KR970074791A - 인터페론 결합체 - Google Patents
인터페론 결합체 Download PDFInfo
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- KR970074791A KR970074791A KR1019970022223A KR19970022223A KR970074791A KR 970074791 A KR970074791 A KR 970074791A KR 1019970022223 A KR1019970022223 A KR 1019970022223A KR 19970022223 A KR19970022223 A KR 19970022223A KR 970074791 A KR970074791 A KR 970074791A
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- ifnα
- conjugate
- peg
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/52—Cytokines; Lymphokines; Interferons
- C07K14/555—Interferons [IFN]
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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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- 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
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- Genetics & Genomics (AREA)
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- Gastroenterology & Hepatology (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
- Toxicology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
본 발명은 다음과 같은 화학식(1)으로 표시되는 생리적으로 활성인 PEG-IFN α결합제 (conjugate)에 관한 것이다.
상기 식에서, R과 R′는 독립적으로 저급 알킬이고; X는NH또는 0이고; n과 n′은 600 내지 1500의 합을 갖는 정수이다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (14)
- 폴리에틸렌 글리콜 단위의 평균 분자량이 약 26,000 내지 약 66,000돌턴(dalton)인, 다음 화확식 (1)으로 표시되는 생리적으로 활성인 폴리에틸렌 글리콜-인터페론 α(PEG_IFNα) 결합체 (conjugate) :상기 식에서, R과 R′는 독립적으로 저급 알킬이고; X는 NH또는 0이고; n과 n′은 600 내지 1500의 합을 갖는 정수이다.
- 제1항에 있어서, 상기 폴리에틸렌 글리콜 단위의 분자량이 약 35,000 내지 약 45000 돌턴인 결합체.
- 제2항에 있어서, 상기 폴리에틸렌 글리콜 단위의 분자량이 약 40,000돌턴인 결합체.
- 제1항에 있어서, 상기 R과 R′이 메틸인 결합체.
- 제1항에 있어서, 상기 X가 NH인 결합체.
- 제1항에 있어서, IFN α가 IFN α2a인 결합체.
- 제1항에 있어서, 상기 n과 N′의 합의 평균이 850 내지 1000인 결합체.
- 제1항에 있어서, 상기 R과 R′이 메틸이고; X가 NH이고; IFNα가 IFNα2a이고; 또한 n과 n′ 중 하나 또는 둘다가 420인 결합체.
- 제1항에 있어서, 상기 R과 R′이 메틸이고; X가 NH이고; IFNα가 IFNα2a이고; 또한 n과 n′중 하나 또는 둘다가 520인 걸합체.
- 제1항에 있어서, 항증식성 활성이 IFNα보다 높고, 항바이러스성 활성이 IFNα보다 낮은 결합체.
- 다음 화화식(2)로 표시되는 시약을 IFNα와 공유 결합시켜서 다음 화학식(1)로 표시되는 PEG-IFNα 결합체를 생성하는 것으로 이루어진, IFNα와 비교할 때 항증식성 활성이 증가되고 항바이러스성 활성이 감소되 다음 화학식(1)로 표시되는 PEG-IFNα 결합체를 생성하는 방법.상기 식에서, R과 R′는 독립적으로 저급 알킬이고; X는 NH또는 0이고; n과 n′ 은 600 내지 1500의 합을 갖는 정수이다.상기 식에서, R과 R′는 독립적으로 저급 알킬이고; n과 n′는 600 내지 1500의 합을 갖는 정수이다.
- 면역조절 장애를 치료 또는 예방하기 위한, 제1항 내지 제10항 중 어느 한 항에 따른 PEG-IFNα 결합체 및 치료적으로 불활성인 담체를 포함하는 약학 조성물.
- 제12항에 있어서, 종양성 질병 또는 감염성 질병을 치료 또는 예방하기 위한, 제1항 내지 제10항 중 어느 한 항에 따른PEG-IFNα 결합체 및 치료적으로 불활성인 담체를 포함하는 약학 조성물.
- 제 11항에 따른 방법에 따라 제조되는 제1항 내지 제10항 중 어느 한 항에 따른PEG-IFNα 결합체.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US1883496P | 1996-05-31 | 1996-05-31 | |
US60/018,834 | 1996-05-31 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR970074791A true KR970074791A (ko) | 1997-12-10 |
KR100254097B1 KR100254097B1 (ko) | 2000-05-01 |
Family
ID=21790006
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019970022223A KR100254097B1 (ko) | 1996-05-31 | 1997-05-30 | 인터페론결합체 |
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Families Citing this family (135)
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