AU2011349022B2 - Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa - Google Patents
Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa Download PDFInfo
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- AU2011349022B2 AU2011349022B2 AU2011349022A AU2011349022A AU2011349022B2 AU 2011349022 B2 AU2011349022 B2 AU 2011349022B2 AU 2011349022 A AU2011349022 A AU 2011349022A AU 2011349022 A AU2011349022 A AU 2011349022A AU 2011349022 B2 AU2011349022 B2 AU 2011349022B2
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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
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
- C07K5/06121—Asp- or Asn-amino acid the second amino acid being aromatic or cycloaliphatic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- C07K5/06104—Dipeptides with the first amino acid being acidic
-
- 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
- C07K5/06104—Dipeptides with the first amino acid being acidic
- C07K5/06113—Asp- or Asn-amino acid
-
- 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
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201061425597P | 2010-12-21 | 2010-12-21 | |
| US61/425,597 | 2010-12-21 | ||
| PCT/CA2011/001398 WO2012083436A1 (en) | 2010-12-21 | 2011-12-21 | Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors iia and xa |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2011349022A1 AU2011349022A1 (en) | 2013-07-11 |
| AU2011349022B2 true AU2011349022B2 (en) | 2017-04-13 |
Family
ID=46312955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2011349022A Ceased AU2011349022B2 (en) | 2010-12-21 | 2011-12-21 | Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8497245B2 (Direct) |
| EP (1) | EP2655399B1 (Direct) |
| JP (1) | JP5923110B2 (Direct) |
| CN (1) | CN103403018B (Direct) |
| AU (1) | AU2011349022B2 (Direct) |
| CA (1) | CA2822350A1 (Direct) |
| ES (1) | ES2654440T3 (Direct) |
| NO (1) | NO2655399T3 (Direct) |
| WO (1) | WO2012083436A1 (Direct) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | The Medicines Company (Leipzig) GmbH | Serine protease inhibitors |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CN109073662A (zh) * | 2016-04-25 | 2018-12-21 | 仪器实验室公司 | 用于鉴定与抗磷脂综合征相关的狼疮抗凝物(la)的方法和试剂盒 |
| EP3541381B1 (en) * | 2016-11-18 | 2022-12-28 | Merck Sharp & Dohme LLC | Inhibitors of factor xiia |
| GB201805174D0 (en) | 2018-03-29 | 2018-05-16 | Univ Leeds Innovations Ltd | Compounds |
| GB201807014D0 (en) * | 2018-04-30 | 2018-06-13 | Univ Leeds Innovations Ltd | Factor xlla inhibitors |
| JP7603939B2 (ja) * | 2019-03-29 | 2024-12-23 | メディシナル バイオコンバージェンス リサーチ センター | 抗がん活性を有する新規化合物及びその製造方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994017817A1 (en) * | 1993-02-12 | 1994-08-18 | Corvas International, Inc. | Inhibitors of thrombosis |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0040149B1 (en) * | 1980-05-12 | 1984-05-09 | Choay S.A. | Oligopeptides with specific inhibiting properties of collagen induced aggregation, process for preparing the same and pharmaceutical compositions containing them |
| CA1241120A (en) | 1985-10-01 | 1988-08-23 | Sami A. Aly | Alternate mark inversion (ami) receiver |
| US5955576A (en) * | 1992-02-14 | 1999-09-21 | Corvas International, Inc. | Inhibitors of thrombosis |
| EP0648780A1 (en) * | 1993-08-26 | 1995-04-19 | Bristol-Myers Squibb Company | Heterocyclic thrombin inhibitors |
| JPH07138298A (ja) * | 1993-11-19 | 1995-05-30 | Japan Energy Corp | ヒルジン類縁体硫酸エステル化体またはその塩の製造方法 |
| AU1025795A (en) * | 1994-01-27 | 1995-08-03 | Mitsubishi Chemical Corporation | Prolineamide derivatives |
| IL112795A (en) * | 1994-03-04 | 2001-01-28 | Astrazeneca Ab | Peptide derivatives as antithrombic agents their preparation and pharmaceutical compositions containing them |
| US5914319A (en) * | 1995-02-27 | 1999-06-22 | Eli Lilly And Company | Antithrombotic agents |
| JP3947229B2 (ja) * | 1996-06-25 | 2007-07-18 | 株式会社日清製粉グループ本社 | デプシペプチドおよびこれを有効成分とする医薬 |
| TWI222441B (en) | 1997-11-26 | 2004-10-21 | Dimensional Pharm Inc | Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
| DE10029014A1 (de) | 2000-06-15 | 2001-12-20 | Univ Schiller Jena | Urokinase-Hemmstoffe |
| DE10029015A1 (de) | 2000-06-15 | 2001-12-20 | Curacyte Ag | Hemmstoffe für den Gerinnungsfaktor Xa |
| JP2004516286A (ja) | 2000-12-18 | 2004-06-03 | メルク エンド カムパニー インコーポレーテッド | ベンジルアミン誘導体およびそれのトロンビン阻害薬としての使用 |
| DE10102878A1 (de) * | 2001-01-23 | 2002-08-01 | Haemosys Gmbh | Oligo- oder Polyalkylengekoppelte Thrombininhibitoren |
| AU2003219039A1 (en) | 2002-03-11 | 2003-09-22 | Curacyte Ag | Urokinase inhibitors, production and use thereof |
| DE10227668A1 (de) | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Arzneimittel zur Behandlung des systemic inflammatory response syndrome |
| DE10227666A1 (de) | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | (R)-2-(4-Amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)- ethyl]-benzimidazol, dessen Monohydrochlorid, Verfahren zu deren Herstellung sowie Verwendung als Arzneimittel |
| DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
| DE10322191B4 (de) | 2003-05-16 | 2014-02-27 | The Medicines Company (Leipzig) Gmbh | N-sulfonylierte Aminosäurederivate, Verfahren zu ihrer Herstellung und ihre Verwendung |
| DE10342108A1 (de) | 2003-09-11 | 2005-04-14 | Curacyte Chemistry Gmbh | Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung |
| DE102005044319A1 (de) * | 2005-09-16 | 2007-03-22 | Curacyte Chemistry Gmbh | 2-(Aminomethyl)-5-Chlor-Benzylamid-Derivate und ihre Verwendung als Hemmstoffe des Gerinnungsfaktors Xa |
| DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
| CN101541743A (zh) * | 2006-11-08 | 2009-09-23 | 于崇曦 | 多肽及相关化合物的透皮给药系统 |
| EP2590945B1 (en) | 2010-07-07 | 2014-04-30 | The Medicines Company (Leipzig) GmbH | Serine protease inhibitors |
-
2011
- 2011-12-21 NO NO11850640A patent/NO2655399T3/no unknown
- 2011-12-21 JP JP2013544981A patent/JP5923110B2/ja not_active Expired - Fee Related
- 2011-12-21 WO PCT/CA2011/001398 patent/WO2012083436A1/en not_active Ceased
- 2011-12-21 ES ES11850640.1T patent/ES2654440T3/es active Active
- 2011-12-21 EP EP11850640.1A patent/EP2655399B1/en not_active Not-in-force
- 2011-12-21 CN CN201180065191.4A patent/CN103403018B/zh not_active Expired - Fee Related
- 2011-12-21 AU AU2011349022A patent/AU2011349022B2/en not_active Ceased
- 2011-12-21 US US13/332,900 patent/US8497245B2/en not_active Expired - Fee Related
- 2011-12-21 CA CA2822350A patent/CA2822350A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994017817A1 (en) * | 1993-02-12 | 1994-08-18 | Corvas International, Inc. | Inhibitors of thrombosis |
Non-Patent Citations (4)
| Title |
|---|
| Helvetica Chimica Acta, 1982, Vol. 65, pages 775-784 * |
| Journal of Medicinal Chemistry, 1984, Vol. 27, pages 106-115 * |
| Journal of Medicinal Chemistry, 2006, Vol. 49, pages 5339-5351 * |
| Journal of Medicinal Chemistry, 2010, Vol. 53, pages 559-572 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2011349022A1 (en) | 2013-07-11 |
| CN103403018A (zh) | 2013-11-20 |
| WO2012083436A1 (en) | 2012-06-28 |
| CN103403018B (zh) | 2015-08-19 |
| EP2655399A4 (en) | 2014-07-30 |
| US8497245B2 (en) | 2013-07-30 |
| US20120252743A1 (en) | 2012-10-04 |
| CA2822350A1 (en) | 2012-06-28 |
| JP2014500280A (ja) | 2014-01-09 |
| JP5923110B2 (ja) | 2016-05-24 |
| EP2655399B1 (en) | 2017-09-27 |
| EP2655399A1 (en) | 2013-10-30 |
| ES2654440T3 (es) | 2018-02-13 |
| NO2655399T3 (Direct) | 2018-02-24 |
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