CA2822350A1 - 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
CA2822350A1
CA2822350A1 CA2822350A CA2822350A CA2822350A1 CA 2822350 A1 CA2822350 A1 CA 2822350A1 CA 2822350 A CA2822350 A CA 2822350A CA 2822350 A CA2822350 A CA 2822350A CA 2822350 A1 CA2822350 A1 CA 2822350A1
Authority
CA
Canada
Prior art keywords
group
inclusively
integer
compound
amino protecting
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.)
Abandoned
Application number
CA2822350A
Other languages
English (en)
French (fr)
Inventor
Peter Herold
Stjepan Jelakovic
Mohammed Daghish
Claudia Reichelt
Alexander Schulze
Andrea Schweinitz
Friedrich-Alexander Ludwig
Adel Rafai Far
Ting Kang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Medicines Company Leipzig GmbH
Original Assignee
Medicines Company Leipzig GmbH
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Medicines Company Leipzig GmbH filed Critical Medicines Company Leipzig GmbH
Publication of CA2822350A1 publication Critical patent/CA2822350A1/en
Abandoned legal-status Critical Current

Links

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)
  • 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)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2822350A 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 Abandoned CA2822350A1 (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 (1)

Publication Number Publication Date
CA2822350A1 true CA2822350A1 (en) 2012-06-28

Family

ID=46312955

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2822350A Abandoned CA2822350A1 (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 (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
WO2018093716A1 (en) * 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. FACTOR XIIa INHIBITORS
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 HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCTION THEREOF

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3163469D1 (en) * 1980-05-12 1984-06-14 Choay Sa 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
EP0684830B1 (en) * 1993-02-12 1999-06-16 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
EP0960885A4 (en) * 1996-06-25 2002-08-28 Nisshin Seifun Group Inc DEPSIPEPTIDES AND MEDICATIONS, WHICH CONTAIN THE SAME AS ACTIVE INGREDIENCIES
EP1036063B1 (en) 1997-11-26 2006-11-02 Ortho-McNeil Pharmaceuticals, 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
JP4898091B2 (ja) 2002-03-11 2012-03-14 ザ メディシンズ カンパニー （ライプツィヒ） ゲーエムベーハー ウロキナーゼの阻害剤、それらの製造および使用
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
JP5424887B2 (ja) * 2006-11-08 2014-02-26 チョンシー ユー ペプチド及び関連化合物の経皮送達システム
WO2012004678A2 (en) 2010-07-07 2012-01-12 The Medicines Company (Leipzig) Gmbh Serine protease inhibitors

Also Published As

Publication number Publication date
US8497245B2 (en) 2013-07-30
AU2011349022B2 (en) 2017-04-13
AU2011349022A1 (en) 2013-07-11
US20120252743A1 (en) 2012-10-04
ES2654440T3 (es) 2018-02-13
CN103403018B (zh) 2015-08-19
NO2655399T3 (enExample) 2018-02-24
JP5923110B2 (ja) 2016-05-24
JP2014500280A (ja) 2014-01-09
EP2655399A4 (en) 2014-07-30
EP2655399B1 (en) 2017-09-27
WO2012083436A1 (en) 2012-06-28
CN103403018A (zh) 2013-11-20
EP2655399A1 (en) 2013-10-30

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Effective date: 20161215

FZDE Dead

Effective date: 20181221