JPH10502918A - 核酸を含有する組成物、その製造および使用 - Google Patents
核酸を含有する組成物、その製造および使用Info
- Publication number
- JPH10502918A JPH10502918A JP8504741A JP50474196A JPH10502918A JP H10502918 A JPH10502918 A JP H10502918A JP 8504741 A JP8504741 A JP 8504741A JP 50474196 A JP50474196 A JP 50474196A JP H10502918 A JPH10502918 A JP H10502918A
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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
- C12N15/87—Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
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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
- C12N15/87—Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation
- C12N15/88—Introduction of foreign genetic material using processes not otherwise provided for, e.g. co-transformation using microencapsulation, e.g. using amphiphile liposome vesicle
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- 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
-
- 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
- A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Genetics & Genomics (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Engineering & Computer Science (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Biotechnology (AREA)
- Pharmacology & Pharmacy (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Biophysics (AREA)
- Physics & Mathematics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Microbiology (AREA)
- Plant Pathology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
- Polyamides (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.少なくとも1種の核酸および一般式(I) (式中、 −Rは水素原子または式 で示される基であることができ、 −nは2〜10の間の整数であり、 −pおよびqは整数であるが、 ただし、合計p+qが、ポリマーの平均分子量が100〜107の間になるよう なものであることが理解されているものとする) で示されるカチオン性ポリマーを含んでなる組成物。 2.式(I)中で、nが2〜5の間にあることを特徴とする請求の範囲1に記 載の組成物。 3.ポリマーが103〜5×106の間の平均分子量を有することを特徴とする 請求の範囲1または2に記載の組成物。 4.ポリマーがポリエチレンイミン(PEI)およびポリプロピレンイミン( PPI)から選ばれることを特徴とする請求の範囲1〜3のいずれか一項に記載 の組成物。 5.ポリマーが平均分子量50,000のポリエチレンイミン(PEI50K )および平均分子量800,000のポリエチレンイミン(PEI80K)から 選ばれることを特徴とする請求の範囲4に記載の組成物。 6.ポリマーと核酸との各比率が、ポリマーアミン/核酸リン酸エステルの比 率Rが0.5〜50の間になるように選ばれることを特徴とする請求の範囲1〜 5のいずれか一項に記載の組成物。 7.比率Rが2〜50の間にあることを特徴とする請求の範囲6に記載の組成 物。 8.比率Rが5〜30の間にあることを特徴とする請求の範囲7に記載の組成 物。 9.さらに、ポリマー/核酸複合体と組合せることができ、そしてトランスフ ェクション力を増強することができる1種またはそれ以上の補助剤を含んでなる ことを特徴とする請求の範囲1〜8のいずれか一項に記載の組成物。 10.補助剤が脂質、タンパク質、リポポリアミンおよび合成ポリマーから選 ばれることを特徴とする請求の範囲9に記載の組成物。 11.補助剤がカチオン性脂質であることを特徴とする請求の範囲10に記載 の組成物。 12.カチオン性脂質が1種またはそれ以上のリポポリアミンであることを特 徴とする請求の範囲11に記載の組成物。 13.リポポリアミンが、一般式H2N−(−(CH)m−NH−)l−H(式中 、mは2を超えるかまたは等しい整数であり、lは1を超えるかまたは等しい整 数であるが、ただしmが2つのアミンの間に在る各 種炭素基の間を変化することが可能である)に対応することを特徴とする請求の 範囲12に記載の組成物。。 14.リポポリアミンが、ジオクタデシルアミドグリシルスペルミン(DOG S)またはパルミトイルホスファチジルエタノールアミン=5−カルボキシスペ ルミルアミド(DPPES)から選ばれることを特徴とする請求の範囲13に記 載の組成物。 15.補助剤が1種またはそれ以上の中性脂質であることを特徴とする請求の 範囲10に記載の組成物。 16.中性脂質または中性脂質類が、両性イオンであるかまたは生理学的条件 下でイオン性電荷を欠く合成または天然脂質から選ばれることを特徴とする請求 の範囲15に記載の組成物。 17.中性脂質または中性脂質類が2つの脂肪鎖を含有する脂質であることを 特徴とする請求の範囲16に記載の組成物。 18.中性脂質または中性脂質類がジオレオイルホスファチジルエタノールア ミン(DOPE)、オレオイルパルミトイルホスファチジルエタノールアミン( POPE)、ジステアロイル−、−パルミトイル−および−ミリストイルホスフ ァチジルエタノールアミン並びにそれらの1〜3重Nメチル化誘導体;ホスファ チジルグリセロール、ジアシルグリセロール、グリコシルジアシルグリセロール 、セレブロシド(特に、ガラクトセレブロシドのような)、スフィンゴ脂質(特 に、スフィンゴミエリンのような)またはその他としてアシアロガングリオシド (特に、アシアロGM1および−GM2のような)から選ばれることを特徴とす る請求の範囲16に記載の組成物。 19.核酸がデオキシリボ核酸であることを特徴とする請求の範囲1 に記載の組成物。 20.核酸がリボ核酸であることを特徴とする請求の範囲1に記載の組成物。 21.核酸が化学的に修飾されることを特徴とする請求の範囲19または20 に記載の組成物。 22.核酸がアンチセンス配列であることを特徴とする請求の範囲19〜21 のいずれか一項に記載の組成物。 23.核酸が治療的遺伝子を含有することを特徴とする請求の範囲19〜22 のいずれか一項に記載の組成物。 24.核酸リン酸エステルのモル当量当たり0.1〜20モル当量、さらに好 適には1〜5モル当量の補助剤を含んでなることを特徴とする請求の範囲9に記 載の組成物。。 25.標的指向要素(targeting element)を含んでなるこ とを特徴とする請求の範囲1〜24のいずれか一項に記載の組成物。 26.標的指向要素が、抗体もしくは抗体断片のような糖および/またはペプ チド、細胞受容体リガンドもしくはそれらの断片、または受容体もしくは受容体 断片よりなることを特徴とする請求の範囲25に記載の組成物。 27.標的指向要素が、式(I)で示されるポリマーに共有結合的に結合して いることを特徴とする請求の範囲25または26に記載の組成物。 28.注射剤のための薬学的に許容される賦形剤を含んでなることを特徴とす る請求の範囲1〜27のいずれか一項に記載の組成物。 29.皮膚および/または粘膜への適用のための薬学的に許容される賦形剤を 含んでなることを特徴とする請求の範囲1〜28のいずれか一項に記載の組成物 。 30.核酸の細胞中への移入のための、請求の範囲1に記載のカチオン性ポリ マーの使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR94/08735 | 1994-07-13 | ||
FR9408735A FR2722506B1 (fr) | 1994-07-13 | 1994-07-13 | Composition contenant des acides nucleiques, preparation et utilisations |
PCT/FR1995/000914 WO1996002655A1 (fr) | 1994-07-13 | 1995-07-07 | Composition contenant des acides nucleiques, preparation et utilisations |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10502918A true JPH10502918A (ja) | 1998-03-17 |
JP4275728B2 JP4275728B2 (ja) | 2009-06-10 |
Family
ID=9465376
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP50474196A Expired - Lifetime JP4275728B2 (ja) | 1994-07-13 | 1995-07-07 | 核酸を含有する組成物、その製造および使用 |
Country Status (18)
Country | Link |
---|---|
US (1) | US6013240A (ja) |
EP (1) | EP0770140B1 (ja) |
JP (1) | JP4275728B2 (ja) |
KR (1) | KR100424802B1 (ja) |
AT (1) | ATE367448T1 (ja) |
AU (1) | AU2930795A (ja) |
CA (1) | CA2194797C (ja) |
DE (1) | DE69535540T9 (ja) |
DK (1) | DK0770140T3 (ja) |
ES (1) | ES2290952T3 (ja) |
FI (1) | FI119738B (ja) |
FR (1) | FR2722506B1 (ja) |
IL (1) | IL114566A (ja) |
MX (1) | MX9700270A (ja) |
NO (1) | NO323110B1 (ja) |
PT (1) | PT770140E (ja) |
WO (1) | WO1996002655A1 (ja) |
ZA (1) | ZA955849B (ja) |
Cited By (3)
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JP2002541125A (ja) * | 1999-04-02 | 2002-12-03 | リサーチ ディベロップメント ファンデーション | エアロゾル送達のためのポリエチレンイミン:dna製剤 |
JP4827358B2 (ja) * | 2000-02-18 | 2011-11-30 | アバンテイス・フアルマ・エス・アー | 機能的ポリアルキレンイミンの製造方法、前記化合物を含む組成物及びその使用 |
JP2015518874A (ja) * | 2012-06-08 | 2015-07-06 | エスリス ゲーエムベーハーethris GmbH | メッセンジャーrnaの肺送達 |
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US7422902B1 (en) | 1995-06-07 | 2008-09-09 | The University Of British Columbia | Lipid-nucleic acid particles prepared via a hydrophobic lipid-nucleic acid complex intermediate and use for gene transfer |
FR2739292B1 (fr) * | 1995-09-28 | 1997-10-31 | Rhone Poulenc Rorer Sa | Composition pharmaceutique utile pour la transfection d'acides nucleiques et ses utilisations |
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US6071533A (en) | 1996-11-12 | 2000-06-06 | The Regents Of The University Of California | Preparation of stable formulations of lipid-nucleic acid complexes for efficient in vivo delivery |
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- 1995-07-07 DE DE69535540T patent/DE69535540T9/de active Active
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2002541125A (ja) * | 1999-04-02 | 2002-12-03 | リサーチ ディベロップメント ファンデーション | エアロゾル送達のためのポリエチレンイミン:dna製剤 |
JP4827358B2 (ja) * | 2000-02-18 | 2011-11-30 | アバンテイス・フアルマ・エス・アー | 機能的ポリアルキレンイミンの製造方法、前記化合物を含む組成物及びその使用 |
JP2015518874A (ja) * | 2012-06-08 | 2015-07-06 | エスリス ゲーエムベーハーethris GmbH | メッセンジャーrnaの肺送達 |
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NO970049D0 (no) | 1997-01-07 |
US6013240A (en) | 2000-01-11 |
JP4275728B2 (ja) | 2009-06-10 |
KR970704889A (ko) | 1997-09-06 |
DE69535540T2 (de) | 2008-06-19 |
CA2194797C (fr) | 2010-03-23 |
FI119738B (fi) | 2009-02-27 |
IL114566A (en) | 2005-08-31 |
EP0770140B1 (fr) | 2007-07-18 |
WO1996002655A1 (fr) | 1996-02-01 |
ZA955849B (en) | 1996-02-21 |
NO323110B1 (no) | 2007-01-02 |
FI970115A (fi) | 1997-01-10 |
DK0770140T3 (da) | 2007-11-19 |
IL114566A0 (en) | 1995-11-27 |
ATE367448T1 (de) | 2007-08-15 |
DE69535540D1 (de) | 2007-08-30 |
FI970115A0 (fi) | 1997-01-10 |
KR100424802B1 (ko) | 2004-06-23 |
FR2722506A1 (fr) | 1996-01-19 |
ES2290952T3 (es) | 2008-02-16 |
MX9700270A (es) | 1997-05-31 |
EP0770140A1 (fr) | 1997-05-02 |
DE69535540T9 (de) | 2012-03-15 |
FR2722506B1 (fr) | 1996-08-14 |
NO970049L (no) | 1997-01-07 |
AU2930795A (en) | 1996-02-16 |
CA2194797A1 (fr) | 1996-02-01 |
PT770140E (pt) | 2007-10-19 |
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