CN104302306A - Tfpi抑制剂及其使用方法 - Google Patents
Tfpi抑制剂及其使用方法 Download PDFInfo
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- CN104302306A CN104302306A CN201380024521.4A CN201380024521A CN104302306A CN 104302306 A CN104302306 A CN 104302306A CN 201380024521 A CN201380024521 A CN 201380024521A CN 104302306 A CN104302306 A CN 104302306A
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- aminoacid
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- peptide
- tfpi
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- 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
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- 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
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- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/81—Protease inhibitors
- C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
- C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
- C07K14/8114—Kunitz type inhibitors
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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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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/86—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving blood coagulating time or factors, or their receptors
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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
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/81—Protease inhibitors
- G01N2333/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
- G01N2333/811—Serine protease (E.C. 3.4.21) inhibitors
- G01N2333/8114—Kunitz type inhibitors
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/04—Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/20—Screening for compounds of potential therapeutic value cell-free systems
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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 | k结合(1/Ms) | k解离(1/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 | 9.17x10-7 |
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 (43)
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CN201810933447.2A CN109111505A (zh) | 2012-03-21 | 2013-01-31 | Tfpi抑制剂及其使用方法 |
CN201810934767.XA CN109134614A (zh) | 2012-03-21 | 2013-01-31 | Tfpi抑制剂及其使用方法 |
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EP (1) | EP2827883B1 (zh) |
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CN (3) | CN109134614A (zh) |
AU (2) | AU2013235741C1 (zh) |
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