BR9911100A - Inibidores de pirazinona protease - Google Patents
Inibidores de pirazinona proteaseInfo
- Publication number
- BR9911100A BR9911100A BR9911100-4A BR9911100A BR9911100A BR 9911100 A BR9911100 A BR 9911100A BR 9911100 A BR9911100 A BR 9911100A BR 9911100 A BR9911100 A BR 9911100A
- Authority
- BR
- Brazil
- Prior art keywords
- blood
- compounds
- inhibiting
- formation
- thrombi
- Prior art date
Links
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 title abstract 2
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title abstract 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title abstract 2
- 210000004369 blood Anatomy 0.000 abstract 6
- 239000008280 blood Substances 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- 230000002401 inhibitory effect Effects 0.000 abstract 5
- 230000015572 biosynthetic process Effects 0.000 abstract 4
- 108090000190 Thrombin Proteins 0.000 abstract 2
- 210000001772 blood platelet Anatomy 0.000 abstract 2
- 239000000463 material Substances 0.000 abstract 2
- 229960004072 thrombin Drugs 0.000 abstract 2
- 108090000317 Chymotrypsin Proteins 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
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 108090000631 Trypsin Proteins 0.000 abstract 1
- 102000004142 Trypsin Human genes 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
- 230000017531 blood circulation Effects 0.000 abstract 1
- 229960002376 chymotrypsin Drugs 0.000 abstract 1
- 238000000502 dialysis Methods 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
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229940012957 plasmin Drugs 0.000 abstract 1
- 230000003389 potentiating effect Effects 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
- 238000012800 visualization Methods 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
''INIBIDORES DE PIRAZINONA PROTEASE'' São descritos compostos de pirazinona, incluindo compostos da fórmula (I), em que X é 0, NR^ 11^ ou CH=N, R^ 3^-R^ 11^, R^ a^, R^ b^, R^ c^, W, m e n são apresentados na especificação, assim como hidratos, solvatos ou sais seus aceitáveis do ponto de vista farmacêutico. Os compostos da invenção são inibidores potentes de proteases, especialmente das proteases de serina semelhante a tripsina, tais como quimotripsina, tripsina, trombina, plasmina e fator Xa. Determinados compostos apresentam atividade antitrombótica através da inibição direta e seletiva de trombina. São descritas as composições para a inibição de perda de plaquetas sang³íneas, inibição de formação de agregados de plaquetas sang³íneas, inibição de formação de fibrina, inibição de formação de trombos, e inibição de formação de êmbolos. Outros empregos dos compostos da invenção são como anti-coagulantes quer embutidos nos materiais empregados na fabricação de dispositivos empregados na coleta de sangue, circulação de sangue e armazenagem de sangue, tais como cateteres, máquinas de diálise sang³íneas, seringas e tubos para a coleta de sangue, tubulações para sangue e stents quer fisicamente ligados a tais materiais. Além disso os compostos podem ser rotulados de modo a serem detectáveis e empregados para a visualização dos trombos in vivo.
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 (1)
| Publication Number | Publication Date |
|---|---|
| BR9911100A true BR9911100A (pt) | 2001-02-13 |
Family
ID=22214697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9911100-4A BR9911100A (pt) | 1998-06-11 | 1999-06-11 | Inibidores de pirazinona protease |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US6204263B1 (pt) |
| EP (2) | EP1589029B1 (pt) |
| JP (1) | JP4554077B2 (pt) |
| KR (1) | KR100669953B1 (pt) |
| CN (2) | CN1769274A (pt) |
| AT (2) | ATE302794T1 (pt) |
| AU (1) | AU759427B2 (pt) |
| BR (1) | BR9911100A (pt) |
| CA (1) | CA2334679C (pt) |
| DE (2) | DE69926884T2 (pt) |
| DK (1) | DK1086122T3 (pt) |
| EA (1) | EA004884B1 (pt) |
| ES (2) | ES2249012T3 (pt) |
| HU (1) | HUP0103283A3 (pt) |
| IL (1) | IL139867A0 (pt) |
| NO (1) | NO20006300L (pt) |
| NZ (1) | NZ508669A (pt) |
| PL (1) | PL344749A1 (pt) |
| SI (1) | SI1086122T1 (pt) |
| WO (1) | WO1999064446A1 (pt) |
| ZA (1) | ZA200007306B (pt) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI222441B (en) * | 1997-11-26 | 2004-10-21 | Dimensional Pharm Inc | Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
| US6750342B1 (en) | 1999-05-19 | 2004-06-15 | 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 |
| US6653316B1 (en) | 1999-05-19 | 2003-11-25 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones 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 |
| US6716838B1 (en) | 1999-05-19 | 2004-04-06 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents |
| US6867217B1 (en) | 1999-05-19 | 2005-03-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade |
| EP1586565A1 (en) * | 1999-05-19 | 2005-10-19 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrazinones 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 |
| IL146245A0 (en) * | 1999-05-19 | 2002-07-25 | Pharmacia Corp | Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade |
| WO2001068605A1 (en) | 2000-03-13 | 2001-09-20 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade |
| EP1268428A2 (en) | 2000-04-05 | 2003-01-02 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade |
| ATE289299T1 (de) | 2000-04-05 | 2005-03-15 | Pharmacia Corp | Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess |
| JP2004501077A (ja) | 2000-04-17 | 2004-01-15 | ファルマシア・コーポレーション | 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換１，４−キノン |
| CA2415932A1 (en) * | 2000-07-17 | 2002-01-24 | 3-Dimensional Pharmaceuticals, Inc. | Cyclic oxyguanidine pyrazinones as protease inhibitors |
| EP1351686A2 (en) | 2000-11-20 | 2003-10-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade |
| 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 |
| 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 |
| US7262211B2 (en) | 2001-12-04 | 2007-08-28 | Dendreon Corporation | Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation |
| AU2003302238A1 (en) | 2002-12-03 | 2004-06-23 | Axys Pharmaceuticals, Inc. | 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors |
| 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 |
| US7468350B2 (en) | 2004-06-16 | 2008-12-23 | Pneumrx, Inc. | Glue composition for lung volume reduction |
| US7678767B2 (en) | 2004-06-16 | 2010-03-16 | Pneumrx, Inc. | Glue compositions for lung volume reduction |
| US7608579B2 (en) | 2004-06-16 | 2009-10-27 | Pneumrx, Inc. | Lung volume reduction using glue compositions |
| US7553810B2 (en) | 2004-06-16 | 2009-06-30 | Pneumrx, Inc. | Lung volume reduction using glue composition |
| US7766938B2 (en) | 2004-07-08 | 2010-08-03 | Pneumrx, Inc. | Pleural effusion treatment device, method and material |
| WO2007044278A2 (en) * | 2005-10-05 | 2007-04-19 | Gurbel Paul A | The detection of restenosis risk in patients receiving a stent |
| JP5872751B2 (ja) | 2006-02-06 | 2016-03-01 | バーナム インスティテュート フォー メディカル リサーチ | 腫瘍および損傷のターゲティングに関する方法および組成物 |
| US20080021044A1 (en) * | 2006-05-22 | 2008-01-24 | Patel Mitul N | N-[2-[[(diaminomethylene)amino]oxy]ethyl]-3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxo-1(2h)-pyrazineacetamide |
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| RU2365380C1 (ru) * | 2008-05-20 | 2009-08-27 | Дмитрий Павлович Столяров | Способ лечения острого инфаркта миокарда |
| 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 |
| WO2011075725A1 (en) | 2009-12-18 | 2011-06-23 | Sanford-Burnham Medical Research Institute | Methods and compositions related to clot-binding compounds |
| SG10201704812TA (en) | 2009-12-23 | 2017-07-28 | Sanford-Burnham Medical Res Inst | Methods and compositions related to annexin 1-binding compounds |
| WO2011127405A1 (en) | 2010-04-08 | 2011-10-13 | Sanford-Burnham Medical Research Institute | Methods and compositions for enhanced delivery of compounds |
| CA2824599C (en) * | 2010-12-31 | 2020-03-10 | Astrazeneca Uk Limited | Arginase inhibitors and methods of use thereof |
| US9788539B2 (en) | 2011-05-17 | 2017-10-17 | Velico Medical, Inc. | Platelet protection solution having beta-galactosidase and sialidase inhibitors |
| JP2014515352A (ja) | 2011-05-17 | 2014-06-30 | ベリコ メディカル インコーポレイティッド | シアリダーゼ阻害剤を用いた血小板の保存の改善法 |
| US20130156803A1 (en) | 2011-06-04 | 2013-06-20 | Rochester General Hospital Research Institute | Compositions and methods related to p6 |
| EP2903430A1 (en) | 2012-10-05 | 2015-08-12 | 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 |
| SG10201707409PA (en) | 2013-03-13 | 2017-10-30 | Forma Therapeutics Inc | Novel compounds and compositions for inhibition of fasn |
| CN106379607A (zh) * | 2016-10-08 | 2017-02-08 | 周末 | 一种瓶身机械印模制药装置 |
| EP3807627A4 (en) * | 2018-06-13 | 2022-11-09 | The New Zealand Institute for Plant and Food Research Limited | BIOSENSOR DEVICE AND METHOD |
| 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 |
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| US4418052A (en) | 1980-08-12 | 1983-11-29 | Wong Dennis W | Diagnostic compositions and method for radiologic imaging of fibrinogen deposition in the body |
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| WO1998008840A1 (en) * | 1996-08-29 | 1998-03-05 | Merck & Co., Inc. | Integrin antagonists |
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| BR9712000A (pt) * | 1996-09-06 | 1999-08-24 | Nippon Kayaku Kk | Derivados de acetamida sais dos mesmos composi-Æo farmac-utica inibidores de protease de quimase de desgranula-Æo de mastÄcitos ou de libera-Æo de histamina de mastÄcitos e de ativa-Æo de eosinÄfilo ou de libera-Æo de oxig-nio ativo de eosinÄfilo e processo para produzir os dervados de acetamida |
| 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 |
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| AU2001278997A1 (en) * | 2000-07-28 | 2002-02-13 | Merck And Co., Inc. | Thrombin inhibitors |
-
1999
- 1999-06-11 JP JP2000553454A patent/JP4554077B2/ja not_active Expired - Fee Related
- 1999-06-11 US US09/330,128 patent/US6204263B1/en not_active Expired - Lifetime
- 1999-06-11 ES ES99928582T patent/ES2249012T3/es not_active Expired - Lifetime
- 1999-06-11 EA EA200100025A patent/EA004884B1/ru not_active IP Right Cessation
- 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 AT AT99928582T patent/ATE302794T1/de not_active IP Right Cessation
- 1999-06-11 AT AT05007726T patent/ATE461210T1/de not_active IP Right Cessation
- 1999-06-11 BR BR9911100-4A patent/BR9911100A/pt not_active Application Discontinuation
- 1999-06-11 CN CNA2005100939896A patent/CN1769274A/zh active Pending
- 1999-06-11 DK DK99928582T patent/DK1086122T3/da active
- 1999-06-11 PL PL99344749A patent/PL344749A1/xx not_active Application Discontinuation
- 1999-06-11 WO PCT/US1999/013228 patent/WO1999064446A1/en not_active Ceased
- 1999-06-11 EP EP05007726A patent/EP1589029B1/en not_active Expired - Lifetime
- 1999-06-11 ES ES05007726T patent/ES2343120T3/es not_active Expired - Lifetime
- 1999-06-11 SI SI9930839T patent/SI1086122T1/sl unknown
- 1999-06-11 IL IL13986799A patent/IL139867A0/xx unknown
- 1999-06-11 DE DE69926884T patent/DE69926884T2/de not_active Expired - Lifetime
- 1999-06-11 DE DE69942159T patent/DE69942159D1/de not_active Expired - Lifetime
- 1999-06-11 CN CNB998072753A patent/CN1224629C/zh not_active Expired - Fee Related
- 1999-06-11 KR KR1020007014068A patent/KR100669953B1/ko not_active Expired - Fee Related
- 1999-06-11 NZ NZ508669A patent/NZ508669A/xx unknown
- 1999-06-11 AU AU45618/99A patent/AU759427B2/en not_active Ceased
- 1999-06-11 EP EP99928582A patent/EP1086122B1/en 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
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