JP2019070032A5 - - Google Patents
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- Publication number
- JP2019070032A5 JP2019070032A5 JP2019005976A JP2019005976A JP2019070032A5 JP 2019070032 A5 JP2019070032 A5 JP 2019070032A5 JP 2019005976 A JP2019005976 A JP 2019005976A JP 2019005976 A JP2019005976 A JP 2019005976A JP 2019070032 A5 JP2019070032 A5 JP 2019070032A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- amino
- optionally substituted
- phenyl
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 70
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 239000012453 solvate Substances 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- -1 2- (6-Carbamoyl-2- (4- (2-((diethylamino) methyl) -4- (trifluoromethyl) phenoxy) phenyl) pyrimidin-4-yl) ethyl Chemical group 0.000 claims 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000004663 dialkyl amino group Chemical group 0.000 claims 8
- 208000002193 Pain Diseases 0.000 claims 7
- HKSQZEGSMBFHGC-UHFFFAOYSA-N pyrimidine-4-carboxamide Chemical compound NC(=O)C1=CC=NC=N1 HKSQZEGSMBFHGC-UHFFFAOYSA-N 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 5
- 230000036407 pain Effects 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000005518 carboxamido group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 3
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 3
- 125000004990 dihydroxyalkyl group Chemical group 0.000 claims 3
- 125000004476 heterocycloamino group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims 3
- QPZVNWNSRAIMET-AWEZNQCLSA-N 6-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-2-[4-[2-(2-methylpyrazol-3-yl)phenoxy]phenyl]pyrimidine-4-carboxamide Chemical compound C[C@H](Nc1cc(nc(n1)-c1ccc(Oc2ccccc2-c2ccnn2C)cc1)C(N)=O)C(N)=O QPZVNWNSRAIMET-AWEZNQCLSA-N 0.000 claims 2
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Natural products CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 2
- 108010052164 Sodium Channels Proteins 0.000 claims 2
- 102000018674 Sodium Channels Human genes 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
- 125000004992 haloalkylamino group Chemical group 0.000 claims 2
- 125000005241 heteroarylamino group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
- UAQAAAZYNALVQM-NRFANRHFSA-N 2-[4-[2-(diethylaminomethyl)-4-(trifluoromethyl)phenoxy]phenyl]-6-[(1R)-1,2-dihydroxyethyl]pyrimidine-4-carboxamide Chemical compound CCN(CC)Cc1cc(ccc1Oc1ccc(cc1)-c1nc(cc(n1)C(N)=O)[C@@H](O)CO)C(F)(F)F UAQAAAZYNALVQM-NRFANRHFSA-N 0.000 claims 1
- UAQAAAZYNALVQM-OAQYLSRUSA-N 2-[4-[2-(diethylaminomethyl)-4-(trifluoromethyl)phenoxy]phenyl]-6-[(1S)-1,2-dihydroxyethyl]pyrimidine-4-carboxamide Chemical compound CCN(CC)Cc1cc(ccc1Oc1ccc(cc1)-c1nc(cc(n1)C(N)=O)[C@H](O)CO)C(F)(F)F UAQAAAZYNALVQM-OAQYLSRUSA-N 0.000 claims 1
- QWBXMHXJKJUMFV-UHFFFAOYSA-N 6-(2-imidazol-1-ylethyl)-2-[4-[2-(morpholin-4-ylmethyl)-4-(trifluoromethyl)phenoxy]phenyl]pyrimidine-4-carboxamide Chemical compound NC(=O)c1cc(CCn2ccnc2)nc(n1)-c1ccc(Oc2ccc(cc2CN2CCOCC2)C(F)(F)F)cc1 QWBXMHXJKJUMFV-UHFFFAOYSA-N 0.000 claims 1
- UANMGMBFKIXLJG-HXUWFJFHSA-N 6-[(1S)-1,2-dihydroxyethyl]-2-[4-[2-(2-methylpyrazol-3-yl)-4-(trifluoromethyl)phenoxy]phenyl]pyrimidine-4-carboxamide Chemical compound Cn1nccc1-c1cc(ccc1Oc1ccc(cc1)-c1nc(cc(n1)C(N)=O)[C@H](O)CO)C(F)(F)F UANMGMBFKIXLJG-HXUWFJFHSA-N 0.000 claims 1
- ZYIVXWLQKLQJGC-UHFFFAOYSA-N 6-carbamoyl-2-[4-[2-(diethylaminomethyl)-4-(trifluoromethyl)phenoxy]phenyl]pyrimidine-4-carboxylic acid Chemical compound CCN(CC)Cc1cc(ccc1Oc1ccc(cc1)-c1nc(cc(n1)C(O)=O)C(N)=O)C(F)(F)F ZYIVXWLQKLQJGC-UHFFFAOYSA-N 0.000 claims 1
- SNBNRCMFNZKFBO-UHFFFAOYSA-N 6-carbamoyl-2-[4-[2-(morpholin-4-ylmethyl)-4-(trifluoromethyl)phenoxy]phenyl]pyrimidine-4-carboxylic acid Chemical compound NC(=O)c1cc(nc(n1)-c1ccc(Oc2ccc(cc2CN2CCOCC2)C(F)(F)F)cc1)C(O)=O SNBNRCMFNZKFBO-UHFFFAOYSA-N 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010008027 Cerebellar atrophy Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000036626 Mental retardation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000028389 Nerve injury Diseases 0.000 claims 1
- 101100070530 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) het-6 gene Proteins 0.000 claims 1
- 208000027520 Somatoform disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 101150046432 Tril gene Proteins 0.000 claims 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000002690 local anesthesia Methods 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 230000008764 nerve damage Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000027753 pain disease Diseases 0.000 claims 1
- 238000002638 palliative care Methods 0.000 claims 1
- 230000001314 paroxysmal effect Effects 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361789502P | 2013-03-15 | 2013-03-15 | |
| US61/789,502 | 2013-03-15 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017146602A Division JP6470358B2 (ja) | 2013-03-15 | 2017-07-28 | カルボキサミド誘導体及びその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019070032A JP2019070032A (ja) | 2019-05-09 |
| JP2019070032A5 true JP2019070032A5 (enExample) | 2019-06-13 |
| JP6830498B2 JP6830498B2 (ja) | 2021-02-17 |
Family
ID=51581639
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501929A Active JP6186494B2 (ja) | 2013-03-15 | 2014-03-13 | カルボキサミド誘導体及びその使用 |
| JP2017146602A Active JP6470358B2 (ja) | 2013-03-15 | 2017-07-28 | カルボキサミド誘導体及びその使用 |
| JP2019005976A Active JP6830498B2 (ja) | 2013-03-15 | 2019-01-17 | カルボキサミド誘導体及びその使用 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501929A Active JP6186494B2 (ja) | 2013-03-15 | 2014-03-13 | カルボキサミド誘導体及びその使用 |
| JP2017146602A Active JP6470358B2 (ja) | 2013-03-15 | 2017-07-28 | カルボキサミド誘導体及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9493449B2 (enExample) |
| EP (2) | EP2968307A4 (enExample) |
| JP (3) | JP6186494B2 (enExample) |
| AU (2) | AU2014235063B2 (enExample) |
| CA (2) | CA3082427A1 (enExample) |
| WO (1) | WO2014151393A2 (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012007836A1 (en) | 2010-07-16 | 2012-01-19 | Purdue Pharma .Lp. | Pyridine compounds as sodium channel blockers |
| EP2616441B1 (en) | 2010-09-17 | 2019-08-07 | Purdue Pharma L.P. | Pyridine compounds and the uses thereof |
| JP2013540130A (ja) | 2010-10-05 | 2013-10-31 | パーデュー、ファーマ、リミテッド、パートナーシップ | ナトリウムチャネル遮断剤としてのキナゾリン化合物 |
| CA2822789A1 (en) | 2010-12-22 | 2012-06-28 | Purdue Pharma L.P. | Substituted pyridines as sodium channel blockers |
| TW201331186A (zh) | 2011-09-02 | 2013-08-01 | Purdue Pharma Lp | 作為鈉通道阻斷劑之嘧啶類 |
| WO2013064884A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| WO2013064883A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
| WO2013072758A1 (en) | 2011-11-15 | 2013-05-23 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| US9206127B2 (en) | 2012-03-16 | 2015-12-08 | Purdue Pharm, L.P. | Substituted pyridines as sodium channel blockers |
| EP3333156A3 (en) | 2012-11-09 | 2018-09-26 | Purdue Pharma L.P. | Benzomorphan analogs and the use thereof |
| US9714252B2 (en) | 2012-12-20 | 2017-07-25 | Purdue Pharma L.P. | Cyclic sulfonamides as sodium channel blockers |
| EP3293184B1 (en) | 2013-03-04 | 2020-12-16 | Purdue Pharma L.P. | Pyrimidine carboxamides as sodium channel blockers |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| CA3082427A1 (en) * | 2013-03-15 | 2014-09-25 | Purdue Pharma L.P. | Carboxamide derivatives and use thereof |
| EP3039019B1 (en) | 2013-08-26 | 2020-04-22 | Purdue Pharma L.P. | Azaspiro[4.5]decane derivatives and use thereof |
| US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
| US9340504B2 (en) | 2013-11-21 | 2016-05-17 | Purdue Pharma L.P. | Pyridine and piperidine derivatives as novel sodium channel blockers |
| US9745287B2 (en) | 2013-12-20 | 2017-08-29 | Purdue Pharma L.P. | Pyrimidines and use thereof |
| WO2015099841A1 (en) | 2013-12-23 | 2015-07-02 | Purdue Pharma L.P. | Indazoles and use thereof |
| US9695144B2 (en) | 2013-12-23 | 2017-07-04 | Purdue Pharma L.P. | Dibenzazepine derivatives and use thereof |
| EP3087073B1 (en) | 2013-12-26 | 2018-07-04 | Purdue Pharma LP | 10-substituted morphinan hydantoins |
| US9902726B2 (en) | 2013-12-30 | 2018-02-27 | Purdue Pharma L.P. | Pyridone-sulfone morphinan analogs as opioid receptor ligands |
| JP6526023B2 (ja) | 2014-01-24 | 2019-06-05 | パーデュー、ファーマ、リミテッド、パートナーシップ | ピリジン類及びピリミジン類並びにその使用 |
| CA2939501C (en) | 2014-02-12 | 2020-07-07 | Purdue Pharma L.P. | Isoquinoline derivatives and use thereof |
| US10730866B2 (en) | 2014-04-07 | 2020-08-04 | Purdue Pharma L.P. | Indole derivatives and use thereof |
| CA2948144A1 (en) | 2014-05-06 | 2015-11-12 | Purdue Pharma L.P. | Benzomorphan analogs and use thereof |
| EP3154972A4 (en) | 2014-06-13 | 2017-11-22 | Purdue Pharma L.P. | Azamophinan derivatives and use thereof |
| MA40170A (fr) | 2014-06-13 | 2017-04-19 | Purdue Pharma Lp | Dérivés hétérocycliques de morphinan et leur utilisation |
| GB201417497D0 (en) * | 2014-10-03 | 2014-11-19 | Convergence Pharmaceuticals | Novel use |
| GB201417500D0 (en) * | 2014-10-03 | 2014-11-19 | Convergence Pharmaceuticals | Novel use |
| AU2016219879A1 (en) | 2015-02-19 | 2017-08-24 | Purdue Pharma L.P. | Methods and compositions for decreasing gastric emptying |
| TWI730002B (zh) | 2015-09-18 | 2021-06-11 | 日商科研製藥股份有限公司 | 聯芳系化合物及含有此化合物之醫藥 |
| WO2017160922A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| US10745402B2 (en) | 2017-01-02 | 2020-08-18 | Purdue Pharma L.P. | Morphinan derivatives and use thereof |
| WO2019126842A1 (en) * | 2017-12-27 | 2019-07-04 | Bionomics Limited | Therapeutic compounds and uses thereof |
| CA3105657A1 (en) | 2018-07-09 | 2020-01-16 | Lieber Institute, Inc. | Pyridine carboxamide compounds for inhibiting nav1.8 |
| CA3105748A1 (en) | 2018-07-09 | 2020-01-16 | Lieber Institute, Inc. | Pyridazine compounds for inhibiting nav1.8 |
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| TW201331186A (zh) | 2011-09-02 | 2013-08-01 | Purdue Pharma Lp | 作為鈉通道阻斷劑之嘧啶類 |
| WO2013064884A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| WO2013064883A1 (en) * | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
| WO2013072758A1 (en) * | 2011-11-15 | 2013-05-23 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| US9206127B2 (en) | 2012-03-16 | 2015-12-08 | Purdue Pharm, L.P. | Substituted pyridines as sodium channel blockers |
| WO2014016673A1 (en) | 2012-07-27 | 2014-01-30 | Purdue Pharma L.P. | Sodium channel blocking peptides and the use thereof |
| US9714252B2 (en) | 2012-12-20 | 2017-07-25 | Purdue Pharma L.P. | Cyclic sulfonamides as sodium channel blockers |
| KR101493882B1 (ko) | 2013-02-28 | 2015-02-17 | 서울대학교산학협력단 | 신규한 헤테로아릴카르복스아마이드 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 ｒａｇｅ 수용체 관련 질환의 예방 또는 치료용 약학적 조성물 |
| EP3293184B1 (en) | 2013-03-04 | 2020-12-16 | Purdue Pharma L.P. | Pyrimidine carboxamides as sodium channel blockers |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| CN105073397A (zh) * | 2013-03-06 | 2015-11-18 | 倍耐力轮胎股份公司 | 用于构建用于车辆车轮的轮胎的处理、用于车辆车轮的轮胎和用于优化轮胎的胎体结构中的载荷分布的方法 |
| CA3082427A1 (en) * | 2013-03-15 | 2014-09-25 | Purdue Pharma L.P. | Carboxamide derivatives and use thereof |
| EP3039019B1 (en) | 2013-08-26 | 2020-04-22 | Purdue Pharma L.P. | Azaspiro[4.5]decane derivatives and use thereof |
| US9359330B2 (en) | 2013-08-26 | 2016-06-07 | Purdue Pharma L.P. | Substituted piperidines as sodium channel blockers |
| US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
| US9340504B2 (en) | 2013-11-21 | 2016-05-17 | Purdue Pharma L.P. | Pyridine and piperidine derivatives as novel sodium channel blockers |
| US9745287B2 (en) | 2013-12-20 | 2017-08-29 | Purdue Pharma L.P. | Pyrimidines and use thereof |
| WO2015099841A1 (en) | 2013-12-23 | 2015-07-02 | Purdue Pharma L.P. | Indazoles and use thereof |
| EP3087079B1 (en) | 2013-12-26 | 2019-04-03 | Purdue Pharma LP | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| AU2014370062A1 (en) | 2013-12-26 | 2016-08-11 | Purdue Pharma L.P. | Ring-contracted morphinans and the use thereof |
| JP6526023B2 (ja) | 2014-01-24 | 2019-06-05 | パーデュー、ファーマ、リミテッド、パートナーシップ | ピリジン類及びピリミジン類並びにその使用 |
| CA2939501C (en) | 2014-02-12 | 2020-07-07 | Purdue Pharma L.P. | Isoquinoline derivatives and use thereof |
| US10730866B2 (en) | 2014-04-07 | 2020-08-04 | Purdue Pharma L.P. | Indole derivatives and use thereof |
-
2014
- 2014-03-13 CA CA3082427A patent/CA3082427A1/en active Pending
- 2014-03-13 AU AU2014235063A patent/AU2014235063B2/en active Active
- 2014-03-13 EP EP14770495.1A patent/EP2968307A4/en not_active Ceased
- 2014-03-13 US US14/776,527 patent/US9493449B2/en active Active
- 2014-03-13 CA CA2939549A patent/CA2939549C/en active Active
- 2014-03-13 WO PCT/US2014/025644 patent/WO2014151393A2/en not_active Ceased
- 2014-03-13 EP EP20155483.9A patent/EP3666274A1/en not_active Withdrawn
- 2014-03-13 JP JP2016501929A patent/JP6186494B2/ja active Active
-
2016
- 2016-10-07 US US15/288,988 patent/US10005768B2/en active Active
-
2017
- 2017-06-23 AU AU2017204263A patent/AU2017204263B2/en active Active
- 2017-07-28 JP JP2017146602A patent/JP6470358B2/ja active Active
-
2019
- 2019-01-17 JP JP2019005976A patent/JP6830498B2/ja active Active
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