WO2002057225A3 - Inhibiteurs de thrombine - Google Patents

Inhibiteurs de thrombine Download PDF

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Publication number
WO2002057225A3
WO2002057225A3 PCT/US2001/048673 US0148673W WO02057225A3 WO 2002057225 A3 WO2002057225 A3 WO 2002057225A3 US 0148673 W US0148673 W US 0148673W WO 02057225 A3 WO02057225 A3 WO 02057225A3
Authority
WO
WIPO (PCT)
Prior art keywords
group
thrombin inhibitors
phenyl
alkyl
och2r
Prior art date
Application number
PCT/US2001/048673
Other languages
English (en)
Other versions
WO2002057225A2 (fr
Inventor
Harold G Selnick
Kenneth E Rittle
James C Barrow
Philippe G Nantermet
Donnette Staas
Matthew M Morrissette
Original Assignee
Merck & Co Inc
Harold G Selnick
Kenneth E Rittle
James C Barrow
Philippe G Nantermet
Donnette Staas
Matthew M Morrissette
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 Merck & Co Inc, Harold G Selnick, Kenneth E Rittle, James C Barrow, Philippe G Nantermet, Donnette Staas, Matthew M Morrissette filed Critical Merck & Co Inc
Priority to AU2002246675A priority Critical patent/AU2002246675A1/en
Publication of WO2002057225A2 publication Critical patent/WO2002057225A2/fr
Publication of WO2002057225A3 publication Critical patent/WO2002057225A3/fr

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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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—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)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des composés utiles dans l'inhibition de la thrombine et des occlusions thrombotiques associées ou un sel pharmaceutiquement acceptable desdits composés, lesquels sont représentés par la formule (I). Dans cette formule, R3 et R4 sont indépendamment choisis dans le groupe constitué par hydrogène, -C(O)R?5, où R5¿ est choisi dans le groupe constitué par OC(CH¿3?), OCH3, CH3, NHCH3 et OCH2R?6 (R6¿ étant phényle), alkyle C¿1-4?, cycloalkyle C3-7, -(CH2)1-2R?7, où R7¿ est choisi dans le groupe constitué par cycloalkyle C¿3-7? et phényle, et SO2R?8 (R8¿ étant alkyle C¿1-4?).
PCT/US2001/048673 2000-12-18 2001-12-14 Inhibiteurs de thrombine WO2002057225A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002246675A AU2002246675A1 (en) 2000-12-18 2001-12-14 Thrombin inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25632100P 2000-12-18 2000-12-18
US60/256,321 2000-12-18

Publications (2)

Publication Number Publication Date
WO2002057225A2 WO2002057225A2 (fr) 2002-07-25
WO2002057225A3 true WO2002057225A3 (fr) 2002-09-06

Family

ID=22971808

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/048673 WO2002057225A2 (fr) 2000-12-18 2001-12-14 Inhibiteurs de thrombine

Country Status (2)

Country Link
AU (1) AU2002246675A1 (fr)
WO (1) WO2002057225A2 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004299433A1 (en) * 2003-12-18 2005-06-30 Astrazeneca Ab New 5,6-dihydropyrin-2-one compounds useful as inhibitors of thrombin
FI120344B (fi) 2004-03-17 2009-09-30 Ranbaxy Lab Ltd Menetelmä amorfisessa muodossa olevan atorvastatiinikalsiumin valmistamiseksi
UY29600A1 (es) * 2005-06-17 2007-01-31 Astrazeneca Ab Nuevos heterociclos como inhibidores de trombina, composiciones farmacéuticas que los contienen, procedimientos para su preparación y aplicaciones

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5866573A (en) * 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5866573A (en) * 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors

Also Published As

Publication number Publication date
WO2002057225A2 (fr) 2002-07-25
AU2002246675A1 (en) 2002-07-30

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