JPH10506622A - ポリエチレングリコール変性されたセラミド脂質類及びそれらのリポソームへの使用 - Google Patents
ポリエチレングリコール変性されたセラミド脂質類及びそれらのリポソームへの使用Info
- Publication number
- JPH10506622A JPH10506622A JP8511229A JP51122996A JPH10506622A JP H10506622 A JPH10506622 A JP H10506622A JP 8511229 A JP8511229 A JP 8511229A JP 51122996 A JP51122996 A JP 51122996A JP H10506622 A JPH10506622 A JP H10506622A
- Authority
- JP
- Japan
- Prior art keywords
- liposome
- peg
- lipid
- liposomes
- alkyl
- 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.)
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Classifications
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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
- A61K9/10—Dispersions; Emulsions
- A61K9/127—Liposomes
- A61K9/1271—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers
- A61K9/1272—Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers with substantial amounts of non-phosphatidyl, i.e. non-acylglycerophosphate, surfactants as bilayer-forming substances, e.g. cationic lipids
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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
- 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
- A61K47/60—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 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
- C08G65/32—Polymers modified by chemical after-treatment
- C08G65/329—Polymers modified by chemical after-treatment with organic compounds
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S424/00—Drug, bio-affecting and body treating compositions
- Y10S424/812—Liposome comprising an antibody, antibody fragment, antigen, or other specific or nonspecific immunoeffector
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Dispersion Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Polymers & Plastics (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.下記式: 〔式中、R1,R2、及びR3は独立して、水素、C1−C6アルキル、アシル又は アリールであり; R4は水素、C1−C30アルキル、C2−C30アルケニル、C2−C30アルキニル 又はアリールであり; R5は水素、アルキル、アシル、アリール又はPEGであり; X1は−O−,−S−、又は−NR6−であり、ここでR6は水素、C1−C6アル キル、アシル又はアリールであり;又はR5がPEGであり、そしてbが1である場 合、X1はさらに、-Y1-alk-Y2-であり; Yは−NR7−であり、ここでR7は水素、C1−C6アルキル、アシル又はアリー ルであり、あるいはYは−O−,−S−又は-Y1-alk-Y2-であり、ここでY1及び Y2は独立して、アミノ、アミド、カルボキシル、カルバメート、カルボニル、 カルボネート、ウレア又はホスホロであり;そしてalkはC1−C6アルキレンで あり; PEGはC1−C3アルキル、アルコキシ、アシル又はアリールにより場合によっ ては置換されている約550〜約8,500ドルトンの平均分子量を有するポリエチレン グリコールであり;ここで、aは0又は1であり;そしてbは0又は1であるが 、R5がPEGでない場 合、bは1である〕で表わされる脂質化合物。 2.R1,R2,R3、及びR5が水素であり;R4がアルキルであり;X1が0で あり;Yがスクシネートであり;そしてPEGが約2,000又は約5,000ドルトンの平 均分子量を有し、そして末端のヒドロキシル位置でメチルにより置換されている 請求の範囲第1項記載の脂質。 3.R1,R2,R3、及びR5が水素であり;R4がアルキルであり;X1が0で あり;Yが−NH−であり;そしてPEGが約2,000又は約5,000の平均分子量を有し 、そして末端のヒドロキシル位置でメチルにより置換されている請求の範囲第1 項記載の脂質。 4.請求の範囲第1項記載の脂質を含んで成るリポソーム。 5.さらに、1又は複数の生物活性剤を含んで成る請求の範囲第4項記載のリ ポソーム。 6.細胞に生物活性剤を供給するための方法であって、リポソーム−生物活性 複合体を形成するために請求の範囲第4項記載のリポソームに前記剤を封入し、 そして前記細胞と前記複合体とを接触せしめることを含んで成る方法。 7.前記生物活性剤が、抗腫瘍剤、抗生物質、免疫改良剤、抗炎症薬物及び中 枢神経系に対して作用する薬物から成る群から選択される請求の範囲第6項記載 の方法。 8.前記生物活性剤がタンパク質又はペプチドである請求の範囲第6項記載の 方法。 9.請求の範囲第4項記載のリポソームに封入された1又は複数の生物活性剤 を含む適切な医薬組成物の治療的有効量を患者に投与することを含んで成る、患 者の疾病を処理するための方法。 10.リポソーム被覆されたワクチンを形成するために請求の範囲第4項記載の リポソームにワクチンのための生物活性剤を封入し、 そして患者に前記リポソーム被覆されたワクチンを投与することを含んで成る、 患者にワクチン供給するための方法。 11.リポソーム封入された抗原を形成するために請求の範囲第4項記載のリポ ソームに抗原を封入し、そして前記リポソーム封入された抗原を患者に投与する ことを含んで成る、患者を免疫化するための方法。 12.請求の範囲第5項記載のリポソーム及び生理学的に許容できるそれらのた めのアジュバントを含んで成る医薬製剤。 13.前記活性剤がビンクリスチンである請求の範囲第12項記載の製剤。 14.少なくとも2つの区画を有する容器を含んで成る、ラベルされたリポソー ムを調製するのに有用なキットであって、前記第1区画がラベルを調製するため の材料を含んで成り、そして前記第2区画が請求の範囲第5項記載のリポソーム を含んで成ることを特徴とするキット。 15.請求の範囲第1項記載の脂質を含んで成る脂質複合体。 16.治療使用のために遺伝子構造体を含んで成る請求の範囲第5項記載のリポ ソーム。 17.治療使用のためにオリゴヌクレオチドを含んで成る請求の範囲第5項記載 のリポソーム。 18.R1,R2,R3及びR5が水素であり;R4がC7−C23アルキルであり;X1 が0であり;Yがスクシネートであり;そしてPEGが約2,000の平均分子量を有 し、そしてモノメトキシにより置換されている請求の範囲第1項記載の脂質。 19.R4がC13−C19アルキルである請求の範囲第18項記載の脂質。 20.R4がC19アルキルである請求の範囲第19項記載の脂質。 21.R4がC13アルキルである請求の範囲第19項記載の脂質。 22.請求の範囲第18項記載の脂質を含んで成るリポソーム。 23.1又は複数の生物活性剤をさらに含んで成る請求の範囲第22項記載のリポ ソーム。 24.DOPE及びDODACをさらに含んで成る請求の範囲第23項記載のリポソーム。 25.前記脂質のモル%割合が約0.01〜約60である請求の範囲第23項記載のリポ ソーム。 26.R4がC13−C19アルキルである請求の範囲第25項記載のリポソーム。 27.細胞に生物活性剤を供給するための方法であって、リポソーム−生物活性 複合体を形成するために前記剤を請求の範囲第22項記載のリポソームにより封入 し、そして前記細胞と前記複合体とを接触せしめることを含んで成る方法。 28.R4がC13−C19アルキルである請求の範囲第27項記載の方法。 29.前記リポソームがさらに、DOPE及びDODACを含んで成る請求の範囲第28項 記載の方法。 30.請求の範囲第22項記載のリポソーム及び生理学的に許容できるそのための アジュバントを含んで成る医薬製剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31642994A | 1994-09-30 | 1994-09-30 | |
US08/316,429 | 1994-09-30 | ||
PCT/CA1995/000556 WO1996010391A1 (en) | 1994-09-30 | 1995-10-02 | Polyethylene glycol modified ceramide lipids and liposome uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH10506622A true JPH10506622A (ja) | 1998-06-30 |
JP3920330B2 JP3920330B2 (ja) | 2007-05-30 |
Family
ID=23229019
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP51122996A Expired - Fee Related JP3920330B2 (ja) | 1994-09-30 | 1995-10-02 | ポリエチレングリコール変性されたセラミド脂質類及びそれらのリポソームへの使用 |
Country Status (10)
Country | Link |
---|---|
US (1) | US5820873A (ja) |
EP (1) | EP0783297B1 (ja) |
JP (1) | JP3920330B2 (ja) |
AT (1) | ATE177943T1 (ja) |
AU (1) | AU3559895A (ja) |
CA (1) | CA2201120C (ja) |
DE (1) | DE69508598T2 (ja) |
DK (1) | DK0783297T3 (ja) |
ES (1) | ES2130651T3 (ja) |
WO (1) | WO1996010391A1 (ja) |
Cited By (3)
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JP2002212106A (ja) * | 2000-12-20 | 2002-07-31 | Biozone Lab Inc | 自己形成する熱力学的安定なリポソームおよびその適用 |
US6562371B1 (en) | 1998-11-02 | 2003-05-13 | Terumo Kabushiki Kaisha | Liposomes |
JP2011063615A (ja) * | 2003-04-25 | 2011-03-31 | Penn State Res Found:The | 増殖抑制性脂質由来生物活性化合物の全身送達方法およびシステム |
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- 1995-10-02 DK DK95932594T patent/DK0783297T3/da active
- 1995-10-02 WO PCT/CA1995/000556 patent/WO1996010391A1/en active IP Right Grant
- 1995-10-02 AT AT95932594T patent/ATE177943T1/de not_active IP Right Cessation
- 1995-10-02 EP EP95932594A patent/EP0783297B1/en not_active Expired - Lifetime
- 1995-10-02 ES ES95932594T patent/ES2130651T3/es not_active Expired - Lifetime
Cited By (4)
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US6562371B1 (en) | 1998-11-02 | 2003-05-13 | Terumo Kabushiki Kaisha | Liposomes |
JP2002212106A (ja) * | 2000-12-20 | 2002-07-31 | Biozone Lab Inc | 自己形成する熱力学的安定なリポソームおよびその適用 |
JP4497765B2 (ja) * | 2000-12-20 | 2010-07-07 | バイオゾーン ラボラトリーズ,インコーポレイテッド | 自己形成する熱力学的安定なリポソームおよびその適用 |
JP2011063615A (ja) * | 2003-04-25 | 2011-03-31 | Penn State Res Found:The | 増殖抑制性脂質由来生物活性化合物の全身送達方法およびシステム |
Also Published As
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ATE177943T1 (de) | 1999-04-15 |
EP0783297A1 (en) | 1997-07-16 |
ES2130651T3 (es) | 1999-07-01 |
AU3559895A (en) | 1996-04-26 |
JP3920330B2 (ja) | 2007-05-30 |
DK0783297T3 (da) | 1999-10-11 |
CA2201120A1 (en) | 1996-04-11 |
DE69508598T2 (de) | 1999-07-15 |
EP0783297B1 (en) | 1999-03-24 |
CA2201120C (en) | 2007-12-04 |
DE69508598D1 (de) | 1999-04-29 |
US5820873A (en) | 1998-10-13 |
WO1996010391A1 (en) | 1996-04-11 |
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