FI120494B - Tekijän Xa inhibiittoreita - Google Patents

Tekijän Xa inhibiittoreita Download PDF

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Publication number
FI120494B
FI120494B FI964317A FI964317A FI120494B FI 120494 B FI120494 B FI 120494B FI 964317 A FI964317 A FI 964317A FI 964317 A FI964317 A FI 964317A FI 120494 B FI120494 B FI 120494B
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FI
Finland
Prior art keywords
chg
arg
paph
leu
pro
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FI964317A
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English (en)
Finnish (fi)
Swedish (sv)
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FI964317A0 (fi
FI964317A (fi
Inventor
Fahad Al-Obeidi
Armin Walser
Pavel Safar
Michal Lebl
James A Ostrem
Alena Stierandova
Peter Strop
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Selectide Corp
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Publication of FI964317A publication Critical patent/FI964317A/fi
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Publication of FI120494B publication Critical patent/FI120494B/fi

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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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
FI964317A 1994-04-26 1996-10-25 Tekijän Xa inhibiittoreita FI120494B (fi)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US23305494A 1994-04-26 1994-04-26
US23305494 1994-04-26
US9505268 1995-04-25
PCT/US1995/005268 WO1995029189A1 (en) 1994-04-26 1995-04-25 FACTOR Xa INHIBITORS

Publications (3)

Publication Number Publication Date
FI964317A0 FI964317A0 (fi) 1996-10-25
FI964317A FI964317A (fi) 1996-10-25
FI120494B true FI120494B (fi) 2009-11-13

Family

ID=22875692

Family Applications (1)

Application Number Title Priority Date Filing Date
FI964317A FI120494B (fi) 1994-04-26 1996-10-25 Tekijän Xa inhibiittoreita

Country Status (27)

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

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US5747458A (en) * 1995-06-07 1998-05-05 Chiron Corporation Urokinase receptor ligands
US6069130A (en) * 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
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US5766932A (en) * 1995-12-20 1998-06-16 Hoechst Marion Roussel, Inc. Process for preparing N-acetyl(L)-4-cyanophenylalanine from a mixture of the corresponding D,L ethyl esters using subtilisin
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6194435B1 (en) 1996-10-11 2001-02-27 Cor Therapeutics, Inc. Lactams as selective factor Xa inhibitors
US6063794A (en) 1996-10-11 2000-05-16 Cor Therapeutics Inc. Selective factor Xa inhibitors
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
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EP0977772A1 (de) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. Selektive faktor xa-inhibitoren
US7109326B2 (en) 1997-04-15 2006-09-19 Genentech, Inc. Halo-alkoxycarbonyl prodrugs
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6218382B1 (en) 1997-08-11 2001-04-17 Cor Therapeutics, Inc Selective factor Xa inhibitors
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EP0987274A1 (de) * 1998-09-15 2000-03-22 Hoechst Marion Roussel Deutschland GmbH Faktor VIIa Inhibitore
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EP1022268A1 (de) * 1999-01-02 2000-07-26 Aventis Pharma Deutschland GmbH Arylalkanoylderivate, Verfahren zu ihrer Herstellung, ihre Verwendung und diese enthaltende pharmazeutische Zubereitungen
EP1059302A1 (de) * 1999-06-08 2000-12-13 Aventis Pharma Deutschland GmbH Faktor VIIa Inhibitore
EP1095933A1 (de) 1999-10-30 2001-05-02 Aventis Pharma Deutschland GmbH N-Guanidinoalkylamide, Verfahren zu ihrer Herstellung, ihre Verwendung und pharmazeutische Zusammensetzungen, die sie enthalten
CN1172905C (zh) 1999-12-14 2004-10-27 昭和电工株式会社 生产氰基苄胺盐的方法
JP5088598B2 (ja) * 1999-12-14 2012-12-05 昭和電工株式会社 シアノベンジルアミン類の塩の製造方法
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DE50310038D1 (de) 2002-03-11 2008-08-07 Curacyte Ag Hemmstoffe der urokinase, ihre herstellung und verwendung
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
US7358268B2 (en) 2002-12-04 2008-04-15 Sanofi-Aventis Deutschland Gmbh Imidazole derivatives as factor Xa inhibitors
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
US7223780B2 (en) 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
EP1479677A1 (de) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Neue Indolderivate als Faktor Xa-Inhibitoren
EP1479680A1 (de) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole-Derivative als Faktor Xa Hemmer
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
EP1479675A1 (de) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazolderivate als Faktor Xa-Inhibitoren
US7741341B2 (en) 2003-05-19 2010-06-22 Sanofi-Aventis Deutschland Gmbh Benzimidazole-derivatives as factor Xa inhibitors
DE10342108A1 (de) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung
EP1568698A1 (de) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrolderivate als faktor-xa-inhibitoren
US7446210B2 (en) 2004-10-26 2008-11-04 Janssen Pharmaceutica N.V. Factor Xa compounds
EP1724269A1 (de) 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroarylcarbonsäure-sulfamoylalkylamidderivate als Faktor Xa-Inhibitoren
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
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Also Published As

Publication number Publication date
ZA953361B (en) 1996-01-12
HUT76346A (en) 1997-08-28
LT4218B (en) 1997-09-25
NZ284977A (en) 1998-09-24
PL188132B1 (pl) 2004-12-31
CZ296439B6 (cs) 2006-03-15
ES2214500T3 (es) 2004-09-16
FI964317A0 (fi) 1996-10-25
CA2186497C (en) 2008-06-17
SK136696A3 (en) 1997-05-07
EE9600146A (et) 1997-04-15
LV11740A (lv) 1997-04-20
PL317067A1 (en) 1997-03-03
EP0758341B1 (de) 2004-03-24
IL113505A0 (en) 1995-07-31
EE03973B1 (et) 2003-02-17
CN1181091C (zh) 2004-12-22
NO964553D0 (no) 1996-10-25
JPH10503477A (ja) 1998-03-31
DK0758341T3 (da) 2004-06-28
AU2368395A (en) 1995-11-16
CZ314096A3 (en) 1997-05-14
WO1995029189A1 (en) 1995-11-02
EP1384725A3 (de) 2007-02-21
DE69532754D1 (de) 2004-04-29
DE69532754T2 (de) 2005-03-10
FI964317A (fi) 1996-10-25
IL113505A (en) 1999-12-31
JP3655632B2 (ja) 2005-06-02
CA2186497A1 (en) 1995-11-02
EP1384725A2 (de) 2004-01-28
AU707653B2 (en) 1999-07-15
SI9520044B (sl) 2004-08-31
ATE262536T1 (de) 2004-04-15
KR100380124B1 (ko) 2003-08-02
EP0758341A1 (de) 1997-02-19
SI9520044A (en) 1997-10-31
HU9602954D0 (en) 1996-12-30
NO318759B1 (no) 2005-05-02
NO964553L (no) 1996-12-27
CN1147261A (zh) 1997-04-09
RU2152954C1 (ru) 2000-07-20
LT96151A (en) 1997-05-26
SK286094B6 (sk) 2008-03-05
LV11740B (en) 1997-12-20
PT758341E (pt) 2004-08-31
TW409129B (en) 2000-10-21

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