CN100488562C - 凝血因子VⅡ或VⅡa样分子 - Google Patents
凝血因子VⅡ或VⅡa样分子 Download PDFInfo
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- CN100488562C CN100488562C CNB018048641A CN01804864A CN100488562C CN 100488562 C CN100488562 C CN 100488562C CN B018048641 A CNB018048641 A CN B018048641A CN 01804864 A CN01804864 A CN 01804864A CN 100488562 C CN100488562 C CN 100488562C
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- Prior art keywords
- polypeptide
- conjugate
- amino acid
- fviia
- fvii
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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
- C07K14/745—Blood coagulation or fibrinolysis factors
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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
- 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
- A61K47/62—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 a protein, peptide or polyamino acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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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
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
- C12N9/6424—Serine endopeptidases (3.4.21)
- C12N9/6437—Coagulation factor VIIa (3.4.21.21)
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
- C12Y304/21—Serine endopeptidases (3.4.21)
- C12Y304/21021—Coagulation factor VIIa (3.4.21.21)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Wood Science & Technology (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Gastroenterology & Hepatology (AREA)
- Toxicology (AREA)
- Biophysics (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
连接基团 | 氨基酸 | 非多肽组分实例 | 偶联方法/活化的PEG | 参考 |
-NH<sub>2</sub> | N-末端,赖氨酸 | 聚合物,如PEG,具有酰胺或亚胺基团 | mPEG-SPATresylatedmPEG | Shearwater Inc.Delgado等,critical reviews inTherapeutic Drug CarrierSystems9(3,4):249-304(1992) |
-COOH | C-末端,天冬氨酸,谷氨酸 | 聚合物,如PEG,具有酯或酰胺基团碳水化合物组分 | mPEG-Hz体外偶联 | Shearwater Inc. |
-SH | 半胱氨酸 | 聚合物,如PEG,具有二硫键,马来酰亚胺或乙烯砜基团碳水化合物组分 | PEG-乙烯砜PEG-马来酰亚胺体外偶联 | Shearwater Inc.Delgado等,critical reviews inTherapeutic Drug CarrierSystems9(3,4):249-304(1992) |
-OH | 丝氨酸、苏氨酸、赖氨酸、OH- | 糖组分具有酯、醚、氨基甲酸酯、碳酸酯基团的PEG | 体内O-连接的糖基化 | |
-CONH<sub>2</sub> | 天冬酰胺作为部分N-糖基化位点 | 糖组分聚合物,如PEG | 体内N-糖基化 | |
芳香族残基 | 苯丙氨酸、酪氨酸、色氨酸 | 碳水化合物组分 | 体外偶联 | |
-CONH<sub>2</sub> | 谷氨酰胺 | 碳水化合物组分 | 体外偶联 | Yan & Wold,Biochemistry,1984,Ju131:23(16):3759-65 |
醛酮 | 氧化的寡糖 | 聚合物,如PEG,PEG-酰肼 | PEG化 | Andresz等,1978,Makromol.Chem.179:301,WO92/16555,WO00/23114 |
胍 | 精氨酸 | 碳水化合物组分 | 体外偶联 | Lundblad & Noyes,Chemical Reagents forProtein Modification,CRCPress Inc.,Florida USA |
咪唑环 | 组氨酸 | 碳水化合物组分 | 体外偶联 | 同胍 |
1 | 丙氨酸(A) 甘氨酸(G) 丝氨酸(S) 苏氨酸(T) |
2 | 天冬氨酸(D) 谷氨酸(E) |
3 | 天冬酰胺(N) 谷氨酰胺(Q) |
4 | 精氨酸(R) 组氨酸(H) 赖氨酸(K) |
5 | 异亮氨酸(I) 亮氨酸(L) 甲硫氨酸(M) 颉氨酸(V) |
6 | 苯丙氨酸(F) 酪氨酸(Y) 色氨酸(W) |
糖基化偶联物 | 酰胺分解活性 | 凝血活性 |
T106NK143N+N145TV253NR290N+A292TG291NR315N+V317TK143N+N145T+R315N+V317T | +++--++ | +ndndndnd+nd |
Claims (21)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DKPA200000218 | 2000-02-11 | ||
DKPA200000218 | 2000-02-11 | ||
DKPA200001558 | 2000-10-18 | ||
DKPA200001558 | 2000-10-18 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNA2009101282432A Division CN101503726A (zh) | 2000-02-11 | 2001-02-12 | 凝血因子Ⅶ或Ⅶa样分子 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1400910A CN1400910A (zh) | 2003-03-05 |
CN100488562C true CN100488562C (zh) | 2009-05-20 |
Family
ID=26068765
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB018048641A Expired - Fee Related CN100488562C (zh) | 2000-02-11 | 2001-02-12 | 凝血因子VⅡ或VⅡa样分子 |
Country Status (18)
Country | Link |
---|---|
US (13) | US6806063B2 (zh) |
EP (3) | EP2319541A1 (zh) |
JP (2) | JP2003521930A (zh) |
CN (1) | CN100488562C (zh) |
AT (1) | ATE428445T1 (zh) |
AU (3) | AU783512B2 (zh) |
CA (2) | CA2739933A1 (zh) |
CY (1) | CY1109614T1 (zh) |
DE (1) | DE60138364D1 (zh) |
DK (1) | DK1257295T3 (zh) |
ES (1) | ES2325877T3 (zh) |
IL (2) | IL150692A0 (zh) |
NO (1) | NO20023804L (zh) |
NZ (1) | NZ521257A (zh) |
PL (2) | PL204285B1 (zh) |
PT (1) | PT1257295E (zh) |
RU (1) | RU2278123C2 (zh) |
WO (1) | WO2001058935A2 (zh) |
Families Citing this family (166)
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US7247708B2 (en) | 1997-10-23 | 2007-07-24 | Regents Of The University Of Minnesota | Modified vitamin K-dependent polypeptides |
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ATE428445T1 (de) * | 2000-02-11 | 2009-05-15 | Bayer Healthcare Llc | Gerinnungsfaktor vii oder viia konjugate |
US7220837B1 (en) | 2000-04-28 | 2007-05-22 | Regents Of The University Of Minnesota | Modified vitamin K-dependent polypeptides |
US7812132B2 (en) * | 2000-04-28 | 2010-10-12 | Regents Of The University Of Minnesota | Modified vitamin K-dependent polypeptides |
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US20030211094A1 (en) * | 2001-06-26 | 2003-11-13 | Nelsestuen Gary L. | High molecular weight derivatives of vitamin k-dependent polypeptides |
US6423826B1 (en) | 2000-06-30 | 2002-07-23 | Regents Of The University Of Minnesota | High molecular weight derivatives of vitamin K-dependent polypeptides |
US7160540B2 (en) | 2000-06-30 | 2007-01-09 | Regents Of The University Of Minnesota | Methods for detecting activity of clottings factors |
BR0113854A (pt) | 2000-09-13 | 2004-07-06 | Novo Nordisk As | Polipeptìdeo do fator vii, construção de ácido nucleìco, célula hospedeira recombinante animal transgênico, planta transgênica, método para produzir o polipeptìdeo do fator vii, composição farmacêutica, uso de um polipeptìdeo do fator vii, e, métodos para o tratamento de episódios de sangramento e para tratamento ou profilaxia de distúrbios de sangramento em um indivìduo ou para a intensificação do sistema hemostático normal |
PL204888B1 (pl) * | 2000-09-13 | 2010-02-26 | Novo Nordisk Healthcare Ag | Wariant polipeptydu czynnika VII, konstrukcja kwasu nukleinowego, rekombinowana komórka gospodarza, zwierzę transgeniczne, sposób wytwarzania wariantu polipeptydu czynnika VII, kompozycja farmaceutyczna i zastosowanie wariantu polipeptydu czynnika VII |
WO2002038162A1 (en) | 2000-11-09 | 2002-05-16 | The Scripps Research Institute | MODIFIED FACTOR VIIa |
US7235638B2 (en) | 2001-03-22 | 2007-06-26 | Novo Nordisk Healthcare A/G | Coagulation factor VII derivatives |
EP1373493B1 (en) * | 2001-03-22 | 2013-07-31 | Novo Nordisk Health Care AG | Coagulation factor vii derivative |
ATE532858T1 (de) * | 2001-09-27 | 2011-11-15 | Novo Nordisk Healthcare Ag | Menschliche gerinnungsfaktor-vii-polypeptide |
US7052868B2 (en) | 2001-09-27 | 2006-05-30 | Novo Nordisk Healthcare A/G | Human coagulation factor VII polypeptides |
WO2004099231A2 (en) | 2003-04-09 | 2004-11-18 | Neose Technologies, Inc. | Glycopegylation methods and proteins/peptides produced by the methods |
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EP2322229B1 (en) * | 2001-10-10 | 2016-12-21 | Novo Nordisk A/S | Remodeling and glycoconjugation of Factor IX |
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