BG105985A - Prodrugs of thrombin inhibitors - Google Patents

Prodrugs of thrombin inhibitors

Info

Publication number
BG105985A
BG105985A BG105985A BG10598501A BG105985A BG 105985 A BG105985 A BG 105985A BG 105985 A BG105985 A BG 105985A BG 10598501 A BG10598501 A BG 10598501A BG 105985 A BG105985 A BG 105985A
Authority
BG
Bulgaria
Prior art keywords
prodrugs
thrombin inhibitors
relates
amidines
trypsin
Prior art date
Application number
BG105985A
Other languages
Bulgarian (bg)
Inventor
Dorit Baucke
Helmut Mack
Werner Seitz
Wilfried Hornberger
Gisela Backfisch
Juergen DELZER
Original Assignee
Abbott Gmbh & Co. Kg
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26004346&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BG105985(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbott Gmbh & Co. Kg filed Critical Abbott Gmbh & Co. Kg
Publication of BG105985A publication Critical patent/BG105985A/en

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
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B43/00—Formation or introduction of functional groups containing nitrogen
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. Pro, Trp
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

The present invention relates to prodrugs of general formula (I) given in the description. Disclosed are the prodrugs of pharmaceutically active, heterocyclic amidines. In vivo compounds, which are competitive inhibitors of trypsin-like serine proteases, especially thrombin, are produced from the amidines. The invention also relates to the production and use of the prodrugs as medicaments. 10 claims
BG105985A 1999-04-09 2001-10-05 Prodrugs of thrombin inhibitors BG105985A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19915930 1999-04-09
DE10006799 2000-02-15
PCT/EP2000/003008 WO2000061577A1 (en) 1999-04-09 2000-04-05 Prodrugs of thrombin inhibitors

Publications (1)

Publication Number Publication Date
BG105985A true BG105985A (en) 2002-06-28

Family

ID=26004346

Family Applications (1)

Application Number Title Priority Date Filing Date
BG105985A BG105985A (en) 1999-04-09 2001-10-05 Prodrugs of thrombin inhibitors

Country Status (16)

Country Link
EP (1) EP1169318A1 (en)
JP (1) JP2002541254A (en)
KR (1) KR20020004995A (en)
CN (1) CN1349526A (en)
AU (1) AU3659200A (en)
BG (1) BG105985A (en)
BR (1) BR0009653A (en)
CA (1) CA2368830A1 (en)
HK (1) HK1045516A1 (en)
HU (1) HUP0202431A3 (en)
IL (1) IL145670A0 (en)
NO (1) NO20014807L (en)
PL (1) PL352834A1 (en)
SK (1) SK14092001A3 (en)
TR (1) TR200102914T2 (en)
WO (1) WO2000061577A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10064797A1 (en) * 2000-12-22 2002-06-27 Knoll Ag Combination pack useful for the treatment of e.g. deep vein thrombosis and post-operative thrombosis, containing oral and parenteral formulations of thrombin inhibitor prodrugs
ATE437642T1 (en) * 2002-06-14 2009-08-15 Takeda Pharmaceutical IMIDAZOLE DERIVATIVE PRODRUGS FOR USE AS PROTON PUMP INHIBITORS FOR THE TREATMENT OF E.G. PEPTIC STOMACH ULCERS
KR101299322B1 (en) 2004-08-23 2013-08-26 록코 시스템즈 피티이 리미티드 Supply mechanism for the chuck of an integrated circuit dicing device

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4421052A1 (en) * 1994-06-17 1995-12-21 Basf Ag New thrombin inhibitors, their production and use
SK104697A3 (en) * 1995-02-17 1998-11-04 Basf Ag Novel dipeptide amidines as thrombin inhibitors
DE19631084A1 (en) * 1996-08-01 1998-02-05 Basf Ag Use of (meth) acrylic acid copolymers to increase the permeability of the mucosa
DE19635674A1 (en) * 1996-09-03 1998-03-05 Basf Ag Process for the preparation of amidines

Also Published As

Publication number Publication date
NO20014807L (en) 2001-12-04
SK14092001A3 (en) 2002-05-09
PL352834A1 (en) 2003-09-08
NO20014807D0 (en) 2001-10-03
KR20020004995A (en) 2002-01-16
TR200102914T2 (en) 2002-01-21
WO2000061577A1 (en) 2000-10-19
HUP0202431A2 (en) 2002-11-28
HK1045516A1 (en) 2002-11-29
BR0009653A (en) 2002-01-08
JP2002541254A (en) 2002-12-03
CN1349526A (en) 2002-05-15
AU3659200A (en) 2000-11-14
CA2368830A1 (en) 2000-10-19
IL145670A0 (en) 2002-06-30
HUP0202431A3 (en) 2003-03-28
EP1169318A1 (en) 2002-01-09

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