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 PDF

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Publication number
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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group
inclusively
integer
pharmaceutically acceptable
acceptable salt
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AU2011349022A
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AU2011349022A1 (en
Inventor
Mohammed Daghish
Adel Rafai Far
Peter Herold
Stjepan Jelakovic
Ting Kang
Friedrich-Alexander Ludwig
Claudia Reichelt
Alexander Schulze
Andrea Schweinitz
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Medicines Company Leipzig GmbH
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Medicines Company Leipzig GmbH
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (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)
AU2011349022A 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 Ceased AU2011349022B2 (en)

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)

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US (1) US8497245B2 (enExample)
EP (1) EP2655399B1 (enExample)
JP (1) JP5923110B2 (enExample)
CN (1) CN103403018B (enExample)
AU (1) AU2011349022B2 (enExample)
CA (1) CA2822350A1 (enExample)
ES (1) ES2654440T3 (enExample)
NO (1) NO2655399T3 (enExample)
WO (1) WO2012083436A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
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
WO2012004678A2 (en) 2010-07-07 2012-01-12 The Medicines Company (Leipzig) Gmbh Serine protease inhibitors
GB201311888D0 (en) * 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
EP3449261B1 (en) * 2016-04-25 2023-08-30 Instrumentation Laboratory Company Method and kit for identifying lupus anticoagulant (la) associated with antiphospholipid syndrome
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
EP3939968A4 (en) * 2019-03-29 2022-12-14 Medicinal Bioconvergence Research Center NOVEL COMPOUND WITH ANTI-CANCER ACTIVITIES AND METHOD FOR PRODUCTION THEREOF

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994017817A1 (en) * 1993-02-12 1994-08-18 Corvas International, Inc. Inhibitors of thrombosis

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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
CA2140598C (en) * 1994-01-27 2010-03-09 Masahiro Ohshima Prolineamide derivatives
ZA951617B (en) * 1994-03-04 1997-02-27 Lilly Co Eli Antithrombotic agents.
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
JP2001524467A (ja) 1997-11-26 2001-12-04 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 ヘテロアリールアミノグアニジンおよびアルコキシグアニジンおよびプロテアーゼインヒビターとしてのこれらの使用
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
US7838560B2 (en) 2002-03-11 2010-11-23 The Medicines Company (Leipzig) Gmbh Urokinase inhibitors, production and use thereof
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
DE10227668A1 (de) 2002-06-20 2004-01-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Arzneimittel zur Behandlung des systemic inflammatory response syndrome
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
AU2006350707A1 (en) * 2006-11-08 2008-05-15 Chongxi Yu Transdermal delivery systems of peptides and related compounds
WO2012004678A2 (en) 2010-07-07 2012-01-12 The Medicines Company (Leipzig) Gmbh Serine protease inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
US8497245B2 (en) 2013-07-30
CN103403018B (zh) 2015-08-19
CA2822350A1 (en) 2012-06-28
JP5923110B2 (ja) 2016-05-24
AU2011349022A1 (en) 2013-07-11
EP2655399A1 (en) 2013-10-30
EP2655399B1 (en) 2017-09-27
JP2014500280A (ja) 2014-01-09
US20120252743A1 (en) 2012-10-04
CN103403018A (zh) 2013-11-20
ES2654440T3 (es) 2018-02-13
NO2655399T3 (enExample) 2018-02-24
EP2655399A4 (en) 2014-07-30
WO2012083436A1 (en) 2012-06-28

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MK14 Patent ceased section 143(a) (annual fees not paid) or expired