ATE338030T1 - Amidine-inhibitoren der serine-proteasen - Google Patents
Amidine-inhibitoren der serine-proteasenInfo
- Publication number
- ATE338030T1 ATE338030T1 AT01968579T AT01968579T ATE338030T1 AT E338030 T1 ATE338030 T1 AT E338030T1 AT 01968579 T AT01968579 T AT 01968579T AT 01968579 T AT01968579 T AT 01968579T AT E338030 T1 ATE338030 T1 AT E338030T1
- Authority
- AT
- Austria
- Prior art keywords
- serine proteases
- inhibitors
- factor
- amidine
- compounds
- Prior art date
Links
- 108010022999 Serine Proteases Proteins 0.000 title abstract 2
- 102000012479 Serine Proteases Human genes 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001409 amidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 108010054265 Factor VIIa Proteins 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 108010088842 Fibrinolysin Proteins 0.000 abstract 1
- 108060005987 Kallikrein Proteins 0.000 abstract 1
- 102000001399 Kallikrein Human genes 0.000 abstract 1
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 108010000499 Thromboplastin Proteins 0.000 abstract 1
- 102000002262 Thromboplastin Human genes 0.000 abstract 1
- 108090000631 Trypsin Proteins 0.000 abstract 1
- 102000004142 Trypsin Human genes 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 229940012414 factor viia Drugs 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000014508 negative regulation of coagulation Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229940012957 plasmin Drugs 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
- 239000012588 trypsin Substances 0.000 abstract 1
- 229960001322 trypsin Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
- C07D207/48—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Detergent Compositions (AREA)
- Treating Waste Gases (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23167900P | 2000-09-11 | 2000-09-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE338030T1 true ATE338030T1 (de) | 2006-09-15 |
Family
ID=22870229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT01968579T ATE338030T1 (de) | 2000-09-11 | 2001-09-05 | Amidine-inhibitoren der serine-proteasen |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US6410733B1 (de) |
| EP (1) | EP1317429B1 (de) |
| JP (1) | JP2004509104A (de) |
| AT (1) | ATE338030T1 (de) |
| AU (1) | AU2001288819A1 (de) |
| CA (1) | CA2421548C (de) |
| DE (1) | DE60122750T2 (de) |
| WO (1) | WO2002022575A1 (de) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6291514B1 (en) * | 1998-02-09 | 2001-09-18 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors |
| AU2001288819A1 (en) * | 2000-09-11 | 2002-03-26 | Genentech, Inc. | Amidine inhibitors of serine proteases |
| US7105559B2 (en) | 2001-10-03 | 2006-09-12 | Pharmacia Corporation | Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade |
| US20030180804A1 (en) * | 2001-10-29 | 2003-09-25 | Corvas International, Inc | Solid phase synthesis of chemical libraries |
| US7138530B2 (en) * | 2002-05-28 | 2006-11-21 | 3-Dimensional Pharmaceuticals, Inc. | Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions |
| US7659305B2 (en) | 2002-10-31 | 2010-02-09 | Pfizer Inc. | Therapeutic proline derivatives |
| 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 |
| NZ543366A (en) | 2003-04-03 | 2008-11-28 | Merck Patent Gmbh | Carbonyl compounds |
| JP2007500221A (ja) * | 2003-05-20 | 2007-01-11 | ジェネンテック・インコーポレーテッド | 第ＶＩＩａ因子のベンゾフラン阻害剤 |
| NZ545805A (en) * | 2003-08-29 | 2009-12-24 | Ono Pharmaceutical Co | Compound capable of binding S1P receptor and pharmaceutical use thereof |
| US7550487B2 (en) | 2004-03-26 | 2009-06-23 | Hoffmann-La Roche Inc. | Pyrrolidine-3,4-dicarboxamide derivatives |
| EP1637141B1 (de) * | 2004-09-21 | 2011-11-16 | Trobio AB | Stabilisierte Protease Zusammensetzungen enthaltend eine Serinprotease, Morpholin-Derivate und reversible Serinprotease- Inhibitoren |
| WO2006073167A1 (ja) * | 2005-01-07 | 2006-07-13 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| AU2005336535B2 (en) * | 2005-09-22 | 2012-05-24 | Trobio Ab | Stabilized protease composition |
| CN102380100A (zh) * | 2005-09-22 | 2012-03-21 | 特罗比奥股份公司 | 稳定的蛋白酶组合物 |
| EP1951717A1 (de) * | 2005-11-16 | 2008-08-06 | F.Hoffmann-La Roche Ag | Neue pyrrolidinderivate als inhibitoren von koagulationsfaktor xa |
| WO2008115641A2 (en) * | 2007-02-15 | 2008-09-25 | Yale University | Modular nanoparticles for adaptable vaccines |
| US8236792B2 (en) * | 2008-05-23 | 2012-08-07 | Janssen Pharmaceutica Nv | Substituted pyrrolidine amides as modulators of the histamine H3 receptor |
| EP2520566A1 (de) * | 2011-05-06 | 2012-11-07 | Orion Corporation | Neue pharmazeutische Verbindungen |
| US9249239B2 (en) | 2013-07-17 | 2016-02-02 | Exxonmobil Chemical Patents Inc. | Metallocenes and catalyst compositions derived therefrom |
| ES2703344T3 (es) | 2013-07-17 | 2019-03-08 | Exxonmobil Chemical Patents Inc | Metalocenos y composiciones catalíticas derivadas de ellos |
| WO2015009473A1 (en) | 2013-07-17 | 2015-01-22 | Exxonmobil Chemical Patents Inc. | Cyclopropyl substituted metallocene catalysts |
| CN103396351B (zh) * | 2013-08-09 | 2015-10-21 | 山东大学 | 吡咯烷类Bcl-2蛋白小分子抑制剂化合物及其制备、药物组合物与制药用途 |
| CN111499562B (zh) * | 2013-12-27 | 2023-12-26 | 株式会社Api | 5-羟基哌啶-2-甲酸的制造方法 |
| WO2017204830A1 (en) | 2016-05-27 | 2017-11-30 | Exxonmobil Chemical Patents, Inc. | Metallocene catalyst compositions and polymerization process therewith |
| US11472828B2 (en) | 2019-10-11 | 2022-10-18 | Exxonmobil Chemical Patents Inc. | Indacene based metallocene catalysts useful in the production of propylene polymers |
| US20230192606A1 (en) * | 2020-04-17 | 2023-06-22 | Baylor College Of Medicine | Direct thrombin inhibitors and methods of use thereof |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5589173A (en) | 1986-11-04 | 1996-12-31 | Genentech, Inc. | Method and therapeutic compositions for the treatment of myocardial infarction |
| US5580560A (en) | 1989-11-13 | 1996-12-03 | Novo Nordisk A/S | Modified factor VII/VIIa |
| US5374617A (en) | 1992-05-13 | 1994-12-20 | Oklahoma Medical Research Foundation | Treatment of bleeding with modified tissue factor in combination with FVIIa |
| US5504064A (en) | 1991-04-10 | 1996-04-02 | Oklahoma Medical Research Foundation | Treatment of bleeding with modified tissue factor in combination with an activator of FVII |
| WO1993009804A1 (en) | 1991-11-18 | 1993-05-27 | The Scripps Research Institute | Serine protease derived-polypeptides and anti-peptide antibodies, systems and therapeutic methods for inhibiting coagulation |
| WO1993015756A1 (en) | 1992-02-14 | 1993-08-19 | Corvas International, Inc. | Inhibitors of thrombosis |
| JPH08504769A (ja) | 1992-12-15 | 1996-05-21 | コルバス・インターナショナル、インコーポレイテッド | 因子Ｘａの新規インヒビター |
| US5656600A (en) | 1993-03-25 | 1997-08-12 | Corvas International, Inc. | α-ketoamide derivatives as inhibitors of thrombosis |
| US5726159A (en) | 1994-03-04 | 1998-03-10 | Eli Lilly And Company | Antithrombotic agents |
| US5681844A (en) | 1994-04-18 | 1997-10-28 | Corvas International, Inc. | Methionine sulfone and s-substituted cysteine sulfone derivatives as enzyme inhibitors |
| IL115420A0 (en) | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
| US5998379A (en) * | 1994-11-21 | 1999-12-07 | Cortech Inc. | Serine protease inhibitors-proline analogs |
| PL184824B1 (pl) | 1994-12-02 | 2002-12-31 | Yamanouchi Pharmaceu | Pochodne amidynonaftylowe oraz ich sole oraz kompozycja farmaceutyczna zawierająca pochodną amidynonaftylową lub jej sól |
| US5656645A (en) | 1994-12-13 | 1997-08-12 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5658930A (en) | 1994-12-13 | 1997-08-19 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5612353A (en) | 1995-06-07 | 1997-03-18 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds |
| WO1997030073A1 (en) | 1996-02-13 | 1997-08-21 | Akzo Nobel N.V. | Serine protease inhibitors |
| US6057342A (en) | 1996-08-16 | 2000-05-02 | Dupont Pharmaceutical Co. | Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof |
| US6291514B1 (en) * | 1998-02-09 | 2001-09-18 | 3-Dimensional Pharmaceuticals, Inc. | Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors |
| EP1086946A4 (de) * | 1998-06-08 | 2003-03-05 | Ajinomoto Kk | Benzamidinderivate |
| AU2001288819A1 (en) * | 2000-09-11 | 2002-03-26 | Genentech, Inc. | Amidine inhibitors of serine proteases |
-
2001
- 2001-09-05 AU AU2001288819A patent/AU2001288819A1/en not_active Abandoned
- 2001-09-05 JP JP2002526828A patent/JP2004509104A/ja active Pending
- 2001-09-05 EP EP01968579A patent/EP1317429B1/de not_active Expired - Lifetime
- 2001-09-05 US US09/947,424 patent/US6410733B1/en not_active Expired - Fee Related
- 2001-09-05 US US10/363,557 patent/US6838479B2/en not_active Expired - Fee Related
- 2001-09-05 WO PCT/US2001/027640 patent/WO2002022575A1/en not_active Ceased
- 2001-09-05 DE DE60122750T patent/DE60122750T2/de not_active Expired - Lifetime
- 2001-09-05 AT AT01968579T patent/ATE338030T1/de not_active IP Right Cessation
- 2001-09-05 CA CA002421548A patent/CA2421548C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US6410733B1 (en) | 2002-06-25 |
| EP1317429A1 (de) | 2003-06-11 |
| US20020055469A1 (en) | 2002-05-09 |
| CA2421548A1 (en) | 2002-03-21 |
| AU2001288819A1 (en) | 2002-03-26 |
| CA2421548C (en) | 2007-10-30 |
| EP1317429B1 (de) | 2006-08-30 |
| DE60122750D1 (de) | 2006-10-12 |
| DE60122750T2 (de) | 2006-12-21 |
| US20030229133A1 (en) | 2003-12-11 |
| WO2002022575A1 (en) | 2002-03-21 |
| US6838479B2 (en) | 2005-01-04 |
| JP2004509104A (ja) | 2004-03-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| UEP | Publication of translation of european patent specification |
Ref document number: 1317429 Country of ref document: EP |
|
| REN | Ceased due to non-payment of the annual fee |