AR090906A1 - Conjugados que contienen tetragalnac y procedimientos para la administracion de oligonucleotidos - Google Patents
Conjugados que contienen tetragalnac y procedimientos para la administracion de oligonucleotidosInfo
- Publication number
- AR090906A1 AR090906A1 ARP130101481A ARP130101481A AR090906A1 AR 090906 A1 AR090906 A1 AR 090906A1 AR P130101481 A ARP130101481 A AR P130101481A AR P130101481 A ARP130101481 A AR P130101481A AR 090906 A1 AR090906 A1 AR 090906A1
- Authority
- AR
- Argentina
- Prior art keywords
- tetragalnac
- oligonucleotides
- administration
- procedures
- conjugates containing
- Prior art date
Links
- 108091034117 Oligonucleotide Proteins 0.000 title abstract 2
- 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
- 238000000034 method Methods 0.000 title 1
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 239000003446 ligand Substances 0.000 abstract 2
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 150000002632 lipids Chemical class 0.000 abstract 1
- 230000000873 masking effect Effects 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
- C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/11—Antisense
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/10—Type of nucleic acid
- C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2310/00—Structure or type of the nucleic acid
- C12N2310/30—Chemical structure
- C12N2310/35—Nature of the modification
- C12N2310/351—Conjugate
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Immunology (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- General Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Physics & Mathematics (AREA)
- Biophysics (AREA)
- Plant Pathology (AREA)
- Microbiology (AREA)
- Transplantation (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
Abstract
En el presente documento se desvela una composición modular que comprende I) un oligonucleótido; II) uno o más ligandos de tetraGalNAc de fórmula (1), que pueden ser iguales o diferentes; opcionalmente, III) uno o más ligadores, que pueden ser iguales o diferentes; y opcionalmente IV) uno o más ligandos que eligen diana, agentes solubilizantes, agentes potenciadores de la farmacocinética, lípidos y/o agentes de enmascaramiento.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261641761P | 2012-05-02 | 2012-05-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR090906A1 true AR090906A1 (es) | 2014-12-17 |
Family
ID=49514844
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130101481A AR090906A1 (es) | 2012-05-02 | 2013-04-30 | Conjugados que contienen tetragalnac y procedimientos para la administracion de oligonucleotidos |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US9540639B2 (es) |
| EP (1) | EP2844663B1 (es) |
| JP (2) | JP6239592B2 (es) |
| AR (1) | AR090906A1 (es) |
| AU (1) | AU2013256400B2 (es) |
| CA (1) | CA2872100A1 (es) |
| HK (1) | HK1208227A1 (es) |
| TW (2) | TWI595885B (es) |
| WO (1) | WO2013166121A1 (es) |
Families Citing this family (58)
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| EP3453761A1 (en) | 2011-08-29 | 2019-03-13 | Ionis Pharmaceuticals, Inc. | Oligomer-conjugate complexes and their use |
| AR090905A1 (es) * | 2012-05-02 | 2014-12-17 | Merck Sharp & Dohme | Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica |
| SG10201906382QA (en) | 2013-05-01 | 2019-08-27 | Ionis Pharmaceuticals Inc | Compositions and methods for modulating hbv and ttr expression |
| JP6702862B2 (ja) * | 2013-07-11 | 2020-06-03 | アルニラム ファーマスーティカルズ インコーポレイテッドＡｌｎｙｌａｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | オリゴヌクレオチド−リガンドコンジュゲートおよびそれらの調製方法 |
| WO2015069586A2 (en) * | 2013-11-06 | 2015-05-14 | Merck Sharp & Dohme Corp. | Dual molecular delivery of oligonucleotides and peptide containing conjugates |
| US10239957B2 (en) * | 2013-11-06 | 2019-03-26 | Merck Sharp & Dohme Corp. | Peptide containing conjugates for dual molecular delivery of oligonucleotides |
| JP6466637B2 (ja) * | 2013-11-28 | 2019-02-06 | ソマール株式会社 | 糖鎖含有ポリマー、および、糖鎖含有ポリマー複合体 |
| US9926556B2 (en) | 2014-04-28 | 2018-03-27 | Ionis Pharmaceuticals, Inc. | Linkage modified oligomeric compounds |
| CN110903337A (zh) | 2014-05-01 | 2020-03-24 | Ionis制药公司 | 用于调节生长激素受体表达的组合物和方法 |
| JP2017521045A (ja) | 2014-05-01 | 2017-08-03 | アイオーニス ファーマシューティカルズ， インコーポレーテッドＩｏｎｉｓ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | アンジオポエチン様因子３発現を調節するための組成物及び方法 |
| WO2015168532A2 (en) | 2014-05-01 | 2015-11-05 | Isis Pharmaceuticals, Inc. | Compositions and methods for modulating pkk expression |
| SG10201809953QA (en) * | 2014-05-01 | 2018-12-28 | Ionis Pharmaceuticals Inc | Compositions and methods for modulating complement factor b expression |
| US10570169B2 (en) | 2014-05-22 | 2020-02-25 | Ionis Pharmaceuticals, Inc. | Conjugated antisense compounds and their use |
| WO2016040748A1 (en) | 2014-09-12 | 2016-03-17 | Ionis Pharmaceuticals, Inc. | Compositions and methods for detection of smn protein in a subject and treatment of a subject |
| WO2016057932A1 (en) | 2014-10-10 | 2016-04-14 | Dicerna Pharmaceuticals, Inc. | Therapeutic inhibition of lactate dehydrogenase and agents therefor |
| AU2016294347B2 (en) | 2015-07-10 | 2022-07-28 | Ionis Pharmaceuticals, Inc. | Modulators of diacyglycerol acyltransferase 2 (DGAT2) |
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| US20210155926A1 (en) * | 2018-04-05 | 2021-05-27 | Silence Therapeutics Gmbh | siRNAs WITH AT LEAST TWO LIGANDS AT DIFFERENT ENDS |
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| US12496311B2 (en) | 2018-07-17 | 2025-12-16 | Aronora, Inc. | Methods for safely reducing thrombopoietin |
| US20210292768A1 (en) | 2018-08-08 | 2021-09-23 | Arcturus Therapeutics, Inc. | Compositions and agents against nonalcoholic steatohepatitis |
| TWI856973B (zh) | 2018-09-19 | 2024-10-01 | 美商Ionis製藥公司 | Pnpla3表現之調節劑 |
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| EP1622572B1 (en) | 2003-04-30 | 2017-12-20 | Sirna Therapeutics, Inc. | Conjugates and compositions for cellular delivery |
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| EP2555777B1 (en) | 2010-04-09 | 2019-02-20 | Sirna Therapeutics, Inc. | Novel single chemical entities and methods for delivery of oligonucleotides |
| AR090905A1 (es) * | 2012-05-02 | 2014-12-17 | Merck Sharp & Dohme | Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica |
-
2013
- 2013-04-30 TW TW102115516A patent/TWI595885B/zh active
- 2013-04-30 AR ARP130101481A patent/AR090906A1/es unknown
- 2013-04-30 TW TW106117248A patent/TW201808342A/zh unknown
- 2013-05-01 HK HK15108687.4A patent/HK1208227A1/xx unknown
- 2013-05-01 WO PCT/US2013/039025 patent/WO2013166121A1/en not_active Ceased
- 2013-05-01 CA CA2872100A patent/CA2872100A1/en not_active Abandoned
- 2013-05-01 AU AU2013256400A patent/AU2013256400B2/en active Active
- 2013-05-01 JP JP2015510418A patent/JP6239592B2/ja active Active
- 2013-05-01 US US14/398,317 patent/US9540639B2/en active Active
- 2013-05-01 EP EP13784779.4A patent/EP2844663B1/en active Active
-
2016
- 2016-11-29 US US15/363,490 patent/US10214742B2/en active Active
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2017
- 2017-11-01 JP JP2017211436A patent/JP2018048186A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20150203843A1 (en) | 2015-07-23 |
| US9540639B2 (en) | 2017-01-10 |
| CA2872100A1 (en) | 2013-11-07 |
| US10214742B2 (en) | 2019-02-26 |
| AU2013256400B2 (en) | 2017-09-21 |
| TWI595885B (zh) | 2017-08-21 |
| JP2015520742A (ja) | 2015-07-23 |
| EP2844663A1 (en) | 2015-03-11 |
| US20170233731A1 (en) | 2017-08-17 |
| AU2013256400A1 (en) | 2014-11-06 |
| WO2013166121A1 (en) | 2013-11-07 |
| TW201808342A (zh) | 2018-03-16 |
| JP6239592B2 (ja) | 2017-11-29 |
| EP2844663A4 (en) | 2015-09-30 |
| JP2018048186A (ja) | 2018-03-29 |
| HK1208227A1 (en) | 2016-02-26 |
| EP2844663B1 (en) | 2020-03-25 |
| TW201350131A (zh) | 2013-12-16 |
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