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1. WO2020111280 - NUCLEIC ACID COMPLEX

Publication Number WO/2020/111280
Publication Date 04.06.2020
International Application No. PCT/JP2019/047044
International Filing Date 02.12.2019
IPC
A61K 31/7105 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
7105Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/713 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
713Double-stranded nucleic acids or oligonucleotides
A61K 48/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07H 15/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of a saccharide radical
A61K 47/54 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
CPC
A61K 31/7105
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
7105Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/713
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7088Compounds having three or more nucleosides or nucleotides
713Double-stranded nucleic acids or oligonucleotides
A61K 47/54
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
A61K 48/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07H 15/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of the saccharide radical
Applicants
  • 協和キリン株式会社 KYOWA KIRIN CO., LTD. [JP]/[JP]
Inventors
  • 岩井 宏徒 IWAI, Hiroto
  • 今枝 隆 IMAEDA, Takashi
  • 有山 博之 ARIYAMA, Hiroyuki
  • 村上 拓也 MURAKAMI, Takuya
Agents
  • 稲葉 良幸 INABA, Yoshiyuki
  • 大貫 敏史 ONUKI, Toshifumi
Priority Data
2018-22582930.11.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) NUCLEIC ACID COMPLEX
(FR) COMPLEXE D'ACIDE NUCLÉIQUE
(JA) 核酸複合体
Abstract
(EN)
The present invention provides a nucleic acid complex represented by formula 1. Formula 1: (In formula 1, X is a double-stranded nucleic acid that comprises a sense strand and an antisense strand and that includes a duplex region of at least 11 base pairs; the double-stranded nucleic acid is complementary with any of the target APCS mRNA sequences listed in Tables 1-1 to 1-13 in an oligonucleotide strand having a strand length of 17-30 nucleotides in the antisense strand, and the 3' end or 5' end of the sense strand bonds to S3; L1 and L2 each independently represent a sugar ligand; S1, S2, and S3 each independently represent a linker.)
(FR)
La présente invention concerne un complexe d'acide nucléique représenté par la formule 1. Formule 1 : (Dans la formule 1, X représente un acide nucléique double brin qui comprend un brin sens et un brin antisens et qui comprend une région duplex d'au moins 11 paires de bases ; l'acide nucléique double brin est complémentaire à l'une quelconque des séquences d'ARNm de CPA cibles reprises dans les tableaux 1-1 à 1-13 dans un brin d'oligonucléotide présentant une longueur de brin de 17 à 30 nucléotides dans le brin antisens, et l'extrémité 3' ou 5' du brin sens se lie à S3 ; L1 et L2 représentent chacun indépendamment un ligand de sucre ; S1, S2, et S3 représentent chacun indépendamment un lieur.)
(JA)
本発明は、下記式1で表される核酸複合体を提供する。 式1:(式1中、 Xは、センス鎖およびアンチセンス鎖からなり、少なくとも11個の塩基対の二重鎖領域を含む二本鎖核酸であり、 該二本鎖核酸は、該アンチセンス鎖中の、17個~30個のヌクレオチドの鎖長のオリゴヌクレオチド鎖において、表1-1~表1-13に記載された標的APCS mRNA配列のいずれかと相補的であり、 該センス鎖の3'末端または5'末端はS3に結合し、 L1およびL2は、それぞれ独立して、糖リガンドであり、 S1、S2およびS3は、それぞれ独立して、リンカーである。)
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