SG11202112741XA - Modified gapmer oligonucleotides and methods of use - Google Patents
Modified gapmer oligonucleotides and methods of useInfo
- Publication number
- SG11202112741XA SG11202112741XA SG11202112741XA SG11202112741XA SG11202112741XA SG 11202112741X A SG11202112741X A SG 11202112741XA SG 11202112741X A SG11202112741X A SG 11202112741XA SG 11202112741X A SG11202112741X A SG 11202112741XA SG 11202112741X A SG11202112741X A SG 11202112741XA
- Authority
- SG
- Singapore
- Prior art keywords
- methods
- gapmer oligonucleotides
- modified gapmer
- modified
- oligonucleotides
- Prior art date
Links
- 108091034117 Oligonucleotide Proteins 0.000 title 1
- JLCPHMBAVCMARE-UHFFFAOYSA-N [3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[3-[[3-[[3-[[3-[[3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-[[5-(2-amino-6-oxo-1H-purin-9-yl)-3-hydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(6-aminopurin-9-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-5-(4-amino-2-oxopyrimidin-1-yl)oxolan-2-yl]methyl [5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-yl] hydrogen phosphate Polymers Cc1cn(C2CC(OP(O)(=O)OCC3OC(CC3OP(O)(=O)OCC3OC(CC3O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c3nc(N)[nH]c4=O)C(COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3COP(O)(=O)OC3CC(OC3CO)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3ccc(N)nc3=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cc(C)c(=O)[nH]c3=O)n3cc(C)c(=O)[nH]c3=O)n3ccc(N)nc3=O)n3cc(C)c(=O)[nH]c3=O)n3cnc4c3nc(N)[nH]c4=O)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)n3cnc4c(N)ncnc34)O2)c(=O)[nH]c1=O JLCPHMBAVCMARE-UHFFFAOYSA-N 0.000 title 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7088—Compounds having three or more nucleosides or nucleotides
- A61K31/7125—Nucleic acids or oligonucleotides having modified internucleoside linkage, i.e. other than 3'-5' phosphodiesters
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
- C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
- C12N15/1131—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against viruses
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- C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
- C12N15/09—Recombinant DNA-technology
- C12N15/63—Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- C12N15/79—Vectors or expression systems specially adapted for eukaryotic hosts
- C12N15/85—Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
- C12N15/86—Viral vectors
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/11—Antisense
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- C12N2310/00—Structure or type of the nucleic acid
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- C12N2310/30—Chemical structure
- C12N2310/32—Chemical structure of the sugar
- C12N2310/323—Chemical structure of the sugar modified ring structure
- C12N2310/3231—Chemical structure of the sugar modified ring structure having an additional ring, e.g. LNA, ENA
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/33—Chemical structure of the base
- C12N2310/334—Modified C
- C12N2310/3341—5-Methylcytosine
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/33—Chemical structure of the base
- C12N2310/335—Modified T or U
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- C12N2310/00—Structure or type of the nucleic acid
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/341—Gapmers, i.e. of the type ===---===
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/34—Spatial arrangement of the modifications
- C12N2310/346—Spatial arrangement of the modifications having a combination of backbone and sugar modifications
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- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/352—Nature of the modification linked to the nucleic acid via a carbon atom
- C12N2310/3521—Methyl
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- C12N2320/00—Applications; Uses
- C12N2320/30—Special therapeutic applications
- C12N2320/32—Special delivery means, e.g. tissue-specific
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Engineering & Computer Science (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Plant Pathology (AREA)
- Microbiology (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962855793P | 2019-05-31 | 2019-05-31 | |
| US201962937760P | 2019-11-19 | 2019-11-19 | |
| US201962943532P | 2019-12-04 | 2019-12-04 | |
| PCT/US2020/035212 WO2020243490A2 (en) | 2019-05-31 | 2020-05-29 | Modified gapmer oligonucleotides and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11202112741XA true SG11202112741XA (en) | 2021-12-30 |
Family
ID=72179172
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11202112741XA SG11202112741XA (en) | 2019-05-31 | 2020-05-29 | Modified gapmer oligonucleotides and methods of use |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11466274B2 (https=) |
| EP (1) | EP3976056A2 (https=) |
| JP (1) | JP2022535735A (https=) |
| KR (1) | KR20220024192A (https=) |
| CN (1) | CN113905744A (https=) |
| AU (1) | AU2020282828A1 (https=) |
| BR (1) | BR112021023488A2 (https=) |
| CA (1) | CA3141874A1 (https=) |
| CO (1) | CO2021018034A2 (https=) |
| IL (1) | IL288259A (https=) |
| MX (1) | MX2021014206A (https=) |
| PE (1) | PE20220574A1 (https=) |
| SG (1) | SG11202112741XA (https=) |
| TW (1) | TW202113079A (https=) |
| WO (1) | WO2020243490A2 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20210189392A1 (en) * | 2019-12-12 | 2021-06-24 | Aligos Therapeutics, Inc. | S-antigen transport inhibiting oligonucleotide polymers and methods |
| AU2021318943A1 (en) * | 2020-07-27 | 2023-03-02 | Aligos Therapeutics, Inc. | HBV binding oligonucleotides and methods of use |
| TW202229554A (zh) * | 2020-12-31 | 2022-08-01 | 中山大學附屬第一醫院 | 用於降低血管收縮素轉化酶２（ａｃｅ２）之表現的寡核苷酸及其用於治療病毒感染的用途 |
| US20250243491A1 (en) | 2021-09-01 | 2025-07-31 | Aligos Therapeutics, Inc. | Pnpla3-targeting short interfering rna (sirna) molecules and uses thereof |
| CN118234862A (zh) | 2021-09-08 | 2024-06-21 | 阿利戈斯治疗公司 | 经修饰的短干扰核酸分子(siNA)及其用途 |
| TW202340468A (zh) | 2022-01-10 | 2023-10-16 | 中國大陸商杭州浩博醫藥有限公司 | B型肝炎病毒(hbv)表現之調節 |
| KR20240158340A (ko) * | 2022-03-17 | 2024-11-04 | 알리고스 테라퓨틱스 인코포레이티드 | 변형 갭머 올리고머 및 이의 사용 방법 |
| WO2024182446A2 (en) | 2023-02-28 | 2024-09-06 | Aligos Therapeutics, Inc. | Pnpla3-targeting short interfering rna (sirna) molecules and uses thereof |
| US20240352464A1 (en) | 2023-03-07 | 2024-10-24 | Aligos Therapeutics, Inc. | Modified Short Interfering Nucleic Acid (siNA) Molecules and Uses Thereof |
| CN121175419A (zh) * | 2023-04-14 | 2025-12-19 | 苏州炫景生物科技有限公司 | 抑制c3基因表达的化合物、药物组合物及其用途 |
| US20250368996A1 (en) | 2024-05-14 | 2025-12-04 | Aligos Therapeutics, Inc. | Modified antisense oligonucleotides for treating hepatitis b virus |
| CN120796266A (zh) * | 2024-07-08 | 2025-10-17 | 北京悦康科创医药科技股份有限公司 | 一种降低hbv基因表达的反义寡核苷酸及其应用 |
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| US20040127446A1 (en) | 1992-05-14 | 2004-07-01 | Lawrence Blatt | Oligonucleotide mediated inhibition of hepatitis B virus and hepatitis C virus replication |
| US5646262A (en) * | 1994-07-28 | 1997-07-08 | Georgetown University | Antisense oligonucleotides against hepatitis B viral replication |
| US5985662A (en) * | 1995-07-13 | 1999-11-16 | Isis Pharmaceuticals Inc. | Antisense inhibition of hepatitis B virus replication |
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| WO2004046160A2 (en) | 2002-11-18 | 2004-06-03 | Santaris Pharma A/S | Amino-lna, thio-lna and alpha-l-oxy-ln |
| WO2005009346A2 (en) | 2003-06-24 | 2005-02-03 | Mirus Corporation | Inhibition of gene function by delivery of polynucleotide-based gene expression inhibitors to mammalian cells in vivo |
| EP2007888A2 (en) | 2006-04-03 | 2008-12-31 | Santaris Pharma A/S | Pharmaceutical composition comprising anti-mirna antisense oligonucleotides |
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| BR112012008865A2 (pt) * | 2009-10-16 | 2019-09-24 | Glaxo Group Ltd | inibidores de hbv anti-sentido. |
| CA2778171C (en) | 2009-10-29 | 2017-07-25 | Osaka University | Bridged artificial nucleoside and nucleotide |
| EP2673361B1 (en) | 2011-02-08 | 2016-04-13 | Ionis Pharmaceuticals, Inc. | Oligomeric compounds comprising bicyclic nucleotides and uses thereof |
| RS61447B1 (sr) | 2011-04-21 | 2021-03-31 | Glaxo Group Ltd | Modulacija ekspresije virusa hepatitisa b (hbv) |
| WO2013159108A2 (en) | 2012-04-20 | 2013-10-24 | Isis Pharmaceuticals, Inc. | Oligomeric compounds comprising bicyclic nucleotides and uses thereof |
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| KR101707437B1 (ko) | 2012-09-21 | 2017-02-16 | 고꾸리쯔 다이가꾸 호우징 오사까 다이가꾸 | 구아니딘 가교를 갖는 인공 뉴클레오시드 및 올리고뉴클레오티드 |
| CN104837996A (zh) | 2012-11-15 | 2015-08-12 | 罗氏创新中心哥本哈根有限公司 | 抗apob反义缀合物化合物 |
| AU2014211406B2 (en) | 2013-01-30 | 2019-07-18 | Roche Innovation Center Copenhagen A/S | LNA oligonucleotide carbohydrate conjugates |
| DK2992098T3 (da) | 2013-05-01 | 2019-06-17 | Ionis Pharmaceuticals Inc | Sammensætninger og fremgangsmåder til modulering af hbv- og ttr-ekspression |
| WO2015042447A1 (en) | 2013-09-20 | 2015-03-26 | Isis Pharmaceuticals, Inc. | Targeted therapeutic nucleosides and their use |
| CA2935426C (en) | 2014-01-30 | 2023-07-25 | F. Hoffmann-La Roche Ag | Polyoligomer compound with biocleavable conjugates for reducing or inhibiting expression of a nucleic acid target |
| CN106103463B (zh) | 2014-02-18 | 2018-11-30 | 国立大学法人大阪大学 | 桥连型核苷和核苷酸 |
| GB201408623D0 (en) * | 2014-05-15 | 2014-07-02 | Santaris Pharma As | Oligomers and oligomer conjugates |
| CN106795200B (zh) | 2014-10-10 | 2020-06-19 | 豪夫迈·罗氏有限公司 | Galnac亚磷酰胺、其核酸缀合物及其用途 |
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| US20210052631A1 (en) | 2015-09-25 | 2021-02-25 | Ionis Pharmaceuticals, Inc. | Conjugated antisense compounds and their use |
| EP4219767A1 (en) * | 2016-06-17 | 2023-08-02 | F. Hoffmann-La Roche AG | Papd5 and papd7 inhibitors for treating a hepatitis b infection |
| US11286275B2 (en) | 2017-02-21 | 2022-03-29 | Osaka University | Nucleic acid compound and oligonucleotide |
| EP3587576A4 (en) | 2017-02-21 | 2021-01-06 | Osaka University | ANTISENSE OLIGONUCLEIC ACID |
| CN111511914B (zh) * | 2017-10-16 | 2023-11-17 | 豪夫迈·罗氏有限公司 | 减少PAPD5和PAPD7 mRNA的核酸分子用于治疗乙型肝炎感染 |
| PE20211783A1 (es) | 2018-11-08 | 2021-09-08 | Aligos Therapeutics Inc | Polimeros oligonucleotidos que inhiben el transporte de antigenos y metodos |
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2020
- 2020-05-29 SG SG11202112741XA patent/SG11202112741XA/en unknown
- 2020-05-29 TW TW109118218A patent/TW202113079A/zh unknown
- 2020-05-29 JP JP2021570299A patent/JP2022535735A/ja active Pending
- 2020-05-29 AU AU2020282828A patent/AU2020282828A1/en not_active Abandoned
- 2020-05-29 PE PE2021001964A patent/PE20220574A1/es unknown
- 2020-05-29 MX MX2021014206A patent/MX2021014206A/es unknown
- 2020-05-29 EP EP20760617.9A patent/EP3976056A2/en not_active Withdrawn
- 2020-05-29 CN CN202080039766.4A patent/CN113905744A/zh active Pending
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- 2020-05-29 WO PCT/US2020/035212 patent/WO2020243490A2/en not_active Ceased
- 2020-05-29 KR KR1020217042828A patent/KR20220024192A/ko not_active Withdrawn
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| TW202113079A (zh) | 2021-04-01 |
| US20200385735A1 (en) | 2020-12-10 |
| CA3141874A1 (en) | 2020-12-03 |
| KR20220024192A (ko) | 2022-03-03 |
| IL288259A (en) | 2022-01-01 |
| BR112021023488A2 (pt) | 2022-01-18 |
| MX2021014206A (es) | 2022-01-06 |
| AU2020282828A1 (en) | 2022-01-27 |
| EP3976056A2 (en) | 2022-04-06 |
| JP2022535735A (ja) | 2022-08-10 |
| US11466274B2 (en) | 2022-10-11 |
| CO2021018034A2 (es) | 2022-04-19 |
| CN113905744A (zh) | 2022-01-07 |
| PE20220574A1 (es) | 2022-04-20 |
| WO2020243490A2 (en) | 2020-12-03 |
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