DE69715635T2 - Neue amidinoderivate und ihre anwendung als thrombin inhibitoren - Google Patents

Neue amidinoderivate und ihre anwendung als thrombin inhibitoren

Info

Publication number
DE69715635T2
DE69715635T2 DE69715635T DE69715635T DE69715635T2 DE 69715635 T2 DE69715635 T2 DE 69715635T2 DE 69715635 T DE69715635 T DE 69715635T DE 69715635 T DE69715635 T DE 69715635T DE 69715635 T2 DE69715635 T2 DE 69715635T2
Authority
DE
Germany
Prior art keywords
amidine derivatives
new amidine
thrombine
inhibitors
thrombine 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
DE69715635T
Other languages
English (en)
Other versions
DE69715635D1 (de
Inventor
Thomas Antonsson
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.)
AstraZeneca AB
Original Assignee
AstraZeneca AB
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 AstraZeneca AB filed Critical AstraZeneca AB
Publication of DE69715635D1 publication Critical patent/DE69715635D1/de
Application granted granted Critical
Publication of DE69715635T2 publication Critical patent/DE69715635T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/34Sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/71Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/72Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/84Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/14Nitrogen atoms
    • C07D261/16Benzene-sulfonamido isoxazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/50Organo-phosphines
    • C07F9/53Organo-phosphine oxides; Organo-phosphine thioxides
    • C07F9/5304Acyclic saturated phosphine oxides or thioxides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
DE69715635T 1996-07-04 1997-06-26 Neue amidinoderivate und ihre anwendung als thrombin inhibitoren Expired - Fee Related DE69715635T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SE9602646A SE9602646D0 (sv) 1996-07-04 1996-07-04 Pharmaceutically-useful compounds
PCT/SE1997/001150 WO1998001422A1 (en) 1996-07-04 1997-06-26 New amidino derivatives and their use as thrombin inhibitors

Publications (2)

Publication Number Publication Date
DE69715635D1 DE69715635D1 (de) 2002-10-24
DE69715635T2 true DE69715635T2 (de) 2003-08-07

Family

ID=20403276

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69715635T Expired - Fee Related DE69715635T2 (de) 1996-07-04 1997-06-26 Neue amidinoderivate und ihre anwendung als thrombin inhibitoren

Country Status (24)

Country Link
US (2) US6221898B1 (de)
EP (1) EP0917528B1 (de)
JP (1) JP2000515505A (de)
KR (1) KR20000022437A (de)
CN (1) CN1228765A (de)
AR (1) AR007614A1 (de)
AT (1) ATE224365T1 (de)
BR (1) BR9710142A (de)
CA (1) CA2260190A1 (de)
CZ (1) CZ1299A3 (de)
DE (1) DE69715635T2 (de)
EE (1) EE9900006A (de)
HU (1) HUP9902410A3 (de)
ID (1) ID19479A (de)
IL (1) IL127885A0 (de)
IS (1) IS4930A (de)
NO (1) NO986180L (de)
NZ (1) NZ333394A (de)
PL (1) PL331047A1 (de)
SE (1) SE9602646D0 (de)
SK (1) SK172098A3 (de)
TR (1) TR199802767T2 (de)
WO (1) WO1998001422A1 (de)
ZA (1) ZA975591B (de)

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SE9704543D0 (sv) 1997-12-05 1997-12-05 Astra Ab New compounds
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EP2314564A3 (de) * 1999-12-23 2012-04-04 Ampac Fine Chemicals LLC Verbesserte Herstellung von 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-P-nitrobenzensulfonylamid-Hydrochlorid und andere Derivate aus 2-Hydroxy-1,3-diaminen
US6548706B2 (en) 1999-12-23 2003-04-15 Aerojet Fine Chemicals Llc Preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl) -p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
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US7129233B2 (en) 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
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JP4209659B2 (ja) 2001-11-15 2009-01-14 エーザイ・アール・アンド・ディー・マネジメント株式会社 アミジノ誘導体並びにそれを用いた抗血液凝固剤および血栓症治療剤
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GB0815782D0 (en) 2008-08-29 2008-10-08 Xention Ltd Novel potassium channel blockers
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Also Published As

Publication number Publication date
HUP9902410A3 (en) 2001-10-29
ZA975591B (en) 1998-12-24
CN1228765A (zh) 1999-09-15
KR20000022437A (ko) 2000-04-25
ID19479A (id) 1998-07-16
HUP9902410A2 (hu) 1999-11-29
US7074820B2 (en) 2006-07-11
NZ333394A (en) 2000-08-25
EE9900006A (et) 1999-06-15
AU3562897A (en) 1998-02-02
US20020040043A1 (en) 2002-04-04
WO1998001422A1 (en) 1998-01-15
BR9710142A (pt) 1999-08-10
US6221898B1 (en) 2001-04-24
AR007614A1 (es) 1999-11-10
IL127885A0 (en) 1999-10-28
ATE224365T1 (de) 2002-10-15
NO986180D0 (no) 1998-12-29
AU726236B2 (en) 2000-11-02
EP0917528A1 (de) 1999-05-26
NO986180L (no) 1999-03-04
DE69715635D1 (de) 2002-10-24
PL331047A1 (en) 1999-06-21
TR199802767T2 (xx) 1999-04-21
SK172098A3 (en) 1999-06-11
JP2000515505A (ja) 2000-11-21
IS4930A (is) 1998-12-21
CA2260190A1 (en) 1998-01-15
CZ1299A3 (cs) 1999-06-16
EP0917528B1 (de) 2002-09-18
SE9602646D0 (sv) 1996-07-04

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