JP2018527340A5 - - Google Patents
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- JP2018527340A5 JP2018527340A5 JP2018506998A JP2018506998A JP2018527340A5 JP 2018527340 A5 JP2018527340 A5 JP 2018527340A5 JP 2018506998 A JP2018506998 A JP 2018506998A JP 2018506998 A JP2018506998 A JP 2018506998A JP 2018527340 A5 JP2018527340 A5 JP 2018527340A5
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- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- group
- aryl
- cycloalkyl
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 22
- -1 tetrahydropyryl Chemical group 0.000 claims description 7
- 239000007787 solid Substances 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000004076 pyridyl group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 125000001984 thiazolidinyl group Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 3
- 125000002636 imidazolinyl group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 3
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 3
- 125000000160 oxazolidinyl group Chemical group 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 claims 3
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 3
- 125000002755 pyrazolinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 229930194542 Keto Natural products 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims 2
- 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 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010061187 Haematopoietic neoplasm Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 230000001548 androgenic effect Effects 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000004628 isothiazolidinyl group Chemical group S1N(CCC1)* 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 18
- 239000000203 mixture Substances 0.000 description 13
- 235000019439 ethyl acetate Nutrition 0.000 description 9
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 9
- 229920006395 saturated elastomer Polymers 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 239000003480 eluent Substances 0.000 description 3
- 238000003818 flash chromatography Methods 0.000 description 3
- 239000000741 silica gel Substances 0.000 description 3
- 229910002027 silica gel Inorganic materials 0.000 description 3
- MSUCWVADGRZPTK-UHFFFAOYSA-N 8-cyclohexyloxy-6-(1,5-dimethyl-6-oxopyridin-3-yl)-3,4-dihydro-1H-quinolin-2-one Chemical compound Cc1cc(cn(C)c1=O)-c1cc2CCC(=O)Nc2c(OC2CCCCC2)c1 MSUCWVADGRZPTK-UHFFFAOYSA-N 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000012044 organic layer Substances 0.000 description 2
- 239000012074 organic phase Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- WYLZKEAKTKRGKT-UHFFFAOYSA-N 1,3-dimethyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-one Chemical compound CN1C(=O)C(C)=CC(B2OC(C)(C)C(C)(C)O2)=C1 WYLZKEAKTKRGKT-UHFFFAOYSA-N 0.000 description 1
- YCNQPAVKQPLZRS-UHFFFAOYSA-N 2-benzyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane Chemical compound O1C(C)(C)C(C)(C)OB1CC1=CC=CC=C1 YCNQPAVKQPLZRS-UHFFFAOYSA-N 0.000 description 1
- SZYZMTLBWHWQMN-UHFFFAOYSA-N 5-benzyl-6-(1,5-dimethyl-6-oxopyridin-3-yl)-3,4-dihydro-1H-quinolin-2-one Chemical compound C(C1=CC=CC=C1)C1=C2CCC(NC2=CC=C1C1=CN(C(C(=C1)C)=O)C)=O SZYZMTLBWHWQMN-UHFFFAOYSA-N 0.000 description 1
- RZRMZOFTYXSYCZ-UHFFFAOYSA-N 5-chloro-6-(1,5-dimethyl-6-oxopyridin-3-yl)-3,4-dihydro-1H-quinolin-2-one Chemical compound CN1C=C(C=C(C)C1=O)C1=C(Cl)C2=C(NC(=O)CC2)C=C1 RZRMZOFTYXSYCZ-UHFFFAOYSA-N 0.000 description 1
- YCEIEDFTAWMFGB-UHFFFAOYSA-N 6-(1,5-dimethyl-6-oxopyridin-3-yl)-8-(pyridin-3-ylmethylamino)-3,4-dihydro-1H-quinolin-2-one Chemical compound CN1C=C(C=C(C1=O)C)C=1C=C2CCC(NC2=C(C=1)NCC=1C=NC=CC=1)=O YCEIEDFTAWMFGB-UHFFFAOYSA-N 0.000 description 1
- ZYFLZIZCSIPNRB-UHFFFAOYSA-N 6-bromo-5-chloro-1,2,3,4-tetrahydroquinoline Chemical compound N1CCCC2=C1C=CC(Br)=C2Cl ZYFLZIZCSIPNRB-UHFFFAOYSA-N 0.000 description 1
- HGGUWHWVJPOCLK-UHFFFAOYSA-N 6-bromo-7-chloro-3,4-dihydro-1h-quinolin-2-one Chemical compound N1C(=O)CCC2=C1C=C(Cl)C(Br)=C2 HGGUWHWVJPOCLK-UHFFFAOYSA-N 0.000 description 1
- WNKKVKIKEUDRCL-UHFFFAOYSA-N 7-chloro-6-(1,5-dimethyl-6-oxopyridin-3-yl)-3,4-dihydro-1H-quinolin-2-one Chemical compound ClC1=C(C=C2CCC(NC2=C1)=O)C1=CN(C(C(=C1)C)=O)C WNKKVKIKEUDRCL-UHFFFAOYSA-N 0.000 description 1
- QVPNKJKERSHFSW-UHFFFAOYSA-N CC1C=C(Cc(cc(c(CC2)c3)NC2=O)c3C(C=C2C)=CN(C)C2=O)C=CC1 Chemical compound CC1C=C(Cc(cc(c(CC2)c3)NC2=O)c3C(C=C2C)=CN(C)C2=O)C=CC1 QVPNKJKERSHFSW-UHFFFAOYSA-N 0.000 description 1
- ILWNXJWTLKAXSE-UHFFFAOYSA-N CC1C=CC(Cc(c(CC2)c(cc3)NC2=O)c3C(C=C2C)=CN(C)C2=O)=CC1 Chemical compound CC1C=CC(Cc(c(CC2)c(cc3)NC2=O)c3C(C=C2C)=CN(C)C2=O)=CC1 ILWNXJWTLKAXSE-UHFFFAOYSA-N 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- 150000002466 imines Chemical class 0.000 description 1
- 239000010410 layer Substances 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 238000002953 preparative HPLC Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- NDGRWYRVNANFNB-UHFFFAOYSA-N pyrazolidin-3-one Chemical compound O=C1CCNN1 NDGRWYRVNANFNB-UHFFFAOYSA-N 0.000 description 1
- QJZUKDFHGGYHMC-UHFFFAOYSA-N pyridine-3-carbaldehyde Chemical compound O=CC1=CC=CN=C1 QJZUKDFHGGYHMC-UHFFFAOYSA-N 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562203623P | 2015-08-11 | 2015-08-11 | |
| US62/203,623 | 2015-08-11 | ||
| US201662356579P | 2016-06-30 | 2016-06-30 | |
| US62/356,579 | 2016-06-30 | ||
| PCT/CA2016/050943 WO2017024408A1 (en) | 2015-08-11 | 2016-08-11 | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018527340A JP2018527340A (ja) | 2018-09-20 |
| JP2018527340A5 true JP2018527340A5 (enExample) | 2019-09-26 |
Family
ID=57982883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506998A Pending JP2018527340A (ja) | 2015-08-11 | 2016-08-11 | アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US10501438B2 (enExample) |
| EP (1) | EP3334717B1 (enExample) |
| JP (1) | JP2018527340A (enExample) |
| KR (1) | KR20180039117A (enExample) |
| CN (1) | CN108290856A (enExample) |
| AU (1) | AU2016305513A1 (enExample) |
| CA (1) | CA2994472A1 (enExample) |
| HK (1) | HK1256753A1 (enExample) |
| IL (1) | IL257347A (enExample) |
| MX (1) | MX2018001751A (enExample) |
| WO (1) | WO2017024408A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020093162A1 (en) * | 2018-11-07 | 2020-05-14 | Neomed Institute | Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy |
| CN113631535B (zh) * | 2019-03-11 | 2024-04-12 | 协同医药发展有限公司 | 治疗铁死亡相关紊乱的杂芳基和双杂环芳基衍生物 |
| CN112239456B (zh) * | 2020-06-09 | 2021-09-07 | 浙江理工大学 | 一种取代2，3-二氢喹诺酮化合物的制备方法 |
| CN114276333B (zh) * | 2020-09-28 | 2023-05-09 | 中国科学院上海药物研究所 | 二氢喹喔啉类溴结构域二价抑制剂 |
| CN118005653B (zh) * | 2023-04-23 | 2024-12-10 | 信义核新(北京)生物科技有限公司 | 喹诺酮类似物及其用途 |
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| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| ES2635003T3 (es) | 2013-07-09 | 2017-10-02 | Bayer Pharma Aktiengesellschaft | Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas inhibidoras de proteína BET |
| US20150051208A1 (en) | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
| WO2015049629A1 (en) | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
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| MY190835A (en) | 2014-01-09 | 2022-05-12 | Orion Corp | Bicyclic heterrocyclic derivatives as bromodomain inhibitors |
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| CA2966908A1 (en) | 2014-11-13 | 2016-05-19 | Convergene Llc | Methods and compositions for inhibition of bromodomain and extraterminal proteins |
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-
2016
- 2016-08-11 CN CN201680058648.1A patent/CN108290856A/zh active Pending
- 2016-08-11 WO PCT/CA2016/050943 patent/WO2017024408A1/en not_active Ceased
- 2016-08-11 HK HK18115833.9A patent/HK1256753A1/zh unknown
- 2016-08-11 CA CA2994472A patent/CA2994472A1/en not_active Abandoned
- 2016-08-11 AU AU2016305513A patent/AU2016305513A1/en not_active Abandoned
- 2016-08-11 JP JP2018506998A patent/JP2018527340A/ja active Pending
- 2016-08-11 MX MX2018001751A patent/MX2018001751A/es unknown
- 2016-08-11 US US15/751,800 patent/US10501438B2/en active Active
- 2016-08-11 KR KR1020187006580A patent/KR20180039117A/ko not_active Withdrawn
- 2016-08-11 EP EP16834368.9A patent/EP3334717B1/en active Active
-
2018
- 2018-02-04 IL IL257347A patent/IL257347A/en unknown
-
2019
- 2019-10-28 US US16/665,198 patent/US20200299262A1/en not_active Abandoned
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