DK2635265T3 - Hidtil ukendte lavmolekylære cykliske aminholdige kationiske lipider til oligonukleotidfremføring - Google Patents
Hidtil ukendte lavmolekylære cykliske aminholdige kationiske lipider til oligonukleotidfremføring Download PDFInfo
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- DK2635265T3 DK2635265T3 DK11838596.2T DK11838596T DK2635265T3 DK 2635265 T3 DK2635265 T3 DK 2635265T3 DK 11838596 T DK11838596 T DK 11838596T DK 2635265 T3 DK2635265 T3 DK 2635265T3
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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
- C12N15/1137—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 enzymes
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/12—Oxygen or sulfur atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/51—Nanocapsules; Nanoparticles
- A61K9/5107—Excipients; Inactive ingredients
- A61K9/5123—Organic compounds, e.g. fats, sugars
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D223/08—Oxygen atoms
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- 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
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- 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 N.A.
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- 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
- C12N2320/00—Applications; Uses
- C12N2320/30—Special therapeutic applications
- C12N2320/32—Special delivery means, e.g. tissue-specific
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (6)
1. Lipid med formel A:
A hvor: R1 er H eller methyl; n og m er 1; X er 0; Li er valgt blandt Ci2-C24alkyl og Ci2-C24alkenyl; og L2 er Csalkyl eller et hvilket som helst farmaceutisk acceptabelt salt eller en hvilken som helst farmaceutisk acceptabel stereoisomer deraf.
2 . Lipid, som er: trans-l-methyl-3-[((9Z,12Z)-octadeca-9,12-dienyl)oxy]-4-octyloxypyrrolidin (forbindelse 4); trans-l-methyl-3-[(9Z)-octadec-9-en-l-yloxy]-4-(octyloxy)pyrrolidin (forbindelse 5); trans-l-methyl-3-[(12Z)-octadec-12- en-l-yloxy]-4- (octyloxy)pyrrolidin (forbindelse 6); cis-l-methyl-3-[(9Z,12Z)-octadeca-9,12-dien-l-yloxy]-4-(octyloxy)pyrrolidin (forbindelse 11); eller et hvilket som helst farmaceutisk acceptabelt salt eller en hvilken som helst farmaceutisk acceptabel stereoisomer deraf.
3. Anvendelse af et lipid ifølge et hvilket som helst af ovennævnte krav til fremstilling af lipidnanopartikler.
4. Anvendelse af et lipid ifølge et hvilket som helst af kravene 1 eller 2 som en bestanddel i en lipidnanopartikel til fremføring af oligonukleotider.
5. Anvendelse ifølge krav 4, hvor oligonukleotiderne er siRNA eller miRNA.
6. Anvendelse ifølge krav 4, hvor oligonukleotiderne er siRNA.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41047210P | 2010-11-05 | 2010-11-05 | |
PCT/US2011/058498 WO2012061259A2 (en) | 2010-11-05 | 2011-10-31 | Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery |
Publications (1)
Publication Number | Publication Date |
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DK2635265T3 true DK2635265T3 (da) | 2018-07-16 |
Family
ID=46025039
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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DK11838596.2T DK2635265T3 (da) | 2010-11-05 | 2011-10-31 | Hidtil ukendte lavmolekylære cykliske aminholdige kationiske lipider til oligonukleotidfremføring |
Country Status (4)
Country | Link |
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US (3) | US9067882B2 (da) |
EP (1) | EP2635265B1 (da) |
DK (1) | DK2635265T3 (da) |
WO (1) | WO2012061259A2 (da) |
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WO2010054384A1 (en) | 2008-11-10 | 2010-05-14 | Alnylam Pharmaceuticals, Inc. | Lipids and compositions for the delivery of therapeutics |
US20120101148A1 (en) | 2009-01-29 | 2012-04-26 | Alnylam Pharmaceuticals, Inc. | lipid formulation |
CN102421900B (zh) | 2009-03-12 | 2015-07-22 | 阿尔尼拉姆医药品有限公司 | 用于抑制Eg5和VEGF基因表达的脂质配制的组合物以及方法 |
EA028860B1 (ru) | 2009-06-10 | 2018-01-31 | Арбутус Биофарма Корпорэйшн | Улучшенная липидная композиция |
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2011
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- 2011-10-31 WO PCT/US2011/058498 patent/WO2012061259A2/en active Application Filing
- 2011-10-31 US US13/883,487 patent/US9067882B2/en active Active
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2015
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EP2635265B1 (en) | 2018-04-04 |
US20130225836A1 (en) | 2013-08-29 |
EP2635265A2 (en) | 2013-09-11 |
EP2635265A4 (en) | 2014-06-04 |
US20150361434A1 (en) | 2015-12-17 |
US9796977B2 (en) | 2017-10-24 |
US10337014B2 (en) | 2019-07-02 |
US9067882B2 (en) | 2015-06-30 |
WO2012061259A3 (en) | 2012-06-28 |
US20180037893A1 (en) | 2018-02-08 |
WO2012061259A2 (en) | 2012-05-10 |
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