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1. (WO2019027009) NUCLEIC ACID COMPLEX
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Pub. No.: WO/2019/027009 International Application No.: PCT/JP2018/029079
Publication Date: 07.02.2019 International Filing Date: 02.08.2018
IPC:
C12N 15/113 (2010.01) ,A61K 31/7105 (2006.01) ,A61K 31/713 (2006.01) ,A61K 48/00 (2006.01) ,A61P 7/02 (2006.01) ,A61P 15/00 (2006.01) ,A61P 37/02 (2006.01) ,A61P 37/06 (2006.01) ,A61P 43/00 (2006.01)
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
11
DNA or RNA fragments; Modified forms thereof
113
Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7088
Compounds having three or more nucleosides or nucleotides
7105
Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7088
Compounds having three or more nucleosides or nucleotides
713
Double-stranded nucleic acids or oligonucleotides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48
Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15
Drugs for genital or sexual disorders; Contraceptives
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
06
Immunosuppressants, e.g. drugs for graft rejection
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43
Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
Applicants:
協和発酵キリン株式会社 KYOWA HAKKO KIRIN CO., LTD. [JP/JP]; 東京都千代田区大手町一丁目6番1号 1-6-1, Otemachi, Chiyoda-ku, Tokyo 1008185, JP
Inventors:
山田 陽史 YAMADA, Yoji; JP
岩井 宏徒 IWAI, Hiroto; JP
上原 啓嗣 UEHARA, Keiji; JP
鈴木 康裕 SUZUKI, Yasuhiro; JP
福田 裕一 FUKUDA, Yuichi; JP
木内 達人 KIUCHI, Tatsuto; JP
Agent:
稲葉 良幸 INABA, Yoshiyuki; JP
大貫 敏史 ONUKI, Toshifumi; JP
Priority Data:
2017-14975202.08.2017JP
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, the nucleic acid complex being capable of suppressing the expression of β2GPI. Formula 1: (in formula 1, X is a double-stranded nucleic acid that comprises a sense strand and an antisense strand and includes a duplex region of at least 11 base pairs; the double-stranded nucleic acid is complementary with any of the β2GPI mRNA sequences of interest described in Tables 1-1 to 1-16 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 binds to S3; L1 and L2 each independently a sugar ligand; and S1, S2, and S3 each independently represent a linker.)
(FR) L'invention fournit un complexe d'acide nucléique qui est représenté par la formule (1), et qui permet d'inhiber l'expression d'un β2GPI. Formule (1) : (Dans la formule (1), X consiste en un acide nucléique à double-brin constitué d'un brin sens et d'un brin antisens, et contenant les régions double-brin d'au moins 11 paires de base, cet acide nucléique à double-brin est complémentaire vis-à-vis de séquences ARNmβ2GPI cibles énumérées dans les tableaux 1-1 à 1-16, dans un brin d'oligonucléotide long de 17 à 30 nucléotides dans le brin antisens, l'extrémité 3' ou l'extrémité 5' du brin sens est liée en S3, L1 et L2 représentent chacun indépendamment un ligand de sucre, et S1, S2 et S3 représentent chacun indépendamment un lieur.)
(JA) 本発明は、下記式1で表されるβ2GPIの発現を抑制することが可能な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1-16に記載された標的β2GPI 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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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)