HUT76346A - Factor xa inhibitors - Google Patents

Factor xa inhibitors

Info

Publication number
HUT76346A
HUT76346A HU9602954A HU9602954A HUT76346A HU T76346 A HUT76346 A HU T76346A HU 9602954 A HU9602954 A HU 9602954A HU 9602954 A HU9602954 A HU 9602954A HU T76346 A HUT76346 A HU T76346A
Authority
HU
Hungary
Prior art keywords
activity
factor
compound
amino acids
provides
Prior art date
Application number
HU9602954A
Other languages
English (en)
Other versions
HU9602954D0 (en
Inventor
Fahad Al-Obeidi
Michal Lebl
James A Ostrem
Pavel Safar
Alena Stierandova
Peter Strop
Armin Walser
Original Assignee
Selectide Corp
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 Selectide Corp filed Critical Selectide Corp
Publication of HU9602954D0 publication Critical patent/HU9602954D0/hu
Publication of HUT76346A publication Critical patent/HUT76346A/hu

Links

Classifications

    • 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
HU9602954A 1994-04-26 1995-04-25 Factor xa inhibitors HUT76346A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US23305494A 1994-04-26 1994-04-26

Publications (2)

Publication Number Publication Date
HU9602954D0 HU9602954D0 (en) 1996-12-30
HUT76346A true HUT76346A (en) 1997-08-28

Family

ID=22875692

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9602954A HUT76346A (en) 1994-04-26 1995-04-25 Factor xa inhibitors

Country Status (27)

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

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US6069130A (en) * 1995-06-07 2000-05-30 Cor Therapeutics, Inc. Ketoheterocyclic inhibitors of factor Xa
US5747458A (en) * 1995-06-07 1998-05-05 Chiron Corporation Urokinase receptor ligands
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
DE69623038T2 (de) * 1995-12-20 2002-12-12 Aventis Pharma Inc Verfahren zur herstellung von n-acetyl(l)-4-cyanophenylalanin ac-(l)-phe(4-cn)-phe(4-cn)-oh und n-acetyl-(l)-p-amidinophenylalanin-cyclohexylglycin-beta-(3-n-methylpyridinium)-alanin ac-(l)-paph-chg-palme(3)-nh2
US6063794A (en) 1996-10-11 2000-05-16 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
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
NZ500353A (en) 1997-04-14 2002-02-01 Cor Therapeutics Inc Cyclic diaza compounds that are selective inhibitors of factor Xa
NZ500352A (en) 1997-04-14 2001-10-26 Cor Therapeutics Inc Cyclic diaza selective factor Xa inhibitors
JP2001521524A (ja) * 1997-04-14 2001-11-06 シーオーアール セラピューティクス インコーポレイテッド 選択的Ｘａ因子阻害剤
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
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
GB9727123D0 (en) * 1997-12-22 1998-02-25 Int Centre Genetic Eng & Bio Synthesis of diamines
CA2316172C (en) 1997-12-24 2010-02-02 Aventis Pharma Deutschland Gmbh Indole derivatives as inhibitors of factor xa
EP0987274A1 (en) * 1998-09-15 2000-03-22 Hoechst Marion Roussel Deutschland GmbH Factor VIIa Inhibitors
EP1016663A1 (en) * 1999-01-02 2000-07-05 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
CA2358578A1 (en) * 1999-01-02 2000-07-13 Aventis Pharma Deutschland Gmbh Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)
CA2358581C (en) 1999-01-02 2010-02-02 Aventis Pharma Deutschland Gmbh Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
EP1022268A1 (en) * 1999-01-02 2000-07-26 Aventis Pharma Deutschland GmbH Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
EP1059302A1 (en) * 1999-06-08 2000-12-13 Aventis Pharma Deutschland GmbH Factor VIIa inhibitors
EP1095933A1 (en) 1999-10-30 2001-05-02 Aventis Pharma Deutschland GmbH Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
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
AU1890201A (en) * 1999-12-14 2001-06-25 Showa Denko Kabushiki Kaisha Process for producing salt of cyanobenzylamine or derivative
IL150897A0 (en) * 2000-01-28 2003-02-12 Aventis Pharma Gmbh Process for the preparation of acetyl-amidiniophenylalanyl cyclohexylglycyl-pyridinioalaninamides
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
BR0115938A (pt) 2000-12-06 2003-12-23 Aventis Pharma Deustschland Gm Derivados de guanidina e amidina com inibidores do fator xa
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
WO2003076391A2 (de) 2002-03-11 2003-09-18 Curacyte Ag Hemmstoffe der urokinase, ihre herstellung und verwendung
WO2004050637A2 (en) 2002-12-03 2004-06-17 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
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
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis 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
EP1479680A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole 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
EP1479675A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazole-derivatives as factor Xa inhibitors
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 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
EP1807082A4 (en) 2004-10-26 2010-12-01 Janssen Pharmaceutica Nv INHIBITOR COMPOUNDS OF XA FACTORS
EP1724269A1 (en) 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors
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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
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Also Published As

Publication number Publication date
AU2368395A (en) 1995-11-16
CN1147261A (zh) 1997-04-09
EE03973B1 (et) 2003-02-17
EP0758341A1 (en) 1997-02-19
SI9520044B (sl) 2004-08-31
PL188132B1 (pl) 2004-12-31
AU707653B2 (en) 1999-07-15
FI964317A (fi) 1996-10-25
DE69532754D1 (de) 2004-04-29
LV11740B (en) 1997-12-20
EP0758341B1 (en) 2004-03-24
EE9600146A (et) 1997-04-15
LT4218B (en) 1997-09-25
FI964317A0 (fi) 1996-10-25
FI120494B (fi) 2009-11-13
KR100380124B1 (ko) 2003-08-02
IL113505A0 (en) 1995-07-31
ZA953361B (en) 1996-01-12
JPH10503477A (ja) 1998-03-31
ATE262536T1 (de) 2004-04-15
NO318759B1 (no) 2005-05-02
LT96151A (en) 1997-05-26
EP1384725A2 (en) 2004-01-28
DK0758341T3 (da) 2004-06-28
LV11740A (lv) 1997-04-20
CN1181091C (zh) 2004-12-22
CZ296439B6 (cs) 2006-03-15
SI9520044A (en) 1997-10-31
CA2186497A1 (en) 1995-11-02
NO964553D0 (no) 1996-10-25
CA2186497C (en) 2008-06-17
JP3655632B2 (ja) 2005-06-02
EP1384725A3 (en) 2007-02-21
CZ314096A3 (en) 1997-05-14
SK136696A3 (en) 1997-05-07
SK286094B6 (sk) 2008-03-05
HU9602954D0 (en) 1996-12-30
NZ284977A (en) 1998-09-24
NO964553L (no) 1996-12-27
ES2214500T3 (es) 2004-09-16
PL317067A1 (en) 1997-03-03
PT758341E (pt) 2004-08-31
TW409129B (en) 2000-10-21
IL113505A (en) 1999-12-31
RU2152954C1 (ru) 2000-07-20
WO1995029189A1 (en) 1995-11-02
DE69532754T2 (de) 2005-03-10

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TH39843A (th) อะนาลอคของโทโมซิน อัลฟา1

Legal Events

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FC4A Lapse of provisional application due to refusal