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 (https=) | 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 (https=) |
| EP (2) | EP2968307A4 (https=) |
| JP (3) | JP6186494B2 (https=) |
| AU (2) | AU2014235063B2 (https=) |
| CA (2) | CA2939549C (https=) |
| WO (1) | WO2014151393A2 (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013531687A (ja) | 2010-07-16 | 2013-08-08 | 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ピリジン化合物 |
| AU2011303597A1 (en) | 2010-09-17 | 2013-04-11 | Purdue Pharma L.P. | Pyridine compounds and the uses thereof |
| KR20130095772A (ko) | 2010-10-05 | 2013-08-28 | 퍼듀 퍼머 엘피 | 나트륨 채널 차단제로서 퀴나졸린 화합물 |
| EP2655330B1 (en) | 2010-12-22 | 2016-02-10 | Purdue Pharma LP | Substituted pyridines as sodium channel blockers |
| EP3255041A1 (en) | 2011-09-02 | 2017-12-13 | Purdue Pharma L.P. | Pyrimidines as sodium channel blockers |
| WO2013064883A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
| WO2013064884A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| US9133131B2 (en) | 2011-11-15 | 2015-09-15 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| WO2013136170A1 (en) | 2012-03-16 | 2013-09-19 | Purdue Pharma L.P. | Substituted pyridines as sodium channel blockers |
| EP2917182B1 (en) | 2012-11-09 | 2018-01-03 | Purdue Pharma LP | Benzomorphan analogs and the use thereof |
| EP2935257B1 (en) | 2012-12-20 | 2018-02-07 | Purdue Pharma LP | Cyclic sulfonamides as sodium channel blockers |
| WO2014135955A1 (en) | 2013-03-04 | 2014-09-12 | 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 |
| CA2939549C (en) * | 2013-03-15 | 2020-08-18 | Purdue Pharma L.P. | Carboxamide derivatives and use thereof |
| CN105612152A (zh) | 2013-08-26 | 2016-05-25 | 普渡制药公司 | 氮杂螺[4.5]癸烷衍生物及其用途 |
| 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 |
| JP6337124B2 (ja) | 2013-12-23 | 2018-06-06 | パーデュー、ファーマ、リミテッド、パートナーシップ | インダゾール及びその使用 |
| US9695144B2 (en) | 2013-12-23 | 2017-07-04 | Purdue Pharma L.P. | Dibenzazepine derivatives and use thereof |
| WO2015097547A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | 10-substituted morphinan hydantoins |
| EP3089978B1 (en) | 2013-12-30 | 2018-08-29 | 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 |
| AU2015217185B2 (en) | 2014-02-12 | 2018-04-05 | 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 |
| MA40171A (fr) | 2014-06-13 | 2017-04-19 | Purdue Pharma Lp | Dérivés d'azamophinan et leur utilisation |
| WO2015192039A1 (en) | 2014-06-13 | 2015-12-17 | Purdue Pharma L.P. | Heterocyclic morphinan derivatives and use thereof |
| GB201417497D0 (en) * | 2014-10-03 | 2014-11-19 | Convergence Pharmaceuticals | Novel use |
| GB201417500D0 (en) * | 2014-10-03 | 2014-11-19 | Convergence Pharmaceuticals | Novel use |
| BR112017017619A2 (pt) | 2015-02-19 | 2018-05-08 | Purdue Pharma Lp | métodos e composições para diminuir esvaziamento gástrico |
| SG11201801856XA (en) | 2015-09-18 | 2018-04-27 | Kaken Pharmaceutical Co Ltd | Biaryl derivative and medicine containing same |
| WO2017160922A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| WO2018125716A1 (en) | 2017-01-02 | 2018-07-05 | 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 |
| AU2019302534B2 (en) | 2018-07-09 | 2024-10-03 | Lieber Institute, Inc. | Pyridazine compounds for inhibiting NaV1.8 |
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| EP2655330B1 (en) * | 2010-12-22 | 2016-02-10 | Purdue Pharma LP | Substituted pyridines as sodium channel blockers |
| EP3255041A1 (en) | 2011-09-02 | 2017-12-13 | Purdue Pharma L.P. | Pyrimidines as sodium channel blockers |
| WO2013064883A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
| WO2013064884A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| US9133131B2 (en) | 2011-11-15 | 2015-09-15 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| WO2013136170A1 (en) | 2012-03-16 | 2013-09-19 | Purdue Pharma L.P. | Substituted pyridines as sodium channel blockers |
| US9718865B2 (en) | 2012-07-27 | 2017-08-01 | Purdue Pharma L.P. | Sodium channel blocking peptides and the use thereof |
| EP2935257B1 (en) | 2012-12-20 | 2018-02-07 | Purdue Pharma LP | 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 |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| WO2014135955A1 (en) | 2013-03-04 | 2014-09-12 | Purdue Pharma L.P. | Pyrimidine carboxamides as sodium channel blockers |
| CN110435360A (zh) * | 2013-03-06 | 2019-11-12 | 倍耐力轮胎股份公司 | 用于车辆车轮的轮胎 |
| CA2939549C (en) * | 2013-03-15 | 2020-08-18 | Purdue Pharma L.P. | Carboxamide derivatives and use thereof |
| US9359330B2 (en) | 2013-08-26 | 2016-06-07 | Purdue Pharma L.P. | Substituted piperidines as sodium channel blockers |
| CN105612152A (zh) | 2013-08-26 | 2016-05-25 | 普渡制药公司 | 氮杂螺[4.5]癸烷衍生物及其用途 |
| 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 |
| JP6337124B2 (ja) | 2013-12-23 | 2018-06-06 | パーデュー、ファーマ、リミテッド、パートナーシップ | インダゾール及びその使用 |
| EP3087057A4 (en) | 2013-12-26 | 2017-06-28 | Purdue Pharma LP | Ring-contracted morphinans and the use thereof |
| WO2015097545A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| 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 |
| AU2015217185B2 (en) | 2014-02-12 | 2018-04-05 | 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 CA2939549A patent/CA2939549C/en active Active
- 2014-03-13 JP JP2016501929A patent/JP6186494B2/ja active Active
- 2014-03-13 CA CA3082427A patent/CA3082427A1/en active Pending
- 2014-03-13 WO PCT/US2014/025644 patent/WO2014151393A2/en not_active Ceased
- 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 EP EP20155483.9A patent/EP3666274A1/en not_active Withdrawn
- 2014-03-13 AU AU2014235063A patent/AU2014235063B2/en active Active
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2016
- 2016-10-07 US US15/288,988 patent/US10005768B2/en active Active
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2017
- 2017-06-23 AU AU2017204263A patent/AU2017204263B2/en active Active
- 2017-07-28 JP JP2017146602A patent/JP6470358B2/ja active Active
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2019
- 2019-01-17 JP JP2019005976A patent/JP6830498B2/ja active Active
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