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
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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Detergent Compositions (AREA)
- Treating Waste Gases (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole 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 |
AU2001288819A1 (en) * | 2000-09-11 | 2002-03-26 | Genentech, Inc. | Amidine inhibitors of serine proteases |
EP1432687A2 (de) * | 2001-10-03 | 2004-06-30 | Pharmacia Corporation | Substitutierte fünfgliedrige polyzyclischen vebindungen für die selektive hemmung der koagulationskaskade |
WO2003037326A1 (en) * | 2001-10-29 | 2003-05-08 | Corvas International, Inc. | Solid phase synthesis of chemical libraries |
JP2005538953A (ja) * | 2002-05-28 | 2005-12-22 | 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 | 新規チオフェンアミジン、それらの組成物、および補体媒介疾患および病気を治療する方法 |
US7659305B2 (en) | 2002-10-31 | 2010-02-09 | Pfizer Inc. | Therapeutic proline derivatives |
DK1569912T3 (en) | 2002-12-03 | 2015-06-29 | Pharmacyclics Inc | 2- (2-hydroxybiphenyl-3-yl) -1h-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors. |
JP4705015B2 (ja) | 2003-04-03 | 2011-06-22 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | カルボニル化合物 |
US7273886B2 (en) | 2003-05-20 | 2007-09-25 | Genentech, Inc. | Benzofuran inhibitors of factor VIIa |
JP4947406B2 (ja) * | 2003-08-29 | 2012-06-06 | 小野薬品工業株式会社 | S1p受容体結合能を有する化合物およびその医薬用途 |
US7550487B2 (en) | 2004-03-26 | 2009-06-23 | Hoffmann-La Roche Inc. | Pyrrolidine-3,4-dicarboxamide derivatives |
ATE533491T1 (de) * | 2004-09-21 | 2011-12-15 | 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 |
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 |
CA2621059C (en) * | 2005-09-22 | 2013-08-13 | Trobio Ab | Stabilized protease composition |
WO2007057317A1 (en) * | 2005-11-16 | 2007-05-24 | F. Hoffmann-La Roche Ag | Novel pyrrolidine derivatives as inhibitors of coagulation factor xa |
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 |
WO2015009473A1 (en) | 2013-07-17 | 2015-01-22 | Exxonmobil Chemical Patents Inc. | Cyclopropyl substituted metallocene catalysts |
WO2015009470A1 (en) | 2013-07-17 | 2015-01-22 | Exxonmobil Chemical Patents Inc. | Metallocenes and catalyst compositions derived therefrom |
WO2015009472A1 (en) | 2013-07-17 | 2015-01-22 | Exxonmobil Chemcal 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 |
CN105899487B (zh) * | 2013-12-27 | 2018-10-19 | 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 |
WO2021211913A1 (en) * | 2020-04-17 | 2021-10-21 | 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 |
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 |
US5374617A (en) | 1992-05-13 | 1994-12-20 | Oklahoma Medical Research Foundation | Treatment of bleeding with modified tissue factor in combination with FVIIa |
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 |
US5869501A (en) | 1994-12-02 | 1999-02-09 | Yamanouchi Pharmaceutical Co. Ltd | Amidinonaphthyl derivative or salt thereof |
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 |
WO1999064392A1 (fr) | 1998-06-08 | 1999-12-16 | Ajinomoto Co., Inc. | Derive de benzamidine |
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 US US09/947,424 patent/US6410733B1/en not_active Expired - Fee Related
- 2001-09-05 WO PCT/US2001/027640 patent/WO2002022575A1/en active IP Right Grant
- 2001-09-05 AT AT01968579T patent/ATE338030T1/de not_active IP Right Cessation
- 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 CA CA002421548A patent/CA2421548C/en not_active Expired - Fee Related
- 2001-09-05 JP JP2002526828A patent/JP2004509104A/ja active Pending
- 2001-09-05 US US10/363,557 patent/US6838479B2/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
US20020055469A1 (en) | 2002-05-09 |
EP1317429A1 (de) | 2003-06-11 |
DE60122750T2 (de) | 2006-12-21 |
WO2002022575A1 (en) | 2002-03-21 |
US6410733B1 (en) | 2002-06-25 |
ATE338030T1 (de) | 2006-09-15 |
CA2421548C (en) | 2007-10-30 |
AU2001288819A1 (en) | 2002-03-26 |
CA2421548A1 (en) | 2002-03-21 |
EP1317429B1 (de) | 2006-08-30 |
JP2004509104A (ja) | 2004-03-25 |
US20030229133A1 (en) | 2003-12-11 |
US6838479B2 (en) | 2005-01-04 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
8364 | No opposition during term of opposition |