DE60122750D1 - Amidine-inhibitoren der serine-proteasen - Google Patents
Amidine-inhibitoren der serine-proteasenInfo
- Publication number
- DE60122750D1 DE60122750D1 DE60122750T DE60122750T DE60122750D1 DE 60122750 D1 DE60122750 D1 DE 60122750D1 DE 60122750 T DE60122750 T DE 60122750T DE 60122750 T DE60122750 T DE 60122750T DE 60122750 D1 DE60122750 D1 DE 60122750D1
- Authority
- DE
- Germany
- Prior art keywords
- serine proteases
- inhibitors
- factor
- amidine
- compounds
- 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
- 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)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23167900P | 2000-09-11 | 2000-09-11 | |
| US231679P | 2000-09-11 | ||
| PCT/US2001/027640 WO2002022575A1 (en) | 2000-09-11 | 2001-09-05 | Amidine inhibitors of serine proteases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60122750D1 true DE60122750D1 (de) | 2006-10-12 |
| DE60122750T2 DE60122750T2 (de) | 2006-12-21 |
Family
ID=22870229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60122750T Expired - Lifetime DE60122750T2 (de) | 2000-09-11 | 2001-09-05 | Amidin-Inhibitoren von Serin-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 |
| WO2002022575A1 (en) * | 2000-09-11 | 2002-03-21 | Genentech, Inc. | Amidine inhibitors of serine proteases |
| AU2002367752A1 (en) | 2001-10-03 | 2003-11-17 | 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 |
| ZA200408711B (en) * | 2002-05-28 | 2006-10-25 | Dimensional Pharamaceuticals I | Novel thiophene amidines, composition thereof, and methods of treating complement-mediated diseases and conditions |
| US7659305B2 (en) | 2002-10-31 | 2010-02-09 | Pfizer Inc. | Therapeutic proline derivatives |
| HUE025683T2 (hu) | 2002-12-03 | 2016-04-28 | Pharmacyclics Llc | VIIA faktor inhibitor 2-(2-hidroxi-bifenil-3-il)-1H-benzoimidazol-5-karboxamidin-származékok |
| BRPI0408420A (pt) * | 2003-04-03 | 2006-03-21 | Merck Patent Gmbh | compostos de carbonila |
| 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 |
| EP1661881B1 (de) * | 2003-08-29 | 2014-12-17 | Ono Pharmaceutical Co., Ltd. | Zur bindung an den s1p-rezeptor fähige verbindung und deren pharmazeutische verwendung |
| US7550487B2 (en) * | 2004-03-26 | 2009-06-23 | Hoffmann-La Roche Inc. | Pyrrolidine-3,4-dicarboxamide derivatives |
| PL1637141T3 (pl) * | 2004-09-21 | 2012-04-30 | Trobio Ab | Stabilizowana kompozycja proteazy zawierająca proteazę serynową, pochodne morfoliny i odwracalne inhibitory tej proteazy serynowej |
| WO2006073167A1 (ja) * | 2005-01-07 | 2006-07-13 | Ono Pharmaceutical Co., Ltd. | ピロリジン誘導体 |
| 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 |
| AU2005336535B2 (en) * | 2005-09-22 | 2012-05-24 | Trobio Ab | Stabilized protease composition |
| US7601752B2 (en) | 2005-11-16 | 2009-10-13 | Hoffmann-La Roche Inc. | Pyrrolidine derivatives |
| US8889117B2 (en) * | 2007-02-15 | 2014-11-18 | 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 |
| ES2703344T3 (es) | 2013-07-17 | 2019-03-08 | Exxonmobil Chemical Patents Inc | Metalocenos y composiciones catalíticas derivadas de ellos |
| SG10201802959WA (en) | 2013-07-17 | 2018-05-30 | Exxonmobil Chemical Patents Inc | Cyclopropyl substituted metallocene catalysts |
| US9464145B2 (en) | 2013-07-17 | 2016-10-11 | Exxonmobil Chemical Patents Inc. | Metallocenes and catalyst compositions derived therefrom |
| 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 |
| CN107573277B (zh) * | 2013-12-27 | 2020-10-16 | 株式会社Api | 5-羟基哌啶-2-甲酸的制造方法 |
| CN109312013A (zh) | 2016-05-27 | 2019-02-05 | 埃克森美孚化学专利公司 | 茂金属催化剂组合物和使用其的聚合方法 |
| 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 |
| JP3194953B2 (ja) | 1992-02-14 | 2001-08-06 | コルバス・インターナショナル、インコーポレイテッド | 血栓症抑制剤 |
| CA2151044A1 (en) | 1992-12-15 | 1994-06-23 | Terence K. Brunck | Novel inhibitors for factor xa |
| 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 |
| ATE233240T1 (de) | 1994-12-02 | 2003-03-15 | Yamanouchi Pharma Co Ltd | Neues amidinonaphthylderivat oder dessen salz |
| US5658930A (en) | 1994-12-13 | 1997-08-19 | Corvas International, Inc. | Aromatic heterocyclic derivatives as enzyme inhibitors |
| US5656645A (en) | 1994-12-13 | 1997-08-12 | 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 |
| WO2002022575A1 (en) * | 2000-09-11 | 2002-03-21 | Genentech, Inc. | Amidine inhibitors of serine proteases |
-
2001
- 2001-09-05 WO PCT/US2001/027640 patent/WO2002022575A1/en active IP Right Grant
- 2001-09-05 US US09/947,424 patent/US6410733B1/en not_active Expired - Fee Related
- 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 DE DE60122750T patent/DE60122750T2/de not_active Expired - Lifetime
- 2001-09-05 US US10/363,557 patent/US6838479B2/en not_active Expired - Fee Related
- 2001-09-05 AU AU2001288819A patent/AU2001288819A1/en not_active Abandoned
- 2001-09-05 CA CA002421548A patent/CA2421548C/en not_active Expired - Fee Related
- 2001-09-05 AT AT01968579T patent/ATE338030T1/de not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1317429A1 (de) | 2003-06-11 |
| US20030229133A1 (en) | 2003-12-11 |
| WO2002022575A1 (en) | 2002-03-21 |
| ATE338030T1 (de) | 2006-09-15 |
| JP2004509104A (ja) | 2004-03-25 |
| US6838479B2 (en) | 2005-01-04 |
| AU2001288819A1 (en) | 2002-03-26 |
| EP1317429B1 (de) | 2006-08-30 |
| CA2421548A1 (en) | 2002-03-21 |
| CA2421548C (en) | 2007-10-30 |
| DE60122750T2 (de) | 2006-12-21 |
| US6410733B1 (en) | 2002-06-25 |
| US20020055469A1 (en) | 2002-05-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| DE60122750D1 (de) | Amidine-inhibitoren der serine-proteasen | |
| ATE438615T1 (de) | Biarylverbindungen als serinproteaseinhibitoren | |
| DE60023266D1 (de) | Serinprotease-inhibitoren | |
| TR200402535T4 (tr) | Serin proteaz inhibitörleri. | |
| DK1086122T3 (da) | Pyrazinonproteaseinhibitorer | |
| DE60011430D1 (de) | Stickstoff enthaltende heterobicyclen als factor xa inhibitoren | |
| NO20091647L (no) | Trypsinlignende serinproteaseinhibitorer og deres fremstilling og anvendelse | |
| TR200002904T2 (tr) | Amidin bileşikleri | |
| WO1996035788A3 (en) | Kunitz type protease inhibitors | |
| TW200745062A (en) | Macrocyclic factor VIIA inhibitors useful as anticoagulants | |
| DE69902754D1 (de) | Heteroaryl-amidinen,-methylamidinen und -guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren | |
| ATE275544T1 (de) | Serinprotease-inhibitoren | |
| IS5511A (is) | Ný efnasambönd | |
| TR199801704T2 (xx) | Serin proteaz inhibit�rleri. | |
| DE60113252D1 (de) | Inhibitoren von serin proteasen | |
| MXPA01008084A (es) | Heteroarilamidinas, metilamidinas y guanidinas como inhibidores de proteasa. | |
| WO1999063090A3 (en) | Protease inhibitor peptides | |
| ATE250056T1 (de) | Heteroaryl protease inhibitoren und diagnostische bilderzeugungsmittel | |
| WO2002006248A3 (en) | Cyclic oxyguanidine pyrazinones as protease inhibitors | |
| ATE407116T1 (de) | Neue amidino-derivate und deren verwendung als thrombin-inhibitoren | |
| MXPA03000963A (es) | Inhibidores de oxiguanidina ciclica proteasa. | |
| IS7162A (is) | Nýjar möndlusýruafleiður og notkun þeirra sem þrombínhemla | |
| TR200102914T2 (tr) | Trombin önleyicilerinin önilaçları | |
| PT1075476E (pt) | Novos benzimidazoles e benzoxazoles |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition |