JP2020522484A5 - - Google Patents
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- JP2020522484A5 JP2020522484A5 JP2019565833A JP2019565833A JP2020522484A5 JP 2020522484 A5 JP2020522484 A5 JP 2020522484A5 JP 2019565833 A JP2019565833 A JP 2019565833A JP 2019565833 A JP2019565833 A JP 2019565833A JP 2020522484 A5 JP2020522484 A5 JP 2020522484A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- pharmaceutically acceptable
- acceptable salt
- compound according
- 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 27
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 201000009030 Carcinoma Diseases 0.000 claims 4
- 206010039491 Sarcoma Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 238000010276 construction Methods 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 208000003200 Adenoma Diseases 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- -1 Cyano, Hydroxy Chemical group 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 3
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 2
- 208000016323 C3 glomerulonephritis Diseases 0.000 claims 2
- 206010025219 Lymphangioma Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 201000004458 Myoma Diseases 0.000 claims 2
- 208000034541 Rare lymphatic malformation Diseases 0.000 claims 2
- 208000009956 adenocarcinoma Diseases 0.000 claims 2
- 230000002949 hemolytic effect Effects 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 208000003154 papilloma Diseases 0.000 claims 2
- 201000008171 proliferative glomerulonephritis Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- XGWFJBFNAQHLEF-UHFFFAOYSA-N 9-anthroic acid Chemical compound C1=CC=C2C(C(=O)O)=C(C=CC=C3)C3=CC2=C1 XGWFJBFNAQHLEF-UHFFFAOYSA-N 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010006417 Bronchial carcinoma Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000005262 Chondroma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 201000005171 Cystadenoma Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 206010018910 Haemolysis Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000004451 Membranoproliferative Glomerulonephritis Diseases 0.000 claims 1
- 208000015021 Meningeal Neoplasms Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 230000034196 cell chemotaxis Effects 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 210000004252 chorionic villi Anatomy 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 208000002445 cystadenocarcinoma Diseases 0.000 claims 1
- 208000022401 dense deposit disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000037828 epithelial carcinoma Diseases 0.000 claims 1
- 206010016629 fibroma Diseases 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 201000011066 hemangioma Diseases 0.000 claims 1
- 230000008588 hemolysis Effects 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 208000008798 osteoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000010198 papillary carcinoma Diseases 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000008753 synovium neoplasm Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 210000005239 tubule Anatomy 0.000 claims 1
- 208000013706 tumor of meninges Diseases 0.000 claims 1
- KOFIDSXHWGFEMO-UHFFFAOYSA-N CC(C)CN1CCCC1 Chemical compound CC(C)CN1CCCC1 KOFIDSXHWGFEMO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762513010P | 2017-05-31 | 2017-05-31 | |
| US62/513,010 | 2017-05-31 | ||
| PCT/US2018/034905 WO2018222598A1 (en) | 2017-05-31 | 2018-05-29 | 6-5 FUSED RINGS AS C5a INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020522484A JP2020522484A (ja) | 2020-07-30 |
| JP2020522484A5 true JP2020522484A5 (cg-RX-API-DMAC7.html) | 2021-07-26 |
| JP7141130B2 JP7141130B2 (ja) | 2022-09-22 |
Family
ID=64456009
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019565833A Active JP7141130B2 (ja) | 2017-05-31 | 2018-05-29 | Ｃ５ａ阻害剤としての６－５融合環 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US10562896B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3630775B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP7141130B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR102638253B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN110997674B (cg-RX-API-DMAC7.html) |
| AR (1) | AR111983A1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2018277520B2 (cg-RX-API-DMAC7.html) |
| IL (1) | IL270828B2 (cg-RX-API-DMAC7.html) |
| MA (1) | MA48803A (cg-RX-API-DMAC7.html) |
| MX (1) | MX392259B (cg-RX-API-DMAC7.html) |
| TW (1) | TWI781177B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2018222598A1 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA201907746B (cg-RX-API-DMAC7.html) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10683294B2 (en) | 2017-05-31 | 2020-06-16 | Chemocentryx, Inc. | 5-5 fused rings as C5a inhibitors |
| CN110997674B (zh) | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的6-5稠合环类 |
| ES2980175T3 (es) * | 2017-12-22 | 2024-09-30 | Chemocentryx Inc | Compuestos anulares fusionados en 6,5 sustituidos con diarilo como inhibidores de C5aR |
| KR102852027B1 (ko) | 2017-12-22 | 2025-08-27 | 케모센트릭스, 인크. | C5aR 억제제로서의 디아릴 치환된 5,5-융합 고리 화합물 |
| CN111954525B (zh) * | 2018-04-02 | 2023-12-26 | 凯莫森特里克斯股份有限公司 | 稠合双环C5aR拮抗剂的前药 |
| CN114206338B (zh) | 2019-07-10 | 2025-12-12 | 凯莫森特里克斯股份有限公司 | 作为pd-l1抑制剂的二氢化茚类 |
| CN112625036A (zh) * | 2019-10-08 | 2021-04-09 | 上海海和药物研究开发股份有限公司 | 一类具有brd4抑制活性的化合物、其制备方法及用途 |
| US11713307B2 (en) | 2019-10-16 | 2023-08-01 | Chemocentryx, Inc. | Heteroaryl-biphenyl amides for the treatment of PD-L1 diseases |
| PH12022550877A1 (en) | 2019-10-16 | 2023-03-27 | Chemocentryx Inc | Heteroaryl-biphenyl amines for the treatment of pd-l1 diseases |
| US20220047592A1 (en) * | 2020-08-13 | 2022-02-17 | Chemocentryx, Inc. | METHODS OF TREATING RESPIRATORY DISEASES USING C5a INHIBITORS |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| JP2023548117A (ja) | 2020-10-28 | 2023-11-15 | ケモセントリックス， インコーポレイテッド | 化膿性汗腺炎を処置する方法 |
| CN112979646B (zh) * | 2021-03-08 | 2022-01-14 | 北京富龙康泰生物技术有限公司 | 一种咪唑并吡啶类衍生物 |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK27383A (da) | 1982-02-17 | 1983-08-18 | Lepetit Spa | Fremgangsmaade til fremstilling af pyrazol(4,3-c)pyridiner |
| GB8613591D0 (en) | 1986-06-04 | 1986-07-09 | Roussel Lab Ltd | Chemical compounds |
| FR2761266B1 (fr) | 1997-03-28 | 1999-07-02 | Sanofi Sa | Composition pharmaceutique formee par granulation humide pour l'administration orale d'un derive du n-piperidino-3- pyrazolecarboxamide, de ses sels et de leurs solvates |
| CA2416527C (en) | 2000-08-10 | 2009-12-22 | Pharmacia Italia S.P.A. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| JP5260818B2 (ja) | 2000-09-29 | 2013-08-14 | ノバルティス・インターナショナル・ファーマシューティカル・リミテッド | 高親和性低分子Ｃ５ａ受容体調節物質 |
| SE524438C2 (sv) | 2000-10-05 | 2004-08-10 | Magnus Georg Goertz | Fjärrstyrt dörrelaterat låsarrangemang, första och andra datorpogramprodukt, bärande medium och ett datorlösbart medium |
| JP4196678B2 (ja) * | 2001-04-26 | 2008-12-17 | 味の素株式会社 | 複素環化合物 |
| ITMI20012025A1 (it) | 2001-09-28 | 2003-03-28 | Dompe Spa | Sali di ammonio quaternari di omega-amminoalchilammidi di acidi r 2-aril-propionici e composizioni farmaceutiche che li contengono |
| EP1487796A4 (en) | 2002-03-28 | 2005-11-16 | Neurogen Corp | SUBSTITUTED BIARYLAMIDES AS MODULATORS OF THE C5A RECEPTOR |
| JP2006508894A (ja) | 2002-03-28 | 2006-03-16 | ニューロジェン・コーポレーション | Ｃ５ａ受容体調節因子としての置換テトラヒドロイソキノリン |
| US20040014782A1 (en) | 2002-03-29 | 2004-01-22 | Krause James E. | Combination therapy for the treatment of diseases involving inflammatory components |
| AU2003265395A1 (en) * | 2002-08-14 | 2004-03-03 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| WO2004018460A1 (en) | 2002-08-21 | 2004-03-04 | Neurogen Corporation | Amino methyl imidazoles as c5a receptor modulators |
| ATE552253T1 (de) | 2002-11-08 | 2012-04-15 | Novartis Int Pharm Ltd | 3-substituierte-6-aryl- pyridin derivate als liganden für c5a-rezeptoren |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040214856A1 (en) * | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| AU2003902354A0 (en) | 2003-05-15 | 2003-05-29 | Harkin, Denis W. | Treatment of haemorrhagic shock |
| US20060154917A1 (en) | 2003-07-03 | 2006-07-13 | Neurogen Corporation | Substituted (heterocycloalkyl)methyl azole derivatives as c5a receptor modulators |
| US7906528B2 (en) | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
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| CN101277700B (zh) | 2005-08-04 | 2013-02-20 | 詹森药业有限公司 | 作为5-羟色胺受体调节剂的嘧啶化合物 |
| US20070112015A1 (en) | 2005-10-28 | 2007-05-17 | Chemocentryx, Inc. | Substituted dihydropyridines and methods of use |
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| CN102131390A (zh) | 2008-06-20 | 2011-07-20 | 健泰科生物技术公司 | 三唑并吡啶jak抑制剂化合物和方法 |
| US20110275639A1 (en) | 2008-12-22 | 2011-11-10 | Chemocentryx, Inc. | C5aR ANTAGONISTS |
| SG172338A1 (en) | 2008-12-22 | 2011-07-28 | Chemocentryx Inc | C5ar antagonists |
| BR112012004335A8 (pt) | 2009-09-02 | 2016-06-21 | Merck Sharp & Dohme | Composto, composição farmacêutica, e, uso do composto. |
| HRP20171176T1 (hr) | 2010-06-24 | 2017-10-06 | Chemocentryx, Inc. | C5ar antagonisti |
| US8846656B2 (en) * | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| BR112015003359A2 (pt) | 2012-08-16 | 2017-07-04 | Janssen Pharmaceutica Nv | pirrolopirazóis como bloqueadores de canal de cálcio de tipo-n |
| CN103421006B (zh) * | 2013-08-18 | 2016-06-22 | 上海师范大学 | 2,3,5,7-四取代二氢吡唑并六氢吡啶衍生物及其制备方法和应用 |
| GB201321746D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| JP7121722B2 (ja) | 2016-04-04 | 2022-08-18 | ケモセントリックス，インコーポレイティド | 可溶性Ｃ５ａＲアンタゴニスト |
| US10683294B2 (en) | 2017-05-31 | 2020-06-16 | Chemocentryx, Inc. | 5-5 fused rings as C5a inhibitors |
| CN110997674B (zh) * | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的6-5稠合环类 |
| US10589871B2 (en) | 2017-09-25 | 2020-03-17 | Hamilton Sundstrand Corporation | Prognostic health monitoring and jam detection for use with an aircraft |
| KR102852027B1 (ko) | 2017-12-22 | 2025-08-27 | 케모센트릭스, 인크. | C5aR 억제제로서의 디아릴 치환된 5,5-융합 고리 화합물 |
| ES2980175T3 (es) | 2017-12-22 | 2024-09-30 | Chemocentryx Inc | Compuestos anulares fusionados en 6,5 sustituidos con diarilo como inhibidores de C5aR |
| CN111954525B (zh) | 2018-04-02 | 2023-12-26 | 凯莫森特里克斯股份有限公司 | 稠合双环C5aR拮抗剂的前药 |
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2018
- 2018-05-29 CN CN201880036662.0A patent/CN110997674B/zh active Active
- 2018-05-29 AU AU2018277520A patent/AU2018277520B2/en active Active
- 2018-05-29 MA MA048803A patent/MA48803A/fr unknown
- 2018-05-29 JP JP2019565833A patent/JP7141130B2/ja active Active
- 2018-05-29 EP EP18809537.6A patent/EP3630775B1/en active Active
- 2018-05-29 WO PCT/US2018/034905 patent/WO2018222598A1/en not_active Ceased
- 2018-05-29 KR KR1020197038669A patent/KR102638253B1/ko active Active
- 2018-05-29 US US15/991,703 patent/US10562896B2/en active Active
- 2018-05-29 MX MX2019014294A patent/MX392259B/es unknown
- 2018-05-31 AR ARP180101449A patent/AR111983A1/es unknown
- 2018-05-31 TW TW107118601A patent/TWI781177B/zh active
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2019
- 2019-11-21 IL IL270828A patent/IL270828B2/en unknown
- 2019-11-22 ZA ZA2019/07746A patent/ZA201907746B/en unknown
- 2019-12-20 US US16/723,433 patent/US11384079B2/en active Active
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2022
- 2022-05-03 US US17/735,283 patent/US11773091B2/en active Active