EA200100025A1 - Соединения пиразинона, фармацевтическая композиция (варианты) и лекарственная форма, способ ингибирования протеазы, способ снижения тромбообразующей способности поверхности, способ лечения нарушенного протеолиза и тромбоза, связанного с различными заболеваниями, способ снижения свертывания крови и способ определения тромбина у млекопитающего - Google Patents
Соединения пиразинона, фармацевтическая композиция (варианты) и лекарственная форма, способ ингибирования протеазы, способ снижения тромбообразующей способности поверхности, способ лечения нарушенного протеолиза и тромбоза, связанного с различными заболеваниями, способ снижения свертывания крови и способ определения тромбина у млекопитающегоInfo
- Publication number
- EA200100025A1 EA200100025A1 EA200100025A EA200100025A EA200100025A1 EA 200100025 A1 EA200100025 A1 EA 200100025A1 EA 200100025 A EA200100025 A EA 200100025A EA 200100025 A EA200100025 A EA 200100025A EA 200100025 A1 EA200100025 A1 EA 200100025A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- blood
- inhibiting
- thrombin
- formation
- Prior art date
Links
- 108090000190 Thrombin Proteins 0.000 title abstract 3
- 208000007536 Thrombosis Diseases 0.000 title abstract 3
- 229960004072 thrombin Drugs 0.000 title abstract 3
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical class OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 title abstract 2
- 230000005764 inhibitory process Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title 5
- 241000124008 Mammalia Species 0.000 title 1
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
- 230000023555 blood coagulation Effects 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 239000002552 dosage form Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 230000017854 proteolysis Effects 0.000 title 1
- 230000002885 thrombogenetic effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 230000002401 inhibitory effect Effects 0.000 abstract 5
- 210000004369 blood Anatomy 0.000 abstract 4
- 239000008280 blood Substances 0.000 abstract 4
- 230000015572 biosynthetic process Effects 0.000 abstract 3
- 210000001772 blood platelet Anatomy 0.000 abstract 2
- 239000000463 material Substances 0.000 abstract 2
- 108090000317 Chymotrypsin Proteins 0.000 abstract 1
- 208000005189 Embolism Diseases 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 102000009123 Fibrin Human genes 0.000 abstract 1
- 108010073385 Fibrin Proteins 0.000 abstract 1
- BWGVNKXGVNDBDI-UHFFFAOYSA-N Fibrin monomer Chemical compound CNC(=O)CNC(=O)CN BWGVNKXGVNDBDI-UHFFFAOYSA-N 0.000 abstract 1
- 108010088842 Fibrinolysin Proteins 0.000 abstract 1
- 108090000631 Trypsin Proteins 0.000 abstract 1
- 102000004142 Trypsin Human genes 0.000 abstract 1
- 238000004220 aggregation Methods 0.000 abstract 1
- 230000002776 aggregation Effects 0.000 abstract 1
- 230000002785 anti-thrombosis Effects 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 239000002473 artificial blood Substances 0.000 abstract 1
- 230000017531 blood circulation Effects 0.000 abstract 1
- 229960002376 chymotrypsin Drugs 0.000 abstract 1
- 238000000502 dialysis Methods 0.000 abstract 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 abstract 1
- 229950003499 fibrin Drugs 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 1
- 229940012957 plasmin Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000012588 trypsin Substances 0.000 abstract 1
- 229960001322 trypsin Drugs 0.000 abstract 1
- 108010036927 trypsin-like serine protease Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Peptides Or Proteins (AREA)
Abstract
Описаны соединения пиразинона, включая соединения формулы (I), где X означает O, NRили CH=N, R-R, R, R, R, W, m и n определены в описании изобретения, а также их гидраты, сольваты или фармацевтически приемлемые соли. Соединения по настоящему изобретению являются эффективными ингибиторами протеаз, прежде всего, трипсинподобных сериновых протеаз, таких как химотрипсин, трипсин, тромбин, плазмин и фактор Xa. Некоторые соединения проявляют антитромботическую активность, благодаря прямому селективному ингибированию тромбина. Описаны также композиции для ингибирования потери тромбоцитов крови, ингибирования агрегации тробмоцитов, ингибирования образования фибрина, ингибирования образования тромбов и ингибирования образования эмбола. Другой областью применения соединений по изобретению является их использование в качестве антикоагулянтов, либо введенных в материалы, либо физически связанных с материалами, которые используются для производства устройств для сбора крови, искусственного кровообращения и хранения крови, таких как катетеры, аппараты для диализа крови, шприцы и пробирки для отбора крови, системы кровообращения и стенты. Кроме того, соединения могут содержать детектируемую метку и быть использованы для получения изображения тромбов in vivo.Международная заявка была опубликована вместе с отчетом о международном поиске.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8898998P | 1998-06-11 | 1998-06-11 | |
| PCT/US1999/013228 WO1999064446A1 (en) | 1998-06-11 | 1999-06-11 | Pyrazinone protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200100025A1 true EA200100025A1 (ru) | 2001-06-25 |
| EA004884B1 EA004884B1 (ru) | 2004-08-26 |
Family
ID=22214697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200100025A EA004884B1 (ru) | 1998-06-11 | 1999-06-11 | Соединения пиразинона, фармацевтическая композиция (варианты) и лекарственная форма, способ ингибирования сериновой протеазы, способ снижения тромбообразующей способности поверхности, способ лечения нарушенного протеолиза и тромбоза, связанного с различными заболеваниями, способ снижения свертывания крови у млекопитающего |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US6204263B1 (ru) |
| EP (2) | EP1086122B1 (ru) |
| JP (1) | JP4554077B2 (ru) |
| KR (1) | KR100669953B1 (ru) |
| CN (2) | CN1769274A (ru) |
| AT (2) | ATE302794T1 (ru) |
| AU (1) | AU759427B2 (ru) |
| BR (1) | BR9911100A (ru) |
| CA (1) | CA2334679C (ru) |
| DE (2) | DE69942159D1 (ru) |
| DK (1) | DK1086122T3 (ru) |
| EA (1) | EA004884B1 (ru) |
| ES (2) | ES2343120T3 (ru) |
| HU (1) | HUP0103283A3 (ru) |
| IL (1) | IL139867A0 (ru) |
| NO (1) | NO20006300L (ru) |
| NZ (1) | NZ508669A (ru) |
| PL (1) | PL344749A1 (ru) |
| SI (1) | SI1086122T1 (ru) |
| WO (1) | WO1999064446A1 (ru) |
| ZA (1) | ZA200007306B (ru) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001524467A (ja) | 1997-11-26 | 2001-12-04 | ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド | ヘテロアリールアミノグアニジンおよびアルコキシグアニジンおよびプロテアーゼインヒビターとしてのこれらの使用 |
| US6716838B1 (en) | 1999-05-19 | 2004-04-06 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents |
| US6750342B1 (en) | 1999-05-19 | 2004-06-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade |
| US6664255B1 (en) | 1999-05-19 | 2003-12-16 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| US6653316B1 (en) | 1999-05-19 | 2003-11-25 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade |
| US7015230B1 (en) | 1999-05-19 | 2006-03-21 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade |
| CN1351595A (zh) * | 1999-05-19 | 2002-05-29 | 法玛西雅公司 | 可用于选择性抑制凝血级联的取代的多环芳基与杂芳基吡嗪酮 |
| EP1586565A1 (en) * | 1999-05-19 | 2005-10-19 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| US6867217B1 (en) | 1999-05-19 | 2005-03-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade |
| US6458952B1 (en) | 1999-05-19 | 2002-10-01 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade |
| US6660885B2 (en) | 2000-03-13 | 2003-12-09 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade |
| AU2001249870A1 (en) | 2000-04-05 | 2001-10-23 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade |
| US6693121B2 (en) | 2000-04-05 | 2004-02-17 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade |
| WO2001079155A2 (en) | 2000-04-17 | 2001-10-25 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade |
| MXPA03000512A (es) * | 2000-07-17 | 2003-10-06 | Dimensional Pharm Inc | Oxiguanidina-pirazinonas ciclicas como inhibidores de proteasas. |
| US7119094B1 (en) | 2000-11-20 | 2006-10-10 | Warner-Lambert Company | Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade |
| WO2002042272A2 (en) | 2000-11-20 | 2002-05-30 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade |
| US7015223B1 (en) | 2000-11-20 | 2006-03-21 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade |
| MXPA04003163A (es) | 2001-10-03 | 2004-07-08 | Pharmacia Corp | Compuestos heterociclicos de 6 elementos utiles para inhibicion selectiva de la casdada de coagulacion. |
| WO2003093242A2 (en) | 2001-10-03 | 2003-11-13 | Pharmacia Corporation | Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade |
| WO2003048127A1 (en) | 2001-12-04 | 2003-06-12 | Corvas International, Inc. | Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation |
| PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
| JP2005213213A (ja) * | 2004-01-30 | 2005-08-11 | Fuji Oil Co Ltd | 大豆トリプシンインヒビター濃縮物の製造法 |
| US20050281800A1 (en) | 2004-06-16 | 2005-12-22 | Glen Gong | Targeting sites of damaged lung tissue |
| US7678767B2 (en) | 2004-06-16 | 2010-03-16 | Pneumrx, Inc. | Glue compositions for lung volume reduction |
| US7766938B2 (en) | 2004-07-08 | 2010-08-03 | Pneumrx, Inc. | Pleural effusion treatment device, method and material |
| US8070678B2 (en) * | 2005-10-05 | 2011-12-06 | Gurbel Paul A | Detection of restenosis risk in patients receiving a stent by measuring the characteristics of blood clotting including the measurement of maximum thrombin-induced clot strength |
| US8815804B2 (en) | 2006-02-06 | 2014-08-26 | Sanford-Burnham Medical Research Institute | Methods and compositions related to targeting tumors and wounds |
| US20070269512A1 (en) * | 2006-05-22 | 2007-11-22 | Wang Wenhua W | Gastroretentive sustained release formulations |
| WO2007146553A2 (en) * | 2006-05-22 | 2007-12-21 | Janssen Pharmaceutica, N.V. | N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2h)-pyrazineacetamide |
| US9101671B2 (en) | 2007-01-03 | 2015-08-11 | Sanford-Burnham Medical Research Institute | Methods and compositions related to clot binding compounds |
| JP5244477B2 (ja) * | 2008-07-08 | 2013-07-24 | 関東化学株式会社 | ガドリニウムの影響を回避したカルシウムの測定試薬 |
| US20110081293A1 (en) | 2009-10-07 | 2011-04-07 | Sanford-Burnham Medical Research Institute | Methods and compositions related to clot-binding lipid compounds |
| WO2011049964A1 (en) | 2009-10-19 | 2011-04-28 | Lab Scientific Group | Rna detection and quantitation |
| US8912136B2 (en) | 2009-12-18 | 2014-12-16 | Sanford-Burnham Medical Research Institute | Methods and compositions related to clot-binding compounds |
| JP6184101B2 (ja) | 2009-12-23 | 2017-08-23 | サンフォード−バーナム メディカル リサーチ インスティテュート | アネキシン１結合化合物に関する方法および組成物 |
| JP2013525285A (ja) | 2010-04-08 | 2013-06-20 | サンフォード−バーナム メディカル リサーチ インスティテュート | 化合物の送達を増強するための方法および組成物 |
| CN104857005B (zh) | 2010-12-31 | 2019-04-26 | 阿斯利康公司 | 精氨酸酶抑制剂及其使用方法 |
| US9788539B2 (en) | 2011-05-17 | 2017-10-17 | Velico Medical, Inc. | Platelet protection solution having beta-galactosidase and sialidase inhibitors |
| EP2709446A2 (en) | 2011-05-17 | 2014-03-26 | Velico Medical, Inc. | Platelet storage using a sialidase inhibitor |
| US20130156803A1 (en) | 2011-06-04 | 2013-06-20 | Rochester General Hospital Research Institute | Compositions and methods related to p6 |
| WO2014055988A1 (en) | 2012-10-05 | 2014-04-10 | Velico Medical, Inc. | Platelet additive solution having a beta-galactosidase inhibitor |
| WO2014120886A1 (en) | 2013-01-30 | 2014-08-07 | Velico Medical, Inc. | Platelet additive solution having a self-assembling hydrogel-forming peptide |
| DK2968316T3 (da) | 2013-03-13 | 2019-10-07 | Forma Therapeutics Inc | 2-hydroxy-1-{4-[(4-phenylphenyl)carbonyl]piperazin-1-yl}ethan-1-on-derivater og relaterede forbindelser som fedtsyresyntase (fasn)-inhibitorer til behandlingen af cancer |
| CN106379607A (zh) * | 2016-10-08 | 2017-02-08 | 周末 | 一种瓶身机械印模制药装置 |
| AU2019285559A1 (en) * | 2018-06-13 | 2020-12-10 | Scentian Bio Limited | Biosensor device and methods |
| TWI767148B (zh) | 2018-10-10 | 2022-06-11 | 美商弗瑪治療公司 | 抑制脂肪酸合成酶(fasn) |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4418052A (en) | 1980-08-12 | 1983-11-29 | Wong Dennis W | Diagnostic compositions and method for radiologic imaging of fibrinogen deposition in the body |
| US4980148A (en) | 1985-02-06 | 1990-12-25 | Mallinckrodt, Inc. | Methods for enhancing magnetic resonance imaging |
| US5011686A (en) | 1987-09-21 | 1991-04-30 | Creative Biomolecules, Inc. | Thrombus specific conjugates |
| ZA897514B (en) | 1988-10-07 | 1990-06-27 | Merrell Dow Pharma | Novel peptidase inhibitors |
| US5024829A (en) | 1988-11-21 | 1991-06-18 | Centocor, Inc. | Method of imaging coronary thrombi |
| US5122361A (en) | 1989-04-17 | 1992-06-16 | Trustees Of The University Of Pennsylvania | Dopamine receptor ligands and imaging agents |
| EP0604022A1 (en) | 1992-12-22 | 1994-06-29 | Advanced Cardiovascular Systems, Inc. | Multilayered biodegradable stent and method for its manufacture |
| US5656600A (en) | 1993-03-25 | 1997-08-12 | Corvas International, Inc. | α-ketoamide derivatives as inhibitors of thrombosis |
| GB9318637D0 (en) | 1993-09-08 | 1993-10-27 | Ferring Res Ltd | Enzyme inhibitors |
| US6087479A (en) | 1993-09-17 | 2000-07-11 | Nitromed, Inc. | Localized use of nitric oxide-adducts to prevent internal tissue damage |
| US5466811A (en) | 1994-07-18 | 1995-11-14 | Merck & Co., Inc. | Dioxolenylmethyl carbamates pro moieties for amine drugs |
| EP0761251B1 (en) | 1994-10-17 | 2004-12-29 | Kabushikikaisha Igaki Iryo Sekkei | Drug-releasing stent |
| US5643580A (en) | 1994-10-17 | 1997-07-01 | Surface Genesis, Inc. | Biocompatible coating, medical device using the same and methods |
| US5637113A (en) | 1994-12-13 | 1997-06-10 | Advanced Cardiovascular Systems, Inc. | Polymer film for wrapping a stent structure |
| US6011158A (en) * | 1994-12-13 | 2000-01-04 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| MX9704439A (es) * | 1994-12-13 | 1997-10-31 | Corvas Int Inc | Derivados heterociclicos aromaticos como inhibidores de enzima. |
| DE19514104C2 (de) | 1995-04-13 | 1997-05-28 | Behringwerke Ag | Beschichtung für in den Blutstrom oder in das Gewebe des menschlichen Körpers einbringbares Biomaterial |
| AU703744B2 (en) * | 1995-06-27 | 1999-04-01 | Merck & Co., Inc. | Pyridinone-thrombin inhibitors |
| DE69625505T2 (de) | 1995-09-29 | 2003-11-13 | Dimensional Pharm Inc | Guanidino proteiase inhibitoren |
| AU720616B2 (en) | 1996-02-22 | 2000-06-08 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
| US5891909A (en) | 1996-03-29 | 1999-04-06 | 3-Dimensional Pharmaceuticals, Inc. | Amidinohydrazones as protease inhibitors |
| WO1997040024A1 (en) * | 1996-04-23 | 1997-10-30 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
| EP0934305A4 (en) * | 1996-08-29 | 2001-04-11 | Merck & Co Inc | INTEGRINE ANTAGONISTS |
| KR20000068354A (ko) * | 1996-09-06 | 2000-11-25 | 다께다 가즈히꼬 | 신규 아세트아미드 유도체 및 프로테아제 저해제 |
| AU4172397A (en) | 1996-09-06 | 1998-03-26 | Biochem Pharma Inc. | Lactam inhibitors of thrombin |
| TW499412B (en) * | 1996-11-26 | 2002-08-21 | Dimensional Pharm Inc | Aminoguanidines and alkoxyguanidines as protease inhibitors |
| JP2001514227A (ja) | 1997-09-05 | 2001-09-11 | メルク エンド カムパニー インコーポレーテッド | ピラジノン系トロンビン阻害薬 |
| JP2001524467A (ja) * | 1997-11-26 | 2001-12-04 | ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド | ヘテロアリールアミノグアニジンおよびアルコキシグアニジンおよびプロテアーゼインヒビターとしてのこれらの使用 |
| WO2002009711A1 (en) * | 2000-07-28 | 2002-02-07 | Merck & Co., Inc. | Thrombin inhibitors |
-
1999
- 1999-06-11 AU AU45618/99A patent/AU759427B2/en not_active Ceased
- 1999-06-11 AT AT99928582T patent/ATE302794T1/de not_active IP Right Cessation
- 1999-06-11 DE DE69942159T patent/DE69942159D1/de not_active Expired - Lifetime
- 1999-06-11 BR BR9911100-4A patent/BR9911100A/pt not_active Application Discontinuation
- 1999-06-11 HU HU0103283A patent/HUP0103283A3/hu unknown
- 1999-06-11 CA CA2334679A patent/CA2334679C/en not_active Expired - Fee Related
- 1999-06-11 EP EP99928582A patent/EP1086122B1/en not_active Expired - Lifetime
- 1999-06-11 JP JP2000553454A patent/JP4554077B2/ja not_active Expired - Fee Related
- 1999-06-11 EP EP05007726A patent/EP1589029B1/en not_active Expired - Lifetime
- 1999-06-11 DK DK99928582T patent/DK1086122T3/da active
- 1999-06-11 EA EA200100025A patent/EA004884B1/ru not_active IP Right Cessation
- 1999-06-11 DE DE69926884T patent/DE69926884T2/de not_active Expired - Lifetime
- 1999-06-11 ES ES05007726T patent/ES2343120T3/es not_active Expired - Lifetime
- 1999-06-11 PL PL99344749A patent/PL344749A1/xx not_active Application Discontinuation
- 1999-06-11 IL IL13986799A patent/IL139867A0/xx unknown
- 1999-06-11 NZ NZ508669A patent/NZ508669A/xx unknown
- 1999-06-11 CN CNA2005100939896A patent/CN1769274A/zh active Pending
- 1999-06-11 CN CNB998072753A patent/CN1224629C/zh not_active Expired - Fee Related
- 1999-06-11 US US09/330,128 patent/US6204263B1/en not_active Expired - Lifetime
- 1999-06-11 KR KR1020007014068A patent/KR100669953B1/ko not_active IP Right Cessation
- 1999-06-11 SI SI9930839T patent/SI1086122T1/sl unknown
- 1999-06-11 AT AT05007726T patent/ATE461210T1/de not_active IP Right Cessation
- 1999-06-11 WO PCT/US1999/013228 patent/WO1999064446A1/en not_active Application Discontinuation
- 1999-06-11 ES ES99928582T patent/ES2249012T3/es not_active Expired - Lifetime
-
2000
- 2000-12-08 ZA ZA200007306A patent/ZA200007306B/xx unknown
- 2000-12-11 NO NO20006300A patent/NO20006300L/no unknown
-
2001
- 2001-02-02 US US09/773,730 patent/US6514978B2/en not_active Expired - Lifetime
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA200100025A1 (ru) | Соединения пиразинона, фармацевтическая композиция (варианты) и лекарственная форма, способ ингибирования протеазы, способ снижения тромбообразующей способности поверхности, способ лечения нарушенного протеолиза и тромбоза, связанного с различными заболеваниями, способ снижения свертывания крови и способ определения тромбина у млекопитающего | |
| EA199900544A1 (ru) | Аминогуанидины и алкоксигуанидины в качестве ингибиторов протеаз (варианты), способ их получения (варианты), фармацевтическая композиция, способ лечения с ее использованием, способ ингибирования протеолиза у млекопитающих, способ ингибирования тромбин-индуцированной агрегации тромбоцитов и образования сгустков фибриногена в плазме, способ ингибирования тромбина, образования агрегации тромбоцитов и тромбов в крови, устройство для сбора, циркуляции и хранения крови | |
| EA200000578A1 (ru) | Гетероарильные производные аминогуанидинов и алкоксигуанидинов (варианты), способ их получения, способ и фармацевтическая композиция для ингибирования протеолиза у млекопитающих, способ лечения панкреатита, тромбоза, ишемии, инсульта, рестеноза, эмфиземы или воспалительного процесса у млекопитающих, способ ингибирования индуцированной тромбином агрегации тромбоцитов и свертывания фибриногена в плазме, способ ингибирования тромбина в крови, способ ингибирования агрегации | |
| ZA200303091B (en) | Aminopyridinyl-, aminoguanidinyl- and alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors. | |
| EA200001024A1 (ru) | Производные аминогуанидина и алкоксигуанидина и способ их получения (варианты), фармацевтическая композиция и способ ингибирования протеолиза у млекопитающего, способ лечения различных заболеваний млекопитающего, способы ингибирования индуцированной тромбином агрегации тромбоцитов и свертывания фибриногена в плазме, тромбина, агрегации тромбоцитов и образования тромбов в крови, устройство для сбора крови, искусственного кровообращения и хранения крови | |
| US5077281A (en) | Novel use of taurolin | |
| Kumada et al. | Comparative study on heparin and a synthetic thrombin inhibitor No. 805 (MD-805) in experimental antithrombin III-deficient animals | |
| TR199902692T2 (xx) | Serin proteaz inhibit�rleri. | |
| Sharrock et al. | Comparison of extradural and general anaesthesia on the fibrinolytic response to total knee arthroplasty | |
| RU2125450C1 (ru) | Применение 2-фенил-3-ароилбензотиофенов для увеличения экспрессии тромбомодулина | |
| JPS61112018A (ja) | 線溶増強剤 | |
| ATE250056T1 (de) | Heteroaryl protease inhibitoren und diagnostische bilderzeugungsmittel | |
| WO2002006248A3 (en) | Cyclic oxyguanidine pyrazinones as protease inhibitors | |
| TW200508200A (en) | Substituted phenyl acetamides and their use as protease inhibitors | |
| MXPA03000963A (es) | Inhibidores de oxiguanidina ciclica proteasa. | |
| Arnljots et al. | Antithrombotic and platelet activating effects of heparin in prevention of microarterial thrombosis |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): BY RU |