710922A2 (en) * | 2019-07-30 | 2026-03-18 | Oregon State University | Aryl hydrocarbon receptor activators |
| EP4061484A1 (en) * | 2019-11-22 | 2022-09-28 | Senda Biosciences, Inc. | Pyridopyrimidinone derivatives as ahr antagonists |
| PT4065582T (pt) * | 2019-11-26 | 2025-05-22 | Ikena Oncology Inc | Derivados polimórficos do carbazol e utilizações dos mesmos |
| US20230041743A1 (en) * | 2019-11-26 | 2023-02-09 | Hoffmann-La Roche Inc. | 1,8-naphthyridin-2-one compounds for the treatment of autoimmune disease |
| BR112022010143A2 (pt) | 2019-11-26 | 2022-08-09 | Ikena Oncology Inc | Inibidores de ahr e usos respectivos |
| TW202146416A (zh) | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
| KR20220125323A (ko) | 2020-01-10 | 2022-09-14 | 이케나 온콜로지, 인코포레이티드 | Ahr 억제제 및 이의 용도 |
| US20230279000A1 (en) | 2020-02-26 | 2023-09-07 | Jaguahr Therapeutics Pte Ltd | Pyridopyrimidine derivatives useful in modulation of ahr signalling |
| CN115397818A (zh) * | 2020-03-27 | 2022-11-25 | 东亚St株式会社 | 氨基嘧啶衍生物及其作为芳烃受体调节剂的应用 |
| WO2021236717A1 (en) | 2020-05-20 | 2021-11-25 | Senda Biosciences, Inc. | Fused imidazole derivatives as ahr antagonists |
| US11857551B1 (en) | 2020-07-10 | 2024-01-02 | Ting Therapeutics Llc | Methods for the prevention and treatment of hearing loss |
| WO2022029063A1 (en) * | 2020-08-04 | 2022-02-10 | Bayer Aktiengesellschaft | Pyrido[1,2,4]triazolo[1,5-c]pyrimidin-5-amines |
| WO2022078356A1 (zh) * | 2020-10-15 | 2022-04-21 | 山东轩竹医药科技有限公司 | 杂芳环类AhR抑制剂 |
| IL302346A (en) | 2020-10-28 | 2023-06-01 | Ikena Oncology Inc | Combination of an ahr inhibitor with a pdx inhibitor or doxorubicine |
| CN114644627B (zh) * | 2020-12-18 | 2024-06-11 | 山东轩竹医药科技有限公司 | AhR抑制剂及其用途 |
| CN112656789A (zh) * | 2020-12-31 | 2021-04-16 | 中国科学院生态环境研究中心 | Ficz在抑制肿瘤细胞迁移中的应用 |
| CN114805361B (zh) * | 2021-01-17 | 2024-02-20 | 上海凌达生物医药有限公司 | 一类氨基取代的芳香杂环并吡唑类化合物、制备方法和用途 |
| BR112023018286A2 (pt) | 2021-03-11 | 2023-10-31 | Janssen Pharmaceutica Nv | Lorpucitinib para uso no tratamento de distúrbios mediados por jak |
| WO2023020512A1 (zh) * | 2021-08-16 | 2023-02-23 | 成都奥睿药业有限公司 | 取代的吡啶类似物、其制备方法及作为ahr调节剂的用途 |
| WO2023033741A1 (en) * | 2021-09-02 | 2023-03-09 | Jaguahr Therapeutics Pte Ltd | Compounds useful in modulation of ahr signalling |
| KR20240054994A (ko) * | 2021-09-02 | 2024-04-26 | 재규어 테라퓨틱스 피티이 리미티드 | AhR 시그널링의 조절에 유용한 화합물 |
| WO2023033742A1 (en) * | 2021-09-02 | 2023-03-09 | Jaguahr Therapeutics Pte Ltd | Compounds useful in modulation of ahr signalling |
| CN115093400B (zh) * | 2021-09-18 | 2023-09-05 | 北京华森英诺生物科技有限公司 | AhR抑制剂及其用途和制备方法 |
| WO2023060227A1 (en) | 2021-10-07 | 2023-04-13 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| CN115925684B (zh) * | 2021-12-03 | 2025-02-28 | 徐诺药业(南京)有限公司 | 一种嘧啶类衍生物及其制备方法和应用 |
| JP2025502240A (ja) | 2022-01-11 | 2025-01-24 | ドイッチェス・クレープスフォルシュングスツェントルム | がんの治療のための二環式トリアジン誘導体 |
| AU2023249795A1 (en) | 2022-04-08 | 2024-10-17 | Shy Therapeutics, Llc | Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| CN117624168A (zh) * | 2022-08-19 | 2024-03-01 | 德明药泰生物技术(深圳)有限公司 | 稠环杂环类化合物及其制备方法和应用 |
| CN115850329A (zh) * | 2022-09-16 | 2023-03-28 | 东莞市均成高新材料有限公司 | 环三联芳膦、它们的制备方法及用途 |
| WO2024076300A1 (en) | 2022-10-03 | 2024-04-11 | Jaguahr Therapeutics Pte Ltd | Compounds useful in modulation of ahr signalling |
| CN115804776A (zh) * | 2022-12-16 | 2023-03-17 | 国纳之星(上海)纳米科技发展有限公司 | 一种芳香烃受体抑制剂和5-氟尿嘧啶合用在治疗抑制肿瘤药物中的应用 |
| CN116482278B (zh) * | 2023-05-06 | 2024-02-09 | 广州清瑞生物科技有限责任公司 | 一种用于检测阿昔洛韦的对照品的制备方法 |
| US20250084087A1 (en) * | 2023-08-18 | 2025-03-13 | Incyte Corporation | Bicyclic heterocycles as mrgprx2 antagonists |
| EP4512427A1 (en) | 2023-08-25 | 2025-02-26 | Mablink Bioscience | Antibody-drug conjugates based on molecular glue degraders and uses thereof |
| EP4512806A1 (en) | 2023-08-25 | 2025-02-26 | Mablink Bioscience | Molecular glue degraders and uses thereof |
| CN117229284B (zh) * | 2023-11-10 | 2024-02-06 | 上海泽德曼医药科技有限公司 | 三环稠杂环类化合物、其制备方法及其在医药上的应用 |
| WO2025114771A1 (en) | 2023-11-29 | 2025-06-05 | Latvian Institute Of Organic Synthesis | A new class of aryl hydrocarbon receptor antagonists and their optimisation |
| WO2025254418A1 (ko) * | 2024-06-03 | 2025-12-11 | 동아에스티 주식회사 | 아미노피리미딘 유도체의 결정다형 및 이의 제조방법 |
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- 2018-04-20 FI FIEP18787414.4T patent/FI3612030T3/fi active
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- 2018-04-20 KR KR1020197034489A patent/KR102668371B1/ko active Active
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- 2018-04-20 CN CN201880038301.XA patent/CN110831600B/zh active Active
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