CN104984319A - Tfpi抑制剂和使用方法 - Google Patents
Tfpi抑制剂和使用方法 Download PDFInfo
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- CN104984319A CN104984319A CN201510260670.1A CN201510260670A CN104984319A CN 104984319 A CN104984319 A CN 104984319A CN 201510260670 A CN201510260670 A CN 201510260670A CN 104984319 A CN104984319 A CN 104984319A
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- aminoacid
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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
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
- C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
- C07K14/4702—Regulators; Modulating activity
- C07K14/4703—Inhibitors; Suppressors
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/02—Peptides of undefined number of amino acids; Derivatives thereof
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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
- A61K47/54—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 compound
- A61K47/55—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
- A61K47/551—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 compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
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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
- A61K47/54—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 compound
- A61K47/555—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 compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
- A61K47/557—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 compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells the modifying agent being biotin
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
-
- 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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- 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
TFPI竞争ELISA IC50[nM] | 组 |
<50nM | A |
50≤x<100nM | B |
100≤x<250nM | C |
250≤x<1000nM | D |
1000≤x<5000nM | E |
5000≤x<10000nM | F |
10000≤x<50000nM | G |
肽 | kon(l/Ms) | koff(l/s) | KD(M) |
JBT0047 | 4.0x105 | 1.9x10-2 | 4.7x10-8 |
JBT0120 | 1.17x106 | 4.78x10-2 | 4.08x10-8 |
JBT0131 | 1.4x105 | 6.0x10-2 | 4.31x10-7 |
JBT0132 | 3.55x104 | 3.26x10-2 | 9.17xl0-7 |
JBT0224 | 6.39x104 | 1.95x10-2 | 3.05x10-7 |
JBT0293 | 6.0x105 | 5.6x10-2 | 9.5x10-8 |
JBT0297 | 5.0x105 | 1.4x10-2 | 2.9x10-8 |
JBT0303 | 8.13x105 | 2.75x10-2 | 3.4x10-8 |
JBT0305 | 7.5x105 | 3.1x10-2 | 6.1x10-8 |
Claims (132)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US13927208P | 2008-12-19 | 2008-12-19 | |
US61/139,272 | 2008-12-19 | ||
CN200980156547.8A CN102348462B (zh) | 2008-12-19 | 2009-12-21 | Tfpi抑制剂和使用方法 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200980156547.8A Division CN102348462B (zh) | 2008-12-19 | 2009-12-21 | Tfpi抑制剂和使用方法 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN104984319A true CN104984319A (zh) | 2015-10-21 |
Family
ID=42269298
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201510260670.1A Pending CN104984319A (zh) | 2008-12-19 | 2009-12-21 | Tfpi抑制剂和使用方法 |
CN200980156547.8A Active CN102348462B (zh) | 2008-12-19 | 2009-12-21 | Tfpi抑制剂和使用方法 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN200980156547.8A Active CN102348462B (zh) | 2008-12-19 | 2009-12-21 | Tfpi抑制剂和使用方法 |
Country Status (16)
Country | Link |
---|---|
US (3) | US8466108B2 (zh) |
EP (1) | EP2379096B1 (zh) |
JP (3) | JP5739816B2 (zh) |
KR (3) | KR101792032B1 (zh) |
CN (2) | CN104984319A (zh) |
AU (1) | AU2009327338B2 (zh) |
BR (2) | BR122021014783B1 (zh) |
CA (1) | CA2747721C (zh) |
DK (1) | DK2379096T3 (zh) |
ES (1) | ES2773766T3 (zh) |
HR (1) | HRP20192282T8 (zh) |
HU (1) | HUE046951T2 (zh) |
LT (1) | LT2379096T (zh) |
NZ (2) | NZ607892A (zh) |
SI (1) | SI2379096T1 (zh) |
WO (1) | WO2010071894A2 (zh) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2010071894A2 (en) | 2008-12-19 | 2010-06-24 | Baxter International Inc. | Tfpi inhibitors and methods of use |
DK2379600T4 (da) * | 2008-12-22 | 2021-01-04 | Novo Nordisk As | Antistoffer mod tissue factor pathway inhibitor |
JP2013507927A (ja) * | 2009-10-14 | 2013-03-07 | エルロン・セラピューティクス・インコーポレイテッド | 改善されたペプチド模倣大環状分子 |
NZ702494A (en) | 2010-03-01 | 2016-09-30 | Bayer Healthcare Llc | Optimized monoclonal antibodies against tissue factor pathway inhibitor (tfpi) |
DK2547355T3 (en) | 2010-03-19 | 2017-03-20 | Baxalta GmbH | TFPI INHIBITORS AND METHODS OF USE |
US9228022B2 (en) | 2010-06-30 | 2016-01-05 | Novo Nordisk A/S | Antibodies that are capable of specifically binding tissue factor pathway inhibitor |
WO2012001087A1 (en) | 2010-06-30 | 2012-01-05 | Novo Nordisk A/S | Antibodies that are capable of specifically binding tissue factor pathway inhibitor |
TWI483733B (zh) * | 2011-02-11 | 2015-05-11 | Baxter Int | Tfpi抑制劑及使用方法 |
WO2012109675A1 (en) * | 2011-02-11 | 2012-08-16 | Baxter International Inc. | Aptamers to tissue factor pathway inhibitor and their use as bleeding disorder therapeutics |
WO2012178063A1 (en) | 2011-06-23 | 2012-12-27 | The Regents Of The University Of Michigan | Compound and method for modulating opioid receptor activity |
NZ629130A (en) * | 2012-03-21 | 2016-10-28 | Baxalta Inc | Tfpi inhibitors and methods of use |
CN104215707B (zh) * | 2014-09-02 | 2016-01-20 | 福建中医药大学 | 栝楼桂枝汤的质量检测方法 |
MY178445A (en) | 2015-02-25 | 2020-10-13 | Mogam Inst Biomedical Res | Novel antibody binding to tfpi and composition comprising the same |
RU2705540C2 (ru) * | 2015-08-19 | 2019-11-07 | Пфайзер Инк. | Антитела против ингибитора пути тканевого фактора и их применения |
JP7152084B1 (ja) * | 2022-02-22 | 2022-10-12 | 株式会社血栓トランスレーショナルリサーチラボ | 組織因子経路インヒビターの抗凝固活性の検査試薬、検査試薬セット、および検査方法 |
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