CN110139871A - 用于治疗中风和相关凝血障碍的凝血酶抑制剂 - Google Patents
用于治疗中风和相关凝血障碍的凝血酶抑制剂 Download PDFInfo
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- CN110139871A CN110139871A CN201780078158.2A CN201780078158A CN110139871A CN 110139871 A CN110139871 A CN 110139871A CN 201780078158 A CN201780078158 A CN 201780078158A CN 110139871 A CN110139871 A CN 110139871A
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- HKYTWJOWZTWBQB-AVGNSLFASA-N Tyr-Glu-Asp Chemical compound OC(=O)C[C@@H](C(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](N)CC1=CC=C(O)C=C1 HKYTWJOWZTWBQB-AVGNSLFASA-N 0.000 description 1
- ZRPLVTZTKPPSBT-AVGNSLFASA-N Tyr-Glu-Ser Chemical compound [H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(O)=O ZRPLVTZTKPPSBT-AVGNSLFASA-N 0.000 description 1
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- 101000926072 Varicella-zoster virus (strain Dumas) Envelope glycoprotein C Proteins 0.000 description 1
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- NERFNHBZJXXFGY-UHFFFAOYSA-N [4-[(4-methylphenyl)methoxy]phenyl]methanol Chemical compound C1=CC(C)=CC=C1COC1=CC=C(CO)C=C1 NERFNHBZJXXFGY-UHFFFAOYSA-N 0.000 description 1
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- 229940127217 antithrombotic drug Drugs 0.000 description 1
- 229960003856 argatroban Drugs 0.000 description 1
- KXNPVXPOPUZYGB-XYVMCAHJSA-N argatroban Chemical compound OC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[C@H](C)C2 KXNPVXPOPUZYGB-XYVMCAHJSA-N 0.000 description 1
- 108010091818 arginyl-glycyl-aspartyl-valine Proteins 0.000 description 1
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- 108010021908 aspartyl-aspartyl-glutamyl-aspartic acid Proteins 0.000 description 1
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- 229960002376 chymotrypsin Drugs 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 239000000701 coagulant Substances 0.000 description 1
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- 230000002860 competitive effect Effects 0.000 description 1
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- 238000013461 design Methods 0.000 description 1
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- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
- 235000019800 disodium phosphate Nutrition 0.000 description 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000002526 effect on cardiovascular system Effects 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000010228 ex vivo assay Methods 0.000 description 1
- 239000003527 fibrinolytic agent Substances 0.000 description 1
- 108010055341 glutamyl-glutamic acid Proteins 0.000 description 1
- 108010049041 glutamylalanine Proteins 0.000 description 1
- 229960003180 glutathione Drugs 0.000 description 1
- 108010051307 glycyl-glycyl-proline Proteins 0.000 description 1
- 210000002288 golgi apparatus Anatomy 0.000 description 1
- 150000003278 haem Chemical class 0.000 description 1
- 238000001631 haemodialysis Methods 0.000 description 1
- 230000000322 hemodialysis Effects 0.000 description 1
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- 238000002017 high-resolution X-ray diffraction Methods 0.000 description 1
- 108010045383 histidyl-glycyl-glutamic acid Proteins 0.000 description 1
- 238000005984 hydrogenation reaction Methods 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
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- 201000004332 intermediate coronary syndrome Diseases 0.000 description 1
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- 230000000302 ischemic effect Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000000816 matrix-assisted laser desorption--ionisation Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 229940127234 oral contraceptive Drugs 0.000 description 1
- 239000003539 oral contraceptive agent Substances 0.000 description 1
- 229940055729 papain Drugs 0.000 description 1
- 235000019834 papain Nutrition 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 238000010647 peptide synthesis reaction Methods 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
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- 108010029020 prolylglycine Proteins 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 238000003259 recombinant expression Methods 0.000 description 1
- 230000010410 reperfusion Effects 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000003998 snake venom Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 108010004034 stable plasma protein solution Proteins 0.000 description 1
- 239000004575 stone Substances 0.000 description 1
- 230000001180 sulfating effect Effects 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 125000004213 tert-butoxy group Chemical group [H]C([H])([H])C(O*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- ZGYICYBLPGRURT-UHFFFAOYSA-N tri(propan-2-yl)silicon Chemical compound CC(C)[Si](C(C)C)C(C)C ZGYICYBLPGRURT-UHFFFAOYSA-N 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Medicinal Preparation (AREA)
- Enzymes And Modification Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2016905231A AU2016905231A0 (en) | 2016-12-16 | Thrombin inhibitors for treatment of stroke and related coagulative disorders | |
| AU2016905231 | 2016-12-16 | ||
| PCT/AU2017/051405 WO2018107247A1 (en) | 2016-12-16 | 2017-12-15 | Thrombin inhibitors for treatment of stroke and related coagulative disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110139871A true CN110139871A (zh) | 2019-08-16 |
Family
ID=62557849
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780078158.2A Pending CN110139871A (zh) | 2016-12-16 | 2017-12-15 | 用于治疗中风和相关凝血障碍的凝血酶抑制剂 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US11091535B2 (https=) |
| EP (1) | EP3555116A4 (https=) |
| JP (2) | JP2020501561A (https=) |
| CN (1) | CN110139871A (https=) |
| AU (1) | AU2017376839B2 (https=) |
| CA (1) | CA3047159A1 (https=) |
| NZ (1) | NZ754781A (https=) |
| WO (1) | WO2018107247A1 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110590911A (zh) * | 2019-09-30 | 2019-12-20 | 华南理工大学 | 一种含酪氨酸硫酸化修饰的多肽合成方法及其应用 |
| CN114887123A (zh) * | 2022-04-18 | 2022-08-12 | 南通大学 | 水蛭素接枝纳米纤维血管支架材料、制备方法与应用 |
| CN119462906A (zh) * | 2024-11-11 | 2025-02-18 | 武汉元启合生科技有限公司 | 一种酪氨酸硫酸化的重组水蛭素、制备方法及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001000667A2 (en) * | 1999-06-29 | 2001-01-04 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Anti-thrombin peptide from anopheles albimanus salivary gland |
| CN101029079A (zh) * | 2006-07-31 | 2007-09-05 | 浙江中医药大学 | 硫酸化丝素蛋白的制备方法及其在抗凝血药物上的应用 |
| CN102026652A (zh) * | 2007-06-18 | 2011-04-20 | 自然环境研究会 | 凝血酶抑制剂 |
| CN102574909A (zh) * | 2009-05-05 | 2012-07-11 | 自然环境研究会 | 修饰丝氨酸蛋白酶抑制剂的方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4323754C1 (de) | 1993-07-15 | 1994-12-01 | Gruenenthal Gmbh | Bifunktionelle Urokinasevarianten mit verbesserten fibrinolytischen Eigenschaften und thrombinhemmender Wirkung |
| US6759384B1 (en) * | 1994-04-26 | 2004-07-06 | Aventis Pharmaceuticals Inc. | Factor Xa inhibitors |
| CA2394803A1 (en) * | 1999-11-24 | 2001-05-31 | Sugen, Inc. | Novel human protein kinases and protein kinase-like enzymes |
| EP1425296B1 (de) * | 2001-09-10 | 2011-04-13 | Novel Science International GmbH | Organische verbindungen mit biologischer wirkung als thrombinhemmer und ihre verwendung |
| JP3648548B2 (ja) * | 2001-10-15 | 2005-05-18 | 国立大学法人三重大学 | 血液凝固阻害活性を有するハマダラカ由来のＡｓ−１蛋白質 |
| DE10301255A1 (de) | 2003-01-15 | 2004-07-29 | Cpi Creative Pharma International Gmbh | Organische Verbindungen mit biologischer Wirkung als Thrombinhemmer und ihre Verwendung |
| JP2008532490A (ja) * | 2005-02-15 | 2008-08-21 | アポロ ライフ サイエンシズ リミテッド | 分子およびそのキメラ分子 |
| WO2007067983A2 (en) * | 2005-12-09 | 2007-06-14 | Wyeth | Sulfotyrosine specific antibodies and uses therefor |
| JP2013540995A (ja) * | 2010-08-18 | 2013-11-07 | カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス．アー．エール．エル． | 疾患に対する循環バイオマーカー |
| WO2014194015A1 (en) * | 2013-05-30 | 2014-12-04 | Virginia Commonwealth University | Sulfated beta-o4 low molecular weight lignins |
| WO2014194361A1 (en) * | 2013-06-04 | 2014-12-11 | The University Of Sydney | Peptide ligation |
| CN106687482B (zh) * | 2014-09-17 | 2022-01-25 | 诺和诺德股份有限公司 | 能够结合组织因子途径抑制剂(1-161)上的两个表位的抗体 |
| JP2023529993A (ja) * | 2020-06-19 | 2023-07-12 | ザ・ユニバーシティ・オブ・シドニー | 血栓塞栓状態の治療のための改良されたトロンビン阻害剤 |
-
2017
- 2017-12-15 JP JP2019531876A patent/JP2020501561A/ja active Pending
- 2017-12-15 AU AU2017376839A patent/AU2017376839B2/en active Active
- 2017-12-15 US US16/469,804 patent/US11091535B2/en active Active
- 2017-12-15 CA CA3047159A patent/CA3047159A1/en active Pending
- 2017-12-15 CN CN201780078158.2A patent/CN110139871A/zh active Pending
- 2017-12-15 WO PCT/AU2017/051405 patent/WO2018107247A1/en not_active Ceased
- 2017-12-15 NZ NZ754781A patent/NZ754781A/en unknown
- 2017-12-15 EP EP17881550.2A patent/EP3555116A4/en active Pending
-
2022
- 2022-06-22 JP JP2022100650A patent/JP2022130527A/ja active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001000667A2 (en) * | 1999-06-29 | 2001-01-04 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Anti-thrombin peptide from anopheles albimanus salivary gland |
| CN101029079A (zh) * | 2006-07-31 | 2007-09-05 | 浙江中医药大学 | 硫酸化丝素蛋白的制备方法及其在抗凝血药物上的应用 |
| CN102026652A (zh) * | 2007-06-18 | 2011-04-20 | 自然环境研究会 | 凝血酶抑制剂 |
| CN102574909A (zh) * | 2009-05-05 | 2012-07-11 | 自然环境研究会 | 修饰丝氨酸蛋白酶抑制剂的方法 |
Non-Patent Citations (3)
| Title |
|---|
| ANA C. FIGUEIREDO等: "The Tick-Derived Anticoagulant Madanin Is Processed by Thrombin and Factor Xa", PLOS ONE, vol. 8, no. 8, pages 1 - 11 * |
| ANA C. FIGUEIREDO等: "Unique thrombin inhibition mechanism by anophelin,an anticoagulant from the malaria vector", 《PNAS》 * |
| ANA C. FIGUEIREDO等: "Unique thrombin inhibition mechanism by anophelin,an anticoagulant from the malaria vector", 《PNAS》, 5 December 2012 (2012-12-05), pages 3649 * |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110590911A (zh) * | 2019-09-30 | 2019-12-20 | 华南理工大学 | 一种含酪氨酸硫酸化修饰的多肽合成方法及其应用 |
| CN110590911B (zh) * | 2019-09-30 | 2021-10-22 | 华南理工大学 | 一种含酪氨酸硫酸化修饰的多肽合成方法及其应用 |
| CN114887123A (zh) * | 2022-04-18 | 2022-08-12 | 南通大学 | 水蛭素接枝纳米纤维血管支架材料、制备方法与应用 |
| CN114887123B (zh) * | 2022-04-18 | 2023-07-04 | 南通大学 | 水蛭素接枝纳米纤维血管支架材料、制备方法与应用 |
| CN119462906A (zh) * | 2024-11-11 | 2025-02-18 | 武汉元启合生科技有限公司 | 一种酪氨酸硫酸化的重组水蛭素、制备方法及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018107247A1 (en) | 2018-06-21 |
| AU2017376839A1 (en) | 2019-07-11 |
| JP2022130527A (ja) | 2022-09-06 |
| US11091535B2 (en) | 2021-08-17 |
| US20190367583A1 (en) | 2019-12-05 |
| EP3555116A4 (en) | 2020-07-22 |
| NZ754781A (en) | 2021-12-24 |
| JP2020501561A (ja) | 2020-01-23 |
| CA3047159A1 (en) | 2018-06-21 |
| EP3555116A1 (en) | 2019-10-23 |
| AU2017376839B2 (en) | 2021-01-14 |
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