HUP9800634A2 - p-Amidino-benzil-amid-származék trombin-inhibitorok, intermedierjeik és alkalmazásuk - Google Patents

p-Amidino-benzil-amid-származék trombin-inhibitorok, intermedierjeik és alkalmazásuk

Info

Publication number
HUP9800634A2
HUP9800634A2 HU9800634A HUP9800634A HUP9800634A2 HU P9800634 A2 HUP9800634 A2 HU P9800634A2 HU 9800634 A HU9800634 A HU 9800634A HU P9800634 A HUP9800634 A HU P9800634A HU P9800634 A2 HUP9800634 A2 HU P9800634A2
Authority
HU
Hungary
Prior art keywords
group
general formula
intermediates
tube
divalent
Prior art date
Application number
HU9800634A
Other languages
English (en)
Inventor
Hans-Joachim Böhm
Wilfried Hornberger
Hans Wolfgang Höffken
Stefan Koser
Helmut Mack
Thomas Pfeiffer
Werner Seitz
Thomas Zierke
Original Assignee
Basf Ag.,
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 claimed from DE1995104504 external-priority patent/DE19504504A1/de
Priority claimed from DE1995106610 external-priority patent/DE19506610A1/de
Application filed by Basf Ag., filed Critical Basf Ag.,
Publication of HUP9800634A2 publication Critical patent/HUP9800634A2/hu
Publication of HUP9800634A3 publication Critical patent/HUP9800634A3/hu

Links

Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • 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
    • 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
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or 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
    • C07K5/06—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
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • 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
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Mutual Connection Of Rods And Tubes (AREA)

Abstract

A cím szerinti vegyületek (I) általánős képletében R1 hidrőxilcsőpőrt,adőtt esetben szűbsztitűált alkilcsőpőrt, ciklőalkil-, aril-,heterőarilcsőpőrt; A kétértékű a-aminősavcsőpőrt; B kétértékű,ciklűsős a-aminősav-csőpőrt; D adőtt esetben gyűrűben és/vagymetiléncsőpőrtőn szűbsztitűált benzil-, azőlil- vagy azinilcsőpőrt. Atalálmány tárgykörébe tartőznak a fenti vegyületek sztereőizőmerjei ésfiziőlógiailag elviselhető savakkal alkőtőtt sói, amelyekben azamidinfűnkció lehet egyszeresen vagy kétszeresen védett főrmában. Atalálmány tárgyát képezik tővábbá a (VII), (VIII), (IX) és (X)általánős képletű intermedierek, valamint a (XI) általánős képletűszerkezeti részletet tartalmazó vegyületek. ŕ
HU9800634A 1995-02-10 1996-02-06 P-amidino-benzylamide derivatives as thrombin inhibitors, intermediates and use thereof HUP9800634A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE1995104504 DE19504504A1 (de) 1995-02-10 1995-02-10 Heterocyclische Thrombininhibitoren
DE1995106610 DE19506610A1 (de) 1995-02-24 1995-02-24 Thrombininhibitoren

Publications (2)

Publication Number Publication Date
HUP9800634A2 true HUP9800634A2 (hu) 1999-06-28
HUP9800634A3 HUP9800634A3 (en) 2000-04-28

Family

ID=26012343

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9800634A HUP9800634A3 (en) 1995-02-10 1996-02-06 P-amidino-benzylamide derivatives as thrombin inhibitors, intermediates and use thereof

Country Status (15)

Country Link
US (1) US5932567A (hu)
EP (1) EP0809651A1 (hu)
JP (1) JPH10513462A (hu)
KR (1) KR19980702112A (hu)
CN (1) CN1173872A (hu)
AU (1) AU706834B2 (hu)
BR (1) BR9607412A (hu)
CA (1) CA2210989A1 (hu)
CZ (1) CZ237697A3 (hu)
EA (1) EA002767B1 (hu)
FI (1) FI973282A0 (hu)
HU (1) HUP9800634A3 (hu)
MX (1) MX9705970A (hu)
NO (1) NO973657L (hu)
WO (1) WO1996024609A1 (hu)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9900043D0 (sv) * 1999-01-11 1999-01-11 Astra Ab New use
US5705487A (en) * 1994-03-04 1998-01-06 Eli Lilly And Company Antithrombotic agents
US5707966A (en) * 1994-03-04 1998-01-13 Eli Lilly And Company Antithrombotic agents
US5726159A (en) * 1994-03-04 1998-03-10 Eli Lilly And Company Antithrombotic agents
US5710130A (en) * 1995-02-27 1998-01-20 Eli Lilly And Company Antithrombotic agents
US5914319A (en) * 1995-02-27 1999-06-22 Eli Lilly And Company Antithrombotic agents
SE9602263D0 (sv) 1996-06-07 1996-06-07 Astra Ab New amino acid derivatives
US6200967B1 (en) 1996-06-25 2001-03-13 Eli Lilly And Company Anticoagulant agents
EP1110968B1 (en) * 1996-06-25 2003-10-01 Eli Lilly & Company Intermediate for the preparation of Thrombininhibitors as anticoagulant agents
US5863929A (en) * 1996-06-25 1999-01-26 Eli Lilly And Company Anticoagulant agents
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
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
WO1998046626A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. 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
CA2285659A1 (en) 1997-04-14 1998-10-22 Cor Therapeutics, Inc. Selective factor xa inhibitors
US7109326B2 (en) 1997-04-15 2006-09-19 Genentech, Inc. Halo-alkoxycarbonyl prodrugs
AR013084A1 (es) 1997-06-19 2000-12-13 Astrazeneca Ab Derivados de amidino utiles como inhibidores de la trombina, composicion farmaceutica, utilizacion de dichos compuestos para la preparacion demedicamentos y proceso para la preparacion de los compuestos mencionados
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
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
KR20000047461A (ko) * 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
US6486193B2 (en) 1998-12-31 2002-11-26 Aventis Pharmaceuticals Inc. 3-substituted pyrrolidines useful as inhibitors of matrix metalloproteinases
DE50008510D1 (de) * 1999-04-09 2004-12-09 Abbott Gmbh & Co Kg Niedermolekulare inhibitoren von komplementproteasen
US6586405B2 (en) 2000-08-11 2003-07-01 Corvas International, Inc. Non-covalent inhibitors of urokinase and blood vessel formation
IL149042A0 (en) * 2000-08-11 2002-11-10 Corvas Int Inc Non-covalent inhibitors of urokinase and blood vessel formation
DE10049937A1 (de) * 2000-10-06 2002-04-11 Knoll Ag Niedermolekulare Inhibitoren von Serinproteasen mit Polyhydroxyalkyl- und Polyhydroxycycloalkylresten
US6716869B2 (en) * 2001-12-17 2004-04-06 Pharmacia Corporation Protease inhibitors of the coagulation cascade isolated from Dysidea sponges
WO2003070229A2 (de) * 2002-02-22 2003-08-28 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Verwendung von proteinaseinhibitoren zur behandlung von autoimmunerkrankungen
DE102004022897A1 (de) * 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
DE102008041214A1 (de) 2008-08-13 2010-02-18 Bayer Cropscience Ag N-substituierte Azinylakyl-azincarboxamide und deren Analoge
US10597863B2 (en) 2018-01-19 2020-03-24 Resource Fiber LLC Laminated bamboo platform and concrete composite slab system

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU675981B2 (en) * 1992-12-02 1997-02-27 Bristol-Myers Squibb Company Guanidinyl-substituted heterocyclic thrombin inhibitors
SE9301916D0 (sv) * 1993-06-03 1993-06-03 Ab Astra New peptides derivatives
AU1025795A (en) * 1994-01-27 1995-08-03 Mitsubishi Chemical Corporation Prolineamide derivatives
IL112795A (en) * 1994-03-04 2001-01-28 Astrazeneca Ab Derivatives of peptides as antithrombotic drugs, their preparation, and pharmaceutical preparations containing them

Also Published As

Publication number Publication date
NO973657D0 (no) 1997-08-08
BR9607412A (pt) 1998-07-07
JPH10513462A (ja) 1998-12-22
EA002767B1 (ru) 2002-08-29
NO973657L (no) 1997-10-03
EP0809651A1 (de) 1997-12-03
FI973282A (fi) 1997-08-08
CZ237697A3 (cs) 1998-04-15
CN1173872A (zh) 1998-02-18
HUP9800634A3 (en) 2000-04-28
KR19980702112A (ko) 1998-07-15
WO1996024609A1 (de) 1996-08-15
US5932567A (en) 1999-08-03
MX9705970A (es) 1997-11-29
AU706834B2 (en) 1999-06-24
FI973282A0 (fi) 1997-08-08
CA2210989A1 (en) 1996-08-15
AU4787596A (en) 1996-08-27
EA199700155A1 (ru) 1997-12-30

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