NO318759B1 - Forbindelse som spesifikt inhiberer faktor Xa-aktivitet, farmasoytisk preparat som inneholder forbindelsen, anvendelse av forbindelsen for fremstilling av et farmasoytisk preparat og anvendelse av forbindelsen som antikoagulant. - Google Patents

Forbindelse som spesifikt inhiberer faktor Xa-aktivitet, farmasoytisk preparat som inneholder forbindelsen, anvendelse av forbindelsen for fremstilling av et farmasoytisk preparat og anvendelse av forbindelsen som antikoagulant. Download PDF

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Publication number
NO318759B1
NO318759B1 NO19964553A NO964553A NO318759B1 NO 318759 B1 NO318759 B1 NO 318759B1 NO 19964553 A NO19964553 A NO 19964553A NO 964553 A NO964553 A NO 964553A NO 318759 B1 NO318759 B1 NO 318759B1
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Prior art keywords
compound
group
peptide
acid
activity
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NO19964553A
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English (en)
Norwegian (no)
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NO964553L (no
NO964553D0 (no
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Fahad Al-Obeidi
Michal Lebl
James A Ostrem
Pavel Safar
Alena Stierandova
Peter Strop
Armin Walser
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Aventis Pharma Inc
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Publication of NO964553D0 publication Critical patent/NO964553D0/no
Publication of NO964553L publication Critical patent/NO964553L/no
Publication of NO318759B1 publication Critical patent/NO318759B1/no

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors
    • C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
    • 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
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • 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
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/56—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving blood clotting factors, e.g. involving thrombin, thromboplastin, fibrinogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biotechnology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
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  • Crystallography & Structural Chemistry (AREA)
  • Neurosurgery (AREA)
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  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Diabetes (AREA)
  • General Engineering & Computer Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
NO19964553A 1994-04-26 1996-10-25 Forbindelse som spesifikt inhiberer faktor Xa-aktivitet, farmasoytisk preparat som inneholder forbindelsen, anvendelse av forbindelsen for fremstilling av et farmasoytisk preparat og anvendelse av forbindelsen som antikoagulant. NO318759B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23305494A 1994-04-26 1994-04-26
PCT/US1995/005268 WO1995029189A1 (en) 1994-04-26 1995-04-25 FACTOR Xa INHIBITORS

Publications (3)

Publication Number Publication Date
NO964553D0 NO964553D0 (no) 1996-10-25
NO964553L NO964553L (no) 1996-12-27
NO318759B1 true NO318759B1 (no) 2005-05-02

Family

ID=22875692

Family Applications (1)

Application Number Title Priority Date Filing Date
NO19964553A NO318759B1 (no) 1994-04-26 1996-10-25 Forbindelse som spesifikt inhiberer faktor Xa-aktivitet, farmasoytisk preparat som inneholder forbindelsen, anvendelse av forbindelsen for fremstilling av et farmasoytisk preparat og anvendelse av forbindelsen som antikoagulant.

Country Status (27)

Country Link
EP (2) EP0758341B1 (cs)
JP (1) JP3655632B2 (cs)
KR (1) KR100380124B1 (cs)
CN (1) CN1181091C (cs)
AT (1) ATE262536T1 (cs)
AU (1) AU707653B2 (cs)
CA (1) CA2186497C (cs)
CZ (1) CZ296439B6 (cs)
DE (1) DE69532754T2 (cs)
DK (1) DK0758341T3 (cs)
EE (1) EE03973B1 (cs)
ES (1) ES2214500T3 (cs)
FI (1) FI120494B (cs)
HU (1) HUT76346A (cs)
IL (1) IL113505A (cs)
LT (1) LT4218B (cs)
LV (1) LV11740B (cs)
NO (1) NO318759B1 (cs)
NZ (1) NZ284977A (cs)
PL (1) PL188132B1 (cs)
PT (1) PT758341E (cs)
RU (1) RU2152954C1 (cs)
SI (1) SI9520044B (cs)
SK (1) SK286094B6 (cs)
TW (1) TW409129B (cs)
WO (1) WO1995029189A1 (cs)
ZA (1) ZA953361B (cs)

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CA2186497A1 (en) 1995-11-02
CN1147261A (zh) 1997-04-09
AU2368395A (en) 1995-11-16
PL317067A1 (en) 1997-03-03
LT96151A (en) 1997-05-26
EE9600146A (et) 1997-04-15
DE69532754D1 (de) 2004-04-29
DE69532754T2 (de) 2005-03-10
EE03973B1 (et) 2003-02-17
EP1384725A3 (en) 2007-02-21
LV11740B (en) 1997-12-20
JPH10503477A (ja) 1998-03-31
PL188132B1 (pl) 2004-12-31
EP1384725A2 (en) 2004-01-28
SI9520044A (en) 1997-10-31
JP3655632B2 (ja) 2005-06-02
KR100380124B1 (ko) 2003-08-02
CZ314096A3 (en) 1997-05-14
CZ296439B6 (cs) 2006-03-15
PT758341E (pt) 2004-08-31
TW409129B (en) 2000-10-21
EP0758341A1 (en) 1997-02-19
LT4218B (en) 1997-09-25
CA2186497C (en) 2008-06-17
FI964317A7 (fi) 1996-10-25
HU9602954D0 (en) 1996-12-30
IL113505A0 (en) 1995-07-31
IL113505A (en) 1999-12-31
LV11740A (lv) 1997-04-20
SI9520044B (sl) 2004-08-31
NO964553L (no) 1996-12-27
HUT76346A (en) 1997-08-28
EP0758341B1 (en) 2004-03-24
AU707653B2 (en) 1999-07-15
FI120494B (fi) 2009-11-13
NO964553D0 (no) 1996-10-25
CN1181091C (zh) 2004-12-22
ATE262536T1 (de) 2004-04-15
ZA953361B (en) 1996-01-12
SK136696A3 (en) 1997-05-07
SK286094B6 (sk) 2008-03-05
FI964317A0 (fi) 1996-10-25
DK0758341T3 (da) 2004-06-28
RU2152954C1 (ru) 2000-07-20
ES2214500T3 (es) 2004-09-16
NZ284977A (en) 1998-09-24
WO1995029189A1 (en) 1995-11-02

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