EP2052079A2 - INHIBITION MÉDIÉE PAR UNE INTERFÉRENCE DE L'ARN DE L'EXPRESSION DU GÈNE DE LA PROPROTÉINE CONVERTASE SUBTILISINE KEXINE DE TYPE 9 (PCSK9) AU MOYEN DE PETITS ACIDES NUCLÉIQUES INTERFÉRANTS(ANsi) - Google Patents

INHIBITION MÉDIÉE PAR UNE INTERFÉRENCE DE L'ARN DE L'EXPRESSION DU GÈNE DE LA PROPROTÉINE CONVERTASE SUBTILISINE KEXINE DE TYPE 9 (PCSK9) AU MOYEN DE PETITS ACIDES NUCLÉIQUES INTERFÉRANTS(ANsi)

Info

Publication number
EP2052079A2
EP2052079A2 EP07813032A EP07813032A EP2052079A2 EP 2052079 A2 EP2052079 A2 EP 2052079A2 EP 07813032 A EP07813032 A EP 07813032A EP 07813032 A EP07813032 A EP 07813032A EP 2052079 A2 EP2052079 A2 EP 2052079A2
Authority
EP
European Patent Office
Prior art keywords
nucleotides
nucleic acid
sina
strand
double stranded
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.)
Withdrawn
Application number
EP07813032A
Other languages
German (de)
English (en)
Inventor
James Mcswiggen
Vasant Jadhav
Narendra K. Vaish
Roberto Guerciolini
Chandra Vargeese
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sirna Therapeutics Inc
Original Assignee
Sirna Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US11/487,788 external-priority patent/US20070173473A1/en
Application filed by Sirna Therapeutics Inc filed Critical Sirna Therapeutics Inc
Publication of EP2052079A2 publication Critical patent/EP2052079A2/fr
Withdrawn legal-status Critical Current

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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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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.
    • 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
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
    • 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
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/322—2'-R Modification

Abstract

La présente invention concerne des composés, des compositions et des procédés destinés à l'étude, au diagnostic et au traitement de caractères, de maladies et de pathologies qui répondent à la modulation de l'expression et/ou de l'activité du gène de la proprotéine convertase subtilisine kexine de type 9 (PCSK9). La présente invention concerne également des composés, des compositions et des procédés associés à des caractères, des maladies et des pathologies qui répondent à la modulation de l'expression et/ou de l'activité de gènes impliqués dans les voies de l'expression du gène de la proprotéine convertase subtilisine kexine de type 9 (PCSK9) ou d'autres processus cellulaires qui médient le maintien ou le développement desdits caractères, desdites maladies et pathologies. Spécifiquement, l'invention concerne des molécules d'acide nucléique double brin, incluant de petites molécules d'acide nucléique, telles que les molécules de petits acides nucléiques interférants (ANsi), de petits ARN interférants (ARNsi), d'ARN double brin (ARNds), de micro-ARN (ARNmi), et de petits ARN en épingle à cheveux (ARNsh), capables de médier une interférence de l'ARN (ARNi) contre l'expression du gène de la proprotéine convertase subtilisine kexine de type 9 (PCSK9), incluant des cocktails de telles petites molécules d'acide nucléique et de formulations de nanoparticules lipidiques (LNP) de telles petites molécules d'acide nucléique. La présente invention concerne également de petites molécules d'acide nucléique, telles que des ANsi, des ARNsi et d'autres, qui peuvent inhiber le fonctionnement de molécules d'ARN endogènes, telles que les micro-ARN endogènes (ARNmi) (notamment des inhibiteurs de l'ARNmi) ou les petits ARN interférants endogènes (ARNsi) (notamment des inhibiteurs de l'ARNsi), ou qui peuvent inhiber le fonctionnement de la protéine RISC (notamment des inhibiteurs de la RISC), pour moduler l'expression du gène par une interférence avec la fonction de régulation de tels ARN endogènes ou de protéines associées avec de tels ARN endogènes (notamment la protéine RISC), incluant des cocktails de telles petites molécules d'acide nucléique et de formulations de nanoparticules lipidiques (LNP) de telles petites molécules d'acide nucléique. De telles petites molécules d'acide nucléique se révèlent utiles, par exemple, pour l'élaboration de compositions destinées à prévenir, à inhiber ou à restreindre des maladies, des caractères et des pathologies métaboliques, incluant, mais sans s'y limiter, l'hyperlipidémie, l'hypercholestérolémie, une maladie cardiovasculaire, l'athérosclérose, l'hypertension, le diabète (notamment le diabète de type I et/ou de type II), la résistance à l'insuline, l'obésité et/ou d'autres états maladifs, pathologies ou caractères qui sont associés à l'expression du gène ou à l'activité chez un sujet ou un organisme.
EP07813032A 2006-07-17 2007-07-17 INHIBITION MÉDIÉE PAR UNE INTERFÉRENCE DE L'ARN DE L'EXPRESSION DU GÈNE DE LA PROPROTÉINE CONVERTASE SUBTILISINE KEXINE DE TYPE 9 (PCSK9) AU MOYEN DE PETITS ACIDES NUCLÉIQUES INTERFÉRANTS(ANsi) Withdrawn EP2052079A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11/487,788 US20070173473A1 (en) 2001-05-18 2006-07-17 RNA interference mediated inhibition of proprotein convertase subtilisin Kexin 9 (PCSK9) gene expression using short interfering nucleic acid (siNA)
US86136906P 2006-11-28 2006-11-28
PCT/US2007/073723 WO2008011431A2 (fr) 2006-07-17 2007-07-17 INHIBITION MÉDIÉE PAR UNE INTERFÉRENCE DE L'ARN DE L'EXPRESSION DU GÈNE DE LA PROPROTÉINE CONVERTASE SUBTILISINE KEXINE DE TYPE 9 (PCSK9) AU MOYEN DE PETITS ACIDES NUCLÉIQUES INTERFÉRANTS(ANsi)

Publications (1)

Publication Number Publication Date
EP2052079A2 true EP2052079A2 (fr) 2009-04-29

Family

ID=38957565

Family Applications (1)

Application Number Title Priority Date Filing Date
EP07813032A Withdrawn EP2052079A2 (fr) 2006-07-17 2007-07-17 INHIBITION MÉDIÉE PAR UNE INTERFÉRENCE DE L'ARN DE L'EXPRESSION DU GÈNE DE LA PROPROTÉINE CONVERTASE SUBTILISINE KEXINE DE TYPE 9 (PCSK9) AU MOYEN DE PETITS ACIDES NUCLÉIQUES INTERFÉRANTS(ANsi)

Country Status (6)

Country Link
EP (1) EP2052079A2 (fr)
JP (1) JP2010503382A (fr)
CN (1) CN102124107A (fr)
AU (1) AU2007275365A1 (fr)
CA (1) CA2658183A1 (fr)
WO (1) WO2008011431A2 (fr)

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Publication number Publication date
WO2008011431A8 (fr) 2009-11-05
WO2008011431A3 (fr) 2008-07-17
AU2007275365A1 (en) 2008-01-24
CA2658183A1 (fr) 2008-01-24
WO2008011431A2 (fr) 2008-01-24
JP2010503382A (ja) 2010-02-04
CN102124107A (zh) 2011-07-13

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