AT262536T - Factor xa inhibitors - Google Patents

Factor xa inhibitors

Info

Publication number
AT262536T
AT262536T AT95917736T AT95917736T AT262536T AT 262536 T AT262536 T AT 262536T AT 95917736 T AT95917736 T AT 95917736T AT 95917736 T AT95917736 T AT 95917736T AT 262536 T AT262536 T AT 262536T
Authority
AT
Austria
Prior art keywords
factor xa
xa inhibitors
inhibitors
factor
Prior art date
Application number
AT95917736T
Other languages
German (de)
Inventor
Fahad Al-Obeidi
Michal Lebl
James A Ostrem
Pavel Safar
Alena Stierandova
Peter Strop
Armin Walser
Original Assignee
Aventis Pharma Inc
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
Priority to US23305494A priority Critical
Application filed by Aventis Pharma Inc filed Critical Aventis Pharma Inc
Priority to PCT/US1995/005268 priority patent/WO1995029189A1/en
Publication of AT262536T publication Critical patent/AT262536T/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81Protease inhibitors
    • C07K14/8107Endopeptidase (E.C. 3.4.21-99) inhibitors
    • C07K14/811Serine protease (E.C. 3.4.21) inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0821Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/101Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1016Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING 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
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/56Measuring 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of products other than chlorine, adipic acid, caprolactam, or chlorodifluoromethane, e.g. bulk or fine chemicals or pharmaceuticals
    • Y02P20/55Synthetic design, e.g. reducing the use of auxiliary or protecting groups
AT95917736T 1994-04-26 1995-04-25 Factor xa inhibitors AT262536T (en)

Priority Applications (2)

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

Publications (1)

Publication Number Publication Date
AT262536T true AT262536T (en) 2004-04-15

Family

ID=22875692

Family Applications (1)

Application Number Title Priority Date Filing Date
AT95917736T AT262536T (en) 1994-04-26 1995-04-25 Factor xa inhibitors

Country Status (27)

Country Link
EP (2) EP1384725A3 (en)
JP (1) JP3655632B2 (en)
KR (1) KR100380124B1 (en)
CN (1) CN1181091C (en)
AT (1) AT262536T (en)
AU (1) AU707653B2 (en)
CA (1) CA2186497C (en)
CZ (1) CZ296439B6 (en)
DE (2) DE69532754D1 (en)
DK (1) DK0758341T3 (en)
EE (1) EE03973B1 (en)
ES (1) ES2214500T3 (en)
FI (1) FI120494B (en)
HU (1) HUT76346A (en)
IL (1) IL113505A (en)
LT (1) LT4218B (en)
LV (1) LV11740B (en)
NO (1) NO318759B1 (en)
NZ (1) NZ284977A (en)
PL (1) PL188132B1 (en)
PT (1) PT758341E (en)
RU (1) RU2152954C1 (en)
SI (1) SI9520044B (en)
SK (1) SK286094B6 (en)
TW (1) TW409129B (en)
WO (1) WO1995029189A1 (en)
ZA (1) ZA9503361B (en)

Families Citing this family (52)

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MX9706069A (en) * 1995-02-17 1997-10-31 Basf Ag Novel dipeptide amidines as thrombin inhibitors.
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
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
BR9612059A (en) * 1995-12-20 1999-02-23 Hoechst Marion Roussel Inc new process for preparing N-acetyl (L) -4-cyanophenylalanine c (L) -Phe (4-CN) -OH and N-Acetyl- (L) -p-amidinophenylalanine cicloexilglicina-beta- (3-n -metilpriridínio) -alanine ac- (l) -pAph-Chg-Pal-me (3) -NH2
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
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
US6133256A (en) * 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
AU6896398A (en) 1997-04-14 1998-11-11 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0977772A1 (en) 1997-04-14 2000-02-09 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
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
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
GB9727123D0 (en) * 1997-12-22 1998-02-25 Int Centre Genetic Eng & Bio Synthesis of diamines
DE69829879T2 (en) 1997-12-24 2006-03-02 Sanofi-Aventis Deutschland Gmbh Indole derivatives as factor xa inhibitors
EP0987274A1 (en) * 1998-09-15 2000-03-22 Hoechst Marion Roussel Deutschland GmbH Factor VIIa Inhibitors
WO2000040571A1 (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
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)
EP1059302A1 (en) * 1999-06-08 2000-12-13 Aventis Pharma Deutschland GmbH Factor VIIa inhibitors
KR100979069B1 (en) * 1999-06-08 2010-08-31 사노피-아벤티스 도이칠란트 게엠베하 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
KR100806326B1 (en) * 1999-12-14 2008-02-27 쇼와 덴코 가부시키가이샤 Process for producing salts of cyanobenzylamines
CA2355266C (en) 1999-12-14 2009-11-10 Showa Denko K.K. Process for producing salt of cyanobenzylamines
CN1176104C (en) 2000-01-28 2004-11-17 阿文蒂斯药物德国有限公司 Process for preparation of acetyl-guanylphenylalanyl-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 (en) 2000-06-15 2001-12-20 Curacyte Ag Coagulation Factor Xa inhibitor, useful for treatment, prophylaxis or diagnosis of thromboembolic disease, comprising acylated 3- or 4-amidino-benzylamine derivative
HU0302604A3 (en) 2000-12-06 2005-09-28 Aventis Pharma Gmbh Guanidine and amidine derivatives as factor xa inhibitors
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
JP4898091B2 (en) 2002-03-11 2012-03-14 ザ メディシンズ カンパニー (ライプツィヒ) ゲーエムベーハー Inhibitors of urokinase, their production and use
US7479502B2 (en) 2002-12-03 2009-01-20 Pharmacyclics, 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 (en) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Use of acylated 4-amidino- and 4-guanidinobenzylamines for the inhibition of plasma kallikrein
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis 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
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
US7741341B2 (en) 2003-05-19 2010-06-22 Sanofi-Aventis Deutschland Gmbh Benzimidazole-derivatives as factor Xa inhibitors
EP1479675A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Indazole-derivatives as factor Xa inhibitors
DE10342108A1 (en) 2003-09-11 2005-04-14 Curacyte Chemistry Gmbh Basic substituted benzylamine analogs as coagulation factor Xa inhibitors, their preparation and use
EP1568698A1 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
WO2006047415A2 (en) 2004-10-26 2006-05-04 Janssen Pharmaceutica, N.V. Factor xa compounds
EP1724269A1 (en) 2005-05-20 2006-11-22 Sanofi-Aventis Deutschland GmbH Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors
DE102005044319A1 (en) 2005-09-16 2007-03-22 Curacyte Chemistry Gmbh 2- (Aminomethyl) -5-chloro-benzylamide derivatives and their use as inhibitors of coagulation factor Xa
DE102006050672A1 (en) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh New glycylglycine derivatives with a benzylsulfonylamido group and an amidino-organylamido group at the opposite chain ends, used in drugs for reducing loss of blood, e.g. in operations
EP1918718A1 (en) * 2006-10-31 2008-05-07 Roche Diagnostics GmbH Methods and devices for electrochemical determination of factor Xa inhibitors in blood samples
EP2155195B1 (en) 2007-04-13 2014-07-16 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor

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US4275153A (en) * 1978-08-03 1981-06-23 American Hospital Supply Corporation Analytical fluorogenic substrates for proteolytic enzymes
CA1161431A (en) * 1979-05-11 1984-01-31 Lars G. Svendsen Tripeptide derivatives
US4469679A (en) * 1983-02-16 1984-09-04 Smithkline Beckman Corporation Octapeptide vasopressin antagonists
HU191961B (en) * 1984-08-02 1987-04-28 Richter Gedeon Vegyeszet Process for producing 1,5 and 8 substituted peptides of angiotenzin-ii antagonistic activity
DE69321344D1 (en) * 1992-02-14 1998-11-05 Corvas Int Inc Inhibitors of thrombosis

Also Published As

Publication number Publication date
HU9602954D0 (en) 1996-12-30
IL113505D0 (en) 1995-07-31
JPH10503477A (en) 1998-03-31
ZA9503361B (en) 1996-01-12
CA2186497A1 (en) 1995-11-02
FI964317D0 (en)
AU707653B2 (en) 1999-07-15
CZ296439B6 (en) 2006-03-15
LT4218B (en) 1997-09-25
NZ284977A (en) 1998-09-24
LV11740A (en) 1997-04-20
EP1384725A2 (en) 2004-01-28
NO964553L (en) 1996-12-27
EP0758341B1 (en) 2004-03-24
IL113505A (en) 1999-12-31
HUT76346A (en) 1997-08-28
PT758341E (en) 2004-08-31
NO318759B1 (en) 2005-05-02
DE69532754T2 (en) 2005-03-10
SI9520044A (en) 1997-10-31
EP1384725A3 (en) 2007-02-21
ES2214500T3 (en) 2004-09-16
DE69532754D1 (en) 2004-04-29
FI120494B (en) 2009-11-13
RU2152954C1 (en) 2000-07-20
TW409129B (en) 2000-10-21
DK758341T3 (en)
FI964317A0 (en) 1996-10-25
CN1181091C (en) 2004-12-22
SK286094B6 (en) 2008-03-05
EE03973B1 (en) 2003-02-17
WO1995029189A1 (en) 1995-11-02
SK136696A3 (en) 1997-05-07
CN1147261A (en) 1997-04-09
FI120494B1 (en)
LV11740B (en) 1997-12-20
FI964317A (en) 1996-10-25
KR100380124B1 (en) 2003-08-02
LT96151A (en) 1997-05-26
EE9600146A (en) 1997-04-15
SI9520044B (en) 2004-08-31
CA2186497C (en) 2008-06-17
NO964553D0 (en) 1996-10-25
PL317067A1 (en) 1997-03-03
DK0758341T3 (en) 2004-06-28
CZ314096A3 (en) 1997-05-14
JP3655632B2 (en) 2005-06-02
EP0758341A1 (en) 1997-02-19
PL188132B1 (en) 2004-12-31
AU2368395A (en) 1995-11-16

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