SK286094B6 - Zlúčenina špecificky inhibujúca aktivitu faktora Xa, farmaceutická kompozícia s jej obsahom a jej použitie - Google Patents

Zlúčenina špecificky inhibujúca aktivitu faktora Xa, farmaceutická kompozícia s jej obsahom a jej použitie Download PDF

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Publication number
SK286094B6
SK286094B6 SK1366-96A SK136696A SK286094B6 SK 286094 B6 SK286094 B6 SK 286094B6 SK 136696 A SK136696 A SK 136696A SK 286094 B6 SK286094 B6 SK 286094B6
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SK
Slovakia
Prior art keywords
chg
arg
paph
leu
pro
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Application number
SK1366-96A
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English (en)
Slovak (sk)
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SK136696A3 (en
Inventor
Fahad Al-Obeidi
Michal Lebl
James A. Ostrem
Pavel Safar
Alena Stierandova
Peter Strop
Armin Walser
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Aventis Pharmaceuticals Inc.
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Application filed by Aventis Pharmaceuticals Inc. filed Critical Aventis Pharmaceuticals Inc.
Publication of SK136696A3 publication Critical patent/SK136696A3/sk
Publication of SK286094B6 publication Critical patent/SK286094B6/sk

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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)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Wood Science & Technology (AREA)
  • Microbiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Neurosurgery (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • General Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Analytical Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
SK1366-96A 1994-04-26 1995-04-25 Zlúčenina špecificky inhibujúca aktivitu faktora Xa, farmaceutická kompozícia s jej obsahom a jej použitie SK286094B6 (sk)

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 (2)

Publication Number Publication Date
SK136696A3 SK136696A3 (en) 1997-05-07
SK286094B6 true SK286094B6 (sk) 2008-03-05

Family

ID=22875692

Family Applications (1)

Application Number Title Priority Date Filing Date
SK1366-96A SK286094B6 (sk) 1994-04-26 1995-04-25 Zlúčenina špecificky inhibujúca aktivitu faktora Xa, farmaceutická kompozícia s jej obsahom a jej použitie

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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US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
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US7109326B2 (en) 1997-04-15 2006-09-19 Genentech, Inc. Halo-alkoxycarbonyl prodrugs
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
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KR100806326B1 (ko) * 1999-12-14 2008-02-27 쇼와 덴코 가부시키가이샤 시아노벤질아민 염의 제조방법
HUP0301986A2 (hu) 2000-01-28 2003-09-29 Aventis Pharma Deutschland Gmbh. Eljárás acetil-amidinofenilalanil-ciklohexilglicil-piridinioalanin-amidok elżállítására, valamint kiindulási anyagok és köztitermékek
EP1127884A1 (en) * 2000-02-26 2001-08-29 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
DE10029015A1 (de) * 2000-06-15 2001-12-20 Curacyte Ag Hemmstoffe für den Gerinnungsfaktor Xa
PT1345900E (pt) 2000-12-06 2007-03-30 Sanofi Aventis Deutschland Derivados amidina e guanidina como inibidores do factor xa
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
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US7429581B2 (en) 2002-12-23 2008-09-30 Sanofi-Aventis Deutschland Gmbh Pyrazole-derivatives as factor Xa inhibitors
DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
EP1479675A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazole-derivatives as factor Xa inhibitors
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
US7741341B2 (en) 2003-05-19 2010-06-22 Sanofi-Aventis Deutschland Gmbh Benzimidazole-derivatives as factor Xa inhibitors
EP1479680A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole derivatives as Factor Xa inhibitors
EP1479677A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH New indole derivatives as factor xa inhibitors
US7223780B2 (en) 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
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EP1568698A1 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
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EP1724269A1 (en) 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors
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
EP1918718A1 (de) * 2006-10-31 2008-05-07 Roche Diagnostics GmbH Verfahren und Vorrichtungen zur elektrochemischen Bestimmung von Faktor Xa-Inhibitoren in Blutproben
EP2155195B1 (en) 2007-04-13 2014-07-16 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor
DE102023133734A1 (de) 2023-12-01 2025-06-05 Technische Universität Darmstadt, Körperschaft des öffentlichen Rechts Schnelle Bestimmung von Analytgehalten

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Also Published As

Publication number Publication date
LV11740A (lv) 1997-04-20
FI120494B (fi) 2009-11-13
NO964553L (no) 1996-12-27
HUT76346A (en) 1997-08-28
LT4218B (en) 1997-09-25
LT96151A (en) 1997-05-26
ZA953361B (en) 1996-01-12
CN1147261A (zh) 1997-04-09
SI9520044B (sl) 2004-08-31
WO1995029189A1 (en) 1995-11-02
CZ296439B6 (cs) 2006-03-15
DE69532754T2 (de) 2005-03-10
DE69532754D1 (de) 2004-04-29
EP1384725A2 (en) 2004-01-28
ES2214500T3 (es) 2004-09-16
TW409129B (en) 2000-10-21
DK0758341T3 (da) 2004-06-28
CA2186497C (en) 2008-06-17
ATE262536T1 (de) 2004-04-15
CN1181091C (zh) 2004-12-22
EP1384725A3 (en) 2007-02-21
IL113505A0 (en) 1995-07-31
AU2368395A (en) 1995-11-16
EE03973B1 (et) 2003-02-17
KR100380124B1 (ko) 2003-08-02
PT758341E (pt) 2004-08-31
PL188132B1 (pl) 2004-12-31
FI964317A0 (fi) 1996-10-25
PL317067A1 (en) 1997-03-03
HU9602954D0 (en) 1996-12-30
NO964553D0 (no) 1996-10-25
JPH10503477A (ja) 1998-03-31
NZ284977A (en) 1998-09-24
RU2152954C1 (ru) 2000-07-20
CA2186497A1 (en) 1995-11-02
LV11740B (en) 1997-12-20
NO318759B1 (no) 2005-05-02
FI964317A7 (fi) 1996-10-25
SI9520044A (en) 1997-10-31
EP0758341B1 (en) 2004-03-24
EE9600146A (et) 1997-04-15
AU707653B2 (en) 1999-07-15
SK136696A3 (en) 1997-05-07
CZ314096A3 (en) 1997-05-14
IL113505A (en) 1999-12-31
JP3655632B2 (ja) 2005-06-02
EP0758341A1 (en) 1997-02-19

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