DE69716823T2 - Thrombin-Inhibitoren als anticoagulierende Mittel - Google Patents

Thrombin-Inhibitoren als anticoagulierende Mittel

Info

Publication number
DE69716823T2
DE69716823T2 DE69716823T DE69716823T DE69716823T2 DE 69716823 T2 DE69716823 T2 DE 69716823T2 DE 69716823 T DE69716823 T DE 69716823T DE 69716823 T DE69716823 T DE 69716823T DE 69716823 T2 DE69716823 T2 DE 69716823T2
Authority
DE
Germany
Prior art keywords
thrombin inhibitors
compound
anticoagulants
salt
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
DE69716823T
Other languages
English (en)
Other versions
DE69716823D1 (de
Inventor
Valentine Joseph Klimkowski
Aaron Leigh Schacht
Michael Robert Wiley
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of DE69716823D1 publication Critical patent/DE69716823D1/de
Publication of DE69716823T2 publication Critical patent/DE69716823T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/06—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07K5/022—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2
    • C07K5/0222—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -X-C(=O)-(C)n-N-C-C(=O)-Y-; X and Y being heteroatoms; n being 1 or 2 with the first amino acid being heterocyclic, e.g. 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
    • C07K5/06—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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • 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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
DE69716823T 1996-06-25 1997-06-25 Thrombin-Inhibitoren als anticoagulierende Mittel Expired - Fee Related DE69716823T2 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US2037196P 1996-06-25 1996-06-25

Publications (2)

Publication Number Publication Date
DE69716823D1 DE69716823D1 (de) 2002-12-12
DE69716823T2 true DE69716823T2 (de) 2003-07-03

Family

ID=21798273

Family Applications (2)

Application Number Title Priority Date Filing Date
DE69716823T Expired - Fee Related DE69716823T2 (de) 1996-06-25 1997-06-25 Thrombin-Inhibitoren als anticoagulierende Mittel
DE69725354T Expired - Fee Related DE69725354T2 (de) 1996-06-25 1997-06-25 Intermediate zur Herstellung von Thrombininhibitoren als Anticoagulantien

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE69725354T Expired - Fee Related DE69725354T2 (de) 1996-06-25 1997-06-25 Intermediate zur Herstellung von Thrombininhibitoren als Anticoagulantien

Country Status (11)

Country Link
US (5) US5863929A (de)
EP (1) EP0816376B1 (de)
JP (1) JP2000514788A (de)
AT (2) ATE227306T1 (de)
AU (1) AU3496297A (de)
CA (1) CA2258915A1 (de)
DE (2) DE69716823T2 (de)
DK (1) DK0816376T3 (de)
ES (2) ES2185876T3 (de)
PT (1) PT816376E (de)
WO (1) WO1997049404A1 (de)

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WO1997049404A1 (en) * 1996-06-25 1997-12-31 Eli Lilly And Company Anticoagulant agents
US6200967B1 (en) 1996-06-25 2001-03-13 Eli Lilly And Company Anticoagulant agents
EP1135023A4 (de) * 1998-11-12 2003-03-05 Lilly Co Eli Aminobenzisoxazol-verbindungen und sie enthaltende bibliotheken
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WO2000039102A1 (en) * 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
ATE307111T1 (de) * 1999-01-13 2005-11-15 Genentech Inc Serinprotease-inhibitoren
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AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
EP1192132B1 (de) 1999-06-14 2005-09-07 Eli Lilly And Company Inhibitoren von serin proteasen
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
GB0030304D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
GB0030305D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
GB0030306D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
GB0030303D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
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UA75093C2 (en) 2000-10-06 2006-03-15 Dimensional Pharm Inc Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors
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AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
ATE399175T1 (de) * 2002-03-11 2008-07-15 Curacyte Ag Hemmstoffe der urokinase, ihre herstellung und verwendung
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Also Published As

Publication number Publication date
DK0816376T3 (da) 2002-11-25
WO1997049404A1 (en) 1997-12-31
EP0816376A1 (de) 1998-01-07
US6008367A (en) 1999-12-28
DE69725354T2 (de) 2004-06-24
AU3496297A (en) 1998-01-14
US6160176A (en) 2000-12-12
ATE227306T1 (de) 2002-11-15
US6034104A (en) 2000-03-07
US6552038B1 (en) 2003-04-22
JP2000514788A (ja) 2000-11-07
DE69725354D1 (de) 2003-11-06
PT816376E (pt) 2003-02-28
EP0816376B1 (de) 2002-11-06
DE69716823D1 (de) 2002-12-12
ES2208516T3 (es) 2004-06-16
ES2185876T3 (es) 2003-05-01
US5863929A (en) 1999-01-26
CA2258915A1 (en) 1997-12-31
ATE251176T1 (de) 2003-10-15

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8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee