JP2019031560A5 - - Google Patents
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- Publication number
- JP2019031560A5 JP2019031560A5 JP2018206109A JP2018206109A JP2019031560A5 JP 2019031560 A5 JP2019031560 A5 JP 2019031560A5 JP 2018206109 A JP2018206109 A JP 2018206109A JP 2018206109 A JP2018206109 A JP 2018206109A JP 2019031560 A5 JP2019031560 A5 JP 2019031560A5
- Authority
- JP
- Japan
- Prior art keywords
- kinase
- acceptable salt
- hydrate
- solvate
- related disorder
- 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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- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 24
- 239000011780 sodium chloride Substances 0.000 claims 24
- 201000010099 disease Diseases 0.000 claims 22
- 239000000203 mixture Substances 0.000 claims 22
- 239000012453 solvate Substances 0.000 claims 22
- 102000030951 Phosphotransferases Human genes 0.000 claims 20
- 108091000081 Phosphotransferases Proteins 0.000 claims 20
- 208000008466 Metabolic Disease Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 201000011240 frontotemporal dementia Diseases 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 3
- 108040005185 1-phosphatidylinositol-3-kinase activity proteins Proteins 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 3
- 108009000433 Amyotrophic lateral sclerosis (ALS) Proteins 0.000 claims 2
- 206010003816 Autoimmune disease Diseases 0.000 claims 2
- 210000004227 Basal Ganglia Anatomy 0.000 claims 2
- 210000004369 Blood Anatomy 0.000 claims 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims 2
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 claims 2
- 201000001971 Huntington's disease Diseases 0.000 claims 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010061536 Parkinson's disease Diseases 0.000 claims 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 2
- 201000011585 Pick's disease Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004027 cells Anatomy 0.000 claims 2
- 230000001054 cortical Effects 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 200000000018 inflammatory disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 2
- 230000002062 proliferating Effects 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 101700001448 MAPK3 Proteins 0.000 claims 1
- 101710029928 MAPK4 Proteins 0.000 claims 1
- 102100014833 MKNK1 Human genes 0.000 claims 1
- 101700087081 MKNK1 Proteins 0.000 claims 1
- 102100014832 MKNK2 Human genes 0.000 claims 1
- 101700062305 MKNK2 Proteins 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000003419 tautomerization reaction Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1205669.3A GB201205669D0 (en) | 2012-03-30 | 2012-03-30 | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| GB1205669.3 | 2012-03-30 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Division JP6475158B2 (ja) | 2012-03-30 | 2013-04-01 | Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019031560A JP2019031560A (ja) | 2019-02-28 |
| JP2019031560A5 true JP2019031560A5 (US20040106767A1-20040603-C00005.png) | 2019-04-11 |
| JP6662984B2 JP6662984B2 (ja) | 2020-03-11 |
Family
ID=46160013
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Active JP6475158B2 (ja) | 2012-03-30 | 2013-04-01 | Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
| JP2018206109A Active JP6662984B2 (ja) | 2012-03-30 | 2018-10-31 | Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Active JP6475158B2 (ja) | 2012-03-30 | 2013-04-01 | Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 |
Country Status (13)
Families Citing this family (64)
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| WO2013142817A2 (en) | 2012-03-23 | 2013-09-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| TWI574962B (zh) | 2012-11-14 | 2017-03-21 | 加拓科學公司 | 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途 |
| SG11201505493QA (en) | 2013-02-21 | 2015-08-28 | Calitor Sciences Llc | Heteroaromatic compounds as pi3 kinase modulators |
| US9233961B2 (en) | 2013-03-15 | 2016-01-12 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| US9296754B2 (en) | 2013-03-15 | 2016-03-29 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| US9186361B2 (en) | 2013-03-15 | 2015-11-17 | Novartis Ag | Compounds and compositions for the treatment of parasitic diseases |
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| TW201542550A (zh) | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| AR097543A1 (es) * | 2013-09-06 | 2016-03-23 | Lexicon Pharmaceuticals Inc | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
| GB2518873A (en) * | 2013-10-03 | 2015-04-08 | Agency Science Tech & Res | Bicyclic alkyne derivatives and uses thereof |
| CA2930499C (en) * | 2013-12-09 | 2021-11-23 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of tnf activity |
| LT3083627T (lt) | 2013-12-19 | 2018-12-27 | Novartis Ag | [1,2,4]triazolo[1,5-a]pirimidino dariniai kaip protozoano proteasomos inhibitoriai, skirti parazitinių ligų tokių kaip leišmaniozė, gydymui |
| WO2015106158A1 (en) * | 2014-01-09 | 2015-07-16 | Intra-Cellular Therapies, Inc. | Organic compounds |
| PT3636649T (pt) | 2014-01-24 | 2024-04-09 | Turning Point Therapeutics Inc | Diaril macrociclos como moduladores das proteínas quinases |
| ES2672797T3 (es) | 2014-02-13 | 2018-06-18 | Incyte Corporation | Ciclopropilaminas como inhibidores de LSD1 |
| SG11201606689VA (en) | 2014-02-13 | 2016-09-29 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| BR112016018555B1 (pt) | 2014-02-13 | 2024-01-23 | Incyte Holdings Corporation | Ciclopropilaminas como inibidores de lsd1, seu uso, composição farmacêutica que os compreende e método de inibição de lsd1 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| TWI713455B (zh) | 2014-06-25 | 2020-12-21 | 美商伊凡克特治療公司 | ＭｎＫ抑制劑及其相關方法 |
| US9695167B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9944647B2 (en) | 2015-04-03 | 2018-04-17 | Incyte Corporation | Heterocyclic compounds as LSD1 inhibitors |
| KR20180004740A (ko) | 2015-04-20 | 2018-01-12 | 이펙터 테라퓨틱스, 인크. | 암 및 감염 치료에 사용하기 위한 면역 체크포인트 조절 인자의 억제제 |
| MA41988B1 (fr) * | 2015-04-29 | 2021-03-31 | Janssen Pharmaceutica Nv | Azabenzimidazoles et leur utilisation comme modulateurs du recepteur ampa |
| AU2016280255A1 (en) | 2015-06-18 | 2018-02-08 | Cephalon, Inc. | 1, 4-substituted piperidine derivatives |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| WO2017004342A1 (en) | 2015-07-02 | 2017-01-05 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| DK3319969T3 (da) | 2015-07-06 | 2024-07-08 | Turning Point Therapeutics Inc | Diaryl-makrocyklus-polymorf |
| MX2018000718A (es) | 2015-07-21 | 2020-01-20 | Turning Point Therapeutics Inc | Macrociclos de diarilo quirales y usos de los mismos. |
| US10329255B2 (en) | 2015-08-12 | 2019-06-25 | Incyte Corporation | Salts of an LSD1 inhibitor |
| EP3344039A4 (en) * | 2015-09-03 | 2019-08-28 | Arizona Board of Regents on behalf of the University of Arizona | SMALL DYRK1A INHIBITORY MOLECULES AND USES THEREOF |
| EP3365337A1 (en) * | 2015-10-22 | 2018-08-29 | Selvita S.A. | Pyridone derivatives and their use as kinase inhibitors |
| US10851082B2 (en) | 2015-10-28 | 2020-12-01 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2) |
| SG11201803234TA (en) * | 2015-10-29 | 2018-05-30 | Effector Therapeutics Inc | Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit mnk1 and mnk2 |
| CN108602805A (zh) | 2015-10-29 | 2018-09-28 | 效应治疗股份有限公司 | Mnk1和mnk2的异吲哚啉、氮杂异吲哚啉、二氢茚酮和二氢氮杂茚酮抑制剂 |
| WO2017087808A1 (en) | 2015-11-20 | 2017-05-26 | Effector Therapeutics, Inc. | Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers |
| US20170191136A1 (en) | 2015-12-31 | 2017-07-06 | Effector Therapeutics, Inc. | Mnk biomarkers and uses thereof |
| AU2017252328B2 (en) | 2016-04-22 | 2023-02-23 | Incyte Corporation | Formulations of an LSD1 inhibitor |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| GB201700692D0 (en) * | 2017-01-16 | 2017-03-01 | Salvensis | Novel compounds and their use in the treatment of schistosomiasis |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| EP3582776B1 (en) | 2017-02-14 | 2023-11-08 | Effector Therapeutics, Inc. | Piperidine-substituted mnk inhibitors and methods related thereto |
| US11286264B2 (en) | 2017-07-28 | 2022-03-29 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
| PL3728271T3 (pl) | 2017-12-19 | 2023-01-23 | Turning Point Therapeutics, Inc. | Związki makrocykliczne do leczenia chorób |
| EP3753941B1 (en) * | 2018-02-13 | 2024-05-01 | Shanghai Blueray Biopharma Co., Ltd. | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| CN115448923B (zh) * | 2018-02-13 | 2024-03-22 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| EP3564235A1 (en) * | 2018-05-03 | 2019-11-06 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2) |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| EP3856186A4 (en) * | 2018-09-28 | 2022-07-06 | Arizona Board of Regents on behalf of the University of Arizona | SMALL MOLECULE DYRK1/CLK INHIBITORS AND THEIR USES |
| TW202035405A (zh) | 2018-10-24 | 2020-10-01 | 美商伊凡克特治療公司 | Ｍｎｋ抑制劑的結晶形式 |
| CN111978325B (zh) * | 2019-05-22 | 2023-11-17 | 中国药科大学 | 咪唑并哒嗪类mnk1/mnk2激酶抑制剂及其制备方法和应用 |
| CN111978317A (zh) * | 2019-05-22 | 2020-11-24 | 上海道熵生物科技有限公司 | 咪唑并吡啶类mnk1/mnk2激酶抑制剂及其制备方法和应用 |
| KR102459614B1 (ko) * | 2019-08-30 | 2022-10-31 | 주식회사 티에스디라이프사이언스 | 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물 |
| EP4084836A1 (en) * | 2019-12-30 | 2022-11-09 | Devicare, S.L. | Compositions for clinical complications associated to devices implanted in the urinary tract |
| CN112047950B (zh) * | 2020-09-14 | 2023-07-25 | 华东师范大学 | 咪唑并吡嗪类衍生物及其合成方法和应用 |
| WO2022053838A1 (en) * | 2020-09-14 | 2022-03-17 | The University Of Sussex | Small molecule inhibitors of lemur tyrosine kinase 3 |
| US20230000986A1 (en) * | 2021-07-01 | 2023-01-05 | Board Of Regents, The University Of Texas System | Mnk inhibitors and eif4e phosphorylation modulation to treat inflammatory pain in the aged |
| CN117203211A (zh) * | 2021-11-29 | 2023-12-08 | 中国海洋大学 | 咪唑并噻唑衍生物及其制备方法与应用 |
| CN114113639B (zh) * | 2022-01-29 | 2022-04-19 | 北京大有天弘科技有限公司 | 一种血型抗体检测方法及其应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1746099A1 (en) * | 2004-12-23 | 2007-01-24 | DeveloGen Aktiengesellschaft | Mnk1 or Mnk2 inhibitors |
| JP2009502734A (ja) * | 2005-07-29 | 2009-01-29 | アステラス製薬株式会社 | Ｌｃｋ阻害剤としての縮合複素環 |
| WO2007025090A2 (en) * | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| ZA200807715B (en) * | 2006-03-09 | 2009-11-25 | Pharmacopeia Inc | 9-Heteroarylpurine MNK2 inhibitors for treating metabolic disorders |
| WO2007147874A1 (en) * | 2006-06-22 | 2007-12-27 | Biovitrum Ab (Publ) | Pyridine and pyrazine derivatives as mnk kinase inhibitors |
| US20120058997A1 (en) | 2006-11-06 | 2012-03-08 | Supergen, Inc. | Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors |
| JP5357763B2 (ja) * | 2006-11-06 | 2013-12-04 | トレロ ファーマシューティカルズ， インコーポレイテッド | イミダゾ［１，２−ｂ］ピリダジン誘導体およびピラゾロ［１，５−ａ］ピリダジン誘導体およびプロテインキナーゼインヒビターとしてのこれらの使用 |
| AU2007337886C1 (en) | 2006-12-22 | 2014-10-16 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| AR067326A1 (es) * | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| ES2393430T3 (es) * | 2007-10-17 | 2012-12-21 | Novartis Ag | Derivados de imidazo[1,2-A]-piridina útiles como inhibidores de ALK |
| EP2355819A2 (en) * | 2008-11-12 | 2011-08-17 | Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute For Biomedical Research | Treating cancer by modulating a mnk |
| TW201107329A (en) * | 2009-07-30 | 2011-03-01 | Oncotherapy Science Inc | Fused imidazole derivative having ttk inhibitory action |
| IN2012DN01961A (US20040106767A1-20040603-C00005.png) * | 2009-08-17 | 2015-08-21 | Intellikine Llc | |
| UY33241A (es) * | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| JPWO2011136264A1 (ja) * | 2010-04-28 | 2013-07-22 | 第一三共株式会社 | ［５，６］複素環化合物 |
| US8987273B2 (en) * | 2010-07-28 | 2015-03-24 | Bayer Intellectual Property Gmbh | Substituted imidazo[1,2-B]pyridazines |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| US9370515B2 (en) * | 2013-03-07 | 2016-06-21 | Califia Bio, Inc. | Mixed lineage kinase inhibitors and method of treatments |
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2012
- 2012-03-30 GB GBGB1205669.3A patent/GB201205669D0/en not_active Ceased
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2013
- 2013-04-01 PL PL13768800T patent/PL2831079T3/pl unknown
- 2013-04-01 EP EP13768800.8A patent/EP2831079B1/en active Active
- 2013-04-01 JP JP2015503165A patent/JP6475158B2/ja active Active
- 2013-04-01 SG SG10201706594PA patent/SG10201706594PA/en unknown
- 2013-04-01 WO PCT/SG2013/000126 patent/WO2013147711A1/en active Application Filing
- 2013-04-01 DK DK13768800.8T patent/DK2831079T3/da active
- 2013-04-01 SG SG11201406207PA patent/SG11201406207PA/en unknown
- 2013-04-01 ES ES13768800.8T patent/ES2647959T3/es active Active
- 2013-04-01 CN CN201380027654.7A patent/CN104350055B/zh active Active
- 2013-04-01 NO NO13768800A patent/NO2831079T3/no unknown
- 2013-04-01 US US14/363,718 patent/US9908886B2/en active Active
- 2013-04-01 KR KR1020147027686A patent/KR102153320B1/ko active IP Right Grant
- 2013-04-01 AU AU2013240612A patent/AU2013240612B2/en active Active
- 2013-04-01 EP EP17179630.3A patent/EP3321268A1/en active Pending
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2017
- 2017-08-24 AU AU2017219039A patent/AU2017219039A1/en not_active Abandoned
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2018
- 2018-01-16 US US15/872,571 patent/US20180208600A1/en not_active Abandoned
- 2018-10-31 JP JP2018206109A patent/JP6662984B2/ja active Active
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2019
- 2019-06-05 US US16/432,469 patent/US11040978B2/en active Active
