DE69926884D1 - Pyrazine protease inhibitore - Google Patents
Pyrazine protease inhibitoreInfo
- Publication number
- DE69926884D1 DE69926884D1 DE69926884T DE69926884T DE69926884D1 DE 69926884 D1 DE69926884 D1 DE 69926884D1 DE 69926884 T DE69926884 T DE 69926884T DE 69926884 T DE69926884 T DE 69926884T DE 69926884 D1 DE69926884 D1 DE 69926884D1
- Authority
- DE
- Germany
- Prior art keywords
- blood
- inhibiting
- compounds
- formation
- thrombin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title abstract 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title abstract 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 2
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 title 1
- 210000004369 blood Anatomy 0.000 abstract 5
- 239000008280 blood Substances 0.000 abstract 5
- 230000002401 inhibitory effect Effects 0.000 abstract 5
- 230000015572 biosynthetic process Effects 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 108090000190 Thrombin Proteins 0.000 abstract 2
- 210000001772 blood platelet Anatomy 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 229960004072 thrombin Drugs 0.000 abstract 2
- HUTNOYOBQPAKIA-UHFFFAOYSA-N 1h-pyrazin-2-one Chemical compound OC1=CN=CC=N1 HUTNOYOBQPAKIA-UHFFFAOYSA-N 0.000 abstract 1
- 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
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 208000007536 Thrombosis Diseases 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
- 238000011503 in vivo imaging Methods 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 238000000034 method 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Hematology (AREA)
- Public Health (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (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)
- Peptides Or Proteins (AREA)
- Investigating Or Analysing Biological Materials (AREA)
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 |
|---|---|
| DE69926884D1 true DE69926884D1 (de) | 2005-09-29 |
| DE69926884T2 DE69926884T2 (de) | 2006-06-14 |
Family
ID=22214697
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69942159T Expired - Lifetime DE69942159D1 (de) | 1998-06-11 | 1999-06-11 | Pyrazine Protease Inhibitore |
| DE69926884T Expired - Lifetime DE69926884T2 (de) | 1998-06-11 | 1999-06-11 | Pyrazine protease inhibitore |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69942159T Expired - Lifetime DE69942159D1 (de) | 1998-06-11 | 1999-06-11 | Pyrazine Protease Inhibitore |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US6204263B1 (de) |
| EP (2) | EP1589029B1 (de) |
| JP (1) | JP4554077B2 (de) |
| KR (1) | KR100669953B1 (de) |
| CN (2) | CN1769274A (de) |
| AT (2) | ATE461210T1 (de) |
| AU (1) | AU759427B2 (de) |
| BR (1) | BR9911100A (de) |
| CA (1) | CA2334679C (de) |
| DE (2) | DE69942159D1 (de) |
| DK (1) | DK1086122T3 (de) |
| EA (1) | EA004884B1 (de) |
| ES (2) | ES2343120T3 (de) |
| HU (1) | HUP0103283A3 (de) |
| IL (1) | IL139867A0 (de) |
| NO (1) | NO20006300L (de) |
| NZ (1) | NZ508669A (de) |
| PL (1) | PL344749A1 (de) |
| SI (1) | SI1086122T1 (de) |
| WO (1) | WO1999064446A1 (de) |
| ZA (1) | ZA200007306B (de) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE344246T1 (de) * | 1997-11-26 | 2006-11-15 | Ortho Mcneil Pharm Inc | Heteroaryl aminoguanidin- und alkoxyguanidinderivate und ihre verwendung als proteasehemmer |
| 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 |
| EP1586565A1 (de) * | 1999-05-19 | 2005-10-19 | Pharmacia Corporation | Substituierte polycyclische aryl und heteroarylpyrazinone zur selektiven Hemmung von der Blutgerinnungskaskade |
| US7015230B1 (en) | 1999-05-19 | 2006-03-21 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl uracils 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 |
| US6867217B1 (en) | 1999-05-19 | 2005-03-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridones 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 |
| US6750342B1 (en) | 1999-05-19 | 2004-06-15 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyrimidinones 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 |
| WO2001077097A2 (en) | 2000-04-05 | 2001-10-18 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade |
| CA2405306A1 (en) | 2000-04-05 | 2001-10-18 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade |
| US6686484B2 (en) | 2000-04-17 | 2004-02-03 | Pharmacia Corporation | Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade |
| CA2415932A1 (en) * | 2000-07-17 | 2002-01-24 | 3-Dimensional Pharmaceuticals, Inc. | Cyclic oxyguanidine pyrazinones as protease inhibitors |
| 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 |
| CA2430037A1 (en) | 2000-11-20 | 2002-05-30 | Michael S. South | 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 |
| BR0213092A (pt) | 2001-10-03 | 2004-10-19 | Pharmacia Corp | Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação |
| US7105559B2 (en) | 2001-10-03 | 2006-09-12 | 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 |
| DK1569912T3 (en) | 2002-12-03 | 2015-06-29 | Pharmacyclics 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 |
| US7553810B2 (en) | 2004-06-16 | 2009-06-30 | Pneumrx, Inc. | Lung volume reduction using glue composition |
| 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 |
| CA2570261C (en) | 2004-07-08 | 2014-06-10 | 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 |
| CA2638911C (en) | 2006-02-06 | 2018-01-23 | Burnham Institute For Medical Research | Methods and compositions related to targeting tumors and wounds |
| 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 |
| US20070269512A1 (en) * | 2006-05-22 | 2007-11-22 | Wang Wenhua W | Gastroretentive sustained release formulations |
| CA2674378A1 (en) | 2007-01-03 | 2008-07-17 | Burnham Institute For Medical Research | Methods and compositions related to clot binding compounds |
| 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 |
| EP2512497A1 (de) | 2009-12-18 | 2012-10-24 | Sanford-Burnham Medical Research Institute | Verfahren und zusammensetzungen im zusammenhang mit gerinnselbindenden verbndungen |
| US9610359B2 (en) | 2009-12-23 | 2017-04-04 | Burnham Institute For Medical Research | 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 |
| 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 |
| CA2835434A1 (en) | 2011-05-17 | 2012-11-22 | Velico Medical, Inc. | Improved platelet storage using a sialidase inhibitor |
| US9788539B2 (en) | 2011-05-17 | 2017-10-17 | Velico Medical, Inc. | Platelet protection solution having beta-galactosidase and sialidase inhibitors |
| CA2838188C (en) | 2011-06-04 | 2017-04-18 | Rochester General Hospital Research Institute | Compositions and methods related to p6 of haemophilus influenzae |
| CA2887083A1 (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 |
| MX364895B (es) | 2013-03-13 | 2019-05-10 | Forma Therapeutics Inc | Nuevos compuestos y composiciones para la inhibicion de fasn. |
| CN106379607A (zh) * | 2016-10-08 | 2017-02-08 | 周末 | 一种瓶身机械印模制药装置 |
| US20210255184A1 (en) * | 2018-06-13 | 2021-08-19 | The New Zealand Institute For Plant And Food Research 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) |
| WO2020092395A1 (en) | 2018-10-29 | 2020-05-07 | Forma Therapeutics, Inc. | SOLID FORMS OF (4-(2-FLUORO-4-(1-METHYL-1 H-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 |
| US4980148A (en) | 1985-02-06 | 1990-12-25 | Mallinckrodt, Inc. | Methods for enhancing magnetic resonance imaging |
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| CA2263198A1 (en) * | 1996-09-06 | 1998-03-12 | Nippon Kayaku Kabushiki Kaisha | Novel acetamide derivatives and protease inhibitors |
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| 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 |
| ATE344246T1 (de) * | 1997-11-26 | 2006-11-15 | Ortho Mcneil Pharm Inc | Heteroaryl aminoguanidin- und alkoxyguanidinderivate und ihre verwendung als proteasehemmer |
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-
1999
- 1999-06-11 CN CNA2005100939896A patent/CN1769274A/zh active Pending
- 1999-06-11 DE DE69942159T patent/DE69942159D1/de not_active Expired - Lifetime
- 1999-06-11 ES ES05007726T patent/ES2343120T3/es not_active Expired - Lifetime
- 1999-06-11 IL IL13986799A patent/IL139867A0/xx unknown
- 1999-06-11 CA CA2334679A patent/CA2334679C/en not_active Expired - Fee Related
- 1999-06-11 DK DK99928582T patent/DK1086122T3/da active
- 1999-06-11 NZ NZ508669A patent/NZ508669A/xx unknown
- 1999-06-11 SI SI9930839T patent/SI1086122T1/sl unknown
- 1999-06-11 HU HU0103283A patent/HUP0103283A3/hu unknown
- 1999-06-11 WO PCT/US1999/013228 patent/WO1999064446A1/en not_active Ceased
- 1999-06-11 ES ES99928582T patent/ES2249012T3/es not_active Expired - Lifetime
- 1999-06-11 CN CNB998072753A patent/CN1224629C/zh not_active Expired - Fee Related
- 1999-06-11 DE DE69926884T patent/DE69926884T2/de not_active Expired - Lifetime
- 1999-06-11 JP JP2000553454A patent/JP4554077B2/ja not_active Expired - Fee Related
- 1999-06-11 EP EP05007726A patent/EP1589029B1/de not_active Expired - Lifetime
- 1999-06-11 BR BR9911100-4A patent/BR9911100A/pt not_active Application Discontinuation
- 1999-06-11 PL PL99344749A patent/PL344749A1/xx not_active Application Discontinuation
- 1999-06-11 EA EA200100025A patent/EA004884B1/ru not_active IP Right Cessation
- 1999-06-11 AT AT05007726T patent/ATE461210T1/de not_active IP Right Cessation
- 1999-06-11 AU AU45618/99A patent/AU759427B2/en not_active Ceased
- 1999-06-11 US US09/330,128 patent/US6204263B1/en not_active Expired - Lifetime
- 1999-06-11 KR KR1020007014068A patent/KR100669953B1/ko not_active Expired - Fee Related
- 1999-06-11 EP EP99928582A patent/EP1086122B1/de not_active Expired - Lifetime
- 1999-06-11 AT AT99928582T patent/ATE302794T1/de not_active IP Right Cessation
-
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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8327 | Change in the person/name/address of the patent owner |
Owner name: ORTHO-MCNEIL PHARMACEUTICAL, INC., RARITAN, N.J., |