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AU2001252419A1 - Thrombin inhibitors - Google Patents

Thrombin inhibitors

Info

Publication number
AU2001252419A1
AU2001252419A1 AU2001252419A AU5241901A AU2001252419A1 AU 2001252419 A1 AU2001252419 A1 AU 2001252419A1 AU 2001252419 A AU2001252419 A AU 2001252419A AU 5241901 A AU5241901 A AU 5241901A AU 2001252419 A1 AU2001252419 A1 AU 2001252419A1
Authority
AU
Australia
Prior art keywords
thrombin inhibitors
dipeptides
compounds
mimetics
pharmaceutically acceptable
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
AU2001252419A
Inventor
Matej Breznik
Marjana Fortuna
Danijel Kikelj
Petra Marinko
Lucija Peterlin
Mojca Stregnar
Bakija Alenka Trampuz
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.)
Lek Pharmaceuticals dd
Univerza Ljubljana v Fakulteta za Farmazijo
Original Assignee
Univerza Ljubljana v Fakulteta za Farmazijo
Lek Pharmaceuticals and Chemical Co dd
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 Univerza Ljubljana v Fakulteta za Farmazijo, Lek Pharmaceuticals and Chemical Co dd filed Critical Univerza Ljubljana v Fakulteta za Farmazijo
Publication of AU2001252419A1 publication Critical patent/AU2001252419A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • C07D277/82Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof. The compounds are used as thrombin inhibitors
AU2001252419A 2000-05-05 2001-05-04 Thrombin inhibitors Abandoned AU2001252419A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SIP-200000111 2000-05-05
SI200000111A SI20582A (en) 2000-05-05 2000-05-05 Novel thrombine inhibitors, their preparation and use
PCT/GB2001/001997 WO2001085760A1 (en) 2000-05-05 2001-05-04 Thrombin inhibitors

Publications (1)

Publication Number Publication Date
AU2001252419A1 true AU2001252419A1 (en) 2001-11-20

Family

ID=20432649

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2001252419A Abandoned AU2001252419A1 (en) 2000-05-05 2001-05-04 Thrombin inhibitors

Country Status (8)

Country Link
US (1) US7112590B2 (en)
EP (1) EP1287018B1 (en)
AT (1) ATE287416T1 (en)
AU (1) AU2001252419A1 (en)
DE (1) DE60108495T2 (en)
ES (1) ES2239134T3 (en)
SI (1) SI20582A (en)
WO (1) WO2001085760A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050119226A1 (en) * 2003-09-09 2005-06-02 Trigen Limited Methods for synthesizing organoboronic compounds and products thereof
US20050282757A1 (en) * 2002-09-09 2005-12-22 Trigen Limited Peptide boronic acid compounds useful in anticoagulation
US7112572B2 (en) * 2002-09-09 2006-09-26 Trigen Limited Multivalent metal salts of boronic acids
GB0405272D0 (en) * 2004-03-09 2004-04-21 Trigen Ltd Compounds
KR100735639B1 (en) * 2004-12-29 2007-07-04 한미약품 주식회사 Quinazoline derivatives inhibiting the growth of cancer cell and preparation thereof
CN102796167B (en) * 2011-05-26 2014-01-08 首都医科大学 (S)-4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridine-6-formyl-L-prolyl-L-alanyl-L-amino acid and its Preparation method and application
CN102807600B (en) * 2011-06-03 2014-08-13 首都医科大学 Amino acid modified spinacin derivative and preparation method and application thereof
CN104507933B (en) * 2012-05-31 2017-10-31 霍夫曼-拉罗奇有限公司 Amido quinazoline and Pyridopyrimidine derivatives
CN111848730B (en) * 2019-04-30 2022-06-24 首都医科大学 Preparation, Activity and Application of Theanyltetrahydroimidazopyridine-6-formyl Polar Amino Acids

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5510369A (en) * 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
US5523308A (en) 1995-06-07 1996-06-04 Costanzo; Michael J. Peptidyl heterocycles useful in the treatment of thrombin related disorders
US5827866A (en) 1995-06-07 1998-10-27 Ortho Pharmaceutical Corporation Peptidyl heterocycles useful in the treatment of thrombin related disorders
US5811402A (en) 1996-03-22 1998-09-22 Eli Lilly And Company Antithrombotic diamides
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Serine protease inhibiting antithrombotic agents and pharmaceutical compositions comprising them

Also Published As

Publication number Publication date
DE60108495T2 (en) 2006-01-12
EP1287018A2 (en) 2003-03-05
WO2001085760A8 (en) 2002-03-14
WO2001085760A1 (en) 2001-11-15
SI20582A (en) 2001-12-31
ES2239134T3 (en) 2005-09-16
EP1287018B1 (en) 2005-01-19
US7112590B2 (en) 2006-09-26
DE60108495D1 (en) 2005-02-24
ATE287416T1 (en) 2005-02-15
US20030191139A1 (en) 2003-10-09

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